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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 372. Отображено 117.
31-07-2013 дата публикации

Inhibitors of protein kinases

Номер: CN103224497A
Автор: Song Yonghong, Xu Qing, Bauer Shawn M., Jia Zhaozhong J., Mehrotra Mukund, Pandey Anjali
Принадлежит:

The present invention is directed to compounds of formula (I)-(II) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 1
11-05-2017 дата публикации

PROCESS AND COMPOSITIONS FOR ACHIEVING MAMMALIAN ENERGY BALANCE

Номер: US20170128410A1
Автор: MUHAMMED MAJEED, Kalyanam Nagabhushanam, Sarang Bani, Anjali Pandey, MAJEED MUHAMMED, NAGABHUSHANAM KALYANAM, BANI SARANG, PANDEY ANJALI, Nagabhushanam Kalyanam, Bani Sarang, Pandey Anjali
Принадлежит:

Disclosed is a method of achieving optimal mammalian energy balance using forskolin on a particular physiological and developmental stage of the mammalian cellular system. 1. A method of achieving mammalian energy balance using forskolin in a process of adipogenesis inhibition wherein forskolin is added separately to pre-adipocytes before differentiation and also to mature adipocytes to comparatively evaluate adipogenesis inhibition potential , said process comprising steps of:{'sup': '4', 'a) Seeding mammalian adipocyte precursor cells (pre-adipocytes) in wells of microplates wherein approximately 60×10cells are seeded for 48-72 hours to get 70-80% confluence;'}b) Adding forskolin at concentrations of 50 μg/ml and 100 μg/ml in the pre-seeded microplates of step a consisting of undifferentiated pre-adipocytes;c) Adding 200 μl of freshly prepared Adipogenesis induction medium to the wells;d) Adding 200 μl of freshly prepared Adipogenesis progression medium after 72 hours of incubation with the Adipogenesis induction medium in step c;e) Incubating the cells treated with forskolin (step b), adipogenesis induction medium (step c) and adipogenesis progression medium (step d) for 48 hours in a humidified atmosphere (37 deg. C.) of 5% CO2 and 95% air;f) Fixing the cells of step e by adding 100 μl of 10% formalin and staining using the Oil Red O technique;g) Reading the optical density of cells of step f at 492 nm in a microplate reader and expressing the results as inhibitory concentration (IC50) values using the graph pad prism software;h) Calculating the percentage inhibition of adipogenesis in the cells of steps f and g using the formula, C-T/T×100, wherein C is the absorbance of Oil Red O in differentiating/undifferentiated cells and T is the absorbance of Oil Red O in sample treated differentiating/undifferentiated cells.i) Adding 200 μl of freshly prepared Adipogenesis induction medium to the wells of step a.j) Adding 200 μl of freshly prepared Adipogenesis ...

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Номер записи: 2
03-11-2016 дата публикации

BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS

Номер: US20160318852A1
Автор: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey, JIA ZHAOZHONG J, SONG YONGHONG, XU QING, KANE BRIAN, BAUER SHAWN M, PANDEY ANJALI, Jia Zhaozhong J., Song Yonghong, Xu Qing, Kane Brian, Bauer Shawn M., Pandey Anjali
Принадлежит:

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma. 27.-. (canceled)8. The compound of wherein Dis aryl.9. The compound of wherein Dis phenyl or naphthyl.10. The compound of wherein Dis heteroaryl.11. The compound of wherein Dis heterocyclyl.13. (canceled)14. The compound of wherein n is 1.15. The compound of wherein n is 0.1718.-. (canceled)2024.-. (canceled)25. The compound of wherein Dis heterocycloalkyl.2630.-. (canceled)33. (canceled)3545.-. (canceled)4748.-. (canceled)49. The compound of wherein Ris selected from the group consisting of methyl claim 46 , ethyl claim 46 , isopropyl claim 46 , isobutyl claim 46 , benzyl claim 46 , benzyloxymethyl claim 46 , hydroxymethyl claim 46 , methoxymethyl claim 46 , cyclohexylmethyl claim 46 , phenyl claim 46 , cyclopropyl claim 46 , cyclohexyl claim 46 , cyclopropylmethyl claim 46 , ethyl claim 46 , 4-fluorophenylmethyl claim 46 , 3-fluorophenylmethyl claim 46 , 4-pyridinylmethyl claim 46 , 3-pyridinylmethyl claim 46 , 4-hydroxyphenylmethyl claim 46 , 4-methoxyphenylmethyl claim 46 ,5056.-. (canceled)57. A composition of in combination with a pharmaceutically acceptable carrier or diluent.58. A method for inhibiting Syk kinase or a signal transduction pathway mediated at least in part by Syk kinase activity comprising the step of contacting a cell with a compound of .59. A method for treating a condition or disorder mediated at least in part by Syk kinase activity in a subject comprising the step of ...

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Номер записи: 3
04-04-2017 дата публикации

Method for the treatment of hypercholesterolemia

Номер: US0009610273B2
Автор: Muhammed Majeed, Kalyanam Nagabhushanam, Anju Majeed, Sarang Bani, Anjali Pandey, MAJEED MUHAMMED, NAGABHUSHANAM KALYANAM, MAJEED ANJU, BANI SARANG, PANDEY ANJALI, Majeed Muhammed, Nagabhushanam Kalyanam, Majeed Anju, Bani Sarang, Pandey Anjali
Принадлежит: SAMI LABS LIMITED, SAMI LABS LTD

Disclosed is a therapeutic management method of hypercholesterolemia in mammals. More specifically, the present invention relates to a method of reducing high levels of circulating cholesterol (hypercholesterolemia) in the blood stream of mammals, said method involving step of administering therapeutically effective amounts of Calebin A to said mammals to bring about the effects of (i) reducing the amount of total blood cholesterol levels; (ii) reducing the concentrations of low density lipoproteins (LDL) and very low density lipoproteins (VLDL); (iii) increasing the concentrations of high density lipoproteins (HDL) and (iv) reducing concentrations of serum triglycerides.

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Номер записи: 4
31-10-2012 дата публикации

Salts and crystalline forms of a factor xa inhibitor

Номер: CN102762550A
Автор: Pandey Anjali, Quegan Louisa Jane
Принадлежит:

The present invention provides salts and crystalline forms of the compound 5-chloro-N-((1-(4-(2-oxopyridin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide, and pharmaceutical compositions and method of use thereof.

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Номер записи: 5
19-10-2011 дата публикации

Composition for down-regulating pro-inflammatory markers

Номер: CN102218075A
Автор: Majeed Muhammed, Pandey Anjali, Bani Sarang, Bhat Beena
Принадлежит:

The present invention provides a composition for down-regulating pro-inflammatory markers. The composition comprises boswellic acid fraction and polysaccharide faction obtained from Boswellia species at specific concentrations showing enhancement in their activity as compared to boswellic acid fraction and the polysaccharide fraction alone. The invention further comprises use of polysaccharide fraction individually or in combination with boswellic acid fraction for inhibition of PGE2.

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Номер записи: 6
04-09-2013 дата публикации

Benzamides and nicotinamides as syk modulators

Номер: CN103282352A
Автор: Jia Zhaozhong J, Y song, Q xu, Kane Brian, Bauer Shawn M, Pandey Anjali
Принадлежит:

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

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Номер записи: 7
31-10-2012 дата публикации

Methods of synthesizing factor xa inhibitors

Номер: CN102762538A
Автор: Pandey Anjali, Leitao Emilia P. T, Rato Jose, Song Zhiguo Jake
Принадлежит:

Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.

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Номер записи: 8
05-12-2017 дата публикации

Pyridazine compounds as JAK inhibitors

Номер: US0009834548B2
Автор: Qing Xu, Yonghong Song, Anjali Pandey, XU QING, SONG YONGHONG, PANDEY ANJALI, Xu Qing, Song Yonghong, Pandey Anjali
Принадлежит: Portola Pharmaceuticals, Inc., PORTOLA PHARM INC

In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described.

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Номер записи: 9
06-06-2017 дата публикации

Method for the treatment of hypercholesterolemia

Номер: US0009668999B2
Автор: Muhammed Majeed, Kalyanam Nagabhushanam, Anju Majeed, Sarang Bani, Anjali Pandey, MAJEED MUHAMMED, NAGABHUSHANAM KALYANAM, MAJEED ANJU, BANI SARANG, PANDEY ANJALI, Majeed Muhammed, Nagabhushanam Kalyanam, Majeed Anju, Bani Sarang, Pandey Anjali
Принадлежит: SEMI LABS LIMITED, SAMI LABS LTD, SEMI LABS LTD, SAMI LABS LIMITED

Disclosed is a therapeutic management method of hypercholesterolemia in mammals. More specifically, the present invention relates to a method of reducing high levels of circulating cholesterol (hypercholesterolemia) in the blood stream of mammals, said method involving step of administering therapeutically effective amounts of Calebin A to said mammals to bring about the effects of (i) reducing the amount of total blood cholesterol levels; (ii) reducing the concentrations of low density lipoproteins (LDL) and very low density lipoproteins (VLDL); (iii) increasing the concentrations of high density lipoproteins (HDL) and (iv) reducing concentrations of serum triglycerides.

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Номер записи: 10
03-01-2017 дата публикации

Bicyclic dihydropyridone kinase inhibitors

Номер: US0009533986B2
Автор: Anjali Pandey, Yonghong Song, Qing Xu, PANDEY ANJALI, SONG YONGHONG, XU QING, Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит: PORTOLA PHARMACEUTICALS, INC., PORTOLA PHARM INC

Provided are bicyclic dihydropyridone compounds for inhibiting of JAK/Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting JAK/Syk kinase activity, and methods for treating conditions mediated at least in part by JAK/Syk kinase activity.

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Номер записи: 11
09-05-2017 дата публикации

Compounds and methods for purification of serine proteases

Номер: US0009644195B2
Автор: Anjali Pandey, Jack W. Rose, PANDEY ANJALI, ROSE JACK W, Pandey Anjali, Rose Jack W.
Принадлежит: Portola Pharmaceuticals, Inc., PORTOLA PHARM INC

Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

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Номер записи: 12
10-10-2017 дата публикации

Composition comprising scirpusin A and scirpusin B and anti-obesity potential thereof

Номер: US0009782450B2
Автор: Muhammed Majeed, Kalyanam Nagabhushanam, Douglas Kalman, Beena Bhat, Priti Vaidyanathan, Sarang Bani, Anjali Pandey, Suresh Karri, MAJEED MUHAMMED, NAGABHUSHANAM KALYANAM, KALMAN DOUGLAS, BHAT BEENA, VAIDYANATHAN PRITI, BANI SARANG, PANDEY ANJALI, KARRI SURESH, Majeed Muhammed, Nagabhushanam Kalyanam, Kalman Douglas, Bhat Beena, Vaidyanathan Priti, Bani Sarang, Pandey Anjali, Karri Suresh
Принадлежит: SAMI LABS LIMITED, SAMI LABS LTD

Disclosed are methods of managing obesity and hypercholesterolemia using a composition of matter comprising the ethyl acetate fraction of the extract of Cyperus rotundus rhizomes standardized to contain 5% of total stilbenes.

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Номер записи: 13
28-02-2017 дата публикации

Inhibitors of syk and JAK protein kinases

Номер: US0009579320B2
Автор: Zhaozhong J. Jia, Chandrasekar Venkataramani, Wolin Huang, Mukund Mehrotra, Yonghong Song, Qing Xu, Shawn M. Bauer, Jack W. Rose, Brian Kane, Anjali Pandey, JIA ZHAOZHONG J, VENKATARAMANI CHANDRASEKAR, HUANG WOLIN, MEHROTRA MUKUND, SONG YONGHONG, XU QING, BAUER SHAWN M, ROSE JACK W, KANE BRIAN, PANDEY ANJALI, Jia Zhaozhong J., Venkataramani Chandrasekar, Huang Wolin, Mehrotra Mukund, Song Yonghong, Xu Qing, Bauer Shawn M., Rose Jack W., Kane Brian, Pandey Anjali
Принадлежит: Portola Pharmaceuticals, Inc., PORTOLA PHARM INC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 14
21-08-2013 дата публикации

Crystalline forms of a factor Xa inhibitor

Номер: CN103261161A
Автор: Capodanno Vincent R, Corcoran Liam, Mcnevin Michael, Arroyo Itzia Zoraida, Wenslow Robert M, Ball Richard G, Margelefsky Eric L, Maher Timothy K, Pandey Anjali
Принадлежит:

Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof.

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Номер записи: 15
27-02-2018 дата публикации

Benzamides and nicotinamides as Syk modulators

Номер: US0009902688B2
Автор: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey, JIA ZHAOZHONG J, SONG YONGHONG, XU QING, KANE BRIAN, BAUER SHAWN M, PANDEY ANJALI, Jia Zhaozhong J., Song Yonghong, Xu Qing, Kane Brian, Bauer Shawn M., Pandey Anjali
Принадлежит: PORTOLA PHARMACEUTICALS, INC., PORTOLA PHARM INC

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

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Номер записи: 16
16-01-2018 дата публикации

Inhibitors of protein kinases

Номер: US0009868729B2
Автор: Shawn M. Bauer, Anjali Pandey, BAUER SHAWN M, PANDEY ANJALI, Bauer Shawn M., Pandey Anjali
Принадлежит: PORTOLA PHARMACEUTICALS, INC., PORTOLA PHARM INC

Provided are methods of treating inflammatory disorders, autoimmune disorders, or a hematological malignancies using compounds of formula I and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof. Such disorders and conditions include leukemia and Non Hodgkin's Lymphoma.

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Номер записи: 17
18-10-2016 дата публикации

Bicyclic oxa-lactam kinase inhibitors

Номер: US0009469654B2
Автор: Anjali Pandey, Yonghong Song, Qing Xu, PANDEY ANJALI, SONG YONGHONG, XU QING, Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит: PORTOLA PHARMACEUTICALS, INC., PORTOLA PHARM INC

Provided are bicyclic oxa-lactam compounds of formula I: and pharmaceutically acceptable salts thereof which are inhibitors of JAK/Syk kinase. The present disclosure is also directed to intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting JAK/Syk kinase activity, and methods for treating conditions mediated at least in part by JAK/Syk kinase activity.

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Номер записи: 18
13-06-2017 дата публикации

Substituted pyrimidinyl kinase inhibitors

Номер: US0009676756B2
Автор: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Anjali Pandey, BAUER SHAWN M, JIA ZHAOZHONG J, SONG YONGHONG, PANDEY ANJALI, Bauer Shawn M., Jia Zhaozhong J., Song Yonghong, Pandey Anjali
Принадлежит: PORTOLA PHARMACEUTICALS, INC., PORTOLA PHARM INC

Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity.

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Номер записи: 19
16-03-2017 дата публикации

COMPOSITION COMPRISING SCIRPUSIN A AND SCIRPUSIN B AND ANTI-OBESITY POTENTIAL THEREOF

Номер: US20170072003A1
Автор: Muhammed Majeed, Kalyanam Nagabhushanam, Douglas Kalman, Beena Bhat, Priti Vaidyanathan, Sarang Bani, Anjali Pandey, Suresh Karri, MAJEED MUHAMMED, NAGABHUSHANAM KALYANAM, KALMAN DOUGLAS, BHAT BEENA, VAIDYANATHAN PRITI, BANI SARANG, PANDEY ANJALI, KARRI SURESH, Majeed Muhammed, Nagabhushanam Kalyanam, Kalman Douglas, Bhat Beena, Vaidyanathan Priti, Bani Sarang, Pandey Anjali, Karri Suresh
Принадлежит:

Disclosed are methods of managing hypercholesterolemia using a composition of matter comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes. 1Cyperus rotundus. A method of treating hypercholesterolemia in humans , said method comprising step of administering to said humans orally twice a day , composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes to achieve the effects of (a) reduction in the systemic levels of total cholesterol , Low Density Lipoproteins (LDL) , Very Low Density Lipoproteins (VLDL) and serum triglycerides and (b) enhancement in the systemic levels of High Density Lipoproteins (HDL).2Cyperus rotundus. The method according to wherein the composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes consists essentially of piceatannol and dimers thereof.3Cyperus rotundus. The method according to wherein the composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes claim 2 , consists essentially of a combination of piceatannol claim 2 , scirpusin B and scirpusin A.4Cyperus rotundus. A method of treating hypercholesterolemia in humans claim 2 , said method comprising step of administering to said humans orally twice a day claim 2 , composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain greater than 3% of total stilbenes to achieve the effects of (a) reduction in the systemic levels of total cholesterol claim 2 , Low Density Lipoproteins (LDL) claim 2 , Very Low Density Lipoproteins (VLDL) and serum triglycerides and (b) enhancement in the systemic levels of High Density Lipoproteins (HDL).5Cyperus rotundus. The method according to wherein the composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain greater than 3% of ...

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Номер записи: 20
11-12-2013 дата публикации

Anti-obesity potential of Calebin A

Номер: CN103442561A
Автор: Majeed Muhammed, Pandey Anjali
Принадлежит:

The present invention discloses a potential of Calebin A in inhibiting adipogenesis and applications of the Calebin A in obesity management. The present invention elucidates a potential of the Calebin A to favorably modulate mammal biochemical markers associated with obesity. Notable biomodulatory properties of the Calebin A include inhibition of leptin production, capability of increasing adiponectin expression, and capability of inhibiting local (adipocyte) and systemic inflammation which are caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-alpha), Interleukin-6 (IL-6) and Interleukin-1 (IL-1beta).

