公开(公告)号：WO2005085236A3

公开(公告)日：2005-10-20

申请号：PCT/US2005006540

申请日：2005-02-28

Applicant: VERTEX PHARMA ,  CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  MORTIMORE MICHAEL ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  RAMAYA SHARN ,  STUDLEY JOHN R ,  TRUDEAU MARTIN ,  LOOKER ADAM

Inventor： CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  MORTIMORE MICHAEL ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  RAMAYA SHARN ,  STUDLEY JOHN R ,  TRUDEAU MARTIN ,  LOOKER ADAM

IPC: A61K38/04 ,  A61K38/06 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D417/06 ,  C07D417/12 ,  C07K5/02 ,  C07K5/04 ,  A61K31/401 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/443 ,  A61P37/00

CPC classification number: C07D405/12 ,  A61K38/06 ,  C07D207/16 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D417/06 ,  C07D417/12 ,  C07K5/0202

Abstract: The present invention provides a compound of formula (I): wherein the variables are as defined herein. The present invention also provides processes for preparing the compounds of formula (I), and intermediates thereof, pharmaceutical compositions comprising those compounds, and methods of using the compounds and compositions.

Abstract translation: 本发明提供式（I）的化合物：其中变量如本文所定义。 本发明还提供制备式（I）化合物及其中间体，包含那些化合物的药物组合物的方法，以及使用该化合物和组合物的方法。

公开(公告)号：WO2007087283A2

公开(公告)日：2007-08-02

申请号：PCT/US2007/001726

申请日：2007-01-23

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  DURRANT, Steven ,  CHARRIER, Jean-Damien ,  KNEGTEL, Ronald ,  BRENCHLEY, Guy ,  KAY, David ,  SADIQ, Shazia ,  RAMAYA, Sharn

Inventor： DURRANT, Steven ,  CHARRIER, Jean-Damien ,  KNEGTEL, Ronald ,  BRENCHLEY, Guy ,  KAY, David ,  SADIQ, Shazia ,  RAMAYA, Sharn

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4985

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

公开(公告)号：WO2007139816A3

公开(公告)日：2008-01-17

申请号：PCT/US2007012270

申请日：2007-05-23

Applicant: VERTEX PHARMA ,  BRENCHLEY GUY ,  CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  KNEGTEL RONALD ,  RAMAYA SHARN

Inventor： BRENCHLEY GUY ,  CHARRIER JEAN-DAMIEN ,  DURRANT STEVEN ,  KNEGTEL RONALD ,  RAMAYA SHARN

IPC: C07D409/04

CPC classification number: C07D409/04

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。

公开(公告)号：WO2007139816A2

公开(公告)日：2007-12-06

申请号：PCT/US2007/012270

申请日：2007-05-23

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ronald ,  RAMAYA, Sharn

Inventor： BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ronald ,  RAMAYA, Sharn

IPC: C07D409/04

CPC classification number: C07D409/04

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract translation: 本发明涉及用作蛋白激酶抑制剂的化合物。 本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。 本发明还提供了制备本发明化合物的方法。

公开(公告)号：WO2007139795A1

公开(公告)日：2007-12-06

申请号：PCT/US2007/012207

申请日：2007-05-22

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ronald ,  RAMAYA, Sharn ,  SADIQ, Shazia

Inventor： BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ronald ,  RAMAYA, Sharn ,  SADIQ, Shazia

IPC: C07D409/04 ,  C07D409/14 ,  A61K31/381 ,  A61K31/4196 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D409/04 ,  A61K31/4196 ,  A61K45/06 ,  C07D409/14 ,  C12N9/99

Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.

Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还涉及包含所述化合物的药学上可接受的组合物以及在治疗各种疾病，病症或病症中使用该化合物和组合物的方法。 本发明还涉及制备本发明化合物的方法。

公开(公告)号：WO2007087283A3

公开(公告)日：2007-09-13

申请号：PCT/US2007001726

申请日：2007-01-23

Applicant: VERTEX PHARMA ,  DURRANT STEVEN ,  CHARRIER JEAN-DAMIEN ,  KNEGTEL RONALD ,  BRENCHLEY GUY ,  KAY DAVID ,  SADIQ SHAZIA ,  RAMAYA SHARN

Inventor： DURRANT STEVEN ,  CHARRIER JEAN-DAMIEN ,  KNEGTEL RONALD ,  BRENCHLEY GUY ,  KAY DAVID ,  SADIQ SHAZIA ,  RAMAYA SHARN

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4985 ,  A61K31/5025 ,  A61P35/00 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds of formula (I) useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的式（I）化合物。 本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。 本发明还提供了制备本发明化合物的方法。

公开(公告)号：WO2007056221A2

公开(公告)日：2007-05-18

申请号：PCT/US2006043096

申请日：2006-11-03

Applicant: VERTEX PHARMA ,  BINCH HAYLEY ,  MORTIMORE MICHAEL ,  DAVIS CHRIS ,  BOYALL DEAN ,  EVERITT SIMON ,  ROBINSON DANIEL ,  RAMAYA SHARN ,  FRAYSSE DAMIEN ,  STUDLEY JOHN ,  MILIER ANDREW ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  PINDER JOANNE

Inventor： BINCH HAYLEY ,  MORTIMORE MICHAEL ,  DAVIS CHRIS ,  BOYALL DEAN ,  EVERITT SIMON ,  ROBINSON DANIEL ,  RAMAYA SHARN ,  FRAYSSE DAMIEN ,  STUDLEY JOHN ,  MILIER ANDREW ,  O'DONNELL MICHAEL ,  RUTHERFORD ALISTAIR ,  PINDER JOANNE

IPC: A61K31/513

CPC classification number: C07D403/12 ,  C07D239/38 ,  C07D401/14 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

