公开(公告)号：WO0119828A3

公开(公告)日：2001-10-04

申请号：PCT/US0025357

申请日：2000-09-15

Applicant: BASF AG ,  HIRST GAVIN C ,  RAFFERTY PAUL ,  RITTER KURT ,  CALDERWOOD DAVID ,  TWIGGER HELEN L ,  ST GALLAY STEPHEN

Inventor： HIRST GAVIN C ,  RAFFERTY PAUL ,  RITTER KURT ,  CALDERWOOD DAVID ,  TWIGGER HELEN L ,  ST GALLAY STEPHEN

IPC: A61K31/437 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/55 ,  A61K38/00 ,  A61P1/18 ,  A61P3/10 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P15/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P31/12 ,  A61P31/18 ,  A61P33/02 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D471/04 ,  C07D487/04 ,  C07F9/6561 ,  A61K31/4353 ,  A61K31/551 ,  C07D491/04 ,  C07D498/04

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07F9/6561

Abstract: The present invention is directed to a compound of Formula (I) as defined herein which are useful as kinase inhibitors.

Abstract translation: 本发明涉及可用作激酶抑制剂的本文定义的式（I）化合物。

公开(公告)号：WO0119829A2

公开(公告)日：2001-03-22

申请号：PCT/US0025468

申请日：2000-09-15

Applicant: BASF AG ,  HIRST GAVIN C ,  CALDERWOOD DAVID ,  WISHART NEIL ,  RAFFERTY PAUL ,  RITTER KURT ,  ARNOLD LEE D ,  FRIEDMAN MICHAEL M

Inventor： HIRST GAVIN C ,  CALDERWOOD DAVID ,  WISHART NEIL ,  RAFFERTY PAUL ,  RITTER KURT ,  ARNOLD LEE D ,  FRIEDMAN MICHAEL M

IPC: A61K31/519 ,  A61K31/5377 ,  A61K38/22 ,  A61P1/04 ,  A61P1/16 ,  A61P3/10 ,  A61P5/14 ,  A61P7/06 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P15/16 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P31/22 ,  A61P33/02 ,  A61P35/00 ,  A61P35/02 ,  A61P37/06 ,  A61P43/00 ,  C07D487/04 ,  C07F9/6561

CPC classification number: C07D487/04 ,  C07F9/6561

Abstract: The present invention provides compounds of Formula (I), including pharmaceutically acceptable salts and/or prodrugs thereof, where G, Ra, R2, R3 are defined as described herein.

Abstract translation: 本发明提供式（I）化合物，包括其药学上可接受的盐和/或前药，其中G，R a，R 2，R 3如本文所述定义。

公开(公告)号：WO0075139A3

公开(公告)日：2001-03-29

申请号：PCT/US0015324

申请日：2000-06-02

Applicant: BASF AG ,  RAFFERTY PAUL ,  CALDERWOOD DAVID ,  ARNOLD LEE D ,  GONZALEZ PASCUAL BEATRIZ ,  ORTEGO MATINEZ JOSE L ,  PEREZ DE VEGA MARIA J ,  FERNANDEZ ISABEL F

Inventor： RAFFERTY PAUL ,  CALDERWOOD DAVID ,  ARNOLD LEE D ,  GONZALEZ PASCUAL BEATRIZ ,  ORTEGO MATINEZ JOSE L ,  PEREZ DE VEGA MARIA J ,  FERNANDEZ ISABEL F

IPC: C07D265/36 ,  A61K31/42 ,  A61K31/425 ,  A61K31/437 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5415 ,  A61P1/00 ,  A61P3/10 ,  A61P5/14 ,  A61P9/00 ,  A61P9/10 ,  A61P11/16 ,  A61P15/00 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P21/04 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07D20060101 ,  C07D279/16 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/00 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D417/06 ,  C07D265/36 ,  C07D413/06 ,  C07D471/04

Abstract: Q is - N=or CR ; X is S, O or NOR ; Y is-O-, -S-, -SO- or -SO2-; R and R are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl group R is H or a substituent; R is H, or -C(O)R ; R is a substituted or unsubstituted aliphatic or aromatic group; n is an integer from 0 to 1. Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyperproliferative disorders.

