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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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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 89. Отображено 89.
18-08-2016 дата публикации

Mannose Derivatives for Treating Bacterial Infections

Номер: US20160235775A1
Принадлежит:

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: 1112.-. (canceled)114. The method of claim 113 , wherein{'sup': H1', 'H2, 'G is C(J)(J);'}{'sup': 'H1', 'sub': 2', '2, 'Jis OH, F, or —CHCHOH;'}{'sup': 'H2', 'sub': 3', '2', '3', '2', '2', '2', '2', '3, 'Jis OH, CH, cyclopropyl, F, CHCH, —CHCHOH, —CHCH(OH)CHOH, or phenyl optionally substituted with OCH;'}{'sup': H1', 'H2, 'sub': 1-6', '2', '3', '3', '3', '3', '2', '2', '3, 'or Jand J, together with the carbon atom to which they are attached, form ═N—OH or a 6-membered saturated monocyclic ring having 0-2 heteroatoms selected from oxygen, nitrogen, or sulfur; wherein said ring is optionally substituted with Calkyl, OH, NH, —C(O)OCH, —C(O)OC(CH), —C(O)C(CH)OH, or —S(O)CH.'}115. The method of claim 113 , wherein the Ring HH is selected from cyclopentyl claim 113 , cyclohexyl claim 113 , piperidinyl claim 113 , piperazinyl claim 113 , 1 claim 113 ,3-dithianyl claim 113 , or tetrahydropyranyl.116. The method of claim 113 , wherein Xis Calkyl and Qis Ccycloaliphatic claim 113 , oxetanyl claim 113 , tetrahydropyrrolidinyl claim 113 , piperidinyl claim 113 , piperazinyl claim 113 , or morpholinyl.119. The method of claim 118 , wherein Ring HH is cyclopentyl claim 118 , cyclohexyl claim 118 , tetrahydropyranyl claim 118 , 1 claim 118 ,3 dithianyl claim 118 , piperazinyl claim 118 , piperidinyl claim 118 , or oxepanyl.120. The method of claim 119 , wherein Ring HH is piperidinyl or tetrahydropyranyl.122. The method of claim 121 , wherein Jis H claim 121 , C(O)(Calkyl) claim 121 , C(O)O(Calkyl) claim 121 , S(O)(Calkyl) claim 121 , C(O)(Ccycloalkyl) claim 121 , C(O)(3-6 membered heterocyclyl) claim 121 , C(O)(5-6 membered heteroaryl) claim 121 , C(O)—(Calkyl)-(5-6 membered heteroaryl) claim 121 , C(O)—(Calkyl)-(heterocyclyl); wherein said heteroaryl or heterocyclyl has 1-3 heteroatoms selected from oxygen claim 121 , nitrogen claim 121 , or ...

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10-10-2012 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: CN102718744A
Принадлежит:

Compounds represented by formula (I) : or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y<1>, and Z are as defined herein, are useful for treating flavivipdae viral infections Said viral infection is Hepatitis C virus (HCV), bovme viral diarrhea virus (BVDV), hog cholera virus, dengue fever virus, Japanese encephalitis virus or yellow fever virus.

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13-02-2018 дата публикации

Mannose derivatives for treating bacterial infections

Номер: US0009890176B2

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.

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16-01-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: CN102883718A
Принадлежит:

Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4 , R4', R5 , R5'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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21-03-2017 дата публикации

Mannose derivatives for treating bacterial infections

Номер: US0009598454B2

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

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12-06-2013 дата публикации

Compounds and methods for the treatment or prevention of flaviviridae viral infections

Номер: CN103153978A
Принадлежит:

A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.

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05-09-2012 дата публикации

Benzimidazole analogues for the treatment or prevention of flavivirus infections

Номер: CN102656160A
Принадлежит:

Compounds represented by formula (I) or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B', X, Y, R1, R1', R2, R2', R3, R3', R5, R5', R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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10-04-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: CN103038237A
Принадлежит:

Provided are compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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09-01-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: CN102869657A
Принадлежит:

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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08-03-2012 дата публикации

THIOPHENE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20120059170A1

Compounds represented by formula I: 120.-. (canceled)21. A compound selected from:5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHOXY-CYCLOHEXYL)-(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(CIS-4-[1,2,4]TRIAZOL-1-YL-CYCLOHEXYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(TRANS-4-[1,2,4]TRIAZOL-1-YL-CYCLOHEXYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(CIS-4-HYDROXY-CYCLOHEXYL)-(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(1-METHYL-PIPERIDIN-4-YL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID; HYDROCHLORIDE;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(4-CIS-[1,2,3]TRIAZOL-1-YL-CYCLOHEXYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(TRANS-4-[1,2,3]TRIAZOL-1-YL-CYCLOHEXYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;5-(3,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-FLUORO-CYCLOHEXYL)-(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID;and pharmaceutically acceptable salts thereof.2233.-. (canceled)34. A compound of claim 21 , wherein the compound is 5-(3 claim 21 ,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHOXY-CYCLOHEXYL)-(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID.35. A compound of claim 21 , wherein the compound is 5-(3 claim 21 ,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(CIS-4-[1 claim 21 ,2 claim 21 ,4]TRIAZOL-1-YL-CYCLOHEXYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID.36. A compound of claim 21 , wherein the compound is 5-(3 claim 21 ,3-DIMETHYL-BUT-1-YNYL)-3-[(TRANS-4-METHYL-CYCLOHEXANECARBONYL)-(TRANS-4-[1 claim 21 ,2 claim 21 ,4]TRIAZOL-1-YL-CYCLOHEXYL)-AMINO]-THIOPHENE-2-CARBOXYLIC ACID.37. A compound of claim 21 , wherein the compound is 5-(3 claim 21 ,3-DIMETHYL-BUT-1-YNYL)-3-[(CIS ...

