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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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Применить Всего найдено 80. Отображено 79.
13-09-2012 дата публикации

QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS

Номер: US20120232068A1
Принадлежит: Briston-Myers Squibb Company

A compound of formula (I) wherein A, X, Y, Z, Rand Rare described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, Iassociated disorders, and other disorders mediated by ion channel function. 7. The compound claim 6 , enantiomer claim 6 , diastereomer claim 6 , tautomer claim 6 , or salt thereof claim 6 , of claim 6 , wherein:{'sub': 1-10', '1-10', '2', '1', '11', '12, 'X is H, F, Cl, Br, I, Calkoxy, haloCalkyl, —CORor —NRR;'}{'sub': 1-10', '1-10', '2', '11', '11', '12, 'Y is H, F, Cl, Br, I, Calkoxy, haloCalkyl, —CORor —NRR;'}{'sub': 1-10', '1-10', '11', '12, 'Z is H, Cl, Br, I, Calkoxy, haloCalkyl or —NRR;'}{'sub': 11', '12', '1-10', '1-10', '3-10', '6-10', '13, "Rand R, at each occurrence, are independently selected from H, Calkyl, haloCalkyl, Ccycloalkyl, Caryl, a 4- to 12-membered heteroaryl and a 4- to 12-membered heterocyclyl, wherein the alkyl, cycloalkyl, aryl, heteroaryl and heterocyclyl may be optionally substituted with one or more R's and the heteroaryl and heterocyclyl consist of carbon atoms and 1, 2, 3, or 4 heteroatoms independently selected from the group consisting of N, S, or O;"}{'sub': 13a', '1-10', '2-10', '1-10', '3-10', '2-12', '6-10', '1-10', '2', 'm', '2', '14', '14', '2', '14', '14', '14', '2', 'm', '14', '2', '14', '2', 'm', '14', '2', '14', '14', '14', '2', '14', '14', '2', '14', '14', '14', '2', '14', '14', '14', '14', '2', '14', '14', '14', '14a, "Ris independently H, —OH, F, Cl, Br, I, Calkyl, Calkoxy, haloCalkyl, Ccycloalkyl, Calkenyl, Caryl, a 4- to 12-membered heteroaryl, a 4- to 12-membered heterocyclyl, a 4- to 12-membered heteroaryl-Calkyl, —CN, —(CH)—SOR, —NRSOR, —CONRR, —(CH)—NRSOR, —(CH)—NRSONRR, —NRSONRR, —CONRR, —NRCONRR, —NRCOR, —CORor —NRR, wherein the alkyl, cycloalkyl, alkenyl, alkoxy, aryl, heteroaryl and heterocyclyl may be optionally substituted with one or more R's and the heteroaryl and heterocyclyl consist of carbon atoms and 1, 2, 3, ...

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15-08-2013 дата публикации

BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS

Номер: US20130210844A1
Принадлежит: Glenmark Pharmaceuticals S.A.

The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. 2. The compound according to claim 1 , wherein Y is O or NH.3. The compound according to claim 1 , wherein Zis N claim 1 , Zis CH and Gis CH.4. The compound according to claim 1 , wherein Z claim 1 , Zare N and Gis CH.5. The compound according to claim 1 , wherein Zis CH claim 1 , Zis N and Gis CH.6. The compound according to claim 1 , wherein Ris hydrogen claim 1 , methyl or trifluoromethyl.7. The compound according to claim 1 , wherein Ris hydrogen or methyl.8. The compound according to claim 1 , wherein Qis N claim 1 , CH or CR claim 1 , Qis CH or CR claim 1 , Qis N or CH claim 1 , and Qis CR.9. The compound according to claim 1 , wherein Ris OCH claim 1 , CH claim 1 , CHF claim 1 , Cl or F.10. The compound according to claim 1 , wherein Rand Rare hydrogen.11. The compound according to claim 1 , wherein ‘n’ is 1.12. The compound according to claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , tert-butyl claim 1 , 2 claim 1 ,2 claim 1 ,2-trifluoroethyl claim 1 , 3-(trifluoromethyl)phenyl claim 1 , 4-(trifluoromethyl)phenyl claim 1 , 2-fluoro-5-(trifluoromethyl)phenyl claim 1 , 4-fluoro-3-(trifluoromethyl)phenyl claim 1 , 2-fluoro-4-(trifluoromethyl)phenyl claim 1 , 6-(trifluoromethyl)pyridin-3-yl claim 1 , 4 claim 1 ,4-difluorocyclohexyl claim 1 , 4 claim 1 ,4-dimethylcyclohexyl claim 1 , 4-(trifluoromethyl)cyclohexyl claim 1 , (1s claim 1 ,4s)-4-(trifluoromethyl)cyclohexyl or (1r claim 1 ,4r)-4-(trifluoromethyl)cyclohexyl.13. The compound according to claim 1 , wherein W is isopropyl claim 1 , tert- ...

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30-01-2014 дата публикации

QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS

Номер: US20140031345A1
Принадлежит:

A compound of formula I 6. The compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , or salt thereof claim 1 , of claim 1 , wherein X and Y are H.7. The compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , or salt thereof claim 1 , of claim 1 , wherein X claim 1 , Y and Z are H.8. The compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , or salt thereof claim 1 , of claim 1 , wherein Ris F claim 1 , Cl claim 1 , Br or I.9. The compound claim 1 , enantiomer claim 1 , diastereomer claim 1 , tautomer claim 1 , or salt thereof claim 1 , of claim 1 , wherein Ris Cl.10. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound of .11. The pharmaceutical composition of claim 10 , further comprising at least one other therapeutic agent.12. A method of treating or preventing arrhythmia comprising administering to a patient in need thereof an effective amount of at least one compound of .13. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of at least one compound of .14. A method of treating an I-associated condition comprising administering to a patient in need thereof an effective amount of at least one compound of . This application is a continuation of U.S. application Ser. No. 13/393,328 filed Feb. 29, 2012, which was the National Stage of International Application No. PCT/US2010/047430, filed on Sep. 1, 2010, which claims the benefit of U.S. Provisional Application No. 61/239,452, filed on Sep. 3, 2009, each incorporated herein by reference in its entirety.The present invention provides for quinazolines useful as inhibitors of potassium channel function (especially inhibitors of the K1 subfamily of voltage gated K channels, more especially inhibitors of K1.5 (which have been linked to the ultra-rapidly activating delayed rectifier K current I), and/or K1.3 channels, and/or K1.1 ...

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06-01-2022 дата публикации

KIF18A INHIBITORS

Номер: US20220002311A1
Принадлежит: Amgen Inc.

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A. 8. The compound according to wherein Ris H or methyl.9. The compound according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , halo claim 1 , Calk claim 1 , or Chaloalk; and each of Rand Rpair combine with the carbon atom attached to each of them form a saturated 3- claim 1 , 4- claim 1 , or 5-membered monocyclic ring spiro to the Rring; wherein said ring contains 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 or 1 atoms selected from O and S.10. The compound according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , methyl claim 1 , or ethyl; and each of Rand Rpair combine with the carbon atom attached to each of them form a cyclopropyl claim 1 , cyclobutyl claim 1 , or cyclopentyl ring spiro to the Rring.12. The compound according to wherein Z is absent claim 1 , —NH— claim 1 , —NHSO— claim 1 , —O— claim 1 , —SONH— claim 1 , —S(═O)(═NH)— claim 1 , —CH—S(═O)(═NH)— claim 1 , —SO— claim 1 , —CH—SO claim 1 , or CH(CH)—SO.13. The compound according to wherein Ris selected from:a) H;(b) F;{'sub': 1-6', '3', '3', '3', '2, '(c) Calk substituted by 0, 1, 2 or 3 group(s) selected from F, Cl, Br, —CF, —C(═O)CH, —OH, —OCH, —NH, cyclopropyl, cyclopropylmethanol, or 3-(trifluoromethyl)-3H-diazirinyl; or'}{'sub': 3', '1-6', '3', '2, '(d) a saturated, partially-saturated or unsaturated 3-, 4-, 5-, 6-, or 7-membered monocyclic ring containing 0, 1, 2 or 3 N atoms and 0 or 1 atoms selected ...

