公开(公告)号：EP2032562B1

公开(公告)日：2010-08-25

申请号：EP07794722.4

申请日：2007-05-10

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： GREEN, Jeremy ,  CAO, Jingrong ,  BANDARAGE, Upul ,  COME, Jon ,  MARHEFKA, Craig

IPC分类号： C07D409/04 ,  C07D417/04 ,  C07D417/14 ,  A61P35/00 ,  A61K31/427

CPC分类号： C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14

摘要： Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.

公开(公告)号：EP1814883A1

公开(公告)日：2007-08-08

申请号：EP05825542.3

申请日：2005-11-22

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： GREEN, Jeremy ,  CAO, Jingrong ,  BANDARAGE, Upul ,  GAO, Huai ,  FORSTER, Cornelia

IPC分类号： C07D487/04 ,  A61K31/437 ,  A61P25/28 ,  A61P37/06

CPC分类号： C07D487/04 ,  C07D471/04

摘要： The present invention relates to compounds useful as inhibitors of protein kinases, particularly of ROCK. 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.

公开(公告)号：EP1756108A2

公开(公告)日：2007-02-28

申请号：EP05767612.4

申请日：2005-04-04

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： GREEN, Jeremy ,  MILLER, Andrew ,  JIMENEZ, Juan-Miguel ,  MARHEFKA, Craig ,  CAO, Jingrong ,  COURT, John, J. ,  BANDARAGE, Upul, K. ,  GAO, Huai ,  NANTHAKUMAR, Suganthini

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P37/08 ,  A61P29/00

CPC分类号： C07D471/04

摘要： The present invention relates to compounds useful as 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.

公开(公告)号：EP1363906A2

公开(公告)日：2003-11-26

申请号：EP02724922.6

申请日：2002-02-08

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： CAO, Jingrong ,  GREEN, Jeremy ,  HALE, Michael ,  MALTAIS, Francois ,  STRAUB, Judy ,  TANG, Qing ,  ARONOV, Alex

IPC分类号： C07D403/04 ,  C07D401/14 ,  C07D413/14 ,  C07D405/14 ,  C07D403/14 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) wherein Z?1 and Z2¿ are each independently nitrogen or CH and Ring A, T¿m?R?1, QR2, U¿nR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

公开(公告)号：EP1317453A1

公开(公告)日：2003-06-11

申请号：EP01971002.9

申请日：2001-09-14

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： HALE, Michael,Vertex Pharmaceuticals Inc. ,  JANETKA, James ,  MALTAIS, Francois ,  CAO, Jingrong ,  MASHAL, Robert

IPC分类号： C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/422 ,  A61K31/433 ,  A61K31/439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61P35/00

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/14

摘要： Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula (I) wherein Ht is an optionally substituted heteroaryl ring selected from pyrrol-3-yl, pyrazol-3-yl, [1,2,3]triazol-4-yl, or tetrazol-5-yl, and A-B is N-O or O-N. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

公开(公告)号：EP1218369A1

公开(公告)日：2002-07-03

申请号：EP00957485.6

申请日：2000-08-11

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： GREEN, Jeremy ,  BEMIS, Guy ,  GRILLOT, Anne-Laure ,  LEDEBOER, Mark ,  SALITURO, Francis ,  HARRINGTON, Edmund ,  GAO, Huai ,  BAKER, Christopher ,  CAO, Jingrong ,  HALE, Michael

IPC分类号： C07D401/04 ,  C07D405/04 ,  C07D403/04 ,  C07D413/04 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42

CPC分类号： C07D413/04 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  C07D413/14

摘要： The present invention provides compounds of formula (I) where R1 is H, CONH¿2?, T(n)-R, or T(n)-Ar?2¿, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

公开(公告)号：EP1200422A2

公开(公告)日：2002-05-02

申请号：EP01908911.9

申请日：2001-02-05

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： 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分类号： C07D403/04 ,  C07D471/04 ,  C07D403/14 ,  C07D401/04 ,  A61K31/33

CPC分类号： C07D401/14 ,  C07D231/38 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14 ,  C07D471/04

摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula: (I) where R1-4, 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.

公开(公告)号：EP4204423A1

公开(公告)日：2023-07-05

申请号：EP21773242.9

申请日：2021-08-26

申请人： Vertex Pharmaceuticals Incorporated

发明人： AHN, Jun Myun ,  ANGLE, Samantha ,  BRODNEY, Michael Aaron ,  CAO, Jingrong ,  COCHRAN, John E. ,  COME, Jon H. ,  DAKIN, Leslie A. ,  DOLGIKH, Elena ,  MAXWELL, Brad D. ,  NANTHAKUMAR, Suganthini S. ,  O DOWD, Hardwin ,  OLSEN, Jessica Howard ,  SENTER, Timothy J. ,  SHIMIZU, Akira Joseph ,  STONE, Steven David ,  WANG, Haoxuan

IPC分类号： C07D495/20 ,  A61P13/12 ,  C07D519/00 ,  A61K31/438

公开(公告)号：EP1389206B1

公开(公告)日：2006-09-13

申请号：EP02762067.3

申请日：2002-04-10

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： CAO, Jingrong ,  GREEN, Jeremy ,  MOON, Young-Choon ,  WANG, Jian ,  LEDEBOER, Mark ,  HARRINGTON, Edmund ,  GAO, Huai

IPC分类号： C07D409/00

CPC分类号： C07D409/14 ,  C07D409/04 ,  C07D417/14

摘要： The present invention provides compounds of formula (I): or a pharmaceutically acceptable derivative thereof, wherein A, B, Ra, R1, R2, R3 and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli; Lck and Src kinase. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

公开(公告)号：EP1558607A1

公开(公告)日：2005-08-03

申请号：EP03781448.0

申请日：2003-10-30

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： CAO, Jingrong ,  GAO, Huai ,  GREEN, Jeremy ,  MARHEFKA, Craig

IPC分类号： C07D409/04 ,  C07D417/04 ,  C07D417/14 ,  C07D409/14

CPC分类号： C07D417/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04

摘要： The present invention relates to substitute thiazole and thiophene derivatives useful as inhibitors of rock and other protein kinaeses. 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, including proliferative, cardiac and neurodegenerative diseases.