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Номер записи: 21
12-01-2012 дата публикации

INTRAVENOUS AND ORAL DOSING OF A DIRECT-ACTING AND REVERSIBLE P2Y12 INHIBITOR

Номер: US20120009172A1
Автор: Andre Patrick, Conley Pamela B., Gretler Daniel D., Huang Wolin, Hutchaleelaha Athiwat, Pandey Anjali, PHILLIPS David R., Scarborough Carroll Anna Crew, Scarborough Robert M.
Принадлежит: Portola Pharmaceuticals, Inc.

The invention provides methods and compositions for rapid and reversible inhibition of platelet aggregation in human subjects in need thereof by administering compounds of the formula: 2. The method of claim 1 , wherein the composition is formulated as a unit dose containing from 1 to 50 mg of the compound.3. The method of claim 2 , wherein the unit dose contains from 5 to 40 mg of the compound.4. The method of claim 3 , wherein the unit dose contains from 10 to 30 mg of the compound.5. The method of claim 4 , wherein the unit dose contains from 15 to 25 mg of the compound.6. The method of claim 5 , wherein the unit dose contains about 20 mg of the compound.7. The method of claim 1 , wherein the unit dose contains about 25 mg to 45 mg of the compound.8. The method of claim 1 , wherein the subject has an acute coronary syndrome.9. The method of claim 1 , wherein the subject is need of a reversible inhibition of ADP-induced platelet aggregation.10. The method of claim 9 , wherein the subject is to be scheduled for surgery or other medical procedure associated with bleeding within five days of the administration.11. The method of claim 1 , wherein the composition is administered as a bolus over a period of less than 20 minutes.12. The method of claim 11 , wherein the composition is administered as a bolus over a period of less than 10 minutes.13. The method of claim 12 , wherein the composition is administered as a bolus over a period of less than 5 minutes.14. The method of claim 1 , wherein the subject is further administered aspirin.15. The method of claim 14 , wherein the aspirin is administered orally.16. The method of claim 1 , wherein the subject was predosed with aspirin.17. The method of claim 1 , wherein the compound is formulated as a pharmaceutically acceptable salt.18. The method of claim 17 , wherein the salt is a sodium or potassium salt.19. The method of claim 1 , wherein a substantial degree of the platelet aggregation inhibition develops in the ...

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Номер записи: 22
22-03-2012 дата публикации

CRYSTALLINE FORMS OF A FACTOR Xa INHIBITOR

Номер: US20120071519A1
Автор: Arroyo Itzia Zoraida, Ball Richard G., Capodanno Vincent R., Corcoran Liam, Maher Timothy K., Margelefsky Eric L., McNevin Michael, Pandey Anjali, Wenslow Robert M.
Принадлежит:

Provided herein are crystalline forms of a maleate salt of betrixaban, compositions and methods of preparation or use thereof. 1. A crystalline form of betrixaban maleate , which is Form II.2. The crystalline form of claim 1 , having an X-ray powder diffraction pattern having at least the following approximate characteristic peak locations of 5.0 claim 1 , 9.7 claim 1 , 10.1 claim 1 , 15.3 claim 1 , 17.5 claim 1 , and 19.6 degrees 2θ (each ±0.1 degrees 2θ).3. The crystalline form of claim 2 , wherein the X-ray powder diffraction pattern has at least eight approximate characteristic peak locations selected from 5.0 claim 2 , 9.7 claim 2 , 10.1 claim 2 , 14.6 claim 2 , 15.3 claim 2 , 17.5 claim 2 , 18.0 claim 2 , 18.7 claim 2 , 19.2 claim 2 , 19.6 claim 2 , 22.0 claim 2 , 22.6 claim 2 , 23.0 claim 2 , 23.7 claim 2 , 24.5 claim 2 , 26.5 claim 2 , 26.9 claim 2 , 29.2 claim 2 , 29.5 claim 2 , 30.4 claim 2 , and 35.0 degrees 2θ (each ±0.1 degrees 2θ).43. The crystalline form of claim 1 , having an X-ray powder diffraction pattern approximate to the X-ray powder diffraction pattern shown in or .5. The crystalline form of claim 1 , having a melting point of about 213° C.6. The crystalline form of claim 1 , having a unit cell containing two independent salt pairs of betrixaban and maleic acid wherein the imine N of betrixaban is protonated and forms an ionic H-bond to the maleic acid counter-ion.7. The crystalline form of claim 1 , characterized by a unit cell structure with the following cell parameters at 100 K: a=8.284 Å claim 1 , b=18.082 Å claim 1 , c=18.681 Å claim 1 , α=71.22° claim 1 , β=86.76° claim 1 , γ=89.69° claim 1 , and V=2645 Å.8. The crystalline form of claim 1 , characterized by a unit cell structure with the following cell parameters at 273 K: a=8.419 Å claim 1 , b=18.113 Å claim 1 , c=18.73 Å claim 1 , α=86.71 ° claim 1 , γ=89.31° claim 1 , and V=2699 Å.9. The crystalline form of claim 1 , which is an anhydrate.10. A crystalline form of betrixaban maleate ...

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Номер записи: 23
12-04-2012 дата публикации

FACTOR XA INHIBITORS

Номер: US20120088795A1
Автор: Jia Zhaozhong J., Pandey Anjali, Scarborough Carroll, Scarborough Robert M., Song Yonghong
Принадлежит:

The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such a compound, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample. 128.-. (canceled)3032.-. (canceled)33. The method in accordance with claim 29 , wherein the condition is selected from the group consisting of acute coronary syndrome claim 29 , myocardial infarction claim 29 , unstable angina claim 29 , refractory angina claim 29 , occlusive coronary thrombus occurring post-thrombolytic therapy or post-coronary angioplasty claim 29 , a thrombotically mediated cerebrovascular syndrome claim 29 , embolic stroke claim 29 , thrombotic stroke claim 29 , transient ischemic attacks claim 29 , venous thrombosis claim 29 , deep venous thrombosis claim 29 , pulmonary embolus claim 29 , coagulopathy claim 29 , disseminated intravascular coagulation claim 29 , thrombotic thrombocytopenic purpura claim 29 , thromboangiitis obliterans claim 29 , thrombotic disease associated with heparin-induced thrombocytopenia claim 29 , thrombotic complications associated with extracorporeal circulation claim 29 , thrombotic complications associated with instrumentation claim 29 , and conditions requiring the fitting of prosthetic devices.35. The method in accordance with claim 29 , wherein the pharmaceutically acceptable salt is a pharmaceutically acceptable acid addition salt.36. The method in accordance with wherein the acid addition salt is derived from an inorganic acid.37. The method in accordance with claim 36 , wherein the inorganic acid is selected from the group consisting of hydrochloric claim 36 , hydrobromic claim 36 , nitric claim 36 , carbonic claim 36 , monohydrogencarbonic claim 36 , ...

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Номер записи: 24
12-04-2012 дата публикации

COMPOSITION AND A METHOD OF TREATING CNS DISORDERS AND HYPERPIGMENTATION

Номер: US20120088841A1
Автор: Anand-Tathapudi Susmitha, Bani Sarang, Majeed Muhammed, Pandey Anjali
Принадлежит:

The present invention relates to a method of treating CNS disorders, particularly Alzheimer's disease. The method comprise step of administering to a subject in need thereof a therapeutically effective amount of hydroxychavicol and/or its derivatives or a composition comprising hydroxychavicol and/or its derivatives optionally along with pharmaceutically acceptable excipients. The invention also relates to use of hydroxychavicol and/or its derivatives for treating hyperpigmentation. 1. A method of treating CNS disorders , said method comprising step of administering to a subject in need thereof a therapeutically effective amount of hydroxychavicol and/or its derivatives or a composition comprising hydroxychavicol and/or its derivatives optionally along with pharmaceutically acceptable excipients.2. The method of claim 1 , wherein the disorders are selected from a group comprising Alzheimer's disease claim 1 , Parkinson's disease claim 1 , Huntington's disease and Multiple sclerosis.3. The method of claim 1 , wherein the disorder is Alzheimer's disease.4. The method of claim 1 , wherein the hydroxychavicol and/or its derivatives modulates the activity of secretases.5. The method of claim 4 , wherein the secretases are β-secretase and γ-secretase.6. The method of claim 1 , wherein the hydroxychavicol and/or its derivatives modulates pro-inflammatory cytokines claim 1 , nitric oxide claim 1 , malondialdehyde claim 1 , and cell-surface markers.7. The method of claim 6 , wherein the pro-inflammatory cytokines are TNF-α claim 6 , IL-1β and IL-6 and IFN-γ.8. The method of claim 6 , wherein the cell-surface markers are CD3 and CD-19.9. The method of claim 1 , wherein the hydroxychavicol and/or its derivatives modulates acetylcholinesterase and glutathione.10. The method as claimed in claim 1 , wherein the subject is a human.11. A method of modulating β-amyloid protein claim 1 , said method comprising step of exposing the tissue or cells synthesizing secretases to ...

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Номер записи: 25
19-04-2012 дата публикации

METHODS AND FORMULATIONS OF TREATING THROMBOSIS WITH BETRIXABAN AND A P-GLYCOPROTEIN INHIBITOR

Номер: US20120095019A1
Автор: Arroyo Itzia Zoraida, Ball Richard G., Capodanno Vincent R., Corcoran Liam, Denney William, LAURING Brett, Maher Timothy K., Mansoor George A., Margelefsky Eric L., McNevin Michael, Pandey Anjali, Sinha Uma, Vosatka Anne Hermanowski, Wenslow Robert M.
Принадлежит:

This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods. 1. A method for treating thrombosis or inhibiting blood coagulation in a patient receiving administration of a P-glycoprotein inhibitor , the method comprising administering to the patient a subtherapeutic dose of betrixaban.2. The method of claim 1 , wherein the amount of betrixaban administered is about 20% less than the therapeutically effective amount.3. The method of claim 1 , wherein the amount of betrixaban administered is about 50% less than the therapeutically effective amount.4. The method of claim 1 , wherein the patient is a human patient and the patient is administered an aggregate daily dose of about 25 to about 35 mg of betrixaban.5. The method of claim 1 , wherein the patient is a human patient and the patient is administered an aggregate daily dose of about 10 to about 20 mg of betrixaban.6. The method of claim 1 , wherein betrixaban is administered to the patient once daily or twice daily.7. The method of claim 1 , wherein the patient receives the administration of the P-glycoprotein inhibitor at least half an hour before or after administration of betrixaban.8. The method of claim 1 , wherein the patient is concurrently administered with the P-glycoprotein inhibitor and betrixaban.9. The method of claim 1 , wherein the patient receives administration of an therapeutically effective amount of the P-glycoprotein inhibitor.10. The method of claim 1 , wherein the P-glycoprotein inhibitor is in a controlled release form.11. The method of claim 1 , wherein the P-glycoprotein inhibitor is selected from the group consisting of verapamil claim 1 , amiodarone and ketoconazole.12. The method of claim 11 , wherein the P-glycoprotein inhibitor is verapamil.13. The method of claim 12 , wherein verapamil is administered in an amount of about 100 ...

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Номер записи: 26
03-05-2012 дата публикации

NICOTINAMIDES AS JAK KINASE MODULATORS

Номер: US20120108566A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Kane Brian, Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)29. A compound selected from the group consisting of:6-(4-(4-acetylpiperazin-1-yl)phenylamino)-2-(cyclobutylamino)nicotinamide; 6-(4-(4-acetylpiperazin-1-yl)phenylamino)-4-(benzylamino)nicotinamide; (S)-4-(benzylamino)-6-(4-(3-(methylcarbamoyl)piperidin-1-yl)phenylamino)nicotinamide; 6-(4-(4-acetylpiperazin-1-yl)-3-methylphenylamino)-4-(benzylamino)nicotinamide; and (R)-4-(benzylamino)-6-(4-(3-(methylcarbamoyl)piperidin-1-yl)phenylamino)nicotinamide; (-(benzylamino)-6-(3-morpholinophenylamino)nicotinamide; 6-(4-fluoro-3-(pyrrolidine-1-carboxamido)phenylamino)-4-(pyridin-3-ylmethylamino)nicotinamide; (-(4-(4-acetylpiperazin-1-yl)phenylamino)-4-(phenethylamino)nicotinamide; 4-(benzylamino)-6-(4-(dimethylcarbamoyl)phenylamino)-N,N-dimethylnicotinamide; 4-(cyclopentylmethylamino)-6-(4-methoxyphenylamino)nicotinamide; 6-(4-methoxyphenylamino)-4-(p-tolylamino)nicotinamide; 4,6-bis(4-methoxyphenylamino)nicotinamide; 4-((1-acetylpiperidin-4-yl)methylamino)-6-(4-methoxyphenylamino)nicotinamide; (S)-4-(1-acetylpiperidin-3-ylamino)-6-(4-methoxyphenylamino)nicotinamide; (R)-4-(1-acetylpiperidin-3-ylamino)-6-(4-methoxyphenylamino)nicotinamide; (S)-4-((1-acetylpiperidin-3-yl)methylamino)-6-(4- ...

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Номер записи: 27
24-05-2012 дата публикации

[4-(6-FLUORO-7-METHYLAMINO-2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL)-PHENYL]-5-CHLORO-THIOPHEN-2-YL-SULFONYLUREA SALTS, FORMS AND METHODS RELATED THERETO

Номер: US20120129876A1
Автор: Huang Wolin, Nieder Matthew, Pandey Anjali, QUEGAN Louisa Jane, Sharp Emma, Wang Juan
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention provides novel sulfonylurea salts of a salt of formula (I) 29.-. (canceled)1112.-. (canceled)1415.-. (canceled)1718.-. (canceled)20. (canceled)2223.-. (canceled)2526.-. (canceled)2830.-. (canceled)31. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to and a pharmaceutically acceptable vehicle or carrier.3242.-. (canceled)43. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to and an additional therapeutic agent.44. (canceled)45. A pharmaceutical composition for preventing or treating a condition in a mammal characterized by undesired thrombosis comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a salt of .4751.-. (canceled)52. A method for preventing or treating thrombosis and thrombosis related conditions in a mammal comprising the step of administering to a mammal a therapeutically effective amount of a salt of .53. A method for preventing or treating a condition or disorder mediated at least in part by ADP-induced platelet aggregation in a mammal comprising the step of administering to a mammal in need of such treatment in a therapeutically effective amount of a composition of or a pharmaceutically acceptable salt thereof.54. A method for inhibiting the coagulation of a blood sample comprising the step of contacting said sample with said salt a salt of .5564.-. (canceled)65. A method for preventing the occurrence of a secondary ischemic event comprising administering to a patient who has suffered a primary ischemic event a therapeutically effective amount of a salt of claim 1 , together with a pharmaceutically acceptable carrier.6667.-. (canceled)68. A method for the preparation of a pharmaceutical composition comprising admixing a therapeutically effective amount of the salt of with a pharmaceutically acceptable vehicle or carrier. The present application is a continuation of U.S. patent application ...

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Номер записи: 28
24-05-2012 дата публикации

Inhibitors of syk and jak protein kinases

Номер: US20120130073A1
Автор: Anjali Pandey, Brian Kane, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 29
07-06-2012 дата публикации

BENZAMIDES AND NICOTINAMIDES AS SYK MODULATORS

Номер: US20120142671A1
Автор: Bauer Shawn M., Jia Zhaozhong J., Kane Brian, Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma. 630-. (canceled)44. The compound of wherein Ris selected from the group methyl or fluoro.48. The compound of wherein Ris selected from the group consisting of Calkyl claim 47 , Ccycloalkyl claim 47 , aryl claim 47 , heteroaryl and heterocyclyl.49. The compound of wherein Ris selected from the group consisting of methyl claim 47 , ethyl claim 47 , isopropyl claim 47 , isobutyl claim 47 , benzyl claim 47 , benzyloxymethyl claim 47 , hydroxymethyl claim 47 , methoxymethyl claim 47 , cyclohexylmethyl claim 47 , phenyl claim 47 , cyclopropyl claim 47 , cyclohexyl claim 47 , cyclopropylmethyl claim 47 , ethyl claim 47 , 4-fluorophenylmethyl claim 47 , 3-fluorophenylmethyl claim 47 , 4-pyridinylmethyl claim 47 , 3-pyridinylmethyl claim 47 , 4-hydroxyphenylmethyl claim 47 , 4-methoxyphenylmethyl claim 47 ,5056-. (canceled)57. A composition comprising a compound of in combination with a pharmaceutically acceptable carrier or diluent.58. A method for inhibiting Syk kinase or a signal transduction pathway mediated at least in part by Syk kinase activity comprising the step of contacting a cell with a compound of .59. A method for treating a condition or disorder mediated at least in part by Syk kinase activity in a subject comprising the step of administering to a subject in need of such treatment a therapeutically effective amount of a composition of .6068-. (canceled)69. A kit comprising a composition of claim 57 , ...