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28-06-2012 дата публикации

Compounds and Methods for the Treatment or Prevention of Flavivirus Infections

Номер: US20120164103A1

Compounds represented by formula I: 11. A compound according to any one of to , wherein Yis CH , C═CH , CH—CHor a bond.12. A compound according to any one of to , wherein Yis a bond.13. A compound according to any one of to , wherein Y is COOR , CONRRor CON(R)CH(R)—COOR.14. A compound according to claim 13 , wherein Y is COOR claim 13 , CONRRor CONRCHCOOR.15. A compound according to claim 13 , wherein Y is COOH claim 13 , CONH claim 13 , CONHCHCOOH claim 13 , or COOCH.16. A compound according to any one of to claim 13 , wherein Y—Y is COOH.17. A compound according to any one of to claim 13 , wherein claim 13 , R claim 13 , R claim 13 , R claim 13 , R claim 13 , and Rare each independently H or optionally substituted Calkyl.18. A compound according to claim 17 , wherein claim 17 , R claim 17 , R claim 17 , R claim 17 , R claim 17 , and Rare each independently H or methyl.19. A compound according to claim 18 , wherein R claim 18 , R claim 18 , R claim 18 , R claim 18 , Rand Rare each H.20. A compound according to any one of to claim 18 , wherein{'sub': 4', '1-6', '17', '2-6', '17', '2-6', '17, 'Ris H, Calkyl which is unsubstituted or substituted one or more times by R, Calkenyl which is unsubstituted or substituted one or more times by R, or Calkynyl which is unsubstituted or substituted one or more times by R; and'}{'sub': 17', '2', '1-4', '1-4', '2', '2', '1-4', '1-4', '2', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '1-4', '0-2', '0-2', '1-4', '2', '2', '2', '1-4', '2', '1-4', '2', '2', '1-4', '2', '1-4', '2', '1-4', '2', '1-4, 'Ris halogen, oxo, —NH, —NH(Calkyl), —N(Calkyl), —CONH, —CONH(Calkyl), —CON(Calkyl), —NHCOH, —N(Calkyl)COH, —N(Calkyl)COCalkyl, —NHCOCalkyl, —C(O)H, —C(O)Calkyl, carboxy, —C(O)OCalkyl, hydroxyl, Calkoxy, nitro, nitroso, azido, cyano, —S(O)H, —S(O)Calkyl, —SONH, —SONH(Calkyl), —SON(Calkyl), —NHSOH, —N(Calkyl)SOH, —N(Calkyl)SOCalkyl, or —NHSOCalkyl.'}21. A compound according to any ne of to claim 18 , wherein{'sub': 6', '1-6', '17', '2-6', '17', ...

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29-11-2012 дата публикации

Thiophene analogues for the treatment or prevention of flavivirus infections

Номер: US20120301430A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R 1 , X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.

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21-03-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: US20130072523A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R 2 , R 2 ′, R 3 , R 3 ′, R 4 , R 4 ′, R 5′ , R 5′ m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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04-04-2013 дата публикации

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130085150A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I 5. (canceled)6. The compound according to claim 1 , wherein{'sub': 1', 'p, 'each A is independently cyclopropyl, cyclohexyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, piperadinyl, phenyl, naphthalenyl, thienyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, indolyl, indazolyl, benzimidazolyl, benzoxazolyl, benzodioxolyl, benzothiazolyl, benzothiadiazolyl, dihydrobenzodioxine, thienofuranyl, thienothienyl, thienopyrrolyl, quinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, or triazolyl; and wherein each A is independently substituted with (R).'}712.-. (canceled)13. The compound according to claim 1 , wherein B and B′ are independently absent claim 1 , Calkyl or Calkynyl.1416.-. (canceled)1823.-. (canceled)24. The compound according to claim 1 , wherein Ris halogen claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , —C(═O)OR claim 1 , —C(O)NRR claim 1 , hydroxyl claim 1 , cyano claim 1 , or Calkoxy.25. (canceled)26. The compound according to claim 1 , wherein each R′ is independently fluoro claim 1 , or methyl.27. The compound according to claim 26 , wherein s is 0.28. The compound according to claim 1 , wherein each Ris independently fluoro or methyl.29. The compound according to claim 28 , wherein s is 0.30. The compound according to claim 1 , wherein Rand R′ are H or methyl.32. (canceled)33. The compound according to claim 32 , wherein Rand R′ are methyl.34. The compound according to claim 1 , wherein m and n are independently 1 or 2.35. The compound according to claim 34 , wherein m and n are 1.37. The compound according to claim 1 , wherein Rand R′ are each independently claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , Calkenyl which is unsubstituted or substituted one or more times by R claim 1 , Calkynyl which is unsubstituted or substituted one or ...

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11-04-2013 дата публикации

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130090351A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I 2. The compound according claim 1 , wherein{'sub': 1', 'p, 'each A is independently cyclopropyl, cyclohexyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, piperadinyl, phenyl, naphthalenyl, thienyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, indolyl, indazolyl, benzimidazolyl, benzoxazolyl, benzodioxolyl, benzothiazolyl, benzothiadiazolyl, dihydrobenzodioxine, thienofuranyl, thienothienyl, thienopyrrolyl, quinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, or triazolyl; and wherein each A is independently substituted with (R).'}35.-. (canceled)6. The compound according to claim 2 , wherein each A is independently piperazinyl claim 2 , piperadinyl claim 2 , thienyl claim 2 , furanyl claim 2 , pyrrolyl claim 2 , pyrazolyl claim 2 , imidazolyl claim 2 , thiazolyl claim 2 , oxazolyl claim 2 , thiadiazolyl claim 2 , pyrrolidinyl claim 2 , pyridyl claim 2 , pyrimidinyl claim 2 , pyrazinyl claim 2 , pyridazinyl claim 2 , benzoxazolyl claim 2 , benzodioxolyl claim 2 , benzothiazolyl claim 2 , benzothiadiazolyl claim 2 , dihydrobenzodioxinyl claim 2 , thienofuranyl claim 2 , thienothienyl claim 2 , quinolinyl claim 2 , or triazolyl.78.-. (canceled)9. The compound according to claim 1 , wherein B and B′ are independently absent claim 1 , Calkyl or Calkynyl.1011.-. (canceled)1318.-. (canceled)19. The compound according to claim 1 , wherein Ris halogen claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , —C(═O)OR claim 1 , —C(O)NRR claim 1 , hydroxyl claim 1 , cyano claim 1 , or Calkoxy.20. (canceled)21. The compound according to claim 1 , wherein R′ is methyl claim 1 , trifluoromethyl claim 1 , iodo claim 1 , CHOH claim 1 , or NHC(O)CH.22. The compound according to claim 21 , wherein u is 0.23. The compound according to claim 1 , wherein each Ris independently fluoro or methyl.24. The compound according to ...