Abstract translation: Q是-N =或CR <2>; X是S，O或NOR 3; Y是-O - ， - S - ， - SO-或-SO 2 - ; R和R 1各自独立地为H，取代或未取代的脂族，芳族，杂芳族或芳烷基R 2是H或取代基; R 3是H或-C（O）R 4; R 4是取代或未取代的脂族或芳族基团; n是0至1的整数。具有结构式（I）的化合物及其生理上可接受的盐是丝氨酸/苏氨酸和酪氨酸激酶活性的抑制剂。 几种酪氨酸激酶（其活性被这些化合物抑制）参与血管发生过程。 因此，这些化合物可以改善其中血管生成或内皮细胞过度增殖是一个因素的疾病状态。 这些化合物可用于治疗癌症和过度增殖性疾病。

公开(公告)号：BR9913888A

公开(公告)日：2002-01-08

申请号：BR9913888

申请日：1999-09-17

Applicant: BASF AG

Inventor： CALDERWOOD DAVID ,  ARNOLD LEE D ,  MAZDIYASNI HORMOZ ,  HIRST GAVIN ,  DENG BOJUAN B ,  JOHNSTON DAVID N ,  RAFFERTY PAUL ,  TOMETZKI GERALD B ,  TWIGGER HELEN L ,  MUNSCHAUER RAINER

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P27/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases whose activity is inhibited by these compounds are involved in immunologic, hyperproliferative or angiogenic processes. Thus, these compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferative is a factor. These compounds can be used to treat cancer, hyperproliferation disorders, rheumatoid arthritis, disorders of the immune system, transplant rejection, and inflammatory disorders.

公开(公告)号：ID28362A

公开(公告)日：2001-05-17

申请号：ID20010653

申请日：1999-09-17

Applicant: BASF AG

Inventor： CALDERWOOD DAVID ,  ARNOLD LEE D ,  MAZDIYASNI HORMOZ ,  HIRST GAVIN ,  DENG BOJUAN B

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P27/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases whose activity is inhibited by these compounds are involved in immunologic, hyperproliferative or angiogenic processes. Thus, these compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferative is a factor. These compounds can be used to treat cancer, hyperproliferation disorders, rheumatoid arthritis, disorders of the immune system, transplant rejection, and inflammatory disorders.

公开(公告)号：NO20011356A

公开(公告)日：2001-05-16

申请号：NO20011356

申请日：2001-03-16

Applicant: BASF AG

Inventor： HIRST GAVIN C ,  CALDERWOOD DAVID ,  WISHART NEIL ,  RITTER KURT ,  ARNOLD LEE DANIEL

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D487/04 ,  C07F9/6561 ,  C07F9/6584 ,  A61K31/505

CPC classification number: C07D487/04 ,  C07F9/6561 ,  C07F9/65842

公开(公告)号：HU0200355A2

公开(公告)日：2002-06-29

申请号：HU0200355

申请日：1999-09-17

Applicant: BASF AG

Inventor： ARNOLD LEE D ,  CALDERWOOD DAVID ,  DENG BOJUAN B ,  HIRST GAVIN ,  MAZDIYASNI HORMOZ

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P27/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04

Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases whose activity is inhibited by these compounds are involved in immunologic, hyperproliferative or angiogenic processes. Thus, these compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferative is a factor. These compounds can be used to treat cancer, hyperproliferation disorders, rheumatoid arthritis, disorders of the immune system, transplant rejection, and inflammatory disorders.

公开(公告)号：SK3842001A3

公开(公告)日：2002-04-04

申请号：SK3842001

申请日：1999-09-17

Applicant: BASF AG

Inventor： HIRST GAVIN C ,  CALDERWOOD DAVID ,  MUNSCHAUER RAINER ,  RAFFERTY PAUL ,  ARNOLD LEE D ,  JOHNSTON DAVID N

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D487/04 ,  C07F9/6561 ,  C07F9/6584 ,  A61K31/505

Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatoid arthritis, disorders of the immune system, transplant rejections and imflammatory disorders.

公开(公告)号：CZ2001960A3

公开(公告)日：2001-10-17

申请号：CZ2001960

申请日：1999-09-17

Applicant: BASF AG

Inventor： HIRST GAVIN C ,  CALDERWOOD DAVID ,  MUNSCHAUER RAINER ,  ARNOLD LEE D ,  JOHNSTON DAVID N ,  FAFFERTY PAUL

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P5/14 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P31/04 ,  A61P31/12 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D487/04 ,  C07F9/6561 ,  C07F9/6584 ,  A61K31/505

Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatoid arthritis, disorders of the immune system, transplant rejections and imflammatory disorders.

公开(公告)号：NO20011357L

公开(公告)日：2001-05-14

申请号：NO20011357

申请日：2001-03-16

Applicant: BASF AG

Inventor： CALDERWOOD DAVID ,  ARNOLD LEE DANIEL ,  MAZDIYASNI HORMOZ ,  HIRST GAVIN C ,  DENG BOJUAN B

IPC: A61K31/519 ,  A61P1/04 ,  A61P3/10 ,  A61P9/00 ,  A61P11/00 ,  A61P15/00 ,  A61P17/02 ,  A61P19/02 ,  A61P27/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases whose activity is inhibited by these compounds are involved in immunologic, hyperproliferative or angiogenic processes. Thus, these compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferative is a factor. These compounds can be used to treat cancer, hyperproliferation disorders, rheumatoid arthritis, disorders of the immune system, transplant rejection, and inflammatory disorders.