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Номер записи: 30
10-01-2013 дата публикации

Anti-obesity Potential of Calebin A

Номер: US20130012579A1
Автор: Majeed Muhammed, Pandey Anjali
Принадлежит:

The present invention discloses the potential of Calebin A in inhibiting adipogenesis and applications thereof in obesity management. The present invention elucidates the potential of Calebin A to favorably modulate biochemical markers associated with obesity. Notable biomodulatory properties of Calebin A include inhibiting leptin production, increasing adiponectin expression and inhibiting local (adipocyte) and systemic inflammation caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-α), Interleukin-6 (IL-6) and Interleukin-1 (IL-1β). 1. A method of inhibiting adipogenesis , said method comprising step of bringing into contact the adipocytes with an effective amount of Calebin A.2. A method of inhibiting leptin expression in adipocytes , said method comprising step of bringing into contact the adipocytes with an effective amount of Calebin A.3. A method of increasing expression of adiponectin in adipocytes , said method comprising step of bringing into contact the adipocytes with an effective amount of Calebin A.4. A method of inhibiting obesity induced pro-inflammatory cytokines in adipocytes , said method comprising step of bringing into contact the adipocytes with an effective amount of Calebin A.5. The method according to claim 4 , wherein the pro-inflammatory cytokine is Tumor Necrosis Factor-α (TNF-α).6. The method according to claim 4 , wherein the pro-inflammatory cytokine is Interleukin-6 (IL-6).7. The method according to claim 4 , claim 4 , and claim 4 , wherein the adipocytes are human adipocytes.8. A method of reducing obesity induced systemic expression of pro-inflammatory cytokines claim 4 , said method comprising step of administering an effective amount of Calebin A to a subject in need thereof.9. The method according to claim 8 , wherein the pro-inflammatory cytokine is Tumor Necrosis Factor-α (TNF-α).10. The method according to claim 8 , wherein the pro-inflammatory cytokine is Interleukin-6 (IL-6).11. The method according to claim 8 , ...

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Номер записи: 31
31-01-2013 дата публикации

Inhibitors of protein kinases

Номер: US20130029944A1
Автор: Anjali Pandey, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 32
28-03-2013 дата публикации

ADAPTOGENIC ACTIVITY OF LABISIA PUMILA EXTRACT

Номер: US20130078323A1
Автор: Bani Sarang, Chandan Balkrishan, Chauhan Prashant Singh, Gupta Bishan Dutt, Gupta Devinder Kumar, Koul Surrinder, Kour Kiranjeet, Lal Shankar, Marnickavasagar Rajendran, Pandey Anjali, Sangwan Payarelal, Sharma Neelam, Singh Kuldeep
Принадлежит: HOLISTA BIOTECH SDN. BHD.

The present invention provides a process of extracting the leaves of with water into a free flowing powder using accelerated solvent system and drying. The invention also relates to the immunopotentiating effects of the extract against stress. The extract has effects on fatigue, hypoxia time, potentiation of swimming endurance, bod weight, weight of the thymus and spleen and levels of CD244+ NK cells, CD4+ and CD8+ T cells, expression of ThI cytokines IL-2 and IFN-gamma, corticosterone, glutathione, alanine aminotransferase and lipid peroxidation levels. 1Labisia pumila. A process of extracting the leaves of with water into a free flowing powder using accelerated solvent system and drying.2Labisia pumila. The process as claimed in claim 1 , wherein the aqueous leaf extract is administered systemically and orally.3Labisia pumila. The process as claimed in claim 1 , wherein adaptogen activity of the aqueous leaf extract provides anti-fatigue effect with maximum effect at 100 mg/kg p.o.4Labisia pumila. The process as claimed in claim 1 , wherein adaptogen activity of the aqueous leaf extract provides enhancement in the Hypoxia time.5Labisia pumila. The process as claimed in claim 1 , wherein adaptogen activity of the aqueous leaf extract provides higher potentiation in swimming endurance.6Labisia pumila. The process as claimed in claim 1 , wherein adaptogen activity of the aqueous leaf extract provides recovery of restraint stress induced depletion of CD244+ NK cells.7Labisia pumila. The process as claimed in claim 6 , wherein adaptogen activity of the aqueous leaf extract provides recovery in the restraint stress induced depleted CD4+ and CD8+ T cell population.8Labisia pumila. The process as claimed in claim 7 , wherein adaptogen activity of the aqueous leaf extract provides increased expression of Th1 cytokines IL-2 and IFN-gamma in restraint stress induced experimental animals.9Labisia pumila. The process as claimed in claim 1 , wherein adaptogen activity of the ...

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Номер записи: 33
23-05-2013 дата публикации

PYRAZINE KINASE INHIBITORS

Номер: US20130131040A1
Автор: Bauer Shawn M., Jia Zhaozhong J., Kane Brian, Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. 2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is H.3. A compound of or claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.4. A compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , isopropyl claim 1 , sec-butyl claim 1 , tert-butyl claim 1 , methyl claim 1 , ethyl claim 1 , CFCH— claim 1 , CHFCH— claim 1 , methoxymethylene claim 1 , methylsulfinylethylene claim 1 , and methylsulfonylethylene.5. A compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Ccycloalkyl claim 1 , CcycloalkylCalkylene claim 1 , aryl claim 1 , arylCalkylene or heteroarylCalkylene each of which is optionally substituted with one to five groups independently selected from halo claim 1 , C-Calkyl claim 1 , and amino.6. A compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of cyclopropyl claim 5 , cyclopropylmethylene claim 5 , phenyl and benzyl.7. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Rand Rare independently selected from the group consisting of Calkyl and Calkoxy.8. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein V is heteroaryl optionally substituted with one to five Rgroups.9. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein V is cycloalkyl optionally substituted with one to five Rgroups.10. A compound of any one of to claim 5 , or a ...

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Номер записи: 34
30-05-2013 дата публикации

INHIBITORS OF JAK

Номер: US20130137673A1
Автор: Bauer Shawn M., Huang Wolin, Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity. 3. The compound of wherein Yis N.4. The compound of wherein Yis CH.6. The compound of wherein Ris H.8. The compound of any one of the preceding claims wherein Ris Ccycloalkyl claim 1 , optionally substituted with hydroxyl.9. The compound of wherein Ris cyclopropyl claim 8 , cyclobutyl claim 8 , cyclopentyl or cyclohexyl claim 8 , each of which is optionally substituted with hydroxyl.10. The compound of any one of to wherein Ris Calkyl claim 8 , optionally substituted with from 1 to 3 substituents selected from the group consisting of Calkynyl claim 8 , hydroxy claim 8 , halogen claim 8 , Calkoxy claim 8 , cyano claim 8 , aminocarbonyl claim 8 , Ccycloalkyl claim 8 , aryl claim 8 , haloaryl claim 8 , heteroaryl claim 8 , heterocyclyl claim 8 , and heterocyclylcarbonyl.11. The compound of any one of to wherein Ris —CH claim 8 , —CHCH claim 8 , —CH(CH) claim 8 , —C(CH) claim 8 , or —CHCHCH(CH).12. The compound of any one of to wherein Ris Calkyl claim 8 , substituted with from 1 to 3 substituents selected from the group consisting of Calkynyl claim 8 , hydroxy claim 8 , halogen claim 8 , Calkoxy claim 8 , cyano claim 8 , aminocarbonyl and Ccycloalkyl.13. The compound of wherein Ris —CHC≡CH claim 12 , —CHCF claim 12 , —CH-cPr claim 12 , —CHCHOCH claim 12 , or CHCHCHOCH.14. The compound of any one of to wherein Ris Calkyl claim 12 , substituted with from 1 to 3 substituents selected from the group consisting of aryl claim 12 , haloaryl claim 12 , Calkylaryl claim 12 , Calkoxyaryl claim 12 , heteroaryl claim ...

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Номер записи: 35
27-06-2013 дата публикации

INHIBITORS OF SYK AND JAK PROTEIN KINASES

Номер: US20130165431A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Kane Brian, Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Venkataramani Chandrasekar, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 177.-. (canceled)80. The method of claim 79 , wherein the condition or disorder is selected from the group consisting of cardiovascular disease claim 79 , inflammatory disease and autoimmune disease and cell proliferative disorder.81. The method of claim 79 , wherein said cardiovascular disease is selected from the group consisting of restenosis claim 79 , thrombosis claim 79 , immune thrombocytopenic purpura claim 79 , heparin induced thrombocytopenia claim 79 , dilated cardiomyopathy claim 79 , sickle cell disease claim 79 , atherosclerosis claim 79 , myocardial infarction claim 79 , vascular inflammation claim 79 , unstable angina and acute coronary syndromes.82. The method of claim 79 , wherein said inflammatory disease is selected from the group consisting of allergy claim 79 , asthma claim 79 , rheumatoid arthritis claim 79 , B Cell mediated diseases such as Non Hodgkin's Lymphoma claim 79 , anti phospholipid syndrome claim 79 , lupus claim 79 , psoriasis claim 79 , multiple sclerosis and end stage renal disease.83. The method of claim 79 , wherein said cardiovascular disease is selected from the group consisting of thrombosis claim 79 , immune thrombocytopenic purpura claim 79 , and heparin induced thrombocytopenia.84. The method of claim 79 , wherein said inflammatory disease is rheumatoid arthritis or Non Hodgkin's Lymphoma.85. The method of claim 79 ...

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Номер записи: 36
15-08-2013 дата публикации

METHODS OF SYNTHESIZING FACTOR Xa INHIBITORS

Номер: US20130211094A1
Автор: Anjali Pandey, Emilia P.T. Leitao, Jose Rato, Zhiguo Jake Song
Принадлежит: Millennium Pharmaceuticals Inc, Portola Pharmaceuticals LLC

Described herein are novel methods of preparing a compound of Formula II or a pharmaceutically acceptable salt thereof. In some embodiments, the method is for preparing betrixaban or a pharmaceutically acceptable salt thereof. Also described are compositions comprising substantially pure betrixaban free base or salt thereof.

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Номер записи: 37
12-09-2013 дата публикации

Combination therapy of 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide and fludarabine

Номер: US20130237493A1
Автор: Anjali Pandey, Uma Sinha
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma.

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Номер записи: 38
19-09-2013 дата публикации

COMBINATION THERAPY WITH 4-(3-(2H-1,2,3-TRIAZOL-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO)PYRIMIDINE-5-CARBOXAMIDE

Номер: US20130244963A1
Автор: Pandey Anjali, Sinha Uma
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing a SYK inhibitor, or a pharmaceutically acceptable salt thereof, and a antineoplastic or antiinflammatory agent for the treatment of inflammatory, autoimmune and cell proliferative diseases, such as allergic reaction, transplant rejection, rheumatoid arthritis (RA), lupus, multiple sclerosis (MS) or psoriasis undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL) (including diffuse large B cell lymphoma (DLBCL)), mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic (SLL), Lymphoma, multiple myeloma, asthma, vasculitis, Idiopathic thrombocytopenic purpura (ITP), Heparin Induced Thrombocytopenia (HIT) and hemolytic anemia. 1. A composition for treating a cell proliferative disorder selected from the group consisting of leukemia , a lymphoma , myeloproliferative disorders , hematological malignancies , and chronic idiopathic myelofibrosis comprising administering to said mammal a therapeutically effective amount of an agent 4-(3-(2H-1 ,2 ,3-triazol-2-yl)phenylamino)-2-((1R ,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide , or a pharmaceutically acceptable salt thereof; and an antineoplastic agent.2. The composition of claim 1 , wherein the antineoplastic agent is selected from the group consisting of a topoisomerase II inhibitor claim 1 , aribonucleotide reductase inhibitor claim 1 , a DNA polymerase inhibitor claim 1 , and combinations thereof.3. The composition of claim 1 , wherein the antineoplastic agent is selected from the group consisting of azacitidine claim 1 , cladribine claim 1 , decitabine. gemcitabine claim 1 , mercaptopurine claim 1 , thioguanine claim 1 , clofarabine claim 1 , troxacitabine claim 1 , and pentostatin claim 1 , Methotrexate (MTX) claim 1 , sulfosalazine claim 1 , Dexamethasone claim 1 , Bendamustine claim 1 , ...

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Номер записи: 39
26-09-2013 дата публикации

COMBINATION THERAPY OF 4-(3-(2H-1,2,3-TRIAZO-2-YL)PHENYLAMINO)-2-((1R,2S)-2-AMINOCYCLOHEXYLAMINO)PYRIMIDINE-5-CARBOXAMIDE AND FLUDARABINE

Номер: US20130252917A1
Автор: Pandey Anjali, Sinha Uma
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing 4-(3-(2H-1,2,3-triazol-2-yl)phenylamino)-2-(1R,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide, or a pharmaceutically acceptable salt thereof, and fludarabine for the treatment of cell proliferative disorders, such as undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL), including diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic Lymphoma (SLL) and multiple myeloma. 1. A composition for treating a cell proliferative disorder selected from the group consisting of leukemia , a lymphoma , myeloproliferative disorders , hematological malignancies , and chronic idiopathic myelofibrosis comprising administering to said mammal a therapeutically effective amount of an agent 4-(3-(2H-1 ,2 ,3-triazol-2-yl)phenylamino)-2-((1R ,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide , or a pharmaceutically acceptable salt thereof; and fludarabine or a pharmaceutically acceptable salt thereof.2. The composition claim 1 , wherein the pharmaceutically acceptable salt of 4-(3-(2H-1 claim 1 ,2 claim 1 ,3-triazol-2-yl)phenylamino)-2(1R claim 1 ,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide is the hydrochloride or acetate salt.3. The composition of claim 1 , wherein the pharmaceutically acceptable salt of fludarabine is the phosphate salt.4. The composition of claim 1 , wherein at least one of the agents is in a sub-therapeutic dosage.5. The composition of claim 1 , wherein the two of the agents are in sub-therapeutic dosages.6. The composition of claim 1 , wherein the composition is administered intravenously claim 1 , subcutaneously claim 1 , or orally.7. (canceled)8. (canceled)9. (canceled)10. A method for treating a cell proliferative disorder selected from the group consisting of leukemia claim 1 , a ...

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Номер записи: 40
17-10-2013 дата публикации

QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS

Номер: US20130274252A1
Автор: Ichimura Michio, Ide Shinichi, Matsuno Kenji, Nomoto Yuji, Oda Shoji, Pandey Anjali, Sasaki Junko, Scarborough Robert M., TSUKUDA Eiji
Принадлежит:

The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. 112-. (canceled)14. A pharmaceutical composition comprising an effective amount of a nitrogen-containing heterocyclic compound according to claim 13 , or a pharmaceutically acceptable salt or hydrate thereof claim 13 , and a pharmaceutically acceptable diluent or carrier.15. A method of inhibiting phosphorylation of PDGF receptor in a patient comprising the step of administering a compound of and all pharmaceutically acceptable salts and hydrates thereof to the patient.16. A method for inhibiting abnormal cell growth and cell wandering in a patient and thereby preventing or treating a cell-proliferative disease claim 14 , comprising the step of administering a composition according to to the patient.18. The method of claim 17 , wherein Ris a member selected from the group consisting of CN claim 17 , —O-methyl claim 17 , —O-ethyl claim 17 , —O-propyl claim 17 , —O-isopropyl claim 17 , —O-butyl claim 17 , —O-t-butyl claim 17 , —O-isoamyl claim 17 , 1-naphthyloxy claim 17 , 2-naphthyloxy claim 17 , 4-indolyloxy claim 17 , 5-indolyloxy claim 17 , 5-isoquinolyloxy claim 17 ,and all pharmaceutically acceptable salts and hydrates of such compounds.23. The method of claim 22 , wherein Ris a member selected from ...

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Номер записи: 41
28-11-2013 дата публикации

OXYPYRIMIDINES AS SYK MODULATORS

Номер: US20130317029A1
Автор: Huang Wolin, Jia Zhaozhong J., Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 2. The compound of wherein Ris H.3. The compound of wherein Ris Calkyl.67.-. (canceled)8. The compound of wherein Yis phenyl.9. The compound of wherein Dis aryl.1018.-. (canceled)19. The compound of wherein Dis Ccycloalkyl.20. (canceled)21. The compound of wherein Dis heteroaryl.22. The compound of wherein Xis NH.23. The compound of wherein Xis S.2433.-. (canceled)34. The compound of claim 1 , wherein each Ris independently selected from the group consisting of Ris independently selected from the group consisting of Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , hydroxyl claim 1 , Calkoxy claim 1 , oxo claim 1 , halo claim 1 , Calkylcarbonyl claim 1 , aminocarbonyl claim 1 , Calkylcarbonylamino; Calkylaminocarbonyl; aminosulfonyl claim 1 , heteroaryl and heterocyclyl.3544.-. (canceled)4653.-. (canceled)55. (canceled)56. A compound of selected from the group consisting of (R)-2-(1-amino-3-methyl-1-oxobutan-2-ylamino)-4-(3 claim 1 ,5-dimethylphenylamino)-6-methoxypyrimidine-5-carboxamide; (R)-2-(1-amino-3-methyl-1-oxobutan-2-ylamino)-4-(3 claim 1 ,5-dimethylphenylamino)-6-oxo-1 claim 1 ,6-dihydropyrimidine-5-carboxamide; 2-((1R claim 1 ,2S)-2-aminocyclohexylamino)-4-(3-(2H-1 claim 1 ,2 claim 1 ,3-triazol-2-yl)phenylamino)-6-methoxypyrimidine-5-carboxamide; (R)-2-(1-amino-3-methyl-1-oxobutan-2-ylamino)-4-(3 claim 1 ,5-dimethylphenylamino)-6- ...