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11-04-2013 дата публикации

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130090364A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I 6. The compound according to any one of to , wherein{'sub': 1', 'p, 'each A is independently cyclopropyl, cyclohexyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, piperadinyl, phenyl, naphthalenyl, thienyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, indolyl, indazolyl, benzimidazolyl, benzoxazolyl, benzodioxolyl, benzothiazolyl, benzothiadiazolyl, dihydrobenzodioxine, thienofuranyl, thienothienyl, thienopyrrolyl, quinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, or triazolyl; and wherein each A is independently substituted with (R).'}712.-. (canceled)13. The compound according to claim 1 , wherein B and B′ are independently absent claim 1 , Calkyl or Calkynyl.1416.-. (canceled)1823.-. (canceled)24. The compound according to claim 1 , wherein Ris halogen claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , —C(═O)OR claim 1 , —C(O)NRR claim 1 , hydroxyl claim 1 , cyano claim 1 , or Calkoxy.25. The compound according to claim 24 , wherein Ris chloro claim 24 , fluoro claim 24 , bromo claim 24 , methyl claim 24 , ethyl claim 24 , propyl claim 24 , butyl claim 24 , —CHOH claim 24 , difluoromethyl claim 24 , trifluoromethyl claim 24 , —C(═O)OR claim 24 , hydroxyl claim 24 , cyano claim 24 , or methoxy.26. The compound according to claim 1 , wherein R′ is fluoro claim 1 , methyl claim 1 , trifluoromethyl claim 1 , iodo claim 1 , CHOH claim 1 , or NHC(O)CH.27. The compound according to claim 26 , wherein s is 0.28. The compound according to claim 1 , wherein each Ris independently fluoro or methyl.29. The compound according to claim 28 , wherein s is 0.30. The compound according to claim 1 , wherein Rand R′ are H or methyl.3233.-. (canceled)34. The compound according to claim 1 , wherein m and n are independently 1 or 2.35. (canceled)37. The compound according to claim 1 , wherein Rand R′ are each ...

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18-04-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130096106A1

Compounds represented by formula: 3. A compound according to claim 1 , wherein Z is 6-7 membered heterocycle or 6-7 membered cycloalkyl.4. A compound according to claim 1 , wherein Z is cyclohexyl claim 1 , piperidinyl claim 1 , N—(Calkyl)-piperidinyl claim 1 , hexahydrothiopyranyl claim 1 , azepanyl claim 1 , methylazepanyl claim 1 , N—(Calkyl)-piperidinylmethyl claim 1 , tetrahydropyranyl claim 1 , piperidinylmethyl claim 1 , pyridinyl claim 1 , pyridinylmethyl claim 1 , tetrahydrothiopyranyl claim 1 , dioxolanylmethyl or dioxanylmethyl which in each case is unsubstituted or substituted by one or more substituent chosen from halogen claim 1 , nitro claim 1 , nitroso claim 1 , SORf claim 1 , SORf claim 1 , PORcRd claim 1 , CONRgRh claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Caralkyl claim 1 , Caryl claim 1 , Calkyloxy claim 1 , Calkenyloxy claim 1 , Calkynyloxy claim 1 , Caryloxy claim 1 , C(O)Calkyl claim 1 , C(O)Calkenyl claim 1 , C(O)Calkynyl claim 1 , C(O)Caryl claim 1 , C(O)Caralkyl claim 1 , C(O)NHRf claim 1 , Cheterocycle claim 1 , hydroxyl claim 1 , NRgRh claim 1 , C(O)ORf claim 1 , cyano claim 1 , azido claim 1 , amidino or guanido;{'sub': 1-6', '2-6', '2-6', '6-10', '3-10', '3-10', '6-10, 'wherein Rf, Rc, Rd, Rg and Rh in each case is H, Calkyl, Calkenyl, Calkynyl, Caryl, Cheterocycle, Cheteroaralkyl or Caralkyl;'}or Rc and Rd are taken together with the oxygens to form a 5 to 10 membered heterocycle;or Rg and Rh are taken together with the nitrogen to form a 3 to 10 membered heterocycle.5. A compound according to claim 1 , wherein Z is cyclohexyl unsubstituted or substituted by one or more substituent chosen from halogen claim 1 , SORf claim 1 , CONRgRh claim 1 , Calkyl claim 1 , Caralkyl claim 1 , Caryl claim 1 , Calkyloxy claim 1 , C(O)Calkyl claim 1 , Cheterocycle claim 1 , hydroxyl claim 1 , NRgRh claim 1 , C(O)Orf or cyano;{'sub': '1-6', 'wherein Rf, Rg and Rh in each case is H or Calkyl.'}6. A compound according to claim 1 , ...

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25-04-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: US20130102629A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R 1 , R 2 , R 2 ′, R 3 , R 3 ′, R 4 , R 4 ′, R 5 , R 5 ′, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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16-05-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130123242A1

