公开(公告)号：US06699865B2

公开(公告)日：2004-03-02

申请号：US10335793

申请日：2003-01-02

申请人： Michael Hale ,  Xiaoling Xie ,  Jeremy Green ,  Jingrong Cao ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Guy Bemis ,  Michael Mullican ,  Judith Straub ,  Qing Tang

发明人： Michael Hale ,  Xiaoling Xie ,  Jeremy Green ,  Jingrong Cao ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Guy Bemis ,  Michael Mullican ,  Judith Straub ,  Qing Tang

IPC分类号： A61K314155

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: where R1-4, Q, and T are described in the 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.

摘要翻译： 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：US06528509B1

公开(公告)日：2003-03-04

申请号：US09972437

申请日：2001-10-05

申请人： Michael Hale ,  Xiaoling Xie ,  Jeremy Green ,  Jingrong Cao ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Guy Bemis ,  Michael Mullican ,  Judith Straub ,  Qing Tang ,  Robert Mashal

发明人： Michael Hale ,  Xiaoling Xie ,  Jeremy Green ,  Jingrong Cao ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Guy Bemis ,  Michael Mullican ,  Judith Straub ,  Qing Tang ,  Robert Mashal

IPC分类号： A61K315377

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: where R1-4, Q, and T are described in the 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.

摘要翻译： 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R1-4，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：US07056944B2

公开(公告)日：2006-06-06

申请号：US10688613

申请日：2003-10-17

申请人： Michael Hale ,  Xiaoling Xie ,  Jeremy Green ,  Jingrong Cao ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Guy Bemis ,  Michael Mullican ,  Judith Straub ,  Qing Tang ,  Robert Mashal

发明人： Michael Hale ,  Xiaoling Xie ,  Jeremy Green ,  Jingrong Cao ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Guy Bemis ,  Michael Mullican ,  Judith Straub ,  Qing Tang ,  Robert Mashal

IPC分类号： A61K31/40 ,  C07D207/00

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: where R1-4, Q, and T are described in the 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.

摘要翻译： 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：US06593357B1

公开(公告)日：2003-07-15

申请号：US10225719

申请日：2002-08-22

申请人： Jeremy Green ,  Jingrong Cao ,  Michael Hale ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Michael Mullican ,  Guy Bemis ,  Xiaoling Xie ,  Judith Straub ,  Qing Tang

发明人： Jeremy Green ,  Jingrong Cao ,  Michael Hale ,  Christopher Baker ,  Francois Maltais ,  James Janetka ,  Michael Mullican ,  Guy Bemis ,  Xiaoling Xie ,  Judith Straub ,  Qing Tang

IPC分类号： A61K314155

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: where R1-4, Q, and T are described in the 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：US06743791B2

公开(公告)日：2004-06-01

申请号：US10071699

申请日：2002-02-08

申请人： Jingrong Cao ,  Jeremy Green ,  Michael Hale ,  Francois Maltais ,  Judy Straub ,  Qing Tang ,  Alex Aronov

发明人： Jingrong Cao ,  Jeremy Green ,  Michael Hale ,  Francois Maltais ,  Judy Straub ,  Qing Tang ,  Alex Aronov

IPC分类号： C07D40304

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: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, 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.

摘要翻译： 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Z 1和Z 2各自独立地为氮或CH，环A，TmR 1，Q 2，R un R 3， 和Sp如说明书中所述。 该化合物特别可用作ERK2的抑制剂，并且用于治疗由蛋白激酶抑制剂，特别是癌症，炎性疾病，再狭窄，糖尿病和心血管疾病等疾病缓解的哺乳动物疾病。

公开(公告)号：US07253187B2

公开(公告)日：2007-08-07

申请号：US10770814

申请日：2004-02-03

申请人： Jingrong Cao ,  Jeremy Green ,  Michael Hale ,  Francois Maltais ,  Judy Straub ,  Qing Tang ,  Alex Aronov

发明人： Jingrong Cao ,  Jeremy Green ,  Michael Hale ,  Francois Maltais ,  Judy Straub ,  Qing Tang ,  Alex Aronov

IPC分类号： C07D401/04 ,  A61K31/4427

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: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, 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.

摘要翻译： 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Z 1和Z 2各自独立地为氮或CH并且环A，T m 第二，第二，第二，第三，第三和第三，第二，如 规范。 该化合物特别可用作ERK2的抑制剂，并且用于治疗由蛋白激酶抑制剂，特别是癌症，炎性疾病，再狭窄，糖尿病和心血管疾病等疾病缓解的哺乳动物疾病。

公开(公告)号：US06693108B2

公开(公告)日：2004-02-17

申请号：US10074177

申请日：2002-02-12

申请人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco G. Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

发明人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco G. Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

IPC分类号： C07D40104

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, 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.

摘要翻译： 本发明提供式I化合物：其中R 1是H，CONH 2，T（n）-R或T（n）-Ar 2，n可以是0或1，G，XYZ和 Q如下所述。 这些化合物是蛋白激酶的抑制剂，特别是JNK的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

公开(公告)号：US20050026967A1

公开(公告)日：2005-02-03

申请号：US10779532

申请日：2004-02-13

申请人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

发明人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

IPC分类号： 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 ,  C07D261/06 ,  A61K31/34 ,  A61K31/505

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, 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.

摘要翻译： 本发明提供式I化合物：其中R 1是H，CONH 2，T（n）-R或T（n）-Ar 2，n可以是0或1，G，XYZ和 Q如下所述。 这些化合物是蛋白激酶的抑制剂，特别是JNK的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

公开(公告)号：US07169798B2

公开(公告)日：2007-01-30

申请号：US10779532

申请日：2004-02-13

申请人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco G. Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

发明人： Jeremy Green ,  Guy Bemis ,  Anne-Laure Grillot ,  Mark Ledeboer ,  Francesco G. Salituro ,  Edmund Harrington ,  Huai Gao ,  Christopher Baker ,  Jingrong Cao ,  Michael Hale

IPC分类号： C07D401/04 ,  C07D413/04 ,  A61K31/42 ,  C07D403/04

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, 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.

摘要翻译： 本发明提供了式I的化合物：其中R 1是H，CONH 2，T（N，N）-R或T（< n可以是0或1，并且G，XYZ和Q如下所述。 这些化合物是蛋白激酶的抑制剂，特别是JNK的抑制剂，哺乳动物蛋白激酶涉及细胞增殖，细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

公开(公告)号：US06495582B1

公开(公告)日：2002-12-17

申请号：US09953120

申请日：2001-09-14

申请人： Michael Hale ,  James Janetka ,  Francois Maltais ,  Jingrong Cao ,  Robert Mashal

发明人： Michael Hale ,  James Janetka ,  Francois Maltais ,  Jingrong Cao ,  Robert Mashal

IPC分类号： C07D41304

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: where A, B, R1, R2, T and Ht are described in the specification. 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.

摘要翻译： 本文描述了可用作蛋白激酶抑制剂，特别是ERK抑制剂的化合物，其具有下式：其中A，B，R1，R2，T和Ht在说明书中描述。 该化合物可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，炎症性疾病，再狭窄和心血管疾病。