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Номер записи: 42
26-12-2013 дата публикации

1,2,4-triazine-6-carboxamide kinase inhibitors

Номер: US20130345191A1
Автор: Anjali Pandey, Brian Kane, Jack Rose, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

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Номер записи: 43
30-01-2014 дата публикации

INHIBITORS OF PROTEIN KINASES

Номер: US20140031361A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Venkataramani Chandrasekar, Xu Qing
Принадлежит:

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 110.-. (canceled)13. The method of claim 12 , wherein the condition or disorder is selected from the group consisting of cardiovascular disease claim 12 , inflammatory disease and autoimmune disease.14. The method of claim 13 , wherein said cardiovascular disease is selected from the group consisting of restenosis claim 13 , thrombosis claim 13 , immune thrombocytopenic purpura claim 13 , heparin induced thrombocytopenia claim 13 , dilated cardiomyopathy claim 13 , sickle cell disease claim 13 , atherosclerosis claim 13 , myocardial infarction claim 13 , vascular inflammation claim 13 , unstable angina and acute coronary syndromes.15. The method of claim 13 , wherein said inflammatory disease is selected from the group consisting of allergy claim 13 , asthma claim 13 , rheumatoid arthritis claim 13 , B Cell mediated diseases such as Non Hodgkin's Lymphoma claim 13 , anti phospholipid syndrome claim 13 , lupus claim 13 , psoriasis claim 13 , multiple sclerosis and end stage renal disease (platelet component).16. The method of claim 13 , wherein said cardiovascular disease is selected from the group consisting of thrombosis claim 13 , immune thrombocytopenic purpura claim 13 , and heparin induced thrombocytopenia.17. The method of claim 13 , wherein said inflammatory disease is rheumatoid arthritis or Non Hodgkin's Lymphoma.18. The method of ...

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Номер записи: 44
06-01-2022 дата публикации

COMPOUNDS AND METHODS OF USE

Номер: US20220002280A1
Автор: CHEN Ruihong, Duraiswamy Athisayamani Jeyaraj, Jiang Chun, KALITA Biswajit, Pandey Anjali
Принадлежит:

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent. 128-. (canceled)30. The method of claim 29 , wherein the cell is a cancer cell.32. The method of claim 31 , wherein the cancer is adrenocortical cancer claim 31 , anal cancer claim 31 , biliary cancer claim 31 , bladder cancer claim 31 , bone cancer claim 31 , brain cancer claim 31 , breast cancer claim 31 , cervical cancer claim 31 , colon cancer claim 31 , endometrial cancer claim 31 , esophageal cancer claim 31 , head and neck cancer claim 31 , hematologic cancer claim 31 , intestinal cancer claim 31 , liver cancer claim 31 , lung cancer claim 31 , oral cancer claim 31 , ovarian cancer claim 31 , pancreatic cancer claim 31 , renal cancer claim 31 , prostate cancer claim 31 , salivary gland cancer claim 31 , skin cancer claim 31 , stomach cancer claim 31 , testicular cancer claim 31 , throat cancer claim 31 , thyroid cancer claim 31 , uterine cancer claim 31 , vaginal cancer claim 31 , sarcoma claim 31 , or a soft tissue carcinoma.33. The method of claim 32 , wherein the cancer is osteosarcoma claim 32 , glioma claim 32 , astrocytoma claim 32 , neuroblastoma claim 32 , cancer of the small intestine claim 32 , bronchial cancer claim 32 , small cell lung cancer claim 32 , non-small cell lung cancer claim 32 , basal cell carcinoma claim 32 , or melanoma.34. The method of claim 32 , wherein the cancer is a hematologic cancer.35. The method of claim 33 , wherein the hematologic cancer is acute lymphoblastic leukemia (ALL) claim 33 , acute myeloid leukemia (AML) claim 33 , Hodgkin's lymphoma claim 33 , Non-Hodgkin's lymphoma claim 33 , Burkitt's lymphoma claim 33 , chronic lymphocytic leukemia (CLL) claim 33 , chronic myelogenous leukemia (CML) claim 33 , Hairy Cell chronic myelogenous leukemia (CML) claim 33 , or multiple myeloma.36. The method of claim 31 , further ...

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Номер записи: 45
14-01-2016 дата публикации

CYCLOHEXANEDIAMINE COMPOUNDS AND METHODS FOR THEIR PREPARATION

Номер: US20160009694A1
Автор: Pandey Anjali
Принадлежит:

The present invention provides processes for the preparation of cyclohexanediamine compounds of formula Ia and intermediates thereof. The compounds are useful as Syk kinase inhibitors and in various pharmaceutical compositions, and particularly useful for treating conditions mediated at least in part by Syk kinase activity. 2. The process of claim 1 , wherein step (b) further comprises (i) contacting a compound of Formula (Ic) with a deprotecting reagent and subsequently with a base to provide a compound of Formula (Ia) as a free base; and(ii) optionally contacting the free base of Formula (Ia) with an acid to provide a salt of Formula (Ia).4. The process of claim 1 , wherein X is halo or —S(O)C-Calkyl; and n is 0 claim 1 , 1 or 2.5. The process of claim 1 , wherein P is t-Boc.6. The process of claim 3 , wherein the alkoxide is sodium ethoxide.7. The process of claim 1 , wherein in step (a) X is —SCHwhich is contacted with an oxidizing agent before the compound of Formula (Ib) is contacted with a compound of Formula (II).8. The process of claim 7 , wherein in step (a) the oxidizing agent is 3-chloroperbenzoic acid.9. The process of claim 2 , wherein in step (b) the deprotecting reagent is hydrochloric acid.10. The process of claim 2 , wherein in step (b) the acid is acetic acid and the compound of Formula (Ia) is an acetate salt.12. The process of claim 11 , wherein the compound of Formula (II) has an enantiomeric excess of at least 98% e.e.13. The process of claim 11 , wherein the base is potassium carbonate.16. The process of claim 15 , wherein in step (d) the base is sodium hydroxide.17. The process of claim 15 , wherein in step (e) the reducing agent is Hand Pd(OH).18. The process of claim 15 , wherein in step (f) the alkylsulfonylhalide is methanesulfonyl chloride and Y is —OS(O)CHin Formula (VIII).19. The process of claim 15 , wherein in step (g) a crown ether such as 15-crown-5 is added.20. The process of claim 15 , wherein in step (h) the reducing agent is ...

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Номер записи: 46
24-04-2014 дата публикации

SUBSTITUTED PICOLINAMIDE KINASE INHIBITORS

Номер: US20140113931A1
Автор: Bauer Shawn M., Jia Zhaozhong J., Kane Brian, Pandey Anjali, Song Yonghong, Sran Arvinder, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. 2. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein T is phenyl substituted with 1 to 5 R.3. (canceled)4. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein T is monocyclic or bicyclic heteroaryl comprising 1-4 heteroatoms selected from S claim 1 , O and N claim 1 , optionally substituted with 1 to 5 R.5. (canceled)6. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein at least one Ris -L-W.7. (canceled)9. (canceled)10. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein W or Bis substituted with 1 to 3 R.11. A compound of or a tautomer or a pharmaceutically acceptable salt thereof wherein Rand Rare independently selected from the group consisting of halo claim 8 , Calkyl claim 8 , haloCalkyl claim 8 , cyano claim 8 , oxo claim 8 , OH claim 8 , O(Calkyl) claim 8 , and O(haloCalkyl).13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. (canceled)30. (canceled)31. (canceled)32. (canceled)33. (canceled)34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)40. (canceled)41. A compound or a tautomer or a pharmaceutically acceptable salt thereof having a structure selected from:(R)-5-(1-amino-4-methyl-1-oxopentan-2-ylamino)-3-(3-methylisothiazol-5-ylamino)picolinamide;5-((1R,2R)-2-amino-3,3-difluorocyclohexylamino)-3-(3-methylisothiazol-5-ylamino)picolinamide;(R)-5-(1-amino-3-cyclopropyl-1-oxopropan-2-ylamino)-3-(3-methylisothiazol-5-ylamino)picolinamide;5-((1R,2S)-2-aminocyclohexylamino)-3-(3-methylisothiazol-5- ...

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Номер записи: 47
17-02-2022 дата публикации

PHENYLPIPERAZINE PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) MODULATORS AND THEIR USE

Номер: US20220047582A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Monroe Kyle D., Muehlemann Michael M., Pandey Anjali
Принадлежит:

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels. 112.-. (canceled)14. The method of claim 13 , wherein an uptake of LDL by hepatocytes in the subject is modulated.15. The method of claim 13 , wherein said metabolic disease is diabetes.16. The method of claim 13 , wherein the compound of formula I is formulated as a pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient.17. The method of claim 16 , wherein said pharmaceutical composition further comprises a second pharmaceutical drug compound.18. The method of claim 17 , wherein said second pharmaceutical drug compound is selected from the group consisting of a statin claim 17 , a cardiovascular drug claim 17 , a metabolic drug claim 17 , and an antihypertensive drug.19. The method of claim 13 , wherein the compound is selected from the group consisting of:N-phenyl-4-(piperazin-1-yl)benzenesulfonamide;N-isopropyl-4-((4-(piperazin-1-yl)phenyl)sulfonamido)benzamide;N-methyl-4-((4-(piperazin-1-yl)phenyl)sulfonamido)benzamide;N-(3,4-dimethylphenyl)-4-(piperazin-1-yl)benzenesulfonamide;N-(3,5-dimethylphenyl)-4-(piperazin-1-yl)benzenesulfonamide;N-(3,5- ...

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Номер записи: 48
30-01-2020 дата публикации

SOLID FORMS OF CERDULATINIB

Номер: US20200031804A1
Автор: Chen Ying, Fernandes Philippe, Karaborni Sami, Kodersha Gus, Lu Yuelie, Northen Julian Scott, Pandey Anjali
Принадлежит:

Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof. 3. The salt of claim 2 , characterized by an X-ray powder diffractogram comprising peaks at 8.7 claim 2 , 15.9 claim 2 , and 20.0 °2θ claim 2 , each ±0.2 °2θ claim 2 , as determined on a diffractometer using Cu—Kα radiation (Compound I HCl Form I).4. The salt of claim 3 , further characterized by one or more peaks at 11.5 claim 3 , 22.5 claim 3 , and 25.5 °2θ claim 3 , each ±0.2 °2θ.5. The salt of claim 3 , further characterized by a differential scanning calorimetry curve comprising an endotherm with onset at about 288° C.6. A pharmaceutical composition comprising one or more pharmaceutically acceptable carriers claim 1 , and a therapeutically effective amount of a salt of .7. The pharmaceutical composition of claim 1 , wherein the salt comprises at least about 50% w/w of Compound I HCl Form I of .8. A pharmaceutical composition comprising a salt of claim 1 , and another therapeutic agent.9. A method for treating a disease or condition mediated claim 1 , at least in part claim 1 , by a protein kinase in a patient in need thereof claim 1 , comprising administering to the patient a therapeutically effective amount of a salt of .10. The method of claim 9 , wherein the protein kinase is JAK or any mutation thereof.11. The method of claim 9 , wherein the protein kinase is SYK or any mutation thereof.12. The method of claim 9 , wherein the disease or condition is chronic lymphocytic leukemia (CLL) claim 9 , small lymphocytic lymphoma (SLL) claim 9 , follicular lymphoma (FL) claim 9 , transformed follicular lymphoma (tFL) claim 9 , diffuse large B-cell lymphoma (DLBCL) claim 9 , mantle cell lymphoma (MCL) claim 9 , B-cell non-Hodgkin's lymphoma (NHL) claim 9 , peripheral T-cell lymphoma (PTCL) cutaneous T-cell lymphoma (CTCL) claim 9 , marginal ...

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Номер записи: 49
04-02-2021 дата публикации

COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9

Номер: US20210032214A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Pandey Anjali
Принадлежит:

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I). 2. (canceled)4. (canceled)5. (canceled)6. (canceled)7. The compound of claim 1 , wherein m is 1.8. The compound of claim 1 , wherein m is 0 or 1.9. The compound of claim 1 , wherein Ris hydrogen.10. (canceled)11. The compound of any preceding claim claim 1 , wherein Ris hydrogen or Calkyl optionally substituted with halo or hydroxy.12. (canceled)13. The compound of claim 1 , wherein Ris halo claim 1 , Calkyl claim 1 , or aryl claim 1 , wherein Calkyl or aryl is optionally substituted with 1 to 3 halo.14. The compound of claim 1 , wherein Ris chlorine or fluorine.15. The compound of claim 1 , wherein Ris CF.16. (canceled)17. (canceled)19. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of .21. A method of treating a disease or condition mediated claim 18 , at least in part claim 18 , by PCSK9 claim 18 , the method comprising administering to a patient in need thereof a compound of .22. The method of claim 20 , wherein the disease or condition is a cardiovascular disease claim 20 , a metabolic disease claim 20 , or hypocholesterolemia.23. The method of claim 22 , wherein the cardiovascular disease is coronary disease claim 22 , hypertension claim 22 , hypercholesterolemia claim 22 , or atherosclerosis.24. The method of claim 22 , the metabolic disease is diabetes.25. The method of claim 24 , wherein the patient has elevated plasma levels of low density lipoprotein cholesterol.26. (canceled)27. A method of inhibiting the activity of PCSK9 claim 1 , the method comprising binding a compound of to PCSK9 claim 1 , thereby inhibiting the activity of PCSK9. This application is a continuation of U.S. application Ser. No. 16/078,578, filed Aug. 21, 2018, which is the U.S. National Stage of ...

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Номер записи: 50
05-02-2015 дата публикации

Benzamides and nicotinamides as syk modulators

Номер: US20150038492A1
Автор: Anjali Pandey, Brian Kane, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

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Номер записи: 51
25-02-2021 дата публикации

METHODS OF USE AND PHARMACEUTICAL COMPOSITIONS OF A SELECTIVE SYK INHIBITOR

Номер: US20210052582A1
Автор: ABELSON Mark, CHAPIN Matthew, HSU Yung Yueh, Pandey Anjali, PATTERSON Harold
Принадлежит:

Provided herein are methods of using Syk inhibitors, such as a selective Syk inhibitor, Compound 1 or a pharmaceutically acceptable salt thereof, in treating allergic and/or inflammatory diseases or conditions of the eye. Also provided is pharmaceutical compositions, in particular eyedrop ophthalmic compositions, comprising Compound 1 or a pharmaceutically acceptable salt thereof, useful in the methods. 2. An ophthalmic composition comprising about 0.01% w/w to about 10% w/w of Compound 1 or a pharmaceutically acceptable salt thereof , a tonicity modifier , a buffer and water.3. An ophthalmic composition comprising about 0.1% w/w to about 1% w/w of Compound 1 or a pharmaceutically acceptable salt thereof , a tonicity modifier , a buffer and water.4. The ophthalmic composition of any one of - , comprising Compound 1 HCl salt.5. The ophthalmic composition of any one of - , comprising about 0.1% to about 5% of a tonicity modifier , about 0.005 to about 0.02% w/w of a preservative , and a buffer , and having a pH of about 5.5 to 7.6. The ophthalmic composition of any one of - , comprising about 0.2% to about 2% w/w of a tonicity modifier , about 0.005 to about 0.02% w/w of a preservative , and a buffer , and having a pH of about 6.7. The ophthalmic composition of any one of - , comprising about 0.5% to about 1.5% w/w of a tonicity modifier , about 0.01% w/w of a preservative , and a buffer , and having a pH of about 6.8. The ophthalmic composition of any one of - , wherein the tonicity modifier is one or more of glycerin , NaCl , and KCl.9. The ophthalmic composition of any one of - , wherein the tonicity modifier is glycerin.10. The ophthalmic composition of any one of - , wherein the preservative is benzalkonium chloride.11. The ophthalmic composition of any one of - , wherein the buffer is a phosphate buffer.12. The ophthalmic composition of any one of - , wherein the buffer is a citrate buffer.13. An ophthalmic composition comprising about 0.01% to about 1% w/w ...

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Номер записи: 52
27-02-2020 дата публикации

METHODS FOR TREATING LYMPHOMA

Номер: US20200061060A1
Автор: Birrell Matthew, Coffey Gregory, Conley Pamela B., Curnutte John T., Michelson Glenn, Pandey Anjali, Steele Andrew
Принадлежит:

Compositions and methods for treating lymphoma, in particular, T-cell lymphoma and follicular lymphoma, in a human patient are provided. The methods entail administering to the patient an effective amount of cerdulatinib. 1. A method of treating a T-cell lymphoma in a human patient in need thereof , comprising administering to the patient an effective amount of cerdulatinib or a pharmaceutically acceptable salt , co-crystal or solvate thereof.2. The method of claim 1 , wherein the T-cell lymphoma is relapsed or refractory T-cell lymphoma.3. The method of claim 1 , the T-cell lymphoma has not been previously treated with an agent for treating T-cell lymphoma.4. The method of claim 1 , wherein the T-cell lymphoma is selected from peripheral T-cell lymphomas claim 1 , peripheral T-cell lymphomas not otherwise specified claim 1 , angioimmunoblastic T-cell lymphoma claim 1 , follicular T-cell lymphoma claim 1 , anaplastic large cell lymphoma claim 1 , enteropathy-associated T-cell lymphoma claim 1 , adult T-cell leukaemia/lymphoma claim 1 , T-cell leukemia claim 1 , nasal NK/T-cell lymphoma claim 1 , hepatosplenic T-cell lymphoma claim 1 , and cutaneous (skin) T-cell lymphoma.5. The method of claim 1 , wherein the T-cell lymphoma is relapsed or refractory peripheral T-cell lymphoma.6. The method of claim 1 , wherein the T-cell lymphoma is peripheral T-cell lymphoma not otherwise specified.7. The method of claim 1 , wherein the T-cell lymphoma is angioimmunoblastic lymphoma.8. The method of claim 1 , wherein the T-cell lymphoma is anaplastic large cell lymphoma.9. The method of - claim 1 , wherein the T-cell lymphoma is hepatosplenic T-cell lymphoma.10. The method of claim 1 , wherein the T-cell lymphoma is enteropathy-associated T-cell lymphoma.11. The method of claim 1 , wherein the T-cell lymphoma is cutaneous T-cell lymphoma.12. The method of claim 11 , wherein the cutaneous T-cell lymphoma is mycosis fungoides or Sézary syndrome.13. A method of treating a lymphoma in ...