The present invention provides novel compounds represented by formula I: 197.-. (canceled)101. A compound according to claim 98 , wherein Z is H.102. A compound according to claim 98 , wherein Ris Calkyl claim 98 , Caryl claim 98 , or Cheterocycle claim 98 , which in each case is substituted or unsubstituted.103. A compound according to claim 98 , wherein Ris H claim 98 , Calkyl claim 98 , Caralkyl claim 98 , Cheterocycle claim 98 , or Cheteroaralkyl claim 98 , which in each case is substituted or unsubstituted.104. A compound according to claim 98 , wherein{'sub': 3', '3', '3', '12', '3', 'c', 'd', '13', '14', '1-6', '2-6', '2-6', '6-12', '6-12', '1-6', '2-6', '2-6', '6-12', '1-6', '2-6', '2-6', '6-12', '6-12', '3-10', '13', '14', '12, 'Ris H, or Ris methyl, ethyl, isopropyl, cyclopropyl, cyclohexyl, allyl, piperidinyl, piperazinyl, pyrrolidinyl, azetidinyl, aziridinyl, pyridinyl, piperidinylmethyl, dioxanyl, azepanyl or benzyl, which in each case is unsubstituted or substituted by one or more substituents chosen from halogen, nitro, nitroso, SOR, PORR, CONRR, Calkyl, Calkenyl, Calkynyl, Caralkyl, Caryl, Calkyloxy, Calkenyloxy, Calkynyloxy, Caryloxy, C(O)Calkyl, C(O)Calkenyl, C(O)Calkynyl, C(O)Caryl, C(O)Caralkyl, Cheterocycle, hydroxyl, NRR, C(O)OR, cyano, azido, amidino, and guanido; and'}{'sub': 12', 'c', 'd', '13', '14', '1-12', '2-12', '2-12', '6-14', '3-12', '3-18', '6-18, 'R, R, R, Rand Rare each independently H, Calkyl, Calkenyl, Calkynyl, Caryl, Cheterocycle, Cheteroaralkyl, or Caralkyl,'}{'sub': c', 'd, 'or Rand R, taken together with the oxygens, form a 5 to 10 membered heterocycle,'}{'sub': 13', '14, 'or Rand R, taken together with the nitrogen, form a 3 to 10 membered heterocycle.'}105. A compound according to claim 104 , wherein Ris isopropyl or cyclohexyl claim 104 , which in each case is substituted or unsubstituted.106. A compound according to claim 98 , wherein Ris Calkyl claim 98 , Caryl claim 98 , or Cheterocycle claim 98 , which in each case is ...

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30-05-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: US20130136719A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , and R 3 are as defined herein, are useful for treating flaviviridae viral infections.

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20-06-2013 дата публикации

BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130157997A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I: 2. (canceled)4. The compound according to claim 1 , wherein each A is independently cyclopropyl claim 1 , cyclohexyl claim 1 , pyrrolidinyl claim 1 , pyrazolidinyl claim 1 , imidazolidinyl claim 1 , piperazinyl claim 1 , piperadinyl claim 1 , phenyl claim 1 , naphthalenyl claim 1 , thienyl claim 1 , furanyl claim 1 , pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , thiazolyl claim 1 , thiadiazolyl claim 1 , oxazolyl claim 1 , oxadiazolyl claim 1 , pyridyl claim 1 , pyrimidyl claim 1 , pyrazinyl claim 1 , pyridazinyl claim 1 , indolyl claim 1 , indazolyl claim 1 , benzimidazolyl claim 1 , benzoxazolyl claim 1 , benzodioxolyl claim 1 , benzothiazolyl claim 1 , benzothiadiazolyl claim 1 , benzothiophenyl claim 1 , dihydrobenzodioxinyl claim 1 , thienofuranyl claim 1 , thienothienyl claim 1 , thienopyrrolyl claim 1 , quinolinyl claim 1 , quinoxalinyl claim 1 , quinazolinyl claim 1 , cinnolinyl claim 1 , or triazolyl; and wherein each A is independently substituted with (R).57.-. (canceled)8. The compound according to claim 4 , wherein each A is independently piperazinyl claim 4 , piperadinyl claim 4 , thienyl claim 4 , furanyl claim 4 , pyrrolyl claim 4 , pyrazolyl claim 4 , imidazolyl claim 4 , thiazolyl claim 4 , oxazolyl claim 4 , thiadiazolyl claim 4 , pyrrolidinyl claim 4 , pyridyl claim 4 , pyrimidinyl claim 4 , pyrazinyl claim 4 , pyridazinyl claim 4 , benzoxazolyl claim 4 , benzodioxolyl claim 4 , benzothiazolyl claim 4 , benzothiadiazolyl claim 4 , benzothiophenyl claim 4 , dihydrobenzodioxinyl claim 4 , thienofuranyl claim 4 , thienothienyl claim 4 , quinolinyl claim 4 , or triazolyl claim 4 , each of which is substituted with (R).910.-. (canceled)11. The compound according to claim 1 , wherein each A is independently a 5-12 membered heteroaryl wherein the heteroatom(s) are selected from the group consisting of oxygen and sulphur; wherein each A is independently substituted with (R).12. The compound according to ...

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18-07-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: US20130183266A1
Принадлежит: Vertex Pharmaceuticals Inc

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A biological probe comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

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25-07-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130190289A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is represented by Structural Formula (I): 2. (canceled)47-. (canceled)8. The compound of claim 3 , wherein:{'sup': '1', 'sub': 1-6', '1', '6, 'Ris Calkyl optionally substituted with one or more substituents selected from the group consisting of halogen, —CN, —OH, and —O(C-Calkyl);'}{'sup': '2', 'sub': 5', '8', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '2', '1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '1', '6', '1', '6', '2', '2', '1', '6', '1', '6', '1', '6', '3-7', '3-7, 'Ris C-Ccycloalkyl optionally substituted with one or more substituents selected from the group consisting of halogen; oxo; —CN; —OH; —NH; —NH(C-Calkyl); —N(C-Calkyl): —OCO(C-Calkyl); —CO(C-Calkyl); —COH; —CO(C-Calkyl); —O(C-Calkyl); —O(C-Chaloalkyl); and a C-Caliphatic group optionally substituted with one or more substituents selected from the group consisting of halogen, oxo, —CN, —OH, —NH, —NH(C-Calkyl), —N(C-Calkyl), —OCO(C-Calkyl), —CO(C-Calkyl), —COH, —CO(C-Calkyl), —O(C-Calkyl), —O(C-Chaloalkyl), Ccycloalkyl, Ccyclo(haloalkyl), and phenyl.'}{'sup': a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a, 'sub': 2', '2', '2', '7', '3-8, 'each Q independently is selected from the group consisting of halogen; cyano; nitro; —OR; —SR; —S(O)R; —SOR; —NRR; —C(O)R; —C(O)OR; —OC(O)R; —NRC(O)R; —C(O)NRR; —NRC(O)NRR; —NRC(O)OR; —NRC(═NR)NRR, —OCONRR; —C(O)NRC(O)OR; —C(═NR)R; —C(═NOR)R; —SONRR; —NRSOR; —NRSONRR; —OP(O)(OR)OR; optionally substituted Ccarbocyclic; 4-8 membered, optionally substituted heterocyclyl; optionally substituted phenyl; and optionally substituted, 5-6 membered heteroaryl;'}{'sup': 1A', '2A', '7A', '9A', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a, 'sub': 2', '3-8', '3-8, 'each of J, J, J, and Jindependently is halogen, oxo, —CN, —OR, —NRR, —OCOR, —COR, —COR, —NRC(O)R, —C(O)NRR, —NRC(O)NRR, —NRC(O)OR, —OCONRR, Ccycloalkyl, Ccyclo(haloalkyl), or phenyl;'}{'sup': 1B', '2B', '7B', '9B', ...