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15-01-2015 дата публикации

THIAZOLYL- OR THIADIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS

Номер: US20150018344A1
Принадлежит:

Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R, are useful as kinase modulators, including IRAK-4 modulation. 2. A compound of claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein Ris phenyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , naphthyl claim 1 , benzothiazolyl claim 1 , pyrazolopyridinyl claim 1 , benzoisothiazolyl claim 1 , triazolopyridinyl claim 1 , imidazopyridinyl claim 1 , benzooxazolyl claim 1 , triazolopyridinyl claim 1 , imidazopyridinyl claim 1 , pyridopyrazinyl claim 1 , quinazolinyl claim 1 , pyridopyrazinyl claim 1 , benzooxadiazolyl claim 1 , benzothiadiazolyl claim 1 , benzoimidazolyl claim 1 , triazolopyridinyl claim 1 , imdazopyridazinyl claim 1 , pyridopyrazinyl claim 1 , naphthyridinyl claim 1 , quinoxalinyl claim 1 , phthalazinyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , benzothiazolyl claim 1 , benzodioxolyl claim 1 , benzothienyl claim 1 , isoquinolinyl claim 1 , benzopyranyl claim 1 , indolizinyl claim 1 , benzofuranyl claim 1 , chromonyl claim 1 , coumarinyl claim 1 , benzopyranyl claim 1 , cinnolinyl claim 1 , pyrrolopyridyl claim 1 , furopyridyl claim 1 , isoindolyl claim 1 , or quinazolinyl claim 1 , each group substituted by 1-4 groups selected from R.3. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein m is 0.4. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein both Rand Rare hydrogen.8. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein R is —C(═O)—R.9. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein R is —C(═O)NR—R;11. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein X ...

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28-01-2016 дата публикации

System and method for ensuring code quality compliance for various database management systems

Номер: US20160026648A1

A system and computer-implemented method for ensuring code quality compliance for one or more Database Management Systems (DBMSs) is provided. The system comprises a user interface configured to prompt one or more users to select one or more options and provide information for configuring rules corresponding to coding standards and best practices. The system further comprises a rules registration module to register the configured rules in a repository for validation. Furthermore, the system comprises a source selector to provide options to the one or more users to select one or more DBMSs and a source manager to fetch database code from the one or more selected DBMSs. In addition, the system comprises one or more parsers to parse the fetched database code, a validator to validate the parsed code using the registered rules and a report manager to provide results of the validation to the one or more users.

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01-02-2018 дата публикации

QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS

Номер: US20180030034A1
Принадлежит:

A compound of formula I 2. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.3. The pharmaceutical composition of claim 2 , further comprising at least one other therapeutic agent claim 2 , wherein the other therapeutic agent is selected from anti-arrhythmic agents claim 2 , calcium channel blockers claim 2 , anti-platelet agents claim 2 , anti-hypertensive agents claim 2 , anti thrombotic/anti thrombolytic agents claim 2 , anti-coagulants claim 2 , HMG-CoA reductase inhibitors claim 2 , anti diabetic agents claim 2 , thyroid mimetics claim 2 , mineralocorticoid receptor antagonists claim 2 , and cardiac glycosides.4. A method of treating arrhythmia comprising administering to a patient in need thereof an effective amount of the compound of .5. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of the compound of .7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.8. The pharmaceutical composition of claim 7 , further comprising at least one other therapeutic agent claim 7 , wherein the other therapeutic agent is selected from anti-arrhythmic agents claim 7 , calcium channel blockers claim 7 , anti-platelet agents claim 7 , anti-hypertensive agents claim 7 , anti thrombotic/anti thrombolytic agents claim 7 , anti-coagulants claim 7 , HMG-CoA reductase inhibitors claim 7 , anti diabetic agents claim 7 , thyroid mimetics claim 7 , mineralocorticoid receptor antagonists claim 7 , and cardiac glycosides.9. A method of treating arrhythmia comprising administering to a patient in need thereof an effective amount of the compound of .10. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of the compound of .12. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.13. The ...

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24-02-2022 дата публикации

KIF18A INHIBITORS

Номер: US20220056015A1
Принадлежит: Amgen Inc.

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A. 6. The compound according to wherein Ris H or methyl.7. The compound according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , halo claim 1 , Calk claim 1 , or Chaloalk; and each of Rand Rpair combine with the carbon atom attached to each of them form a saturated 3- claim 1 , 4- claim 1 , or 5-membered monocyclic ring spiro to the Rring; wherein said ring contains 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 claim 1 , 1 claim 1 , or 2 atoms selected from O and S.8. The compound according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , methyl claim 1 , or ethyl; and each of Rand Rpair combine with the carbon atom attached to each of them form a cyclopropyl claim 1 , cyclobutyl claim 1 , or cyclopentyl ring spiro to the Rring.11. The compound according to wherein Z is absent claim 1 , —NH— claim 1 , —NHSO— claim 1 , —SONH— claim 1 , —S(═O)(═NH)— claim 1 , —S— claim 1 , —S(═O)— claim 1 , —SO— claim 1 , —(C═O)— claim 1 , or —(C═O)NH—.12. The compound according to wherein Ris selected from (a) H; (b) Calk substituted by 0 claim 1 , 1 claim 1 , 2 or 3 group(s) selected from F claim 1 , Cl claim 1 , Br claim 1 , —OH claim 1 , —OCH claim 1 , or cyclopropyl; or (c) a saturated claim 1 , partially-saturated or unsaturated 3- claim 1 , 4- claim 1 , 5- claim 1 , 6- claim 1 , or 7-membered monocyclic ring containing 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 or 1 atoms selected from ...

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12-02-2015 дата публикации

TRIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS

Номер: US20150045347A1
Принадлежит:

Compounds having the following formula: (I) wherein: A is an optionally substituted triazole, or a stereoisomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation. 3. A compound of claim 1 , or a pharmaceutically-acceptable salt thereof claim 1 , wherein Ris phenyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , naphthyl claim 1 , indolinyl claim 1 , benzothiazolyl claim 1 , pyrazolopyridinyl claim 1 , benzoisothiazolyl claim 1 , triazolopyridinyl claim 1 , imidazopyridinyl claim 1 , benzooxazolyl claim 1 , triazolopyridinyl claim 1 , imidazopyridinyl claim 1 , pyridopyrazinyl claim 1 , quinazolinyl claim 1 , pyridopyrazinyl claim 1 , benzooxadiazolyl claim 1 , benzothiadiazolyl claim 1 , benzoimidazolyl claim 1 , triazolopyridinyl claim 1 , imdazopyridazinyl claim 1 , pyridopyrazinyl claim 1 , naphthyridinyl claim 1 , quinoxalinyl claim 1 , phthalazinyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , benzothiazolyl claim 1 , benzodioxolyl claim 1 , benzothienyl claim 1 , isoquinolinyl claim 1 , benzopyranyl claim 1 , indolizinyl claim 1 , benzofuranyl claim 1 , chromonyl claim 1 , coumarinyl claim 1 , benzopyranyl claim 1 , cinnolinyl claim 1 , pyrrolopyridyl claim 1 , furopyridyl claim 1 , isoindolyl claim 1 , or quinazolinyl claim 1 , each group substituted by 1-4 groups selected from R.4. A compound of claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein m is 0.5. A compound of claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein both Rand Rare hydrogen.12. A compound of claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof wherein Xis N and Xis CR; and R is hydrogen or Calkyl.13. A compound of claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereofis Calkyl substituted with 0-3 Ror phenyl optionally substituted with 0-3 R.14. A pharmaceutical composition comprising a compound of and a ...