Abstract translation: 本发明涉及可用作蛋白激酶抑制剂的化合物。 本发明还提供包含这些化合物的药学上可接受的组合物和使用该化合物和组合物治疗各种疾病，病症和障碍的方法。 本发明还提供了制备本发明化合物的方法。

公开(公告)号：WO2007027729A1

公开(公告)日：2007-03-08

申请号：PCT/US2006/033791

申请日：2006-08-28

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  CHARRIER, Jean-Damien ,  RAMAYA, Sharn ,  DURRANT, Steven ,  JIMENEZ, Juan-Miguel ,  BRENCHLEY, Guy ,  KNEGTEL, Ronald ,  MORTIMORE, Michael

Inventor： CHARRIER, Jean-Damien ,  RAMAYA, Sharn ,  DURRANT, Steven ,  JIMENEZ, Juan-Miguel ,  BRENCHLEY, Guy ,  KNEGTEL, Ronald ,  MORTIMORE, Michael

IPC: C07D401/14 ,  C07D401/04 ,  C07D417/14 ,  A61K31/444 ,  A61P37/00 ,  A61P35/00

CPC classification number: C07D213/64 ,  C07D401/14 ,  C07D417/14

Abstract: The present invention relates to pyrid-2-one compounds of formula (I) useful as inhibitors of protein kinase of Tec family (e.g., Tec, Btk, Itk/Emt/Tsk, Bmx,Txk/Rlk) protein kinases. These compounds and pharmaceutically acceptable compositions thereof are useful for treating or preventing autoimmune, inflammatory, proliferative, hyperproliferative or immunologically-mediated diseases.

Abstract translation: 本发明涉及可用作Tec家族（例如Tec，Btk，Itk / Emt / Tsk，Bmx，Txk / Rlk）蛋白激酶的蛋白激酶抑制剂的式（I）的吡啶-2-酮化合物。 这些化合物及其药学上可接受的组合物可用于治疗或预防自身免疫，炎症，增殖，过度增殖或免疫介导的疾病。

公开(公告)号：WO2006065946A1

公开(公告)日：2006-06-22

申请号：PCT/US2005/045336

申请日：2005-12-15

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  RAMAYA, Sharn ,  JIMENEZ, Juan-Miguel ,  RUTHERFORD, Alistair

Inventor： CHARRIER, Jean-Damien ,  DURRANT, Steven ,  RAMAYA, Sharn ,  JIMENEZ, Juan-Miguel ,  RUTHERFORD, Alistair

IPC: C07D213/22 ,  C07D213/64 ,  C07D213/75 ,  C07D401/14 ,  C07D409/14 ,  C07D407/14 ,  C07D417/14 ,  A61K31/4427 ,  A61K31/444 ,  A61K31/4412 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00

CPC classification number: C07D401/14 ,  C07D213/22 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D213/84 ,  C07D213/85 ,  C07D401/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

Abstract: This invention describes compounds of Formula (I), or a pharmaceutically accepted salt thereof, wherein each R 3 and R 4 is independently H, halogen or C 1-4 aliphatic optionally substituted with halogen, C 1-2 aliphatic, OCH 3 , NO 2 , NH 2 , CN, NHCH 3 , SCH 3 , or N(CH) 2 . R 2 is a 3-8membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R 2 is optionally substituted with J R ; each X 1 and X 2 is independently -C(O)-, -NR-, or -SO 2 - wherein one of X 1 or X 2 is -NR- and other of X 1 or X 2 is -C(O)- or -SO 2 -; R1 and R are as described herein; These compounds are effective as inhibitors of Tec family (e.g., Tec, Btk, Itk/Emt/Tsk, Bmx, Txk/Rlk) protein kinases. These compounds and pharmaceutically acceptable compositions thereof are useful for treating or preventing a variety of diseases, disorders or conditions, including, but not limited to, an autoimmune, inflammatory, proliferative, or hyperproliferative disease or an immunologically-mediated disease.

Abstract translation: 本发明描述了式（I）化合物或其药学上可接受的盐，其中每个R 3和R 4独立地是H，卤素或C 1〜 4脂族，任选被卤素取代，C 1-2脂族基，OCH 3，NO 2，NH 2， CN，NHCH 3，SCH 3或N（CH）2。 R 2是具有0-3个独立地选自氮，氧或硫的杂原子的3-8元饱和，部分不饱和或完全不饱和的单环，或8-12元饱和的，部分不饱和的， 或具有0-5个独立地选自氮，氧或硫的杂原子的完全不饱和的双环体系; R 2任选被J取代; 每个X 1和X 2独立地是-C（O） - ， - NR - 或-SO 2 - ，其中X < SUP> 1或X 2是-NR-，X 1或X 2中的另一个是-C（O） - 或-SO 2 - ; R1和R如本文所述; 这些化合物作为Tec家族（例如，Tec，Btk，Itk / Emt / Tsk，Bmx，Txk / Rlk）蛋白激酶的抑制剂是有效的。 这些化合物及其药学上可接受的组合物可用于治疗或预防各种疾病，病症或病症，包括但不限于自身免疫性，炎性，增殖性或过度增殖性疾病或免疫介导的疾病。

公开(公告)号：WO2007120760A3

公开(公告)日：2007-10-25

申请号：PCT/US2007/009018

申请日：2007-04-12

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ron ,  RAMAYA, Sharn ,  SADIQ, Shazia

Inventor： BRENCHLEY, Guy ,  CHARRIER, Jean-Damien ,  DURRANT, Steven ,  KNEGTEL, Ron ,  RAMAYA, Sharn ,  SADIQ, Shazia

IPC: C07D409/04 ,  A61K31/4178 ,  A61P35/00

Abstract: The present invention relates to compounds of Formula I useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.