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03-10-2013 дата публикации

MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS

Номер: US20130261077A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: 2. The compound of claim 1 , wherein{'sub': 8', '8', '2', 'm', '8', '8', '8', '2', '8', '2', '8', '8', '2', '8', '1', '6', '1', '6', '1', '6', '1', '6', 'n', '1-6', '8', '1-6', '8', '1-6', '1', '6, 'sup': '10', 'Y is absent, or is —NR, —O—, —S—, —C(O)—, —C(R)(OH)—, —C(O)N(R)(CH)—, —N(R)C(O)O—, —OC(O)NR—, —NRSO—, —NR—C(O)—, —SO—, —NRC(O)NR—, —S(O)—, —SONR, —(C-C)alkyl-, —(C-C)alkenyl-, —(C-C)alkynyl-, —(O—(C-Calkyl))-, —O—(Calkyl)NRC(O)—, —O—(Calkyl)C(O)NR, —O—(Calkyl)-C(O)—, or —((C-C)alkyl)-O—;'}{'sub': 3A', '3B', '10', '3', '10', '2', '2', 'n', '4', '2', 'n', '4', '2', 'n', '4', '2', '4', '4', '2', '4', '4', '2', '4', '4', '2', '4', '4', '2', '4', '4', '4', '2', '4', '4', '4', '2', '4', '2, 'each Rand Ris independently —OH, —CN, halogen, —C(R), —C(R)OH, —(CH)OR, —(CH)C(O)OR, —(CH)N(R), —C(O)OR, —C(O)N(R), —N(R)C(O)(R), —OC(O)NHR, —NHC(O)OR, —NHSOR, —NH—C(O)R, —SO—R, —NHC(O)NHR, —S(O)R, —SONHR, —SR, —P(O)(OR), or —P(O)(R); and'}{'sub': 4A', '10', '3', '10', '2', '2', 'n', '4', '2', 'n', '4', '2', 'n', '4', '2', '4', '4', '2', '4', '4', '2', '4', '4', '2', '4', '4', '2', '4', '4', '4', '2', '4', '4', '4', '2', '4', '2, 'Ris —OH, —CN, halogen, —C(R), —C(R)OH, —(CH)OR, —(CH)C(O)OR, —(CH)N(R), —C(O)OR, —C(O)N(R), —N(R)C(O)(R), —OC(O)NHR, —NHC(O)OR, —NHSOR, —NH—C(O)R, —SO—R, —NHC(O)NHR, —S(O)R, —SONHR, —SR, —P(O)(OR), —P(O)(R); and'}{'sup': '7', 'Ris H or mannosyl.'}3. The compound of claim 1 , wherein:X is —OH;{'sub': 8', '2', '1', '6', '1', '6', '1', '6', '1', '6', 'n', '1-6', '8', '1-6', '8', '1-6', '1', '6, 'sup': '10', 'Y is absent, or is —NR, —O—, —S—, —C(O)—, —C(R)(OH)—, —SO—, —S(O)—, —(C-C)alkyl, —(C-C)alkenyl, —(C-C)alkynyl, —(O—(C-Calkyl))-, —O(Calkyl)N—RC(O)—, —O—(Calkyl)-C(O)NR, —O—(Calkyl)C(O)—, or —((C-C)alkyl)-O—;'}{'sub': 2', '6-10', '6-10', '1', '6', '2', '6-10', '6-10', '1', '6, 'Ris Caryl, (Caryl)-(C-Calkyl)-, or 5- ...

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06-03-2014 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRIDAE VIRAL INFECTIONS

Номер: US20140065103A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is selected from the structural formulae depicted in FIG. or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. or a pharmaceutically acceptable salt thereof. 4. A pharmaceutical composition , comprising a compound of or , and a pharmaceutically acceptable carrier or excipient.5. A pharmaceutical composition claim 3 , comprising a compound of and a pharmaceutically acceptable carrier or excipient.63. A method of inhibiting or reducing the activity of HCV polymerase in a biological in vitro sample claims 1 , comprising administering to the sample an effective amount of a compound of any one of -.73. A method of treating a HCV infection in a subject claims 1 , comprising administering to the subject a therapeutically effective amount of a compound of any one of -.83. A method of inhibiting or reducing the activity of HCV polymerase in a subject claims 1 , comprising administering to the subject a therapeutically effective amount of a compound of any one of -.9. The method of or claims 1 , further comprising co-administering one or more additional therapeutic agents to the subject.10. The method of claim 9 , wherein the additional therapeutic agents include an anti-HCV drug.11. The method of claim 10 , wherein the anti-HCV drug is an HCV protease inhibitor.12. The method of ...

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05-05-2022 дата публикации

Mannose Derivatives for Treating Bacterial Infections

Номер: US20220135609A1
Принадлежит:

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I:

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11-04-2019 дата публикации

Mannose Derivatives for Treating Bacterial Infections

Номер: US20190106450A1
Принадлежит:

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: 1112.-. (canceled)114. The compound of claim 113 , wherein Ring H claim 113 , is phenyl claim 113 , napthyl claim 113 , or a 5-6 membered heteroaryl having 1-4 heteroatoms selected from oxygen claim 113 , nitrogen claim 113 , or sulfur.115. (canceled)117. The compound of wherein{'sup': '2', 'sub': 1-6', '1-4, 'Lis Caliphatic or —(Caliphatic)-C(O)NH—;'}{'sup': '3', 'sub': 1-6', '1-4, 'Lis Caliphatic or —NHC(O)—(Caliphatic)-;'}Ring H is phenyl or naphthyl; and{'sup': 'H', 'sub': 2', '1-6', '1-6', '1-6, 'Jis halo, CN, NO, Caliphatic, —OCaliphatic, or C(O)O(Caliphatic); wherein'}{'sup': 'H', 'said Jis optionally substituted with 1-3 occurrences of halo.'}118. The compound of claim 113 , wherein Land Lare each independently C-Calkenyl or C-Calkynyl.120. The compound of claim 119 , wherein Land Lare bonded to the mannose ring via a carbon atom.121. The compound of claim 120 , wherein Land Lare each independently C-Calkenyl or C-Calkynyl.122. The compound of claim 121 , wherein at least one of Land Lis —C≡C—.123. (canceled)125. The compound of claim 124 , wherein Ring H is an optionally substituted 5-6 membered monocyclic aromatic ring optionally having 1-4 heteroatoms selected from nitrogen claim 124 , or sulfur; or an 8-12 membered bicyclic aromatic ring optionally having 1-6 heteroatoms selected from oxygen claim 124 , nitrogen claim 124 , or sulfur; or a 10-14 tricyclic aromatic ring optionally having 1-6 heteroatoms selected from oxygen claim 124 , nitrogen claim 124 , or sulfur.126. The compound of claim 125 , wherein Ring H is optionally substituted phenyl claim 125 , naphthyl claim 125 , thienyl claim 125 , isoxazolyl claim 125 , pyridinyl claim 125 , pyrazinyl claim 125 , indolyl claim 125 , indazolyl claim 125 , thienylthiophenyl claim 125 , quinolinyl claim 125 , quinazolinyl claim 125 , benzothiadiazolyl claim 125 , or ...

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28-08-2014 дата публикации

BENZIMIDAZOLE ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20140243257A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I: 1. (canceled)3. (canceled)4. The compound according to claim 2 , wherein each A is independently cyclopropyl claim 2 , cyclohexyl claim 2 , pyrrolidinyl claim 2 , pyrazolidinyl claim 2 , imidazolidinyl claim 2 , piperazinyl claim 2 , piperadinyl claim 2 , phenyl claim 2 , naphthalenyl claim 2 , thienyl claim 2 , furanyl claim 2 , pyrrolyl claim 2 , pyrazolyl claim 2 , imidazolyl claim 2 , thiazolyl claim 2 , thiadiazolyl claim 2 , oxazolyl claim 2 , oxadiazolyl claim 2 , pyridyl claim 2 , pyrimidyl claim 2 , pyrazinyl claim 2 , pyridazinyl claim 2 , indolyl claim 2 , indazolyl claim 2 , benzimidazolyl claim 2 , benzoxazolyl claim 2 , benzodioxolyl claim 2 , benzothiazolyl claim 2 , benzothiadiazolyl claim 2 , benzothiophenyl claim 2 , dihydrobenzodioxinyl claim 2 , thienofuranyl claim 2 , thienothienyl claim 2 , thienopyrrolyl claim 2 , quinolinyl claim 2 , quinoxalinyl claim 2 , quinazolinyl claim 2 , cinnolinyl claim 2 , or triazolyl; and wherein each A is independently substituted with (R).57-. (canceled)8. The compound according to claim 4 , wherein each A is independently piperazinyl claim 4 , piperadinyl claim 4 , thienyl claim 4 , furanyl claim 4 , pyrrolyl claim 4 , pyrazolyl claim 4 , imidazolyl claim 4 , thiazolyl claim 4 , oxazolyl claim 4 , thiadiazolyl claim 4 , pyrrolidinyl claim 4 , pyridyl claim 4 , pyrimidinyl claim 4 , pyrazinyl claim 4 , pyridazinyl claim 4 , benzoxazolyl claim 4 , benzodioxolyl claim 4 , benzothiazolyl claim 4 , benzothiadiazolyl claim 4 , benzothiophenyl claim 4 , dihydrobenzodioxinyl claim 4 , thienofuranyl claim 4 , thienothienyl claim 4 , quinolinyl claim 4 , or triazolyl claim 4 , each of which is substituted with (R).910.-. (canceled)11. The compound according to claim 2 , wherein each A is independently a 5-12 membered heteroaryl wherein the heteroatom(s) are selected from the group consisting of oxygen and sulphur; wherein each A is independently substituted with (R).12. The compound ...

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28-08-2014 дата публикации

Mannose derivatives for treating bacterial infections

Номер: US20140243283A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

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18-09-2014 дата публикации

MANNOSE DERIVATIVES FOR TREATING BACTERIAL INFECTIONS

Номер: US20140274930A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: 4. (canceled)6. (canceled)810-. (canceled)1224-. (canceled)2629-. (canceled)3139-. (canceled)41. (canceled)4249-. (canceled)5152-. (canceled)5660-. (canceled)62. (canceled)6465-. (canceled)67. A composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.68. A method of treating or preventing a bacteria infection in a subject claim 1 , comprising administering to the subject an effective amount of the compound of or a pharmaceutically acceptable salt thereof.6971-. (canceled)72. A method of inhibiting FimH in a subject claim 1 , comprising administering to the subject an effective amount of the compound of or a pharmaceutically acceptable salt thereof.73E. coli. A method of inhibiting adhesion of in a subject claim 1 , comprising administering to the subject an effective amount of the compound of or a pharmaceutically acceptable salt thereof.74. A method of blocking the interaction between type 1 pili and CEACAM6 in a subject claim 1 , comprising administering to the subject an effective amount of the compound of or a pharmaceutically acceptable salt thereof. This present invention claims the benefit, under 35 U.S.C. §119, of U.S. Provisional Application No. 61/777,398, filed Mar. 12, 2013; the entire contents of which are incorporated herein by reference.Inflammatory bowel disease (IBD) is a complex chronic inflammatory disorder, with the two more common forms being ulcerative colitis (UC) and Crohn's disease (CD). IBD is a multifactorial disease that results from a combination of predisposing genetic factors, environmental triggers, dysbiosis of the gastrointestinal microbiota and an inappropriate inflammatory response (Man et al., 2011, Nat Rev Gastroenterol Hepatol, March, 8(3):152-68).Several studies ...