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10-03-2022 дата публикации

KIF18A INHIBITORS

Номер: US20220073504A1
Принадлежит: Amgen Inc.

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A. 5. The compound according to wherein Ris H or methyl.6. The compound according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , halo claim 1 , Calk claim 1 , or Chaloalk; and each of Rand Rpair combine with the carbon atom attached to each of them form a saturated 3- claim 1 , 4- claim 1 , or 5-membered monocyclic ring spiro to the Rring; wherein said ring contains 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 or 1 atoms selected from O and S.7. The compound according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , methyl claim 1 , or ethyl; and each of Rand Rpair combine with the carbon atom attached to each of them form a cyclopropyl claim 1 , cyclobutyl claim 1 , or cyclopentyl ring spiro to the Rring.10. The compound according to wherein Z is absent claim 1 , NH— claim 1 , —NHSO—(CH)— claim 1 , —N(CH)—SO—(CH)— claim 1 , —NCHSONH claim 1 , —NHSONH—C(═O)—O— claim 1 , —SONH—(CH)— claim 1 , —(CH)—S(═O)(═NH)— claim 1 , —(CH)—S— claim 1 , —(CH)—S(═O)— claim 1 , (CHCH)—S(═O)— claim 1 , —(CH)—SO— claim 1 , —O— claim 1 , —P(═O) claim 1 , —(C═O)— claim 1 , or —NH(C═O).13. The compound according to wherein Ris a group —Z—R claim 1 , wherein Z is —NHSO— or —SONH—; and Ris oxetanyl claim 1 , cyclopropyl claim 1 , or Ris Calk substituted by 0 claim 1 , 1 claim 1 , 2 or 3 OH group(s).14. The compound according to wherein Ris a group —Z—R claim 1 , wherein Z is —NHSO— and Ris —CH—CH—OH.15. The compound according to wherein Ris halo or a ...

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15-03-2018 дата публикации

Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors

Номер: US20180072712A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula: or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R 7 , are useful as kinase modulators, including IRAK-4 modulation.

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24-03-2016 дата публикации

THIAZOLYL- OR THIADIAZOLYL-SUBSTITUTED PYRIDYL COMPOUNDS USEFUL AS KINASE INHIBITORS

Номер: US20160083375A1
Принадлежит:

Compounds having the following formula: 115.-. (canceled)18. The compound according to claim 16 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 16 , wherein Ris —CH(CH).19. The compound according to claim 16 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 16 , wherein:{'sup': 1a', 'b', 'b', '11', '11', '11', '11', 'b', 'c', 'a', 'a, 'sub': 2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '1-3, 'Ris —CN, —(CH)OR, —(CH)C(O)R, —(CH)NRR, —(CH)C(O)NRR, —(CH)NRC(O)R, Calkyl substituted with 0-2 R, cyclopropyl, cyclohexyl, morpholinyl, phenyl, piperidinyl, pyrazinyl, pyridinyl, pyrimidinyl, pyrrolidinyl, tetrahydrofuranyl, or thiophenyl, each substituted with 0-3 R;'}{'sup': 3', '3a, 'Ris propyl substituted with 0-2 R; and'}r is 0, 1, 2, 3, or 4.20. The compound according to claim 16 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 16 , wherein Ris Calkyl substituted with 0-4 Ror Calkynyl substituted with 0-3 R.21. The compound according to claim 16 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 16 , wherein Ris pyrrolidinyl claim 16 , piperidinyl claim 16 , piperazinyl claim 16 , diazepanyl claim 16 , or 1 claim 16 ,3 claim 16 ,8-triazaspiro[4.5]decan-4-onyl claim 16 , each substituted with 0-3 R.22. The compound according to claim 16 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 16 , wherein said compound is selected from:ethyl 2-(6-(benzo[d]thiazol-6-ylamino)-4-(isopropylamino)pyridin-3-yl)thiazole-4-carboxylate (20);(2-(6-(benzo[d]thiazol-6-ylamino)-4-(isopropylamino)pyridin-3-yl)thiazol-4-yl)(3-hydroxypyrrolidin-1-yl)methanone (22);ethyl 2-(6-(benzo[d]thiazol-6-ylamino)-4-(isopropylamino)pyridin-3-yl)-5-methylthiazole-4-carboxylate (23);(2-(6-(benzo[d]thiazol-6-ylamino)-4-(isopropylamino)pyridin-3-yl)thiazol-4-yl)(3-hydroxypiperidin-1-yl)methanone (24);2-(6-(benzo[d]thiazol-6-ylamino)-4-(isopropylamino)pyridin-3-yl)-5-methyl-N-(3-(piperidin-1-yl)propyl) ...

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08-09-2022 дата публикации

KIF18A INHIBITORS

Номер: US20220281843A1
Принадлежит: Amgen Inc.

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A. 7. The compound according to claim 1 , wherein Ris H or methyl.8. The compound according to claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , halo claim 1 , Calk claim 1 , or Chaloalk; and each of Rand Rpair combine with the carbon atom attached to each of them form a saturated 3- claim 1 , 4- claim 1 , or 5-membered monocyclic ring spiro to the piperidinyl ring; wherein said ring contains 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 or 1 atoms selected from O and S.9. The compound according to claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , methyl claim 1 , or ethyl; and each of Rand Rpair combine with the carbon atom attached to each of them form a cyclopropyl claim 1 , cyclobutyl claim 1 , or cyclopentyl ring spiro to the piperidinyl ring.13. The compound according to claim 1 , wherein Ris —CN claim 1 , or a group —Z—R claim 1 , wherein Z is absent claim 1 , —NH— claim 1 , —NHSO— claim 1 , —SONH— claim 1 , —N═S(═O)—(R)(wherein the two Rpair can alternatively combine with the sulfur atom attached to each of them to form a saturated or partially-saturated 3- claim 1 , 4- claim 1 , 5- claim 1 , or 6-membered monocyclic ring containing 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 claim 1 , 1 claim 1 , or 2 atoms selected from O and S) claim 1 , —S(═O)(═NH)— claim 1 , —S— claim 1 , —S(═O)— claim 1 , —SO— claim 1 , —(C═O)— claim 1 , —(C═O)NH— claim 1 , or —NH(C═O)—; ...

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15-09-2022 дата публикации

KIF18A INHIBITORS

Номер: US20220289724A1
Принадлежит: Amgen Inc.

Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like. 3. The compound according to claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , and R claim 1 , is selected from{'sub': 2', '2', '3, 'a) H, F, Cl, methyl, ethyl, propyl, isopropyl, —CHF, —CHF, —CF, or cyclopropyl; or'}{'sup': Xa', 'Xb', 'Xc', 'Xd, 'sub': 1-6', '1-4, 'b) alternatively, each of Rand Rpair, and Rand Rpair, independently, can combine with the carbon atom attached to each of them to form a cyclopropyl ring, cyclobutyl ring, or cyclopentyl ring wherein each ring is spiro to the pyrrolidinyl, piperidinyl, or morpholinyl ring; and wherein each of said ring is is substituted by 0, 1, 2 or 3 group(s) selected from F, Cl, Br, Calk, Chaloalk, or methoxy; or'}{'sup': Xa', 'Xb', 'Xc', 'Xd, 'sub': '3', 'c) alternatively, each of Rand Rpair or Rand Rpair, independently, can combine to form a >C═CH or >C═CH—CH; and'}{'sup': Xe', 'Xf', 'Xg', 'Xh', 'Xi', 'Xj', 'Xk', 'Xl, 'wherein each of R, R, R, R, R, R, Rand Ris H, F, or methyl.'}4. The compound according to claim L wherein L is —NR—(C═O)—.5. The compound according to claim L wherein L is —(C═O)—NR—.9. The compound according to claim 1 , wherein Ris H or methyl.10. The compound according to claim 1 , wherein Z is absent claim 1 , —SO— claim 1 , —CH—SO claim 1 , —NH— claim 1 , —NHSO— claim 1 , —SONH— claim 1 , —SON(CH)— claim 1 , —O— claim 1 , —(C═O)O— claim 1 , —(C═O)NH— claim 1 , —(C═O)N(CH)— claim 1 , —S(═O)(═NH)— claim 1 , —CH—N(CH)— claim 1 , or —C(═N—OH)—.11. The compound according to claim L wherein Ris selected from:a) H, F, Br, OH, or CN;{'sup': '12a', 'sub': 3', '2', '3', '2, 'b) Rselected from a saturated, partially-saturated or unsaturated 3-, 4-, 5-, ...