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Номер записи: 53
31-03-2022 дата публикации

CERDULATINIB FOR THE TREATMENT OF B-CELL MALIGNANCIES

Номер: US20220096471A1
Автор: Coffey Gregory, Leeds Janet, Pandey Anjali
Принадлежит:

Provided herein are compositions and methods for treating a relapsed or refractory hematologic cancer in a human patient in need thereof. The methods entail administering to the patient a daily dose of about 10 mg to about 75 mg of cerdulatinib or a pharmaceutically acceptable salt thereof, wherein the patients suffer one or more of a B-cell malignancy, chronic lymphocytic leukemia (CLL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL) or other transformed FL and/or have relapsed or not responded to a prior chemotherapy. 1. A method of treating a follicular lymphoma in a human patient in need thereof , comprising administering to the patient about 30 mg of cerdulatinib or a pharmaceutically acceptable salt thereof twice daily.2. The method of claim 1 , wherein the follicular lymphoma is relapsed or refractory.3. The method of claim 1 , wherein the follicular lymphoma is transformed follicular lymphoma.4. The method of claim 1 , wherein the patient was previously administered a drug selected from the group consisting of an alkylating agent claim 1 , an anti-CD20 antibody claim 1 , a BCL-2 inhibitor claim 1 , a BTK inhibitor claim 1 , a P13Kδ inhibitor claim 1 , a platinum-based drug claim 1 , an antimetabolite claim 1 , an anthracycline claim 1 , a BCR pathway inhibitor claim 1 , and another chemotherapeutic agent used for treating a follicular lymphoma.5. The method of claim 1 , wherein the patient was previously administered a drug selected from the group consisting of venetoclax claim 1 , rituximab claim 1 , ibrutinib claim 1 , idelalisib claim 1 , and fludarabine.6. The method of claim 1 , wherein the cerdulatinib is administered in a pharmaceutical composition further comprising a pharmaceutically acceptable excipient or carrier.7. The method of claim 1 , wherein the cerdulatinib is not administered in combination with another anticancer drug therapy.8. The method of claim 1 , wherein the patient has a mutation linked to relapse or a resistance ...

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Номер записи: 54
02-04-2015 дата публикации

INHIBITORS OF PROTEIN KINASES

Номер: US20150094298A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Venkataramani Chandrasekar, Xu Qing
Принадлежит:

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 242-. (canceled)4550-. (canceled)5255-. (canceled)5766-. (canceled)67. A composition comprising a compound of any one of the preceding claims , in combination with a pharmaceutically acceptable carrier or diluent.68. A method for inhibiting Syk claim 1 , JAK kinase or a signal transduction pathway mediated at least in part by Syk or JAK kinase activity comprising the step of contacting a cell with a compound of .69. A method for treating a condition or disorder mediated at least in part by syk activity in a subject comprising the step of administering to a subject in need of such treatment a therapeutically effective amount of a composition of .70. The method of claim 69 , wherein the condition or disorder is selected from the group consisting of cardiovascular disease claim 69 , inflammatory disease claim 69 , autoimmune disease and cell proliferative disorder.71. The method of claim 70 , wherein said cardiovascular disease is selected from the group consisting of restenosis claim 70 , thrombosis claim 70 , immune thrombocytopenic purpura claim 70 , heparin induced thrombocytopenia claim 70 , dilated cardiomyopathy claim 70 , sickle cell disease claim 70 , atherosclerosis claim 70 , myocardial infarction claim 70 , vascular inflammation claim 70 , unstable angina and acute coronary syndromes.72. The method of claim 70 , wherein said ...

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Номер записи: 55
03-07-2014 дата публикации

COMPOUNDS AND METHODS FOR PURIFICATION OF SERINE PROTEASES

Номер: US20140186923A1
Автор: Pandey Anjali, Rose Jack W.
Принадлежит: Portola Pharmaceuticals, Inc.

Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods. 6. The compound of claim 1 , wherein Ris —OCH.7. The compound of claim 1 , wherein Ris X-L-R.8. The compound of claim 1 , wherein Ris hydrogen.9. The compound of claim 1 , wherein Ris chloro.10. The compound of claim 1 , wherein X is O.11. The compound of claim 1 , wherein X is a covalent bond.12. The compound of claim 1 , wherein X is S or SO.13. The compound of claim 1 , wherein X is NH.17. The compound of claim 1 , wherein each of q claim 1 , r claim 1 , s claim 1 , and t is at least 3.18. The compound of claim 1 , wherein the compound of Formula I inhibits fXa with an ICof from about 100 nM to about 1 μM.26. The affinity solid support of claim 20 , wherein Ris —OCH.27. The affinity solid support of claim 20 , wherein Ris X-L-Y—Z.28. The affinity solid support of claim 20 , wherein Ris hydrogen.29. The affinity solid support of claim 20 , wherein Ris chloro.30. The affinity solid support of claim 20 , wherein X is O.31. The affinity solid support of claim 20 , wherein X is a covalent bond.32. The affinity solid support of claim 20 , wherein X is S or SO.33. The affinity solid support of claim 20 , wherein X is NH.37. The affinity solid support of claim 20 , wherein each of q claim 20 , r claim 20 , s claim 20 , and t is at least 3.40. The affinity solid support of claim 20 , wherein Z is Sepharose™ resin.41. A method for purifying a serine protease comprising{'claim-ref': [{'@idref': 'CLM-00020', 'claim 20'}, {'@idref': 'CLM-00020', 'claim 20'}], '(1) adding a first composition comprising the serine protease to an affinity solid support of or a salt thereof to form a second composition comprising the serine protease and the affinity solid support of , and'}(2) eluting the serine protease from the second composition with an elution buffer comprising a competitive agent.42. The method of claim 41 ...

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Номер записи: 56
25-08-2022 дата публикации

Compounds for the modulation of proprotein convertase subtilisin/kexin type 9 (pcsk9)

Номер: US20220267269A1
Автор: Anjali Pandey, JIANG Zhu, Jonathan William Bourne, Mark KARBARZ, Simeon Bowers, Thomas E. Barta
Принадлежит: SRX Cardio LLC

The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

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Номер записи: 57
25-04-2019 дата публикации

COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)

Номер: US20190119236A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Pandey Anjali
Принадлежит:

The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I). 8. The compound of claim 1 , wherein m is 0 or 1.9. The compound of claim 1 , wherein Ris hydrogen claim 1 , —C(O)NH claim 1 , or —C(NH)NH.10. The compound of claim 1 , wherein Ris —NHS(O)CHor —NHC(O)CH.11. The compound of claim 1 , wherein Ris hydrogen claim 1 , Calkyl claim 1 , —COH claim 1 , or —C(O)NH.12. The compound of claim 1 , wherein L is a bond claim 1 , —CH— claim 1 , —O— claim 1 , —C(O)— claim 1 , —S(O)— claim 1 , —S(O)NH— claim 1 , or —NH—.13. The compound of claim 1 , wherein Ris hydrogen claim 1 , amino claim 1 , halo claim 1 , Calkyl claim 1 , aryl claim 1 , or Cheterocyclyl claim 1 , wherein Calkyl claim 1 , aryl claim 1 , or Cheterocyclyl is optionally substituted with 1 to 3 halo.14. The compound of claim 1 , wherein L is a bond and Ris hydrogen.15. The compound of claim 1 , wherein L is a bond claim 1 , and Ris CF.17. The compound of claim 16 , wherein Y is —N(R)—.19. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound of .22. The method of claim 20 , wherein the disease or condition is a cardiovascular disease claim 20 , a metabolic disease claim 20 , or hypocholesterolemia.23. The method of claim 21 , wherein the cardiovascular disease is coronary disease claim 21 , hypertension claim 21 , hypercholesterolemia claim 21 , or atherosclerosis.24. The method of claim 21 , the metabolic disease is diabetes.25. The method of claim 20 , wherein the patient has elevated plasma levels of low density lipoprotein cholesterol.26. The method of claim 20 , wherein the patient has depleted plasma levels of low density lipoprotein cholesterol.27. A method of inhibiting the activity of PCSK9 claim 1 , the method comprising binding a compound of to PCSK9 claim 1 , thereby inhibiting the ...

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Номер записи: 58
14-05-2015 дата публикации

QUINAZOLINE DERIVATIVES AS KINASE INHIBITORS

Номер: US20150133439A1
Автор: Ichimura Michio, Ide Shinichi, Matsuno Kenji, Nomoto Yuji, Oda Shoji, Pandey Anjali, Sasaki Junko, Scarborough Robert M., TSUKUDA Eiji
Принадлежит:

The Present invention relates to nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. In a particular aspect the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis. 112.-. (canceled)14. A pharmaceutical composition comprising an effective amount of a compound according to claim 13 , or a pharmaceutically acceptable salt or hydrate thereof claim 13 , and a pharmaceutically acceptable diluent or carrier.15. A method of inhibiting phosphorylation of PDGF receptor in a patient comprising the step of administering a compound of and all pharmaceutically acceptable salts and hydrates thereof to the patient.17. The method of claim 16 , wherein Ris a member selected from the group consisting of CN claim 16 , —O-methyl claim 16 , —O-ethyl claim 16 , —O-propyl claim 16 , —O-isopropyl claim 16 , —O-butyl claim 16 , —O-t-butyl claim 16 , —O— isoamyl claim 16 , 1-naphthyloxy claim 16 , 2-naphthyloxy claim 16 , 4-indolyloxy claim 16 , 5-indolyloxy claim 16 , 5-isoquinolyloxy claim 16 , and all pharmaceutically acceptable salts and hydrates of such compounds. This application is a continuation of U.S. patent application Ser. No. 12/471, 280, filed May 22, 2009; which is a continuation of U.S. patent application Ser. No. 11/210,028, filed Aug. 22, 2005; now U.S. Pat. No. 7,560,461; which is a continuation of U.S. patent application Ser. No. 10/344,736, filed Oct. 16, 2003, now U.S. ...

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Номер записи: 59
08-09-2022 дата публикации

TYK2 INHIBITORS AND USES THEREOF

Номер: US20220281885A1
Автор: CHAUDHURI Bhaskar, Dietsch Gregory, Duraiswamy Athisayamani Jeyaraj, KALVA Sukesh, MANOJVEER Seetharaman, Pandey Anjali, Thakkar Mahesh
Принадлежит:

Described herein are compounds that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity. 2. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , tautomer claim 1 , or solvate thereof claim 1 , wherein:{'sup': 1', '11', '2', '11', '3', '11, 'Xis CR, Xis CR, and Xis CR;'}{'sup': 1', '11', '2', '11', '3, 'or Xis CR, Xis CR, and Xis N;'}{'sup': 1', '11', '2', '3', '11, 'or Xis CR, Xis N, and Xis CR;'}{'sup': 1', '2', '11', '3', '11, 'or Xis N, Xis CR, and Xis CR; and'}{'sup': 11', '17', '16, 'sub': 1', '6', '1', '6', '2, 'each Ris independently hydrogen, halogen, C-Calkyl, C-Cfluoroalkyl, —CN, —OH, —OR, or —N(R).'}3. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , tautomer claim 1 , or solvate thereof claim 1 , wherein:{'sup': 1', '11', '2', '11', '3', '11, 'Xis CR, Xis CR, and Xis CR; and'}{'sup': '11', 'each Ris independently hydrogen or fluoro.'}4. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , tautomer claim 1 , or solvate thereof claim 1 , wherein each Ris independently hydrogen claim 1 , —Cl claim 1 , —F claim 1 , methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , —CD claim 1 , —CHOH claim 1 , —CF; cyclopropyl claim 1 , oxetanyl claim 1 , azetidinyl claim 1 , —CN claim 1 , —OH claim 1 , —COH claim 1 , or —COCH; wherein if Ris attached to a nitrogen atom claim 1 , then Ris hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , —CD claim 1 , —CHOH claim 1 , cyclopropyl claim 1 , oxetanyl claim 1 , azetidinyl claim 1 , —COH claim 1 , or —COCH.5. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , tautomer claim 1 , or solvate thereof claim 1 , wherein each Ris independently hydrogen claim 1 , methyl claim 1 , —CD claim 1 , —OH claim 1 , — ...

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Номер записи: 60
31-05-2018 дата публикации

CERDULATINIB FOR THE TREATMENT OF B-CELL MALIGNANCIES

Номер: US20180147203A1
Автор: Coffey Gregory, Leeds Janet, Pandey Anjali
Принадлежит:

Provided herein are compositions and methods for treating a relapsed or refractory hematologic cancer in a human patient in need thereof. The methods entail administering to the patient a daily dose of about 10 mg to about 75 mg of cerdulatinib or a pharmaceutically acceptable salt thereof, wherein the patients suffer one or more of a B-cell malignancy, chronic lymphocytic leukemia (CLL), follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL) or other transformed FL and/or have relapsed or not responded to a prior chemotherapy. 1. A method of treating a hematologic cancer in a human patient in need thereof , comprising administering to the patient a daily dose of about 10 mg to about 75 mg of cerdulatinib or a pharmaceutically acceptable salt thereof.2. A method for treating a relapsed or refractory hematologic cancer in a patient in need thereof , comprising administering to the patient an effective amount of cerdulatinib , or a pharmaceutically acceptable salt thereof.3. A method for treating a relapsed or refractory hematologic cancer in a patient in need thereof , comprising administering to the patient an effective amount of cerdulatinib , or a pharmaceutically acceptable salt thereof , wherein:the patient has a mutation linked to relapse and/or a resistance to a drug for treating a hematological cancer; andthe effective amount is cerdulatinib, or a pharmaceutically acceptable salt thereof, is a daily dose of about 30 mg to about 80 mg of cerdulatinib.4. The method of or , wherein the patient has a mutation linked to relapse and/or a resistance to a drug for treating a hematological cancer.5. The method of or , wherein the patient has a del17p mutation , a P53 mutation , an ATM mutation , a STAT mutation , a STAT 6 mutation , a C481S STAT6 mutation , a mutation associated with the NOTCH pathway , or a mutation associated with the Caderin pathway.6. The method of any of - , wherein the patient does not have a mutation in all of P53 , BTK , and EP300.7. ...

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Номер записи: 61
04-09-2014 дата публикации

Anti-obesity potential of Calebin A

Номер: US20140249219A1
Автор: Majeed Anju, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali, Sarang Bani
Принадлежит:

The present invention discloses the potential of Calebin A in inhibiting adipogenesis and applications thereof in obesity management. The present invention elucidates the potential of Calebin A to favorably modulate biochemical markers associated with obesity. Notable biomodulatory properties of Calebin A include inhibiting leptin production, increasing adiponectin expression and inhibiting local (adipocyte) and systemic inflammation caused by pro-inflammatory cytokines Tumor Necrosis Factor (TNF-α), Interleukin-6 (IL-6) and Interleukin-1 (IL-1β). 1. A method of obesity management in mammals with risk of excessive accumulation of body fat , said method comprising the step of dietary oral supplementation of effective amounts of Calebin A to said mammals to bring about the effect of adipogenesis inhibition.2. Use of Calebin A in the management of obesity in mammals with risk of excessive accumulation of body fat , said use comprising the step of dietary oral supplementation of effective amounts of Calebin A to said mammals to bring about the effect of adipogenesis inhibition.3. A method of inhibiting adipogenesis in mammals with risk of excessive accumulation of body fat , said method comprising the step of dietary oral supplementation of effective amounts of Calebin A to said mammals.4. A method of reducing body weight of obese mammals , said method comprising step of orally administering effective amounts of Calebin A to said mammals.5. Use of Calebin A in a method to reduce body weight in obese mammals , said use comprising step of orally administering effective amounts of Calebin A to said mammals.6. A method of increasing systemic expression of adiponectin in obese mammals , said method comprising step of dietary oral supplementation of effective amounts of Calebin A to said mammals.7. A method for aiding in preventing , delaying the onset of and/or slowing the progression of diabetes mellitus Type II in an obese mammal , said method comprising step of orally ...

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Номер записи: 62
22-06-2017 дата публикации

PYRIDAZINE COMPOUNDS AS JAK INHIBITORS

Номер: US20170174673A1
Автор: Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит:

In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described. 2. The compound of claim 1 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 1 , wherein A is Caryl.3. The compound of claim 2 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 2 , wherein A is phenyl.4. The compound of claim 1 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 1 , wherein A is 5- to 6-membered heteroaryl.5. The compound of claim 4 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 4 , wherein A is selected from the group consisting of pyrazinyl claim 4 , pyrazolyl claim 4 , pyridinyl claim 4 , and thiazolyl.6. The compound of any one of - claim 4 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 4 , wherein each Ris independently selected from the group consisting of halo claim 4 , Calkyl claim 4 , and Calkoxy claim 4 , or two Rmoieties claim 4 , together with the atoms to which they are attached claim 4 , form a fused 5- to 6-membered ring.7. The compound of claim 1 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 1 , wherein D is Calkyl.8. The compound of claim 7 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 7 , wherein D is selected from the group consisting of methyl and isopropyl.9. The compound of claim 1 , or a tautomer thereof or a pharmaceutically acceptable salt or hydrate thereof claim 1 , wherein D is Caryl which is substituted with from 0 to 3 R.10. The compound of claim 9 , or a tautomer thereof or a pharmaceutically acceptable salt or ...