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27-08-2020 дата публикации

Mannose Derivatives for Treating Bacterial Infections

Номер: US20200270293A1
Принадлежит:

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: 1112.-. (canceled)114. The compound of claim 113 , wherein R is C(O)CH(AG8).116. The process of claim 115 , wherein the suitable base is NaH.117. The process of claim 115 , wherein the suitable solvent is THF.119. The process of claim 118 , wherein acidic conditions correspond to HCl in dioxane.121. The process of claim 120 , wherein the suitable base is triethylamine.122. The process of claim 120 , wherein the suitable solvent is chosen from DMF and CHCl. This application is a continuation application which claims priority to U.S. patent application Ser. No. 15/945,221, filed on Apr. 4, 2018, which is a continuation application which claims priority to U.S. patent application Ser. No. 15/140,045, filed on Apr. 27, 2016, which is a divisional application which claims priority to U.S. patent application Ser. No. 14/132,662, filed on Dec. 18, 2013, which claims the benefit, under 35 U.S.C. § 119, of U.S. Provisional Application No. 61/738,620, filed Dec. 18, 2012; U.S. Provisional Application No. 61/788,241, filed Mar. 15, 2013; and U.S. Provisional Application No. 61/874,501, filed Sep. 6, 2013, the entire contents of each of the above applications being incorporated herein by reference.: Differential scanning calorimetry (DSC) of Compound 162, crystalline form A: X-ray powder diffractogram of Compound 162: Differential scanning calorimetry (DSC) of Compound 202, crystalline form A: X-ray powder diffractogram of Compound 202: Thermal gravimetric analysis (TGA) trace of Compound 202Inflammatory bowel disease (IBD) is a complex chronic inflammatory disorder, with the two more common forms being ulcerative colitis (UC) and Crohn's disease (CD). IBD is a multifactorial disease that results from a combination of predisposing genetic factors, environmental triggers, dysbiosis of the gastrointestinal microbiota and an inappropriate ...

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19-12-2002 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: WO2002100846A1
Принадлежит: Nguyen Ba, Nghe, Shire Biochem Inc.

the present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.

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19-12-2002 дата публикации

Thiophene derivatives as antiviral agents for flavivirus infection

Номер: WO2002100851A2
Принадлежит: Shire Biochem Inc.

The present invention provides novel compounds represented by formula (I): or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

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30-06-2011 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: WO2011079327A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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12-01-2012 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: WO2012006055A2
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is represented by Structural Formula (I), or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

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23-02-2012 дата публикации

Compounds and methods for the treatment or prevention of flaviviridae viral infections

Номер: WO2012024363A2
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.

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01-07-2014 дата публикации

Benzimidazole analogues for the treatment or prevention of flavivirus infections

Номер: US8765731B2
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R 1 , R 1 ′, R 2 , R 2 ′, R 3 , R 3 ′, R 5 , R 5 ′, R 6 , m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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15-07-2014 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: US8779156B2
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R 1 , R 2 , R 2 ′, R 3 , R 3 ′, R 4 , R 4 ′, R 5 , R 5 ′, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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12-06-2012 дата публикации

Benzimidazole analogues for the treatment or prevention of flavivirus infections.

Номер: MX2012000695A
Принадлежит: Vertex Pharma

Los compuestos representados por la fórmula (I): (ver fórmula (I)) o sales y solvatos farmacéuticamente aceptables de los mismos, en donde A, B, B', X, Y, R1, R1', R2, R2', R3, R3', R5, R5´, R6, m, n o p son como se define en la presente, son útiles para el tratamiento de infecciones virales por flaviviridae.

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30-01-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: EP2550267A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R 1 , R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 ', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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31-10-2012 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: EP2515902A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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22-05-2008 дата публикации

Thiophene analogues for the treatment or prevention of flavivirus infections

Номер: WO2008058393A1
Принадлежит: Virochem Pharma Inc.

The present invention relates to compounds represented by formula IA or pharmaceutically acceptable salts and solvates thereof which are useful for treating flaviviridae viral infections wherein R1 is C1-6 alkyl or C3-6 cycloalkyl; X is M is R5 is cyclohexyl which is unsubstituted or substituted one or more times by R13; R6 is or cyclohexyl which is substituted in the 4 position by R14; and Y, R14a and R14 are as defined herein.

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10-03-2004 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: EP1395571A1
Принадлежит: Shire BioChem Inc

the present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.

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30-01-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: EP2550268A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R 1 , R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 ', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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11-10-2012 дата публикации

Analogues for the treatment or prevention of Flavivirus infections

Номер: AU2011232348A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) : or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R, R, R', R, R', R, R', R, R'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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29-09-2011 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: WO2011119853A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R 1 , R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 ', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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16-11-2006 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: WO2006119646A1
Принадлежит: Virochem Pharma Inc.

Compounds represented by formula (I) : or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviπdae viral infections Said viral infection is Hepatitis C virus (HCV), bovme viral diarrhea virus (BVDV), hog cholera virus, dengue fever virus, Japanese encephalitis virus or yellow fever virus

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09-06-2011 дата публикации

5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections

Номер: WO2011068715A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula (I) :or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , and R 3 are as defined herein, are useful for treating flaviviridae viral infections.

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12-01-2012 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: WO2012006070A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A biological probe comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

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20-02-2013 дата публикации

Thiophene analogues for the treatment or prevention of Flavivirus infections

Номер: EP2559691A1
Принадлежит: Virochem Pharma Inc

The present invention relates to compounds represented by formula IA or pharmaceutically acceptable salts and solvates thereof which are useful for treating flaviviridae viral infections wherein R 1 is C 1-6 alkyl or C 3-6 cycloalkyl; X is M is R 5 is cyclohexyl which is unsubstituted or substituted one or more times by R 13 ; R 6 is or cyclohexyl which is substituted in the 4 position by R 14 ; and Y, R 14a and R 14 are as defined herein.

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16-01-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: EP2546246A2
Принадлежит: Virochem Pharma Inc

Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R 1 , X, Y, Y 1 , and Z are as defined herein, are useful for treating flaviviridae viral infections.

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09-01-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: EP2543664A1
Принадлежит: Virochem Pharma Inc

Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R 1 , X, Y, Y 1 , and Z are as defined herein, are useful for treating flaviviridae viral infections.

Подробнее
20-02-2013 дата публикации

Thiophene analogues for the treatment or prevention of Flavivirus infections

Номер: EP2559692A1
Принадлежит: Virochem Pharma Inc

The present invention relates to compounds represented by formula IA or pharmaceutically acceptable salts and solvates thereof which are useful for treating flaviviridae viral infections wherein R 1 is C 1-6 alkyl or C 3-6 cycloalkyl; X is M is R 5 is cyclohexyl which is unsubstituted or substituted one or more times by R 13 ; R 6 is or cyclohexyl which is substituted in the 4 position by R 14 ; and Y, R 14a and R 14 are as defined herein.