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16-05-2019 дата публикации

QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS

Номер: US20190144426A1
Принадлежит:

A compound of formula I 2. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.3. The pharmaceutical composition of claim 2 , further comprising at least one other therapeutic agent claim 2 , wherein the other therapeutic agent is selected from anti-arrhythmic agents claim 2 , calcium channel blockers claim 2 , anti-platelet agents claim 2 , anti-hypertensive agents claim 2 , anti thrombotic/anti thrombolytic agents claim 2 , anti-coagulants claim 2 , HMG-CoA reductase inhibitors claim 2 , anti diabetic agents claim 2 , thyroid mimetics claim 2 , mineralocorticoid receptor antagonists claim 2 , and cardiac glycosides.4. A method of treating arrhythmia comprising administering to a patient in need thereof an effective amount of the compound of .5. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of the compound of .7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.8. The pharmaceutical composition of claim 7 , further comprising at least one other therapeutic agent claim 7 , wherein the other therapeutic agent is selected from anti-arrhythmic agents claim 7 , calcium channel blockers claim 7 , anti-platelet agents claim 7 , anti-hypertensive agents claim 7 , anti thrombotic/anti thrombolytic agents claim 7 , anti-coagulants claim 7 , HMG-CoA reductase inhibitors claim 7 , anti diabetic agents claim 7 , thyroid mimetics claim 7 , mineralocorticoid receptor antagonists claim 7 , and cardiac glycosides.9. A method of treating arrhythmia comprising administering to a patient in need thereof an effective amount of the compound of .10. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of the compound of .12. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.13. The ...

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30-07-2020 дата публикации

KIF18A INHIBITORS

Номер: US20200239441A1
Принадлежит: Amgen Inc.

Compounds of formula (I): 4. The compound of claim 1 , or the pharmaceutically-acceptable salt thereof claim 1 , wherein Ris H or methyl.5. The compound of any one of to claim 1 , or the pharmaceutically-acceptable salt thereof claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , halo claim 1 , Calk claim 1 , or Chaloalk; and each of Rand Rpair combine with the carbon atom attached to each of them form a saturated 3- claim 1 , 4- claim 1 , or 5-membered monocyclic ring spiro to the Rring; wherein said ring contains 0 claim 1 , 1 claim 1 , 2 or 3 N atoms and 0 claim 1 , 1 claim 1 , or 2 atoms selected from O and S.6. The compound of claim 1 , or the pharmaceutically-acceptable salt thereof claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H claim 1 , methyl claim 1 , or ethyl; and each of Rand Rpair combine with the carbon atom attached to each of them form a cyclopropyl claim 1 , cyclobutyl claim 1 , or cyclopentyl ring spiro to the IV ring.10. The compound of claim 1 , or the pharmaceutically-acceptable salt thereof claim 1 , wherein Ris —CN claim 1 , or a group —Z—R claim 1 , wherein Z is a bond claim 1 , —NH— claim 1 , —NHSO— claim 1 , —SONH— claim 1 , —S(═O)(═NH)— claim 1 , —S— claim 1 , —S(═O)— claim 1 , —SO— claim 1 , —(C═O)— claim 1 , —(C═O)NH— claim 1 , or —NH(C═O)—; and{'sup': '12', '(a) Ris H;'}{'sup': '12', '(b) Ris oxetanyl, cyclopropyl; or'}{'sup': '12', 'sub': '1-6', '(c) Ris Calk substituted by 0, 1, 2 or 3 OH group(s).'}12. The compound of claim 1 , or the pharmaceutically-acceptable salt thereof claim 1 , wherein Ris a group —Z—R claim 1 , wherein Z is —NHSO— or —SONH—; and Ris oxetanyl claim 1 , cyclopropyl claim 1 , or Ris Calk substituted by 0 claim 1 , 1 claim 1 , 2 or 3 OH group(s).13. The compound of claim 1 , or the pharmaceutically-acceptable salt thereof claim 1 , wherein Ris a group —Z—R claim 1 , ...

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13-08-2020 дата публикации

QUINAZOLINES AS POTASSIUM ION CHANNEL INHIBITORS

Номер: US20200255407A1
Принадлежит:

A compound of formula I 2. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.3. The pharmaceutical composition of claim 2 , further comprising at least one other therapeutic agent claim 2 , wherein the other therapeutic agent is selected from anti-arrhythmic agents claim 2 , calcium channel blockers claim 2 , anti-platelet agents claim 2 , anti-hypertensive agents claim 2 , anti-thrombotic/anti thrombolytic agents claim 2 , anti-coagulants claim 2 , HMG-CoA reductase inhibitors claim 2 , anti-diabetic agents claim 2 , thyroid mimetics claim 2 , mineralocorticoid receptor antagonists claim 2 , and cardiac glycosides.4. A method of treating arrhythmia comprising administering to a patient in need thereof an effective amount of the compound of .5. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of the compound of .7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of or salt thereof.8. The pharmaceutical composition of claim 7 , further comprising at least one other therapeutic agent claim 7 , wherein the other therapeutic agent is selected from anti-arrhythmic agents claim 7 , calcium channel blockers claim 7 , anti-platelet agents claim 7 , anti-hypertensive agents claim 7 , anti-thrombotic/anti thrombolytic agents claim 7 , anti-coagulants claim 7 , HMG-CoA reductase inhibitors claim 7 , anti-diabetic agents claim 7 , thyroid mimetics claim 7 , mineralocorticoid receptor antagonists claim 7 , and cardiac glycosides.9. A method of treating arrhythmia comprising administering to a patient in need thereof an effective amount of the compound of .10. A method of controlling heart rate comprising administering to a patient in need thereof an effective amount of the compound of . This application is a continuation of U.S. application Ser. No. 16/243,400, filed Jan. 9, 2019 (allowed), which is a continuation of U ...

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25-06-2020 дата публикации

Kif18a inhibitors

Номер: WO2020132648A1
Принадлежит: Amgen Inc.

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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25-06-2020 дата публикации

Kif18a inhibitors

Номер: WO2020132651A1
Принадлежит: Amgen Inc.

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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25-06-2020 дата публикации

Heteroaryl amides useful as kif18a inhibitors

Номер: WO2020132649A1
Принадлежит: Amgen Inc.

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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25-06-2020 дата публикации

Heteroaryl amides useful as kif18a inhibitors

Номер: WO2020132653A1
Принадлежит: Amgen Inc.

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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11-02-2021 дата публикации

Pyridine derivatives as kif18a inhibitors

Номер: WO2021026100A1
Принадлежит: Amgen Inc.

Amide compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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11-02-2021 дата публикации

Kif18a inhibitors

Номер: WO2021026101A1
Принадлежит: Amgen Inc.

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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11-02-2021 дата публикации

Kif18a inhibitors

Номер: WO2021026098A1
Принадлежит: Amgen Inc.

Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like.