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Номер записи: 63
16-07-2015 дата публикации

COMPOSITION AND METHOD FOR THE PROTECTION OF ARTICULAR CARTILAGE

Номер: US20150196524A1
Автор: Bani Sarang, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

The novel therapeutic potential of Calebin A and compositions thereof to prevent pathological damage to mammalian articular cartilage is disclosed. 1. A method of using Calebin A in effective amounts to protect mammalian articular cartilage from pathological damage , said method comprising the step of administering effective dose of Calebin A to mammals in need of said protection.2. A method of protecting mammalian articular cartilage from pathological damage , said method comprising the step of administering effective dose of Calebin A to mammals in need of said protection. 1. Field of the inventionThe present invention in general pertains to protective compositions and methods thereof for articular cartilage. Specifically, the present invention pertains to the potential of Calebin A to prevent pathological damage to articular cartilage.2. Description of prior artArticular cartilage is a specialized connective tissue that covers the articular surfaces of bones forming a synovial joint. Articular cartilage endows the synovial joints the ability to provide low friction and relatively pain free motion. Articular cartilage structures and functions are prone to damage following trauma (fall or accident), wear and tear and underlying pathological disease conditions. Articular cartilage tissue usually does not regenerate (the process of self repair) after injury or disease leading to loss of tissue and formation of a defect. Reasons attributed to such non-regeneration include (i) Fewer cellular components; (ii) poor metabolism and (iii) the restricted capacity of innate chondrocytes to divide and migrate in the tissue on account of dense matrix fibers. Thus, active principles that are capable of protecting articular cartilage from damage due to trauma and disease constitute important technological areas that offer considerable scope to improve the quality of life of individuals who are prone to such trauma.It is the principle of the present invention to disclose the ...

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Номер записи: 64
05-07-2018 дата публикации

INHIBITORS OF PROTEIN KINASES

Номер: US20180186783A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Venkataramani Chandrasekar, Xu Qing
Принадлежит:

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 180.-. (canceled)83. The topical pharmaceutical composition of claim 81 , wherein Ris substituted with from 1 to 2 substituents independently selected from the group consisting of Calkylcarbonyl and Calkylsulfonyl.84. The topical pharmaceutical composition of claim 83 , wherein R1is substituted with a Calkylsulfonyl substituent.85. The topical pharmaceutical composition of claim 83 , wherein Ris substituted with a Calkylcarbonyl substituent.86. The topical pharmaceutical composition of claim 81 , wherein Ris H.89. The topical pharmaceutical composition of claim 81 , wherein said topical pharmaceutical composition is in the form of an emulsion claim 81 , a lotion claim 81 , a gel claim 81 , a foam claim 81 , a cream claim 81 , a jelly claim 81 , a solution claim 81 , a suspension claim 81 , an ointment claim 81 , or a transdermal patch.90. The topical pharmaceutical composition of claim 89 , wherein said topical pharmaceutical composition is in the form of an ointment.91. The topical pharmaceutical composition of claim 89 , wherein said topical pharmaceutical composition is in the form of a lotion or a cream.92. The topical pharmaceutical composition of claim 81 , wherein said topical pharmaceutical composition is suspended or dissolved in said one or more carriers.93. The topical pharmaceutical composition of claim 92 , wherein said ...

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Номер записи: 65
22-07-2021 дата публикации

COMPOSITIONS FOR MANAGING CHRONIC OBSTRUCTIVE PULMONARY DISEASE

Номер: US20210220290A1
Автор: Bani Sarang, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

The invention discloses a composition comprising not less than 20% w/w bisdemethoxycurcumin for regeneration of alveolar cells damaged in emphysematous conditions and for the therapeutic management of chronic obstructive pulmonary disease and acute respiratory distress syndrome. The composition further comprises 10-35% w/w demethoxycurcumin and 10-45% w/w curcumin. The composition is very suitable for treating COPD and ARDS due to viral infections, specifically COVID 19 and for improving lung function during prognosis. 1. A method for regeneration of alveolar cells in mammals with emphysema , said method comprising step of administering a composition comprising not less than 20% w/w bisdemethoxycurcumin to said mammals to bring about a reduction in features of emphysema.2. The method as in claim 1 , wherein the composition further comprises 10-35% w/w demethoxycurcumin and 10-45% w/w curcumin.3. The method as in claim 1 , wherein the features of emphysema are selected from the group consisting of hypoxia claim 1 , decreased levels of lung surfactant proteins claim 1 , increased permeability of the alveolar-capillary barrier claim 1 , inflammation claim 1 , increased accumulation and recruitment of neutrophils claim 1 , elevated alveolar pressure claim 1 , increased oxidative stress claim 1 , elevated inflammatory cytokines and chemokines claim 1 , increased numbers of activated T lymphocytes and muscle damage.4. The method as in claim 1 , wherein emphysema is induced by enzymes claim 1 , viruses claim 1 , bacteria claim 1 , smoke and particulate irritants.5. The method as in claim 1 , wherein the mammal is human.6. A method of therapeutic management of chronic obstructive pulmonary disease in mammals claim 1 , said method comprising step of administering a composition comprising not less than 20% w/w bisdemethoxycurcumin to said mammals to bring about a reduction in features and symptoms of chronic obstructive pulmonary disease.7. The method as in claim 6 , wherein ...

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Номер записи: 66
22-07-2021 дата публикации

THERAPEUTIC COMPOSITIONS AND METHODS FOR PULMONARY FIBROSIS

Номер: US20210220291A1
Автор: Bani Sarang, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

The present invention discloses a method for therapeutic management of pulmonary fibrosis in mammals using a composition comprising iso-garcinol or octahydrocurcumin or a combination of iso-garcinol and octahydrocurcumin. The composition is very suitable for treating pulmonary fibrosis due to viral infections, specifically COVID 19 and for improving lung function during prognosis. 1. A method for therapeutic management of pulmonary fibrosis in mammals , said method comprising step of administering a composition comprising iso-garcinol or octahydrocurcumin or a combination of iso-garcinol and octahydrocurcumin to mammals in need of such management to bring about a reduction in symptoms and features of pulmonary fibrosis.2. The method as in claim 1 , wherein the symptoms of pulmonary fibrosis are selected from the group consisting of shortness of breath claim 1 , chronic dry and hacking cough claim 1 , fatigue and weakness claim 1 , chest discomfort including chest pain claim 1 , loss of appetite claim 1 , weight loss claim 1 , aching joints and muscles claim 1 , clubbing of the tips of the fingers or toes.3. The method as in claim 1 , wherein the features of pulmonary fibrosis include increased hypoxia claim 1 , extracellular matrix generation and deposition of aberrant matrix claim 1 , increased inflammation and influx of inflammatory markers claim 1 , increased migration and proliferation of fibroblasts claim 1 , increased mucus secretion and increased lung index.4. The method as in claim 1 , wherein the inflammatory markers are selected from the group consisting of TGF-β claim 1 , IL-13 claim 1 , IL-1β claim 1 , TNF-α claim 1 , CCL-17.5. The method as in claim 1 , wherein the mammal is human. This is a non-provisional US patent application claiming priority from U.S. Provisional application 62/962,343 filed on 17 Jan. 2020, the details of which are being incorporated herein by reference.The present invention relates to compositions for the management of pulmonary ...

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Номер записи: 67
05-08-2021 дата публикации

COMPOSITION AND METHODS OF USE OF NOVEL PHENYLALANINE SMALL ORGANIC COMPOUNDS TO DIRECTLY MODULATE PCSK9 PROTEIN ACTIVITY

Номер: US20210236481A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Monroe Kyle D., Muehlemann Michael M., Pandey Anjali
Принадлежит:

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels. 112.-. (canceled)14. The method of claim 13 , further comprising administering to the mammal a second active pharmaceutical.15. The method of claim 13 , comprising administering a pharmaceutical composition comprising the compound of Formula I and a pharmaceutically acceptable carrier or excipient.16. The method of claim 15 , wherein said pharmaceutical composition further comprises a second active ingredient.19. The method of claim 18 , further comprising administering to the mammal a second active pharmaceutical.20. The method of claim 18 , comprising administering a pharmaceutical composition comprising the compound of Formula I and a pharmaceutically acceptable carrier or excipient.21. The method of claim 20 , wherein said pharmaceutical composition further comprises a second active ingredient.22. The method of claim 21 , wherein said second active ingredient is selected from the group consisting of a statin claim 21 , a cardiovascular drug claim 21 , a metabolic drug claim 21 , and an antihypertensive drug.25. The method of claim 24 , further comprising administering to the mammal a ...

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Номер записи: 68
16-10-2014 дата публикации

Pyrazine Kinase Inhibitors

Номер: US20140309209A1
Автор: Bauer Shawn M., Jia Zhaozhong J., Kane Brian, Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит:

Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. 2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is H.3. A compound of or claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.4. A compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , isopropyl claim 1 , sec-butyl claim 1 , tert-butyl claim 1 , methyl claim 1 , ethyl claim 1 , CFCH— claim 1 , CHFCH— claim 1 , methoxymethylene claim 1 , methylsulfinylethylene claim 1 , and methylsulfonylethylene.5. A compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Ccycloalkyl claim 1 , CcycloalkylCalkylene claim 1 , aryl claim 1 , arylCalkylene or heteroarylCalkylene each of which is optionally substituted with one to five groups independently selected from halo claim 1 , C-Calkyl claim 1 , and amino.6. A compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of cyclopropyl claim 5 , cyclopropylmethylene claim 5 , phenyl and benzyl.7. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Rand Rindependently ndependently selected from the group consisting of Calkyl and Calkoxy.8. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein V is heteroaryl optionally substituted with one to five Rgroups.9. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein V is cycloalkyl optionally substituted with one to five Rgroups.10. A compound of any one of to claim 5 ...

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Номер записи: 69
27-08-2015 дата публикации

COMPOSITION COMPRISING SCIRPUSIN A AND SCIRPUSIN B AND ANTI-OBESITY POTENTIAL THEREOF

Номер: US20150238438A1
Автор: Bani Sarang, Bhat Beena, Kalman Douglas, Karri Suresh, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali, Vaidyanathan Priti
Принадлежит:

Disclosed are methods of managing obesity and hypercholesterolemia using a composition of matter comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stiibenes. 1Cyperus rotundus. A method of reducing obesity in humans , said method comprising step of administering to said humans orally twice a day , composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes to achieve the effects of reduction in body weight , body mass index and waist circumference2Cyperus rotundus. A method of treating hypercholesterolemia in humans , said method comprising step of administering to said humans orally twice a day , composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes to achieve the effects of (a) reduction in the systemic levels of total cholesterol , Low Density Lipoproteins (LDL) , Very Low Density Lipoproteins (VLDL) and serum triglycerides and (b) enhancement in the systemic levels of High Density Lipoproteins (HDL).3Cyperus rotundus. The methods according to and wherein the composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes consists essentially of piceatannol and dimers thereof.4Cyperus rotundus. The methods according to wherein the composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain 5% of total stilbenes claim 3 , consists essentially of a combination of piceatannol claim 3 , scirpusin B and scirpusin A.5Cyperus rotundus. A method of reducing obesity in humans claim 3 , said method comprising step of administering to said humans orally twice a day claim 3 , composition comprising the ethyl acetate fraction of the extract of rhizomes standardized to contain greater than 3% of total stilbenes to achieve the effects of reduction in body weight claim 3 , body mass index and waist ...

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Номер записи: 70
30-10-2014 дата публикации

SELECTIVE KINASE INHIBITORS

Номер: US20140323418A1
Автор: Bauer Shawn M., Dick Ryan, Jia Zhaozhong J., Kane Brian, Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит: Portola Pharmaceuticals, Inc.

Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. 29.-. (canceled)15. A compound of or a pharmaceutically acceptable salt thereof claim 14 , wherein T is quinolinyl.18. A compound of wherein Ris cyclohexyl substituted with amino and further optionally substituted with one to three halo substituents.20. A compound of or a pharmaceutically acceptable salt thereof claim 19 , wherein Ris Calkyl or haloCalkylene.21. A compound of or a pharmaceutically acceptable salt thereof claim 17 , wherein heteroaryl is selected from the group consisting of: thienyl claim 17 , thiazoyl claim 17 , thiadiazoyl claim 17 , isothiazoyl claim 17 , pyrazoyl claim 17 , triazoyl claim 17 , pyrimidinyl claim 17 , tetrahydroprimidinyl claim 17 , indolyl claim 17 , indolinyl claim 17 , indazoyl claim 17 , benzothiazolyl claim 17 , thieno[2 claim 17 ,3-b]pyridinyl claim 17 , pyrazolo[1 claim 17 ,5-a]pyridine claim 17 , 1H-pyrrolo[2 claim 17 ,3-b]pyridine claim 17 , isoquinolinyl claim 17 , tetrahydroquinolinyl and quinolinyl.2331.-. (canceled)32. A composition comprising a compound or a pharmaceutically acceptable salt thereof of in combination with a pharmaceutically acceptable carrier or diluent.33. A method for inhibiting Syk kinase or a signal transduction pathway mediated at least in part by Syk kinase activity comprising the step of contacting a cell with a compound or a pharmaceutically acceptable salt thereof of .3430. A method for treating a condition or disorder mediated at least in part by Syk kinase activity in a subject comprising the step of administering to a subject in need of such treatment a therapeutically effective amount of a composition of claim .3543.-. (canceled)44. A kit comprising a composition of claim 32 , packaging ...

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Номер записи: 71
30-10-2014 дата публикации

METHODS AND FORMULATIONS OF TREATING THROMBOSIS WITH BETRIXABAN AND A P-GLYCOPROTEIN INHIBITOR

Номер: US20140323497A1
Автор: Arroyo Itzia Zoraida, Ball Richard G., Capodanno Vincent R., Corcoran Liam, Denney William, LAURING Brett, Maher Timothy K., Mansoor George A., Margeiefsky Eric L., McNevin Michael, Pandey Anjali, Sinha Uma, Vosatka Anne Hermanowski, Wenslow Robert M.
Принадлежит: Portola Pharmaceuticals, Inc.

This invention is directed to methods of inhibiting coagulation or treating thrombosis using a factor Xa inhibitor and a P-glycoprotein (Pgp) inhibitor. The invention is also directed to formulations used in the methods. 1. A method for treating thrombosis or inhibiting blood coagulation in a patient receiving administration of a P-glycoprotein inhibitor , the method comprising administering to the patient a subtherapeutic dose of betrixaban.2. The method of claim 1 , wherein the amount of betrixaban administered is about 20% less than the therapeutically effective amount.3. The method of claim 1 , wherein the amount of betrixaban administered is about 50% less than the therapeutically effective amount.4. The method of claim 1 , wherein the patient is a human patient and the patient is administered an aggregate daily dose of about 25 to about 35 mg of betrixaban.5. The method of claim 1 , wherein the patient is a human patient and the patient is administered an aggregate daily dose of about 10 to about 20 mg of betrixaban.6. (canceled)7. The method of claim 1 , wherein the patient receives the administration of the P-glycoprotein inhibitor at least half an hour before or after administration of betrixaban.8. The method of claim 1 , wherein the patient is concurrently administered with the P-glycoprotein inhibitor and betrixaban.9. The method of claim 1 , wherein the patient receives administration of an therapeutically effective amount of the P-glycoprotein inhibitor.10. The method of claim 1 , wherein the P-glycoprotein inhibitor is in a controlled release form.11. The method of claim 1 , wherein the P-glycoprotein inhibitor is selected from the group consisting of verapamil claim 1 , amiodarone and ketoconazole.12. The method of claim 11 , wherein the P-glycoprotein inhibitor is verapamil.13. The method of claim 12 , wherein verapamil is administered in an amount of about 100 mg to about 300 mg.14. The method of claim 11 , wherein the P-glycoprotein inhibitor is ...

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Номер записи: 72
23-08-2018 дата публикации

COMPOSITION AND METHODS OF USE OF NOVEL PHENYLALANINE SMALL ORGANIC COMPOUNDS TO DIRECTLY MODULATE PCSK9 PROTEIN ACTIVITY

Номер: US20180237381A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Monroe Kyle D., Muehlemann Michael M., Pandey Anjali
Принадлежит:

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels. 2. The compound of claim 1 , formulated as a pharmaceutical composition.3. The compound of claim 2 , wherein said pharmaceutical composition further comprises a pharmaceutical drug.4. The compound of claim 3 , wherein said pharmaceutical drug is selected from the group consisting of a statin claim 3 , a cardiovascular drug claim 3 , a metabolic drug claim 3 , and an antihypertensive drug.5. A method claim 3 , comprising: i) a PCSK9 protein, wherein said protein comprises a binding site that induces allosteric modulation and a low density lipoprotein receptor binding site;', 'ii) a small organic compound capable of binding to said binding site, and selected from the group consisting of a compound of a phenylalanine scaffold of Formula I; and', 'iii) a plurality of hepatocyte cells comprising a low density lipoprotein receptor and low density lipoproteins;, 'a) providing;'}b) binding said small organic compound to said binding site, wherein said small organic compound induces a conformational shift of said protein; andc) modulating the rate of low density lipoprotein receptor ...

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Номер записи: 73
10-09-2015 дата публикации

BICYCLIC OXA-LACTAM KINASE INHIBITORS

Номер: US20150252056A1
Автор: Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит:

Provided are bicyclic oxa-lactam compounds for inhibition of JAK/Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting JAK/Syk kinase activity, and methods for treating conditions mediated at least in part by JAK/Syk kinase activity. 10. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Zor HET is a six-membered heteroaryl ring optionally substituted with 1 to 3 R.11. (canceled)12. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Zor HET is a five-membered heteroaryl ring optionally substituted with 1 to 3 R.13. (canceled)15. A compound of wherein at least one Ris Calkyl.1734.-. (canceled)3854.-. (canceled)56. A composition comprising a compound of or a tautomer or a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier or excipient.57. A method for inhibiting Syk or JAK kinase or a signal transduction pathway mediated at least in part by Syk kinase activity comprising contacting a cell with a compound of .5860.-. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/706,712, filed Sep. 27, 2012; the entire disclosure of which is incorporated herein by reference.Protein kinases constitute a large family of structurally related enzymes that are responsible for the control of a variety of signal transduction processes within cells (see, e.g., Hardie and Hanks, The Protein Kinase Facts Book, I and II, Academic Press, San Diego, Calif., 1995). Protein kinases are thought to have evolved from a common ancestral gene due to the conservation of their structure and catalytic function. Almost all kinases contain a similar 250-300 amino acid catalytic domain. The kinases can be categorized into families by the substrates they phosphorylate (e.g., protein-tyrosine, protein-serine/threonine, lipids, etc.). Sequence ...

