公开(公告)号：CA2381882C

公开(公告)日：2011-01-25

申请号：CA2381882

申请日：2000-08-11

Applicant: VERTEX PHARMA

Inventor： GREEN JEREMY ,  BEMIS GUY ,  GRILLOT ANNE-LAURE ,  LEDEBOER MARK ,  SALITURO FRANCIS ,  HARRINGTON EDMUND ,  GAO HUAI ,  BAKER CHRISTOPHER ,  CAO JINGRONG ,  HALE MICHAEL

IPC: C07D413/04 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D413/14

Abstract: The present invention provides compounds of formula (I) where R1 is H, CONH2, T(n)-R, or T(n)-Ar2, 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：AU2006201392B2

公开(公告)日：2008-05-15

申请号：AU2006201392

申请日：2006-04-04

Applicant: VERTEX PHARMA

Inventor： JANETKA JAMES ,  CAO JINGRONG ,  MALTAIS FRANCOIS ,  HALE MICHAEL ,  MASHAL ROBERT

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

公开(公告)号：HK1052934B

公开(公告)日：2007-01-12

申请号：HK03105158

申请日：2003-07-16

Applicant: VERTEX PHARMA

Inventor： HALE MICHAEL ,  JANETKA JAMES ,  MALTAIS FRANCOIS ,  CAO JINGRONG ,  MASHAL ROBERT

IPC: C07D20060101 ,  A61K20060101 ,  A61K31/42 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/00 ,  A61P20060101 ,  A61P1/00 ,  A61P1/02 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/04 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/20 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

公开(公告)号：AU2006202623A1

公开(公告)日：2006-07-13

申请号：AU2006202623

申请日：2006-06-20

Applicant: VERTEX PHARMA

Inventor： HALE MICHAEL ,  CAO JINGRONG ,  STRAUB JUDY ,  ARONOV ALEX ,  GREEN JEREMY ,  MALTAIS FRANCOIS ,  TANG QING

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

公开(公告)号：AU2006201392A1

公开(公告)日：2006-04-27

申请号：AU2006201392

申请日：2006-04-04

Applicant: VERTEX PHARMA

Inventor： JANETKA JAMES ,  CAO JINGRONG ,  MALTAIS FRANCOIS ,  HALE MICHAEL ,  MASHAL ROBERT

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

公开(公告)号：MXPA02001565A

公开(公告)日：2005-07-14

申请号：MXPA02001565

申请日：2000-08-11

Applicant: VERTEX PHARMA

Inventor： HALE MICHAEL

IPC: A61K31/341 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/04 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P7/02 ,  A61P7/04 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/02 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P37/02 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04

Abstract: La presente invencion proporciona compuestos de la formula (I) en donde R1 es H, CONH2, T(n)-R o T(n)-Ar2, n puede ser cero o uno, y G, XYZ y Q son como se describe mas adelante. Estos compuestos son inhibidores de cinasa proteica, en particulas son inhibidores de JNK, una cinasa proteica de mamifero involucrada en la proliferacion celular, en la muerte de la celula y en la respuesta al estimulo extracelular. La invencion tambien se relaciona con metodos para producir estos inhibidores. La invencion tambien proporciona composiciones farmaceuticas que comprenden los inhibidores de la invencion y metodos para utilizar dichas composiciones en el tratamiento y prevencion de varios desordenes.

公开(公告)号：PL364565A1

公开(公告)日：2004-12-13

申请号：PL36456502

申请日：2002-02-08

Applicant: VERTEX PHARMA

Inventor： CAO JINGRONG ,  GREEN JEREMY ,  HALE MICHAEL ,  MALTAIS FRANCOIS ,  STRAUB JUDY ,  TANG QING ,  ARONOV ALEX

IPC: A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/16 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P17/06 ,  A61P19/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3 , 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：NZ525016A

公开(公告)日：2004-10-29

申请号：NZ52501601

申请日：2001-09-14

Applicant: VERTEX PHARMA

Inventor： HALE MICHAEL ,  JANETKA JAMES ,  MALTAIS FRANCOIS ,  CAO JINGRONG ,  MASHAL ROBERT

IPC: A61K31/42 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/551 ,  A61K45/00 ,  A61P1/00 ,  A61P1/02 ,  A61P1/16 ,  A61P1/18 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P17/00 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P19/04 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/20 ,  A61P25/28 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  A61P37/08 ,  A61P43/00 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  A61K31/422 ,  A61K31/439 ,  A61K31/497

Abstract: Disclosed herein are compounds of formula (I) that are useful as protein kinase inhibitors, especially inhibitors of ERK, wherein Ht is an optionally substituted heteroaryl ring selected from pyrrol-3-yl, pyrazol-3-yl, [1,2,3]triazol-4-yl, [1,2,4]triazol-3-yl, or tetrazol-5-yl, and A-B is N-O or O-N, and wherein R1, R2 and T are as defined in the specification. These 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：HK1062298A1

公开(公告)日：2004-10-29

申请号：HK04103680

申请日：2004-05-24

Applicant: VERTEX PHARMA

Inventor： CAO JINGRONG ,  GREEN JEREMY ,  HALE MICHAEL ,  MALTAIS FRANCOIS ,  STRAUB JUDY ,  TANG QING ,  ARONOV ALEX

IPC: C07D20060101 ,  A61K20060101 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/551 ,  A61P20060101 ,  A61P1/16 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P17/06 ,  A61P19/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3 , 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：HU0304052A2

公开(公告)日：2004-04-28

申请号：HU0304052

申请日：2002-02-08

Applicant: VERTEX PHARMA

Inventor： ARONOV ALEX ,  CAO JINGRONG ,  GREEN JEREMY ,  HALE MICHAEL ,  MALTAIS FRANCOIS ,  STRAUB JUDY ,  TANG QING

IPC: A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/551 ,  A61P1/16 ,  A61P3/10 ,  A61P5/00 ,  A61P7/02 ,  A61P9/08 ,  A61P9/10 ,  A61P17/06 ,  A61P19/00 ,  A61P25/00 ,  A61P25/28 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3 , 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.