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01-02-2022 дата публикации

KIF18A inhibitors

Номер: US11236069B2
Принадлежит: AMGEN INC

Compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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24-06-2021 дата публикации

Heteroaryl amides useful as KIF18A inhibitors

Номер: AU2019401495A1
Принадлежит: AMGEN INC

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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24-06-2021 дата публикации

KIF18A inhibitors

Номер: AU2019403488A1
Принадлежит: AMGEN INC

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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23-08-2017 дата публикации

Triazolyl substituted pyridyl compounds useful as kinase inhibitors

Номер: ES2630705T3
Принадлежит: Bristol Myers Squibb Co

Un compuesto según la fórmula (I):**Fórmula** o un estereoisómero o una sal farmacéuticamente aceptables del mismo, en el que A es un triazol opcionalmente sustituido con 0-2 R; R es hidrógeno, R1, halógeno, ciano, nitro, -OR1, -C(>=O)-R1, -C(>=O)O- R1, -C(>=O)NR11-R1, -S(>=O)2-R1, - NR11C(>=O)- R1, -NR11C(>=O)NR11R1, -NR11C(>=O)O- R1, -NR11S(>=O)2R1 o -NR11R1 o se selecciona entre siguientes grupos:**Fórmula** R1 es alquilo C1-6 sustituido con 0-4 R1a, haloalquilo C1-6, alquenilo C2-6 sustituido con 0-3 R1a, alquinilo C2-6 sustituido con 0-3 R1a, cicloalquilo C3-10 sustituido con 0-3 R1a, arilo C6-10 sustituido con 0-3 R1a, un heterociclo de 5-10 miembros que contiene 1-4 heteroátomos seleccionados entre N, O y S, sustituido con 0-3 R1a, o un heteroarilo de 5-10 miembros que contiene 1-4 heteroátomos seleccionados entre N, O y S, sustituido con 0-3 R1a; R1a es hidrógeno, >=O, F, Cl, Br, OCF3, CN, NO2, -(CH2)rORb, -(CH2)rSRb, -(CH2)rC(O)Rb, -(CH2)rC(O)ORb, - (CH2)rOC(O)Rb, -(CH2)rNR11R11, -(CH2)rC(O)NR11R11, -(CH2)rNRbC(O)Rc, -(CH2)rNRbC(O)ORc, -NRbC(O)NR11R11, -S(O)pNR11R11, -NRbS(O)pRc, -S(O)Rc, -S(O)2Rc, alquilo C1-6 sustituido con 0-2 Ra, haloalquilo C1-6, -(CH2)rcarbociclo de 3-14 miembros sustituido con 0-3 Ra o -(CH2)r-heterociclo o heteroarilo de 5-7 miembros, comprendiendo cada uno átomos de carbono y 1-4 heteroátomos seleccionados entre N, O y S(O)p sustituido con 0-3 Ra; R2 es arilo C6-10 sustituido con 0-4 R2a, un heterociclo de 5-10 miembros que contiene 1-4 heteroátomos seleccionados entre N, O y S, sustituido con 1-4 R2a o un heteroarilo de 5-10 miembros que contiene 1-4 heteroátomos seleccionados entre N, O y S, sustituido con 0-4 R2a; R2a en cada aparición se selecciona independientemente entre hidrógeno, >=O, halo, OCF3, CN, NO2, -(CH2)rORb, -(CH2)rSRb, -(CH2)rC(O)Rb, -(CH2)rC(O)ORb, -(CH2)rOC(O)Rb, -(CH2)rNR11R11, -(CH2)rC(O)NR11R11, - (CH2)rNRbC(O)Rc, -(CH2)rNRbC(O)ORc, -NRbC(O)NR11R11, -S(O)pNR11R11, -NRbS(O)pRc, -S ...

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05-05-2022 дата публикации

Heterocyclic spiro compounds and methods of use

Номер: CA3199082A1
Принадлежит: AMGEN INC

The present disclosure provides compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

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25-06-2020 дата публикации

Heteroaryl amides useful as kif18a inhibitors

Номер: CA3123044A1
Принадлежит: AMGEN INC

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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27-08-2012 дата публикации

QUINAZOLINES AS INHIBITORS OF POTASSIUM ION CHANNELS

Номер: PE20121153A1
Принадлежит: Bristol Myers Squibb Co

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE X ES H, OH, F, Cl, ALQUILO C1-C10, HALOALQUILO C1-C10, ENTRE OTROS; Y ES H, F, Cl, Br, ALQUILO C1-C10, CICLOALQUILO C3-C10, HETEROARILO DE 4-12 MIEMBROS, CN, ENTRE OTROS; Z ES H, Cl, Br, ALQUILO C1-C10, CICLOALQUILO C3-C10, HETEROARILO DE 6-12 MIEMBROS, NO2, ENTRE OTROS; A ES 2-ILMETIL-PIRIDINA, BENZAMIDA, 2-TIAZOL, ENTRE OTROS; R1 ES OH, F, Cl, I, ALQUILO C1-C10, CN, CICLOALQUILO C3-C10, ENTRE OTROS; R24 ES H, CICLOALQUILO C3-C10, ARILO C6-C10, HETEROARILO DE 4-12 MIEMBROS, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 5-FENIL-N-(PIRIDIN-2-ILMETIL)-2-(PIRIMIDIN-5-IL)QUINAZOLIN-4-AMINA; 5-(5-FENIL-4-(PIRIDIN-2-ILMETILAMINO)QUINAZOLIN-2-IL)NICOTINAMIDA; 4-((5-FENIL-2-(PIRIMIDIN-5-IL)QUINAZOLIN-4-ILAMINO)METIL)BENZAMIDA; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBORES DE LA FUNCION DE LOS CANALES DE POTASIO, UTILES EN EL TRATAMIENTO Y PREVENCION DE ARRITMIA, TRASTONOS ASOCIADOS CON Ikur Y OTROS TRASTORNOS MEDIADOS POR LA FUNCION DE LOS CANALES IONICOS REFERRING TO A COMPOUND OF FORMULA I, WHERE X IS H, OH, F, Cl, C1-C10 ALKYL, C1-C10 HALOALKYL, AMONG OTHERS; Y IS H, F, Cl, Br, C1-C10 ALKYL, C3-C10 CYCLOALKYL, 4-12-MEMBER HETEROARYL, CN, AMONG OTHERS; Z IS H, Cl, Br, C1-C10 ALKYL, C3-C10 CYCLOALKYL, 6-12 MEMBER HETEROARYL, NO2, AMONG OTHERS; A IS 2-ILMETHYL-PYRIDINE, BENZAMIDE, 2-THIAZOLE, AMONG OTHERS; R1 IS OH, F, Cl, I, C1-C10 ALKYL, CN, C3-C10 CYCLOALKYL, AMONG OTHERS; R24 IS H, C3-C10 CYCLOALKYL, C6-C10 ARYL, 4-12 MEMBER HETEROARYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE: 5-PHENYL-N- (PYRIDIN-2-ILMETHYL) -2- (PYRIMIDIN-5-IL) QUINAZOLIN-4-AMINE; 5- (5-PHENYL-4- (PYRIDIN-2-ILMETHYLAMINE) QUINAZOLIN-2-IL) NICOTINAMIDE; 4 - ((5-PHENYL-2- (PYRIMIDIN-5-IL) QUINAZOLIN-4-ILAMINO) METHYL) BENZAMIDE; AMONG OTHERS. SAID COMPOUNDS ARE INHIBITORS OF THE FUNCTION OF POTASSIUM CHANNELS, USEFUL IN THE TREATMENT AND PREVENTION OF ARRHYTHMIA, TRASTONS ASSOCIATED WITH Ikur AND OTHER DISORDERS MEDIATED BY THE FUNCTION OF THE ION CHANNELS

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17-03-2022 дата публикации

KIF18A inhibitors

Номер: AU2020326627A1
Принадлежит: AMGEN INC

Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like.

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18-08-2016 дата публикации

Thienopyrrole compounds as s-nitrosoglutathione reductase inhibitors

Номер: WO2016128905A1
Принадлежит: Glenmark Pharmaceuticals S.A.

The present disclosure is directed to compounds of formula (Ib) and pharmaceutically acceptable salts thereof, wherein A, Q, R 1 , R 3 , R 5 and m are as defined herein, which are active as inhibitors of S-Nitrosoglutathione reductase (GSNOR). These compounds prevent, inhibit, or suppress the action of GSNOR and are therefore useful in the treatment of GSNOR mediated diseases, disorders, syndromes or conditions such as, e.g., pulmonary hypertension, acute respiratory distress syndrome (ARDS), asthma, bronchospasm, cough, pneumonia, pulmonary fibrosis, interstitial lung diseases, cystic fibrosis and chronic obstructive pulmonary disease (COPD).