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Номер записи: 74
17-09-2015 дата публикации

SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS

Номер: US20150259328A1
Автор: Bauer Shawn M., Jia Zhaozhong J., Pandey Anjali, Song Yonghong
Принадлежит:

Provided are substituted pyrimidinyl compounds for inhibition of JAK and/or Syk kinase, pharmaceutical compositions thereof, methods for inhibiting JAK and/or Syk kinase activity, and methods for treating conditions mediated at least in part by JAK and/or Syk kinase activity. 23.-. (canceled)515.-. (canceled)1720.-. (canceled)2225.-. (canceled)3233.-. (canceled)3637.-. (canceled)4145.-. (canceled)4749.-. (canceled)51. A composition comprising a compound of in combination with a pharmaceutically acceptable carrier or diluent.52. A method for inhibiting Syk or JAK kinase claim 1 , wherein the method comprises contacting a cell with a compound of .53. A method for treating a condition or disorder mediated at least in part by Syk or JAK kinase activity claim 51 , wherein the method comprises administering to a subject in need of such treatment a therapeutically effective amount of a composition of .54. The method of claim 53 , wherein the condition or disorder is selected from the group consisting of cardiovascular disease claim 53 , inflammatory disease claim 53 , autoimmune disease claim 53 , and cell proliferative disorder.5558.-. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/711,170, filed Oct. 8, 2012; the entire disclosure of which is incorporated herein by reference.This invention is directed to pyrimidine-5-carboxamide compounds that act as inhibitors of spleen tyrosine kinase (Syk) and/or JAK kinases. This invention is also directed to pharmaceutical compositions containing the pyrimidine-5-carboxamide compounds and methods of using the compounds or compositions to treat to treat cardiovascular disease, inflammatory disease, autoimmune disease, and/or cell proliferative disorder. The invention is also directed to methods of making the compounds described herein.Protein kinases constitute a large family of structurally related enzymes that are responsible for the control of a variety of signal transduction processes ...

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Номер записи: 75
30-07-2020 дата публикации

INHIBITORS OF PROTEIN KINASES

Номер: US20200239458A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Venkataramani Chandrasekar, Xu Qing
Принадлежит:

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 268.-. (canceled)7079.-. (canceled)80. A kit comprising a compound of claim 1 , packaging and instructions for use.81. The method of claim 69 , wherein said cell proliferative disorder is a hematopoietic neoplasm.82. The method of claim 81 , wherein said hematopoietic neoplasm is a leukemia claim 81 , a lymphoma claim 81 , or a plasma cell myeloma.8378. The method of claim claim 81 , wherein said hematopoietic neoplasm is multiple myeloma.84. The method of claim 69 , wherein Dis cyclopropyl. This application is a continuation of U.S. application Ser. No. 15/828,154 filed Nov. 30, 2017, which is a continuation of U.S. application Ser. No. 14/561,821 filed Dec. 5, 2014, which is a continuation of U.S. application Ser. No. 13/916,926 filed Jun. 13, 2014, which is a continuation of U.S. application Ser. No. 13/360,862 filed Jan. 30, 2012, which is a continuation of U.S. application Ser. No. 12/386,509 filed Apr. 16, 2009, which claims the benefit of U.S. Provisional Patent Application No. 61/120,348, filed Dec. 5, 2008, U.S. Provisional Patent Application No. 61/120,346, filed Dec. 5, 2008, U.S. Provisional Patent Application No. 61/120,344, filed Dec. 5, 2008, U.S. Provisional Patent Application No. 61/120,341, filed Dec. 5, 2008, U.S. Provisional Patent Application No. 61/045,499, filed Apr. 16, 2008, U.S. Provisional Patent Application No. ...

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Номер записи: 76
06-09-2018 дата публикации

COMPOSITION AND METHODS OF USE OF NOVEL PHENYLALANINE SMALL ORGANIC COMPOUNDS TO DIRECTLY MODULATE PCSK9 PROTEIN ACTIVITY

Номер: US20180250291A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Monroe Kyle D., Muehlemann Michael M., Pandey Anjali
Принадлежит:

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels. 2. The compound of claim 1 , formulated as a pharmaceutical composition.3. The compound of claim 2 , wherein said pharmaceutical composition further comprises a pharmaceutical drug.4. The compound of claim 3 , wherein said pharmaceutical drug is selected from the group consisting of a statin claim 3 , a cardiovascular drug claim 3 , a metabolic drug claim 3 , and an antihypertensive drug.5. A method claim 3 , comprising: i) a PCSK9 protein, wherein said protein comprises a binding site that induces allosteric modulation and a low density lipoprotein receptor binding site;', 'ii) a small organic compound capable of binding to said binding site, and selected from the group consisting of a compound of a phenylalanine scaffold of Formula I; and', 'iii) a plurality of hepatocyte cells comprising a low density lipoprotein receptor and low density lipoproteins;, 'a) providing;'}b) binding said small organic compound to said binding site, wherein said small organic compound induces a conformational shift of said protein; andc) modulating the rate of low density lipoprotein receptor ...

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Номер записи: 77
27-11-2014 дата публикации

Compounds and methods for purification of serine proteases

Номер: US20140346397A1
Автор: Anjali Pandey, Jack W. Rose
Принадлежит: Portola Pharmaceuticals LLC

Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

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Номер записи: 78
24-09-2015 дата публикации

BICYCLIC DIHYDROPYRIDONE KINASE INHIBITORS

Номер: US20150266871A1
Автор: Pandey Anjali, Song Yonghong, Xu Qing
Принадлежит:

Provided are bicyclic dihydropyridone compounds for inhibiting of JAK/Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting JAK/Syk kinase activity, and methods for treating conditions mediated at least in part by JAK/Syk kinase activity. 10. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Zor HET is a six-membered heteroaryl ring optionally substituted with 1 to 3 R.12. A compound of or a tautomer or a pharmaceutically acceptable salt thereof claim 1 , wherein Zor HET is a five-membered heteroaryl ring optionally substituted with 1 to 3 R.13. (canceled)15. A compound of wherein at least one Ris Calkyl.1754-. (canceled)56. A composition comprising a compound of or a tautomer or a pharmaceutically acceptable salt thereof in combination with a pharmaceutically acceptable carrier or excipient.57. A method for inhibiting Syk or JAK kinase or a signal transduction pathway mediated at least in part by Syk kinase activity comprising contacting a cell with a compound of .5860-. (canceled) This application claims the benefit of U.S. Provisional Patent Application No. 61/706,681, filed Sep. 27, 2012; the entire disclosure of which is incorporated herein by reference.Protein kinases constitute a large family of structurally related enzymes that are responsible for the control of a variety of signal transduction processes within cells (see, e.g., Hardie and Hanks, The Protein Kinase Facts Book, I and II, Academic Press, San Diego, Calif., 1995). Protein kinases are thought to have evolved from a common ancestral gene due to the conservation of their structure and catalytic function. Almost all kinases contain a similar 250-300 amino acid catalytic domain. The kinases can be categorized into families by the substrates they phosphorylate (e.g., protein-tyrosine, protein-serine/threonine, lipids, etc.). Sequence motifs have been identified that ...

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Номер записи: 79
13-08-2020 дата публикации

PHENYLPIPERAZINE PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) MODULATORS AND THEIR USE

Номер: US20200253958A1
Автор: Barta Thomas E., Bourne Jonathan William, Bowers Simeon, Monroe Kyle D., Muehlemann Michael M., Pandey Anjali
Принадлежит:

This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels. 112.-. (canceled)14. The method of claim 13 , whereby the rate of low density lipoprotein receptor internalization is increased.15. The method of claim 13 , whereby the rate of low density lipoprotein internalization is increased.16. The method of claim 13 , wherein the compound is formulated as a pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient.17. The method of claim 16 , wherein said pharmaceutical composition further comprises a second pharmaceutical drug compound.18. The method of claim 17 , wherein said second pharmaceutical drug compound is selected from the group consisting of a statin claim 17 , a cardiovascular drug claim 17 , a metabolic drug claim 17 , and an antihypertensive drug.19. The method of claim 13 , where the compound is selected from:1 -(4-benzylphenyl)piperazine;1-(4-(benzyloxy)phenyl)piperazine;1-(4-phenoxyphenyl)piperazine;1-(4-(4-bromophenoxy)phenyl)piperazine;1-(4-(4-(methylthio)phenoxy)phenyl)piperazine;1-4-(4-(piperazin-1-yl)phenoxy)benzoic acid;4-(4-(piperazin-1-yl)phenoxy)benzoic acid;4-(4-(piperazin-1-yl)phenoxy) ...

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Номер записи: 80
29-08-2019 дата публикации

Compounds and method of use

Номер: US20190263802A1
Автор: Anjali Pandey, Athisayamani Jeyaraj DURAISWAMY, Biswajit Kalita, Chun Jiang, Ruihong Chen
Принадлежит: Individual

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.

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Номер записи: 81
09-12-2021 дата публикации

INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR XA DERIVATIVES

Номер: US20210379163A1
Автор: Conley Pamela B., Karbarz Mark, Lu Genmin, Pandey Anjali, Sinha Uma
Принадлежит:

The present disclosure relates to compositions and methods for the treatment of bleeding disorders, such as hemophilia A, hemophilia B, von Willebrand (vWF) disease, and factor XII deficiency, by reducing the circulating concentration of tissue factor pathway inhibitor (TFPI), with a factor Xa derivative. 1. A method for treating a bleeding disorder in a subject in need thereof , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.2. The method of claim 1 , wherein the bleeding disorder is selected from the group consisting of hemophila A claim 1 , hemophilia B claim 1 , a von Willebrand (vWF) disease claim 1 , a factor XII deficiency and combinations thereof.3. A method for improving blood clotting in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.4. A method for reducing the concentration of circulating tissue factor pathway inhibitor (TFPI) in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.5. The method of claim 4 , wherein the subject suffers from a bleeding disorder.6. The method of claim 4 , wherein the subject is experiencing or at risk of experiencing a bleeding episode.7. The method of claim 1 , wherein the modification comprises substitution of Ser379 with dehydro-alanine or ...

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Номер записи: 82
27-08-2020 дата публикации

APHRODISIAC COMPOSITION AND MANAGEMENT OF MALE SEXUAL DYSFUNCTION

Номер: US20200268822A1
Автор: Bani Sarang, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

The present invention discloses a composition for the therapeutic management of male sexual dysfunction and related disorders. Specifically, the invention discloses a composition comprising 60-65% w/w extract, 12-18% w/w extract, 5-10% w/w extract, 12-18% w/w extract, 0.1-2% w/w extract, for use as an aphrodisiac. 1Withania somniferaMucana pruriensColeus forskoliiKaempferia parvifloraPiper nigrum. A method for increasing libido in mammals , said method comprising step of administering an effective dose of a composition , based on the body weight of the mammal , comprising 60-65% w/w extract standardized to contain 0.25% withaferin and 7% withanolides , 12-18% w/w extract standardized to contain 10% w/w L-dopa , 5-10%/o w/w extract standardized to contain 10% w/w forskolin , 12-18% w/w standardized to contain 2.5% w/w of 5 ,7-dimethoxyflavone and not less than 10% w/w Total flavonoids and 0.1-2% w/w extract standardized to contain 95% w/w piperine to mammals in need of such effect.2. The method as in claim 1 , wherein the composition comprises at least one phytochemical selected from the group of phospho diesterase 5 (PDE-5) inhibitor; testosterone enhancer claim 1 , Nitric oxide enhancer claim 1 , cGMP enhancer claim 1 , anti-spasmodic and vasodilator claim 1 , androgen receptor activator and cGMP protein kinase activator.3. The method as in claim 1 , wherein the effect dose of the composition is 50-200 mg/kg body weight.4. The method as in claim 1 , wherein the mammal is preferably male.5. The method as in claim 1 , wherein the mammal is preferably human.6. The method as in claim 1 , wherein the composition is formulated with pharmaceutically/nutraceutically acceptable excipients claim 1 , adjuvants claim 1 , diluents or carriers and administered in the form of tablets claim 1 , capsules claim 1 , syrups claim 1 , gummies claim 1 , powders claim 1 , suspensions claim 1 , emulsions claim 1 , chewable claim 1 , candies or eatables.7Withania somniferaMucana ...

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Номер записи: 83
22-10-2015 дата публикации

INHIBITORS OF SYK AND JAK PROTEIN KINASES

Номер: US20150297595A1
Автор: Bauer Shawn M., Huang Wolin, Jia Zhaozhong J., Kane Brian, Mehrotra Mukund, Pandey Anjali, Rose Jack W., Song Yonghong, Venkataramani Chandrasekar, Xu Qing
Принадлежит:

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. 190.-. (canceled) This application is a continuation of U.S. patent application Ser. No. 13/658,730 (filed Oct. 23, 2012), which is a continuation of U.S. patent application Ser. No. 13/275,253 (filed Oct. 17, 2011), which is a continuation of U.S. patent application Ser. No. 13/269,523 (filed Oct. 7, 2011), which is a continuation of U.S. patent application Ser. No. 12/386,525 (filed Apr. 16, 2009), which claims the benefit of priority under 35 USC §119(e) of U.S. Provisional Patent Application No. 61/120,348, filed Dec. 5, 2008; U.S. Provisional Patent Application No. 61/120,346, filed Dec. 5, 2008; U.S. Provisional Patent Application No. 61/120,341 filed Dec. 5, 2008; U.S. Provisional Patent Application No. 61/045,499, filed Apr. 16, 2008; U.S. Provisional Patent Application No. 61/045,406, filed Apr. 16, 2008; and U.S. Provisional Patent Application No. 61/045,399, filed Apr. 16, 2008, which are herein incorporated by reference in their entirety for all purposes.This invention is directed to pyrimidine-5-carboxamide compounds which act as inhibitors of Spleen tyrosine kinase (syk) and/or ‘JAK kinases. This invention is also directed to pharmaceutical compositions containing the pyrimidine-5-carboxamide compounds and methods of using the compounds or compositions to treat a condition characterized by other indications. The invention is also directed to ...

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Номер записи: 84
29-10-2015 дата публикации

METHOD FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA

Номер: US20150306059A1
Автор: Bani Sarang, Majeed Anju, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

Disclosed is a therapeutic management method of hypercholesterolemia in mammals. More specifically, the present invention relates to a method of reducing high levels of circulating cholesterol (hypercholesterolemia) in the blood stream of mammals, said method involving step of administering therapeutically effective amounts of Calebin A to said mammals to bring about the effects of (i) reducing the amount of total blood cholesterol levels; (ii) reducing the concentrations of low density lipoproteins (LDL) and very low density lipoproteins (VLDL); (iii) increasing the concentrations of high density lipoproteins (HDL) and (iv) reducing concentrations of serum triglycerides. 1. A method of reducing high levels of circulating cholesterol (hypercholesterolemia) in mammalian blood , said method involving step of orally administering therapeutically effective amounts of Calebin A to said mammals to achieve the effect of reducing the concentration of total cholesterol in the blood.2. A method of treating hypercholesterolemia in mammals , said method involving step of orally administering therapeutically effective amounts of Calebin A to bring about effects of (i) reducing the concentrations of low density lipoproteins (LDL) and very low density lipoproteins (VLDL) and (ii) increasing the concentrations of high density lipoproteins (HDL) in the blood of said animals.3. A method of reducing high levels of serum triglycerides in mammals , said method involving the step of orally administering therapeutically effective amounts of Calebin A to mammals in need of such reduction.48-. (canceled) The invention in general relates to therapeutic management methods for hypercholesterolemia. More specifically, the present invention relates to the management of hypercholesterolemia in mammalian subjects using therapeutically effective amounts of Calebin A.Hypercholesterolemia is a condition characterized by very high levels of cholesterol in the blood. The common medical causes of ...

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Номер записи: 85
29-10-2015 дата публикации

METHOD FOR THE TREATMENT OF HYPERCHOLESTEROLEMIA

Номер: US20150306060A1
Автор: Bani Sarang, Majeed Anju, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

Disclosed is a therapeutic management method of hypercholesterolemia in mammals. More specifically, the present invention relates to a method of reducing high levels of circulating cholesterol (hypercholesterolemia) in the blood stream of mammals, said method involving step of administering therapeutically effective amounts of Calebin A to said mammals to bring about the effects of (i) reducing the amount of total blood cholesterol levels; (ii) reducing the concentrations of low density lipoproteins (LDL) and very low density lipoproteins (VLDL); (iii) increasing the concentrations of high density lipoproteins (HDL) and (iv) reducing concentrations of serum triglycerides. 1. A method of reducing high levels of serum triglycerides in mammals, said method involving the step of orally administering therapeutically effective amounts of Calebin A to mammals in need of such reduction. This patent application is a divisional of co-pending U.S. application Ser. No. 14/259,404 filed 23 Apr. 2014 which is included herein in its entirety.The invention in general relates to therapeutic management methods for hypercholesterolemia. More specifically, the present invention relates to the management of hypercholesterolemia in mammalian subjects using therapeutically effective amounts of Calebin A.Hypercholesterolemia is a condition characterized by very high levels of cholesterol in the blood. The common medical causes of hypercholesterolemia include,1. Carcinoma, hepatocellular;2. Hypertriglyceridemia;3. Familial hypercholesterolemia;4. Coronary artery disease;5. Diabetes mellitus;6. Nephritic syndrome;7. Zieve's syndrome;8. Anorexia nervosa;9. Lack of physical activity;10. Obesity; and11. Diet rich in saturated fatWhile the human body requires cholesterol for multifarious functions like building cell membranes, making hormones, and producing, fat digestive compound, excessive cholesterol increases a person's risk of developing heart disease. People with hypercholesterolemia have ...