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03-10-2012 дата публикации

5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections

Номер: EP2504329A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) :or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , and R 3 are as defined herein, are useful for treating flaviviridae viral infections.

Подробнее
18-07-2007 дата публикации

Thiophene derivatives as antiviral agents for flavvivirus infection

Номер: AP1753A
Принадлежит: Shire BioChem Inc, Virochem Pharma Inc

The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection

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19-12-2002 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: CA2449999A1
Принадлежит: Individual

the present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.

Подробнее
29-09-2011 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: CA2794145A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Подробнее
31-07-2012 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: CA2449999C
Принадлежит: Virochem Pharma Inc

the present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.

Подробнее
22-07-2008 дата публикации

Compounds and methods for the treatment or prevention of Flavivirus infections

Номер: US7402608B2
Принадлежит: Virochem Pharma Inc

Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.

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09-08-2011 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: CA2607359C
Принадлежит: Virochem Pharma Inc

Compounds represented by formula (I) : or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flavivi.pi.dae viral infections Said viral infection is Hepatitis C virus (HCV), bovme viral diarrhea virus (BVDV), hog cholera virus, dengue fever virus, Japanese encephalitis virus or yellow fever virus

Подробнее
08-04-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections.

Номер: MX2012014918A
Принадлежит: Vertex Pharma

Un compuesto se representa por la Fórmula Estructural (I) o su sal farmacéuticamente aceptable, en la que las variables de la Fórmula Estructural (I) son como se describe en la memoria descriptiva y las reivindicaciones. Una composición farmacéutica comprende un compuesto representado por Fórmula Estructural (I) o su sal farmacéuticamente aceptable y un portador o excipiente farmacéuticamente aceptable. Un método para tratar una infección por VHC en un sujeto comprende administrar al sujeto una cantidad terapéuticamente efectiva de un compuesto representado por Fórmula Estructural (I) o su sal farmacéuticamente aceptable. Un método de inhibir o reducir la actividad de polimerasa del VHC en un sujeto o en una muestra biológica in vitro comprende administrar al sujeto o a la muestra una cantidad terapéuticamente efectiva de un compuesto representado por Fórmula Estructural (I) o su sal farmacéuticamente aceptable.

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18-08-2011 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: US20110200553A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

Подробнее
09-06-2011 дата публикации

5-alkynyl-thiophene-2-carboxylic acid derivatives and their use for the treatment or prevention of flavivirus infections

Номер: CA2781614A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) :or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.

Подробнее
29-09-2011 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: CA2794181A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) : or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Подробнее
26-07-2011 дата публикации

Compounds and methods for the treatment or prevention of Flavivirus infections

Номер: US7985769B2
Принадлежит: Vertex Pharmaceuticals Inc

The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

Подробнее
01-02-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections.

Номер: MX2012010919A
Принадлежит: Vertex Pharma

Se describen compuestos representados por la formula I o sal farmacéuticamente aceptables de estos, en donde A, B, B, X, Y, R1, R2,. R3, R4, R4, R5, R5´M, n, o p son como se definen en la presente descripción, son útiles para tratar infecciones por el virus flaviviridae.

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30-08-2005 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: US6936629B2
Принадлежит: Virochem Pharma Inc

The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.

Подробнее
09-02-2012 дата публикации

Thiophene derivatives as antiviral agents for flavivirus infection

Номер: AU2009200430B2

The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof for s treating flaviviridae viral infection. \ R, z X (I)

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30-07-2012 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: SG181614A1
Принадлежит: Vertex Pharma

Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5'm, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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28-07-2020 дата публикации

Mannose derivatives for treating bacterial infections

Номер: CA2894536C
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula (I). The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

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02-07-2015 дата публикации

Mannose derivatives for treating bacterial infections

Номер: AU2013361602A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula (I). The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

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16-11-2006 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: CA2607359A1

Compounds represented by formula (I) : or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flavivi.pi.dae viral infections Said viral infection is Hepatitis C virus (HCV), bovme viral diarrhea virus (BVDV), hog cholera virus, dengue fever virus, Japanese encephalitis virus or yellow fever virus

Подробнее
07-03-2013 дата публикации

Compounds and methods for the treatment or prevention of Flaviviridae viral infections

Номер: AU2011292040A1
Принадлежит: Vertex Pharmaceuticals Inc

A compound is selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of selected from the structural formulae depicted in FIG. 1 or a pharmaceutically acceptable salt thereof.

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09-09-2014 дата публикации

Compounds and methods for the treatment or prevention of Flavivirus infections

Номер: US8829030B2
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula: Wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.

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15-01-2013 дата публикации

Benzimidazole analogues for the treatment or prevention of flavivirus infections

Номер: US8354419B2
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B′, X, Y, R 1 , R 1 ′, R 2 , R 2 ′, R 3 , R 3 ′, R 5 , R 5 ′, R 6 , m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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26-02-2015 дата публикации

Mannose derivatives for treating bacterial infections

Номер: WO2014165107A3
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula (I) The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.

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31-08-2016 дата публикации

Αναλογα θειοφαινιου για τη θεραπεια ή την προληψη λοιμωξεων που οφειλονται σε flavivirus

Номер: CY1114162T1

Η παρούσα εφεύρεση σχετίζεται με ενώσεις που αντιπροσωπεύονται από τον τύπο ΙΑ ή με φαρμακευτικώς αποδεκτά άλατα και διαλύματα αυτών, που είναι χρήσιμα για τη θεραπεία ιογενών λοιμώξεων που οφείλονται σε flaviviridae όπου το R1 είναι C1-6 αλκύλιο ή C3-6 κυκλοαλκύλιο. Το Χ είναι Μ είναι R5 είναι κυκλοεξύλιο που είναι μη υποκατεστημένο ή υποκατεστημένο μια ή περισσότερες φορές με R13. Το R6 είναι ή κυκλοεξύλιο που είναι υποκατεστημένο στη θέση 4 με R14 και τα Υ, R14a και R14 είναι όπως ορίζονται στο παρόν.

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08-05-2018 дата публикации

Mannose derivatives for treating bacterial infections

Номер: US09963478B2
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.

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