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01-02-2017 дата публикации

Quinazolines as potassium ion channel inhibitors

Номер: EP3124475A1
Принадлежит: Bristol Myers Squibb Co

A compound of formula I wherein A, X, Y, Z, R 1 and R 24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I Kur -associated disorders, and other disorders mediated by ion channel function.

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22-03-2012 дата публикации

Quinazolines as potassium ion channel inhibitors

Номер: AU2010289641A1
Принадлежит: Bristol Myers Squibb Co

A compound of formula (I) wherein A, X, Y, Z, R and R are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I-associated disorders, and other disorders mediated by ion channel function.

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02-11-2011 дата публикации

QUINAZOLINAS AS INHIBITORS OF THE IONIC CHANNELS OF POTASSIUM AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Номер: AR078326A1
Принадлежит: Bristol Myers Squibb Co

Los compuestos son utiles como inhibidores de la funcion de los canales de potasio y en el tratamiento y prevencion de arritmia, trastornos asociados con IKur y otros trastornos mediados por la funcion de los canales ionicos. Reivindicacion 1: Un compuesto, caracterizado porque tiene la formula (1) o un enantiomero, diastereomero, tautomero o sales del mismo, en la que: X es H, -OH, F, Cl, Br, I, alquilo C1-10, alcoxi C1-10, haloalquilo C1-10, alquenilo C2-12 alquinilo C2-12, cicloalquilo C3-10, un heteroarilo de 4 a 12 miembros, heterociclilo de 4 a 12 miembros, -CN, -NO2, -NR11SO2R12, -SO2NR11R12, -CONR11R12, -NR11CONR11R12, -NCOR11, -NR11SO2NR11R12, -OCONR11R12, -CO2R11 o -NR11R12; Y es H, F, Cl, Br, I, alquilo C1-10, alcoxi C1-10, haloalquilo C1-10, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-10, un heteroarilo de 4 a 12 miembros, heterociclilo de 4 a 12 miembros, -CN, -NO2, -SO2NR11R12, -CONR11R12, -NR11CONR11R12, -NCOR11, -NR11SO2NR11R12, -OCONR11R12, -CO2R11 o -NR11R12; Z es H, Cl, Br, I, alquilo C1-10, alcoxi C1-10, haloalquilo C1-10, alquenilo C2-12, alquinilo C2-12, cicloalquilo C3-10, un heteroarilo de 6 a 12 miembros, heterociclilo de 4 a 12 miembros, -NO2, -NR11SO2R12, -SO2NR11R12, -NR11CONR11R12, -NCOR11, -NR11SO2NR11R12, -OCONR11R12, -CO2R11 o -NR11R12; A es -(CH2)m-R2, -CH(R25)(R26), -CH(R26)CO2-R2a o -(CH2)n-1-NR25-CO2-R24; m es 0 a 4; n es 1 a 4; n-1 es 2 a 4; R1 es -OH, F, Cl, Br, I, alquilo C1-10, haloalquilo C1-10, alquenilo C2-12, cicloalquilo C3-10, -CN, -(CH2)n-SO2NR11R12, -(CH2)n-CO2R11 o -(CH2)n-NR11SO2R12, pudiendo estar el alquenilo y cicloalquilo opcionalmente sustituidos con uno o más R13; o R1 se selecciona del grupo de formulas (2); o R1 es el resto de formula (3); R2 es alquilo C1-10, ciclopropilo opcionalmente sustituido con uno o más R13; cicloalquilo C4-10 opcionalmente sustituido con uno o más R13bb; cicloalquenilo C3-10 opcionalmente sustituido con uno o más R13b; o -NR14R14; con la condicion de que R2 no sea -NR14R14 ...

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17-03-2022 дата публикации

Quinazolines as inhibitors of potassium ion channels

Номер: ES2900504T3
Принадлежит: Bristol Myers Squibb Co

Una composición farmacéutica para administración oral, que comprende un compuesto de fórmulas (Ib) o (Ic) o un enantiómero, un diastereómero, un tautómero o una sal del mismo, y un vehículo o un diluyente farmacéuticamente aceptables: **(Ver fórmula)** en las que: X es H, F, Cl, Br, I, alcoxi C1-10 o haloalquilo C1-10; Y es H, F, Cl, Br, I, alcoxi C1-10 o haloalquilo C1-10; Z es H, Cl, Br, I, alcoxi C1-10 o haloalquilo C1-10; R13a es independientemente H, -OH, F, Cl, Br, I, alquilo C1-10, alcoxi C2-10, haloalquilo C1-10, cicloalquilo C3-10, alquenilo C2-12, arilo C6-10, un heteroarilo de 4 a 12 miembros, un heterociclilo de 4 a 12 miembros, un heteroaril de 4 a 12 miembros-alquilo C1-10, -CN, -(CH2)m-SO2R14, -NR14SO2R14, -CONR14R14, -(CH2)m-NR14SO2R14, -(CH2)n- NR14SO2NR14R14, -CO2R14 o -NR14R14 en donde el alquilo, el cicloalquilo, el alquenilo, el alcoxi, el arilo, el heteroarilo y el heterociclilo pueden estar opcionalmente sustituidos con uno o más R14a y el heteroarilo y el heterociclilo consisten en átomos de carbono y 1, 2, 3 o 4 heteroátomos independientemente seleccionados del grupo que consiste en N, S u O; R13a-2 es independientemente H, -OH, F, Br, I, alquilo C1-10, alcoxi C1-10, haloalquilo C1-10, cicloalquilo C3-10, alquenilo C2-12, arilo C6-10, un heteroarilo de 4 a 12 miembros, un heterociclilo de 4 a 12 miembros, un heteroaril de 4 a 12 miembros-alquilo C1-10, -(CH2)m-SO2R14, -NR14SO2R14, -CONR14R14, -(CH2)m-SO2NR14R14, -(CH2)m-NR14SO2R14, - (CH2)n-NR14SO2NR14R14, -NR14SO2NR14R14, -CO2R14 o -NR14R14, en donde el alquilo, el cicloalquilo, el alquenilo, el alcoxi, el arilo, el heteroarilo y el heterociclilo pueden estar opcionalmente sustituidos con uno o más R14a y el heteroarilo y el heterociclilo consisten en átomos de carbono y 1, 2, 3 o 4 heteroátomos independientemente seleccionados del grupo que consiste en N, S u O; R13b es independientemente H, F, Cl, Br, I, alquilo C1-10, alcoxi C1-10, haloalquilo C1-10, cicloalquilo C3-10, alquenilo C2-12, ...

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08-06-2023 дата публикации

Heterocyclic spiro compounds and methods of use

Номер: AU2021370660A1
Принадлежит: AMGEN INC

The present disclosure provides compounds of Formula (I) having activity as inhibitors of G12C mutant

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28-11-2017 дата публикации

Quinazolines as potassium ion channel inhibitors

Номер: HUE032983T2
Принадлежит: Bristol Myers Squibb Co

A compound of formula I wherein A, X, Y, Z, R 1 and R 24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I Kur -associated disorders, and other disorders mediated by ion channel function.

