公开(公告)号：WO2005113546A1

公开(公告)日：2005-12-01

申请号：PCT/US2005/016801

申请日：2005-05-13

Applicant: VERTEX PHARMACEUTICALS, INCORPORATED ,  MARTINEZ-BOTELLA, Gabriel ,  HALE, Michael, R. ,  MALTAIS, Francois ,  TANG, Qing ,  STRAUB, Judith

Inventor： MARTINEZ-BOTELLA, Gabriel ,  HALE, Michael, R. ,  MALTAIS, Francois ,  TANG, Qing ,  STRAUB, Judith

IPC: C07D403/04

CPC classification number: C07D403/04

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. 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.

Abstract translation: 本发明涉及可用于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。

公开(公告)号：WO2005068468A3

公开(公告)日：2005-10-13

申请号：PCT/US2004040422

申请日：2004-12-02

Applicant: VERTEX PHARMA ,  STRAUB JUDITH ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  MARTINEZ-BOTELLA GABRIEL ,  ARONOV ALEX ,  BEMIS GUY W

Inventor： STRAUB JUDITH ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  MARTINEZ-BOTELLA GABRIEL ,  ARONOV ALEX ,  BEMIS GUY W

IPC: A61K31/506 ,  A61K45/06 ,  C07D239/48 ,  C07D251/18 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D487/08 ,  A61P35/00

CPC classification number: C07D239/48 ,  A61K31/506 ,  A61K45/06 ,  C07D251/18 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  A61K2300/00

Abstract: Described herein are compounds that are useful as protein kinase inhibitors of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ring B, Z , Z , U, p, Q, R , R , R , and R are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.

Abstract translation: 本文描述了可用作式（I）的蛋白激酶抑制剂或其药学上可接受的盐的化合物，其中环B，Z 1，Z 2，U，p，Q，R 1， R 3，R 3和R 3如本文所定义。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种疾病的严重性，包括中风，炎性疾病，自身免疫性疾病如SLE狼疮和牛皮癣，增殖性疾病如癌症，以及与器官移植相关的病症 。

公开(公告)号：WO0157022A2

公开(公告)日：2001-08-09

申请号：PCT/US0103911

申请日：2001-02-05

Applicant: VERTEX PHARMA ,  GREEN JEREMY ,  CAO JINGRONG ,  HALE MICHAEL ,  BAKER CHRISTOPHER ,  MALTAIS FRANCOIS ,  JANETKA JAMES ,  MULLICAN MICHAEL ,  BEMIS GUY ,  XIE XIAOLING ,  STRAUB JUDITH ,  TANG QING ,  MASHALL ROBERT

Inventor： GREEN JEREMY ,  CAO JINGRONG ,  HALE MICHAEL ,  BAKER CHRISTOPHER ,  MALTAIS FRANCOIS ,  JANETKA JAMES ,  MULLICAN MICHAEL ,  BEMIS GUY ,  XIE XIAOLING ,  STRAUB JUDITH ,  TANG QING ,  MASHALL ROBERT

IPC: A61B17/00 ,  A61F2/02 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/00 ,  A61L27/00 ,  A61P1/00 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P11/00 ,  A61P13/00 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/04 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D231/38 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04 ,  C07D403/00

CPC classification number: C07D401/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: (I) where R , Q, and T are described inthe specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

Abstract translation: 本文描述了可用作具有下式的蛋白激酶抑制剂的化合物：其中R 1-4，Q和T在说明书中描述。 该化合物可用于治疗由蛋白激酶抑制剂，特别是诸如癌症，炎症性疾病，再狭窄和心血管疾病等疾病减轻的哺乳动物的疾病状态。

公开(公告)号：WO2006071644A1

公开(公告)日：2006-07-06

申请号：PCT/US2005/046177

申请日：2005-12-20

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  ARONOV, Alex ,  HALE, Michael, R. ,  MALTAIS, François ,  MARTINEZ-BOTELLA, Gabriel ,  STRAUB, Judith ,  TANG, Qing

Inventor： ARONOV, Alex ,  HALE, Michael, R. ,  MALTAIS, François ,  MARTINEZ-BOTELLA, Gabriel ,  STRAUB, Judith ,  TANG, Qing

IPC: C07D403/04 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D403/04

Abstract: Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferate disorders such as cancer.

Abstract translation: 本文描述的是可用作ERK2抑制剂的化合物。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种病症（包括增殖性疾病如癌症）的严重性。

公开(公告)号：WO2005068468A2

公开(公告)日：2005-07-28

申请号：PCT/US2004/040422

申请日：2004-12-02

Applicant: VERTEX PHARMACEUTICALS, INC. ,  STRAUB, Judith ,  HALE, Michael, R. ,  MALTAIS, François ,  MARTINEZ-BOTELLA, Gabriel ,  ARONOV, Alex ,  BEMIS, Guy, W.

Inventor： STRAUB, Judith ,  HALE, Michael, R. ,  MALTAIS, François ,  MARTINEZ-BOTELLA, Gabriel ,  ARONOV, Alex ,  BEMIS, Guy, W.

IPC: C07D487/08

CPC classification number: C07D239/48 ,  A61K31/506 ,  A61K45/06 ,  C07D251/18 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  A61K2300/00

Abstract: Described herein are compounds that are useful as protein kinase inhibitors of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ring B, Z 1 , Z 2 , U, p, Q, R 1 , R 2 , R 3 , and R 3 are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.