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Номер записи: 86
24-09-2020 дата публикации

COMPOUNDS AND METHODS OF USE

Номер: US20200299283A1
Автор: CHEN Ruihong, Duraiswamy Athisayamani Jeyaraj, Jiang Chun, KALITA Biswajit, Pandey Anjali
Принадлежит:

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent. 10. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein ring A is C-Ccycloalkyl.11. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein ring A is heterocyclyl.12. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein ring A is aryl.13. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein ring A is heteroaryl.17. The compound of claim 1 , wherein Ris C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , C-Chaloalkyl claim 1 , C-Ccycloalkyl claim 1 , —CN claim 1 , —C(O)OR claim 1 , —C(O)N(R) claim 1 , —N(R) claim 1 , —OR claim 1 , or —C-Calkyl-OR.18. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Ris —C(O)ORor —C(O)N(R).19. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , or pharmaceutically acceptable salt thereof claim 1 , wherein Ris C-Calkyl.20. The compound of claim 1 , or a tautomer claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , isotopically enriched analog claim 1 , ...

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Номер записи: 87
26-11-2015 дата публикации

Compounds and methods for purification of serine proteases

Номер: US20150337285A1
Автор: Anjali Pandey, Jack W. Rose
Принадлежит: Portola Pharmaceuticals LLC

Disclosed herein are compounds, compositions, methods and kits for purifying a serine protease and serine proteases purified with the compounds, compositions and methods.

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Номер записи: 88
08-10-2020 дата публикации

Compositions and methods for management of atrophic gastritis and colitis

Номер: US20200316143A1
Автор: Anjali Pandey, Kalyanam Nagabhushanam, Muhammed Majeed, Sarang Bani, Shaheem Majeed
Принадлежит: Individual

The present invention discloses a method for therapeutic management of atrophic gastritis and colitis using a composition comprising Bacillus coagulans MTCC 5856 individually or in combination with anthocyanins. The invention further discloses a method for preventing neoplastic transformation of mucosal cells in gastro-intestinal tract and improving gut barrier function in mammals using a composition comprising Bacillus coagulans MTCC 5856 individually or in combination with anthocyanins.

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Номер записи: 89
10-12-2015 дата публикации

INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR XA DERIVATIVES

Номер: US20150352194A1
Автор: Conley Pamela B., Karbarz Mark, Lu Genmin, Pandey Anjali, Sinha Uma
Принадлежит:

The present disclosure relates to compositions and methods for the treatment of bleeding disorders, such as hemophilia A, hemophilia B, von Willebrand (vWF) disease, and factor XII deficiency, by reducing the circulating concentration of tissue factor pathway inhibitor (TFPI), with a factor Xa derivative. 1. A method for treating a bleeding disorder in a subject in need thereof , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.2. The method of claim 1 , wherein the bleeding disorder is selected from the group consisting of hemophila A claim 1 , hemophilia B claim 1 , a von Willebrand (vWF) disease claim 1 , a factor XII deficiency and combinations thereof.3. A method for improving blood clotting in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.4. A method for reducing the concentration of circulating tissue factor pathway inhibitor (TFPI) in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.5. The method of claim 4 , wherein the subject suffers from a bleeding disorder.6. The method of claim 4 , wherein the subject is experiencing or at risk of experiencing a bleeding episode.7. The method of claim 1 , wherein the modification comprises substitution of Ser379 with dehydro-alanine or ...

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Номер записи: 90
22-11-2018 дата публикации

INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR XA DERIVATIVES

Номер: US20180333469A1
Автор: Conley Pamela B., Karbarz Mark, Lu Genmin, Pandey Anjali, Sinha Uma
Принадлежит:

The present disclosure relates to compositions and methods for the treatment of bleeding disorders, such as hemophilia A, hemophilia B, von Willebrand (vWF) disease, and factor XII deficiency, by reducing the circulating concentration of tissue factor pathway inhibitor (TFPI), with a factor Xa derivative. 1. A method for treating a bleeding disorder in a subject in need thereof , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.2. The method of claim 1 , wherein the bleeding disorder is selected from the group consisting of hemophila A claim 1 , hemophilia B claim 1 , a von Willebrand (vWF) disease claim 1 , a factor XII deficiency and combinations thereof.3. A method for improving blood clotting in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.4. A method for reducing the concentration of circulating tissue factor pathway inhibitor (TFPI) in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a polypeptide factor Xa (fXa) derivative (a) that comprises a fXa heavy chain that comprises a modification at an active site and (b) that does not include a light chain or comprises a Gla-deficient or des-Gla fXa light chain.5. The method of claim 4 , wherein the subject suffers from a bleeding disorder.6. The method of claim 4 , wherein the subject is experiencing or at risk of experiencing a bleeding episode.7. The method of claim 1 , wherein the modification comprises substitution of Ser379 with dehydro-alanine or ...

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Номер записи: 91
10-12-2015 дата публикации

Nicotinamides as jak kinase modulators

Номер: US20150353495A1
Автор: Anjali Pandey, Brian Kane, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 92
31-10-2019 дата публикации

Compositions for weight loss

Номер: US20190328818A1
Автор: Anjali Pandey, Kalyanam Nagabhushanam, Lakshmi MUNDKUR, Muhammed Majeed, Sarang Bani
Принадлежит: Individual

The present invention discloses a composition comprising extracts of Cyperus rotundus , standardized to contain 3-5% w/w total stilbenes, extracts of Garcinia sp., standardized to contain 20% w/w garcinol and extracts of Coleus forskohlii standardized to contain not less than 10% w/w forskolin for the therapeutic management of diet induced obesity and weight gain and related conditions like liver dysfunction, NASH, NAFLD, liver cirrhosis, hypercholesterolemia, hyperlipidemia, kidney dysfunction by bringing about a reduction in body weight, increasing lean body mass and by normalizing the levels of liver enzymes, kidney markers and circulating lipids.

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Номер записи: 93
07-11-2019 дата публикации

SYNTHESIS OF CERDULATINIB

Номер: US20190337930A1
Автор: Chen Ying, Fumagalli Tiziano, Pandey Anjali, Poggiali Daniele, Sran Arvinder
Принадлежит:

The present disclosure provides processes for the preparation of cerdulatinib, which is of formula I: 4. The process of claim 3 , wherein X claim 3 , Xand Xare the same.10. The process of or claim 3 , wherein the molar ratio of ammonia to Compound F-1 is between about 1.7:1 to about 2.3:1.11. The process of or claim 3 , wherein the molar ratio of ammonia to Compound F-1 is between about 1.9:1 to about 2.0:1.12. The process of any one of claim 3 , - claim 3 , wherein the contacting of ammonia and Compound F-1 is in a solvent.13. The process of any one of and - claim 3 , wherein the contacting of ammonia and Compound F-1 is at a temperature of about −20° C. to about 0° C.14. The process of any one of claim 3 , claim 3 , and - claim 3 , wherein the molar ratio of cyclopropylamine to Compound E-1 is between about 1:1 to about 2:1.15. The process of any one of claim 3 , and - claim 3 , wherein the contacting of cyclopropylamine and Compound E-1 is in a solvent.16. The process of any one of claim 3 , and - claim 3 , wherein the contacting of cyclopropylamine and Compound E-1 is at a temperature of about 20° C. to about 0° C.17. The process of any one of - and - claim 3 , wherein the molar ratio of Compound A-1 to Compound B is about 1:1.18. The process of any one of - and - claim 3 , wherein contacting of Compound A-1 and Compound B is under a neutral condition.19. The process of any one of - and - claim 3 , wherein the contacting of Compound A-1 and Compound B under a neutral condition is at a temperature of about 70° C. to about 100° C.21. The process of claim 20 , wherein the molar ratio of POClto Compound G is between about 2.5:1 to about 3.5:1.22. The process of or claim 20 , wherein contacting of POCland Compound G is in a solvent.23. The process of any one of - claim 20 , wherein the contacting of POCland Compound G is under reflux conditions.28. The process of any one of - claim 20 , further comprising isolating cerdulatinib.29. The process of any one of - claim ...

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Номер записи: 94
10-12-2020 дата публикации

COMPOSITION FOR PROSTAGLANDIN TRANSPORTER INHIBITION AND RELATED THERAPEUTIC APPLICATIONS

Номер: US20200384059A1
Автор: Bani Sarang, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

The present invention discloses a composition comprising extract standardized to contain not less that 0.3% w/w S-allylcysteine, extract standardized to contain not less than 2% w/w nitrates, extract standardized to contain 0.1%-5% w/w thymoquinone, about 0.01%-10% w/w thymohydroquinone, about 20%-95% w/w fatty acids, about 0.001%-3% w/w α-hederin or hederagenin, and extract standardized to contain 3% w/w arjunoglucosides for use a prostaglandin transporter inhibitor. The invention also discloses the use of the aforementioned composition in the therapeutic management of hypertension and cardiovascular complications.

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Номер записи: 95
23-09-2004 дата публикации

Quinazoline derivatives as tgf-beta inhibitors

Номер: WO2004081009A1
Автор: Anjali Pandey, Meenakshi S. Venkatraman, Robert M. Scarborough
Принадлежит: Millennium Pharmaceuticals, Inc.

This invention provides compounds that are useful for treating patients having a TGF-β-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH2CH2, CH2CH2CH2, CH=CH, CH=N, or N=CH; Z is N or C-F; and G is C1-6 aliphatic or a phenyl, naphthyl, or 5-6 membered heteroaryl ring.

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Номер записи: 96
03-11-2022 дата публикации

COMPOSITIONS FOR MANAGEMENT OF POLYCYSTIC OVARY SYNDROME

Номер: US20220347120A1
Автор: Bani Sarang, Majeed Muhammed, Nagabhushanam Kalyanam, Pandey Anjali
Принадлежит:

The invention discloses compositions comprising bisdemethoxycurcumin and methods for managing polycystic ovary syndrome (PCOS) and its associated conditions which include hormonal imbalance, obesity, hypothyroidism, hyperandrogenism, oxidative stress, inflammation, gut dysbiosis, hypercholesterolemia, cardiovascular complications, hyperglycemia and insulin resistance. The invention also discloses the potential of a curcuminoid composition comprising 20-80% w/w bisdemethoxycurcumin, 10-35% w/w demethoxycurcumin and 10-50% w/w curcumin for use in the therapeutic management of PCOS. 1. A method for the management of polycystic ovary syndrome and its associated conditions in a subject , said method comprising steps of a) identifying a mammalian femaleian subject with polycystic ovary syndrome and b) administering an effective dose of bisdemethoxycurcumin to the said subject to alleviate polycystic ovary syndrome , wherein the bisdemethoxycurcumin is formulated with stabilizing agents , bioavailability enhancers , antioxidants , pharmaceutically or nutraceutically or cosmeceutically accepted excipients , enhancers and administered orally in the form of tablets , capsules , syrups , gummies , powders , suspensions , emulsions , chewables , candies or eatables.2. The method as in claim 1 , wherein the associated conditions are selected from the group consisting of hormonal imbalance claim 1 , obesity claim 1 , hypothyroidism claim 1 , hyperandrogenism claim 1 , oxidative stress claim 1 , inflammation claim 1 , gut dysbiosis claim 1 , hypercholesterolemia claim 1 , cardiovascular complications claim 1 , hyperglycemia and insulin resistance.3. The method as in claim 2 , wherein the hormonal imbalance associated with polycystic ovary syndrome is alleviated by decreasing serum levels of Luteinizing hormone and increasing the levels of 17-β estradiol claim 2 , Progesterone and Follicle Stimulating Hormone.4. The method as in claim 2 , wherein obesity associated with polycystic ...

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Номер записи: 97
04-05-2010 дата публикации

Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Номер: US7709640B2
Автор: Anjali Pandey, James Kanter, James Robinson, Robert M. Scarborough
Принадлежит: Millennium Pharmaceuticals Inc

The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

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Номер записи: 98
10-01-2012 дата публикации

Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Номер: USRE43098E1
Автор: Anjali Pandey, James Kanter, James Robinson, Robert M. Scarborough
Принадлежит: Millennium Pharmaceuticals Inc

The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

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Номер записи: 99
17-09-2013 дата публикации

Nitrogenous heterocyclic compounds and process for making nitrogenous heterocyclic compounds and intermediates thereof

Номер: US8536184B2
Автор: Anjali Pandey, James Kanter, James Robinson, Robert M. Scarborough
Принадлежит: Millennium Pharmaceuticals Inc

The present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof and a process for making thereof. The compounds have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention also provides intermediate compounds useful in the process, as well as final products produced by the process, and salts or prodrugs thereof. The invention further provides a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases comprising administering an effective amount of a compound according to the invention to a patient in need thereof.

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Номер записи: 100
12-11-2009 дата публикации

Inhibitors of syk protein kinase

Номер: WO2009136995A2
Автор: Anjali Pandey, Chandrasekar Venkataramani, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I-V and tattooers thereof or pharmaceutically acceptable salts, esters, and pro drugs thereof which are inhibitors of sky kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 101
03-12-2009 дата публикации

Inhibitors of protein kinases

Номер: US20090298823A1
Автор: Anjali Pandey, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 102
03-12-2009 дата публикации

2, 6-diamino-pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors

Номер: WO2009145856A1
Автор: Anjali Pandey, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder, thrombosis, allergy, asthma, rheumatoid arthritis, leukemia, or non-Hodgkin's lymphoma.

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Номер записи: 103
24-12-2009 дата публикации

Inhibitors of protein kinases

Номер: US20090318407A1
Автор: Anjali Pandey, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrota, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 104
25-02-2010 дата публикации

Inhibitors of syk and JAK protein kinases

Номер: US20100048567A1
Автор: Anjali Pandey, Brian Kane, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrota, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 105
13-01-2011 дата публикации

Inhibitors of jak

Номер: US20110005947A1
Автор: Anjali Pandey, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I and tautomers and pharmaceutically acceptable salts thereof which are selective inhibitors of JAK. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK activity, and methods to prevent or treat a number of conditions mediated at least in part by JAK activity.

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Номер записи: 106
10-05-2012 дата публикации

Benzamides and nicotinamides as syk modulators

Номер: WO2012061418A2
Автор: Anjali Pandey, Brian Kane, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

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Номер записи: 107
10-05-2012 дата публикации

Nicotinamides as jak kinase modulators

Номер: WO2012061428A2
Автор: Anjali Pandey, Brian Kane, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods ofinhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 108
10-05-2012 дата публикации

Oxypyrimidines as syk modulators

Номер: WO2012061415A1
Автор: Anjali Pandey, Qing Xu, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula (I) and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which arc inhibitor of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 109
30-05-2013 дата публикации

Pyrazine kinase inhibitors

Номер: WO2013078466A1
Автор: Anjali Pandey, Brian Kane, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

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Номер записи: 110
15-12-2020 дата публикации

Solid forms of cerdulatinib

Номер: US10865198B2
Автор: Anjali Pandey, Gus Kodersha, Julian Scott Northen, Philippe Fernandes, Sami karaborni, YING Chen, Yuelie Lu
Принадлежит: Alexion Pharmaceuticals Inc

Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.

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Номер записи: 111
10-02-2015 дата публикации

Inhibitors of syk and JAK protein kinases

Номер: US8952027B2
Автор: Anjali Pandey, Brian Kane, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 112
06-08-2013 дата публикации

Inhibitors of protein kinases

Номер: US8501944B2
Автор: Anjali Pandey, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to a compound of the formula: and pharmaceutically acceptable tautomers, or salts thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to pharmaceutical compositions containing such a compound.

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Номер записи: 113
08-01-2013 дата публикации

Inhibitors of syk and JAK protein kinases

Номер: US8349860B2
Автор: Anjali Pandey, Brian Kane, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 114
27-11-2012 дата публикации

Inhibitors of SYK and JAK protein kinases

Номер: US8318755B2
Автор: Anjali Pandey, Brian Kane, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 115
16-08-2022 дата публикации

Inhibitors of protein kinases

Номер: US11414410B2
Автор: Anjali Pandey, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Alexion Pharmaceuticals Inc

The present invention is directed to methods of treating multiple myeloma by administering a compound of Formula (I) or pharmaceutically acceptable salt thereof.

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Номер записи: 116
30-12-2009 дата публикации

2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or jak kinases inhibitors

Номер: WO2009136995A3
Автор: Anjali Pandey, Chandrasekar Venkataramani, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals, Inc.

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods ofinhibilion the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as cardiovascular disease, inflammatory disease and autoimmune disease and cell proliferative disorder. Formula (I) Y 1 is selected from the group consisting of: (a) and (b); Z is O or S; D 1 is selected from the group consisting of: (a) phenyl substituted with a group, R 5 (b) naphthyl (c) C 3-8 cycloalkyl (d) heteroaryl (e) heterocyclyl

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Номер записи: 117