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05-08-2021 дата публикации

KIF18A INHIBITORS

Номер: PE20211475A1
Принадлежит: AMGEN INC

Compuestos de formula (I), donde: X1 es N o -CR6 ; R1 es -CN, o un grupo -Z-R12 en el que Z es -NR11 -, -NR11SO2-, entre otros; R2 es halo o un grupo -Y-R13, en el que Y es -alc C0-4-, -N(alc C0-1)-alc C0-4-, entre otros; R3 es H, alc C1-4, o haloalc C1-4; R4 es H, halo, R4a o R4b; R5 es H, halo, alc C1-8, o haloalc C1-4; R6 es H, halo, alc C1-8, haloalc C1-4, entre otros; R7 es H, halo, alc C1-8, o haloalc C1-4; R8 es H, halo, alc C1-8, haloalc C1-4, entre otros; R9 es H, halo, alc C1-8, o haloalc C1-4; Rx es a), b), c) o d); cada uno de R10a, R10b, R10c, R10d, R10e, R10f, R10g, R10h, R10i, y R10j es H, halo, R10k, o R10l; R11 es H, R11a, o R11b; R12 es H, R12a, o R12b; R13 es R13a o R13b; R4a, R10k, R11a, R12a, y R13a es un anillo monociclico de 3, 4, 5, 6 o 7 miembros saturado, parcialmente saturado o insaturado, entre otros; R4b, R8b, R10l, R11b, R12b, y R13b son alc C1-6 sustituido por 0, 1, 2, 3, 4, o 5 grupo(s) seleccionado(s) entre F, Cl, Br, -ORa , -Ohaloalc C1-4, o CN; Ra es H o Rb ; y Rb es alc C1-6, fenilo o bencilo, en el que el alc C1-6 esta siendo sustituido por 0, 1, 2 o 3 sustituyentes seleccionados entre halo, - OH, -alc OC1-4, -NH2, -NHalc C1-4, -OC(=O)alc C1-4, o -N(alc C1-4)alc C1-4; y el fenilo o bencilo esta siendo sustituido por 0, 1, 2 o 3 sustituyentes seleccionados entre halo, alc C1-4, haloalc C1-3, -OH, -Oalc C1-4, -NH2, entre otros. Dichos compuestos modulan la proteina KIF18A alterando de esta forma el proceso del ciclo celular y la proliferacion celular para tratar el cancer y enfermedades relacionadas con cancer. La invencion tambien incluye composiciones farmaceuticas, que incluyen los compuestos, y metodos para tratar patologias relacionadas con la actividad de KIF18A. Compounds of formula (I), where: X1 is N or -CR6; R1 is -CN, or a group -Z-R12 where Z is -NR11 -, -NR11SO2-, among others; R2 is halo or a group -Y-R13, wherein Y is -alk C0-4-, -N (alk C0-1) -alk C0-4-, among others; R3 is H, C1-4 alk, or C1-4 haloalk; R4 is H, ...

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08-09-2021 дата публикации

KIF18A INHIBITORS

Номер: BR112021011989A2
Принадлежит: Amgen Inc.

inibidores de kif18a. compostos da fórmula (i): (i), como aqui definido, e seus intermediários sintéticos, que são capazes de modular a proteína kif18a, influenciando assim o processo de ciclo celular e proliferação celular para tratar câncer e doenças relacionadas ao câncer. a invenção também inclui composições farmacêuticas, incluindo os compostos e métodos de tratamento de estados de doença relacionados à atividade de kif18a. kif18a inhibitors. compounds of formula (i): (i), as defined herein, and their synthetic intermediates, which are capable of modulating the kif18a protein, thereby influencing the cell cycle process and cell proliferation to treat cancer and cancer-related diseases. the invention also includes pharmaceutical compositions, including the compounds and methods of treating disease states related to kif18a activity.

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01-10-2014 дата публикации

BICYCLE COMPOUNDS AS INHIBITORS OF mPGES-1

Номер: AR089939A1
Принадлежит: Glenmark Pharmaceuticals SA

La presente se refiere a compuestos de fórmula (1) y sales farmacéuticamente aceptables de estos, como inhibidores de mPGES-1. Estos compuestos son inhibidores de la enzima prostaglandina E1 sintasa microsomal (mPGES-1) y por lo tanto son útiles en el tratamiento de dolor y/o inflamación de una variedad de enfermedades o afecciones, tales como asma, osteoartritis, artritis reumatoide, dolor agudo o crónico y enfermedades neurodegenerativas. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable de este, donde Y es O, NH o NRᶜ; Z¹ y Z³, que pueden ser iguales o diferentes, se seleccionan independientemente de N y CR²; G¹ se selecciona de N y CR³; con una condición de que al menos uno de Z¹, Z³ y G¹ sea N; Q¹, Q², Q³ y Q⁴, que pueden ser iguales o diferentes, se seleccionan independientemente de N, CH y CR⁴; con una condición de que Q², Q³ y Q⁴ no sean N simultáneamente; W se selecciona de alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido y tetrahidrofurilo o tetrahidrofuranilo sustituido o no sustituido; R¹ se selecciona de alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈alquilo C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no sustituido, arilo C₆₋₁₄ sustituido o no sustituido, heterociclilo de 3 - 15 miembros sustituido o no sustituido y heteroarilo de 5 - 14 miembros sustituido o no sustituido; cada aparición de R² y R³, que pueden ser iguales o diferentes, se selecciona independientemente de hidrógeno, halógeno, nitro, ciano, hidroxilo, alquilo C₁₋₈ sustituido o no sustituido, alcoxi C₁₋₈ sustituido o no sustituido, haloalquilo C₁₋₈ sustituido o no sustituido, hidroxialquilo C₁₋₈ sustituido o no sustituido, cicloalquilo C₃₋₁₂ sustituido o no ...

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25-06-2020 дата публикации

Kif18a inhibitors

Номер: CA3123042A1
Принадлежит: AMGEN INC

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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11-02-2021 дата публикации

Kif18a inhibitors

Номер: CA3147276A1
Принадлежит: AMGEN INC

Amide compounds of formula (I): as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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26-01-2016 дата публикации

Heterocyclic-substituted pyridyl compounds useful as kinase inhibitors

Номер: US9242975B2
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula: wherein A is, or; and X is N or C—R 7 , or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, are useful as kinase modulators, including IRAK-4 modulation.

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16-08-2021 дата публикации

Kif18a inhibitors.

Номер: MX2021007156A
Принадлежит: AMGEN INC

Compuestos de fórmula (I): (ver Fórmula) (I), como se definen en el presente documento, e intermedios sintéticos de los mismos, que pueden modular la proteína KIF18A alterando de esta forma el proceso del ciclo celular y la proliferación celular para tratar el cáncer y enfermedades relacionadas con cáncer. La invención también incluye composiciones farmacéuticas, que incluyen los compuestos, y métodos para tratar patologías relacionadas con la actividad de KIF18A.

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11-02-2021 дата публикации

Kif18a inhibitors

Номер: CA3147451A1
Принадлежит: AMGEN INC

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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08-06-2022 дата публикации

Kif18a inhibitors

Номер: EP4007752A1
Принадлежит: AMGEN INC

Amide compounds of formula (I): and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of Kinesin Motor Protein KIF18A, such as cancer, psoriasis, atopic dermatitis, an autoimmune disorder, or inflammatory bowel disease, and the like.

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16-11-2023 дата публикации

Inhibidores de KIF18A

Номер: ES2953821T3
Принадлежит: AMGEN INC

Compuestos de fórmula (I): (I), como se define en el presente documento, y sus intermedios sintéticos, que son capaces de modular la proteína KIF18A, influyendo así en el proceso del ciclo celular y la proliferación celular para tratar el cáncer y las enfermedades relacionadas con el cáncer. La invención también incluye composiciones farmacéuticas, incluidos los compuestos, y métodos para tratar estados patológicos relacionados con la actividad de KIF18A. (Traducción automática con Google Translate, sin valor legal)

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30-08-2023 дата публикации

Heterocyclic spiro compounds and methods of use

Номер: EP4232444A1
Принадлежит: AMGEN INC

Provided are compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

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21-12-2023 дата публикации

Heterocyclic spiro compounds and methods of use

Номер: US20230406860A1
Принадлежит: AMGEN INC

The present disclosure provides compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

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22-02-2024 дата публикации

Heterocyclic spiro compounds and methods of use

Номер: US20240059703A1
Принадлежит: AMGEN INC

Provided are compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

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19-11-2014 дата публикации

Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors

Номер: EP2802579A1
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula (I) or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C-R 7 , are useful as kinase modulators, including IRAK-4 modulation.