Abstract translation: 本文描述的是可用作式（I）的蛋白激酶抑制剂或其药学上可接受的盐的化合物，其中环B，Z 1，Z 2 U，p，Q，R 1，R 2，R 3和R 3分别代表 >如本文所定义。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种疾病的严重程度，包括中风，炎性疾病，自身免疫疾病如SLE红斑狼疮和牛皮癣，增殖性疾病如癌症和与器官移植相关的病症

公开(公告)号：WO2006071644A8

公开(公告)日：2006-08-24

申请号：PCT/US2005046177

申请日：2005-12-20

Applicant: VERTEX PHARMA ,  ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  MARTINEZ-BOTELLA GABRIEL ,  STRAUB JUDITH ,  TANG QING

Inventor： ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  MARTINEZ-BOTELLA GABRIEL ,  STRAUB JUDITH ,  TANG QING

IPC: C07D403/04 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D403/04

Abstract: Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferate disorders such as cancer.

Abstract translation: 本文描述的是可用作ERK2抑制剂的化合物。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种病症（包括增殖性疾病如癌症）的严重性。

公开(公告)号：WO2006065820A2

公开(公告)日：2006-06-22

申请号：PCT/US2005045079

申请日：2005-12-13

Applicant: VERTEX PHARMA ,  MARTINEZ-BOTELLA GABRIEL ,  ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  STRAUB JUDITH ,  TANG QING

Inventor： MARTINEZ-BOTELLA GABRIEL ,  ARONOV ALEX ,  HALE MICHAEL R ,  MALTAIS FRANCOIS ,  STRAUB JUDITH ,  TANG QING

CPC classification number: C07D239/48

Abstract: Described herein are compounds that are useful as protein kinase inhibitors of formula (I); or a pharmaceutically acceptable salt thereof, wherein Ring A, Z 1 , Z 2 , U, Q, R 1 , R 2 , and L are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.

Abstract translation: 本文描述的是可用作式（I）的蛋白激酶抑制剂的化合物; 或其药学上可接受的盐，其中环A，Z 1，Z 2，U，Q，R 1，R 2， 和/或L如本文所定义。 这些化合物及其药学上可接受的组合物可用于治疗或减轻各种病症（包括增殖性疾病如癌症）的严重性。

公开(公告)号：WO2005113541A1

公开(公告)日：2005-12-01

申请号：PCT/US2005/016902

申请日：2005-05-13

Applicant: VERTEX PHARMACEUTICALS, INCORPORATED ,  MARTINEZ-BOTELLA, Gabriel ,  HALE, Michael, R. ,  MALTAIS, François ,  TANG, Qing ,  STRAUB, Judith

Inventor： MARTINEZ-BOTELLA, Gabriel ,  HALE, Michael, R. ,  MALTAIS, François ,  TANG, Qing ,  STRAUB, Judith

IPC: C07D401/04

CPC classification number: C07F9/65583 ,  C07D401/04

Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. 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.

Abstract translation: 本发明涉及可用于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。

公开(公告)号：WO2006065820A3

公开(公告)日：2006-06-22

申请号：PCT/US2005/045079

申请日：2005-12-13

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  MARTINEZ-BOTELLA, Gabriel ,  ARONOV, Alex ,  HALE, Michael, R. ,  MALTAIS, François ,  STRAUB, Judith ,  TANG, Qing

Inventor： MARTINEZ-BOTELLA, Gabriel ,  ARONOV, Alex ,  HALE, Michael, R. ,  MALTAIS, François ,  STRAUB, Judith ,  TANG, Qing

IPC: C07D239/30 ,  A61K31/505

Abstract: Described herein are compounds that are useful as protein kinase inhibitors of formula (I); or a pharmaceutically acceptable salt thereof, wherein Ring A, Z 1 , Z 2 , U, Q, R 1 , R 2 , and L are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.

公开(公告)号：WO2003091246A1

公开(公告)日：2003-11-06

申请号：PCT/US2003/013186

申请日：2003-04-25

Applicant: VERTEX PHARMACEUTICALS INCORPORATED ,  HALE, Michael, R. ,  MALTAIS, Francois ,  TANG, Qing ,  STRAUB, Judith ,  ARONOV, Alexander

Inventor： HALE, Michael, R. ,  MALTAIS, Francois ,  TANG, Qing ,  STRAUB, Judith ,  ARONOV, Alexander

IPC: C07D403/04

CPC classification number: C07D401/14 ,  C07D207/333 ,  C07D207/337 ,  C07D403/04 ,  C07D405/14 ,  C07D471/04

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein A 1 , A 2 , TmR 1 , X, R 2 , R 3 , R 9 , R 12 , and R 13 Are as described in the specification. The compounds are especially useful as inhibitors of ERK2, Aurora2, GSK3, CDK2, AKT3, and ROCK protein kinases and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, neurodegenerative disorders, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

Abstract translation: 本文描述了可用作具有下式的蛋白激酶抑制剂的化合物：其中A 1，A 2，T M R 1，X，R 2，R 3，R 9， 12>，R 13如说明书中所述。 该化合物特别可用作ERK2，Aurora2，GSK3，CDK2，AKT3和ROCK蛋白激酶的抑制剂，并用于治疗由蛋白激酶抑制剂缓解的哺乳动物疾病，特别是疾病如癌症，神经退行性疾病，炎症性疾病，再狭窄 ，糖尿病和心血管疾病。