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02-08-2022 дата публикации

Degradadores de smarca2-vhl.

Номер: MX2022008487A
Принадлежит: AMGEN INC

La presente invención proporciona un compuesto de fórmula (I) o una sal farmacéuticamente aceptable del mismo, composiciones farmacéuticas que comprenden un compuesto de la invención, un método para fabricar compuestos de la invención y usos terapéuticos de los mismos. (ver Fórmula).

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12-10-2023 дата публикации

Quinazolines as potassium ion channel inhibitors

Номер: US20230322726A1
Принадлежит: Bristol Myers Squibb Co

A compound of formula Iwherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.

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22-06-2023 дата публикации

Compuestos espiro heterocíclicos y métodos de uso.

Номер: MX2023004802A
Принадлежит: AMGEN INC

La presente divulgación proporciona compuestos de Fórmula I que tienen actividad como inhibidores de la proteína mutante KRAS G12C. (ver fórmula). Esta divulgación también proporciona composiciones farmacéuticas que comprenden los compuestos, usos y métodos para tratar determinados trastornos, tales como el cáncer, que incluyen, pero sin limitación, cáncer de pulmón, cáncer de páncreas y cáncer colorrectal.

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11-04-2024 дата публикации

Tethered heterocyclic inhibitors of kras g12c mutant proteins and uses thereof

Номер: WO2024076670A2
Принадлежит: Amgen Inc.

The present disclosure provides compounds having activity as inhibitors of the G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic, and colorectal cancer. In particular, the disclosure provides compounds of Formula (II) and pharmaceutically acceptable salts thereof, wherein the substituents are as described.

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19-06-2023 дата публикации

Compuestos espiro heterocíclicos y métodos de uso.

Номер: MX2023004518A
Принадлежит: AMGEN INC

La presente divulgación proporciona compuestos de Fórmula I que tienen actividad como inhibidores de la proteína mutante KRAS G12C. (ver fórmula) Esta divulgación también proporciona composiciones farmacéuticas que comprenden los compuestos, usos y métodos para tratar determinados trastornos, tales como el cáncer, que incluyen, pero sin limitación, cáncer de pulmón, cáncer de páncreas y cáncer colorrectal.

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15-07-2021 дата публикации

Smarca2-vhl degraders

Номер: CA3167166A1
Принадлежит: AMGEN INC

The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.

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30-05-2024 дата публикации

Tethered heterocyclic inhibitors of kras g12c mutant proteins and uses thereof

Номер: WO2024076670A3
Принадлежит: Amgen Inc.

The present disclosure provides compounds having activity as inhibitors of the G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic, and colorectal cancer. In particular, the disclosure provides compounds of Formula (II) and pharmaceutically acceptable salts thereof, wherein the substituents are as described.

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11-04-2024 дата публикации

Heterocyclic inhibitors of kras g12c mutant proteins and uses thereof

Номер: WO2024076674A1
Принадлежит: Amgen Inc.

The present disclosure provides compounds having activity as inhibitors of the G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic, and colorectal cancer. In particular, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein the substituents are as described.

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11-04-2024 дата публикации

Heterocyclic inhibitors of kras g12c mutant proteins and uses thereof

Номер: WO2024076672A1
Принадлежит: Amgen Inc.

The present disclosure provides compounds having activity as inhibitors of the G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic, and colorectal cancer. In particular, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein the substituents are as described.

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17-09-2023 дата публикации

مثبطات kif18a

Номер: JOP20210154B1
Принадлежит: AMGEN INC

يتعلق الاختراع الحالي بمركبات بالصيغة (I): كما تم تحديده في هذه الوثيقة، والمركبات الوسيطة المخلقة منها، حيث تكون قادرة على تعديل بروتين KIF18A بالتالي تؤثر على عملية دورة الخلية وتكاثر الخلية لعلاج السرطان والأمراض المتعلقة بالسرطان. يتضمن الاختراع أيضاً تركيبات صيدلانية، تتضمن المركبات، وطرق معالجة حالات مرضية تتعلق بنشاط KIF18A.

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24-03-2023 дата публикации

Κιναζολινες ως αναστολεις διαυλων ιοντων καλιου

Номер: CY1125021T1
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

Φαρμακευτικές συνθέσεις για εκ του στόματος χορήγηση που περιλαμβάνουν μία ένωση του χημικού τύπου (Ib) ή (Ic) ή ένα εναντιομερές, διαστερεομερές, ταυτομερές, ή άλας εξ αυτής, και μία φαρμακευτικώς αποδεκτή ουσία-όχημα ή αραιωτικό:

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06-09-2023 дата публикации

Heterocyclic spiro compounds and methods of use

Номер: EP4237086A1
Принадлежит: AMGEN INC

The present disclosure provides compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

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22-02-2022 дата публикации

Inhibidores de kif18a.

Номер: MX2022001181A
Принадлежит: AMGEN INC

Compuestos de fórmula (I): (ver Fórmula) (I), como se definen en el presente documento, y compuestos intermedios sintéticos de los mismos, que son capaces de modular la proteína KIF18A, alterando de esta forma el proceso del ciclo celular y la proliferación celular para tratar el cáncer y enfermedades relacionadas con el cáncer. La invención también incluye composiciones farmacéuticas que incluyen los compuestos, y métodos para tratar estados patológicos relacionados con la actividad de KIF18A.

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22-02-2022 дата публикации

Inhibidores de kif18a.

Номер: MX2022001295A
Принадлежит: AMGEN INC

Compuestos de amida de fórmula (I): (ver Fórmula) (I), y composiciones que los contienen, así como procesos para preparar dichos compuestos. En el presente documento, también se proporcionan métodos para tratar trastornos o enfermedades que se pueden tratar mediante la inhibición de la proteína motora cinesina KIF18A, tales como cáncer, psoriasis, dermatitis atópica, un trastorno autoinmunitario o enfermedad inflamatoria intestinal y similares.

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06-08-2024 дата публикации

KIF18A inhibitors

Номер: US12054476B2
Принадлежит: AMGEN INC

Compounds of formula (I):as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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26-09-2024 дата публикации

Kif18a inhibitors

Номер: US20240317715A1
Принадлежит: AMGEN INC

Compounds of formula (I):as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

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02-10-2024 дата публикации

Heteroaryl amides useful as kif18a inhibitors

Номер: EP3898616B1
Принадлежит: AMGEN INC

Подробнее
09-01-2018 дата публикации

Thiazolyl- or thiadiazolyl-substituted pyridyl compounds useful as kinase inhibitors

Номер: US09862715B2
Принадлежит: Bristol Myers Squibb Co

Compounds having the following formula: or an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein X is N or C—R 7 , are useful as kinase modulators, including IRAK-4 modulation.

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05-12-2017 дата публикации

System and method for ensuring code quality compliance for various database management systems

Номер: US09836487B2

A system and computer-implemented method for ensuring code quality compliance for one or more Database Management Systems (DBMSs) is provided. The system comprises a user interface configured to prompt one or more users to select one or more options and provide information for configuring rules corresponding to coding standards and best practices. The system further comprises a rules registration module to register the configured rules in a repository for validation. Furthermore, the system comprises a source selector to provide options to the one or more users to select one or more DBMSs and a source manager to fetch database code from the one or more selected DBMSs. In addition, the system comprises one or more parsers to parse the fetched database code, a validator to validate the parsed code using the registered rules and a report manager to provide results of the validation to the one or more users.

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04-10-2016 дата публикации

Quinazolines as potassium ion channel inhibitors

Номер: US09458114B2
Принадлежит: Bristol Myers Squibb Co

A compound of formula I wherein A, X, Y, Z, R 1 and R 24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I Kur -associated disorders, and other disorders mediated by ion channel function.

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