公开(公告)号：AU9603998A

公开(公告)日：1999-04-27

申请号：AU9603998

申请日：1998-10-06

Applicant: BASF AG

Inventor： ARNOLD LEE D ,  XU YAJUN ,  BARLOZZARI TERESA ,  RAFFERTY PAUL ,  HOCKLEY MICHAEL ,  TURNER ALLYSON

IPC: A61K31/415

公开(公告)号：DE60004685D1

公开(公告)日：2003-09-25

申请号：DE60004685

申请日：2000-09-15

Applicant: BASF AG

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

Abstract: The present invention is directed to pyrazolopyrimidine derivatives which are useful as kinase inhibitors and as such are useful for affecting angiogenesis and diseases and conditions associated with angiogenesis.

公开(公告)号：SK3852001A3

公开(公告)日：2003-03-04

申请号：SK3852001

申请日：1999-09-17

Applicant: BASF AG

Inventor： JOHNSTON DAVID N ,  RAFFERTY PAUL ,  TOMETZKI GERALD B ,  TWIGGER HELEN L ,  MUNSCHAUER RAINER ,  CALDERWOOD DAVID ,  ARNOLD LEE ,  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：TR200102277T2

公开(公告)日：2002-01-21

申请号：TR200102277

申请日：1999-11-04

Applicant: BASF AG AG

Inventor： DOYLE KEVIN J ,  RAFFERTY PAUL ,  STEELE ROBERT W ,  WILKINS DAVID J ,  HOCKLEY MICHAEL ,  ARNOLD LEE D ,  ERICSSON ANNA M

IPC: A61K31/416 ,  A61K31/4162 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61P1/04 ,  A61P1/16 ,  A61P5/14 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P15/08 ,  A61P17/02 ,  A61P17/06 ,  A61P19/02 ,  A61P19/08 ,  A61P27/00 ,  A61P27/06 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D409/04 ,  C07D413/04 ,  C07D417/12 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04 ,  A61K31/415 ,  A61K31/425 ,  A61K31/44 ,  A61K31/445

Abstract: This invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion which are inhibitors of protein kinase activity, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.

公开(公告)号：BG105346A

公开(公告)日：2001-12-31

申请号：BG10534601

申请日：2001-03-15

Applicant: BASF AG

Inventor： HIRST GAVIN C ,  CALDERWOOD DAVID ,  MUNSCHAUER RAINER ,  ARNOLD LEE D ,  JOHNSTON DAVID N ,  RAFFERTY 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: The compounds and their physiologically acceptable salts and metabolites have the formula wherein their substituents have the meanings listed in the description. The compounds 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 inflammatory disorders. 72 claims

公开(公告)号：BG105355A

公开(公告)日：2001-11-30

申请号：BG10535501

申请日：2001-03-16

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: A61K31/505 ,  C07D487/04

Abstract: Chemical compounds having the structural formula 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. 45 claims

公开(公告)号：TR200101395T2

公开(公告)日：2001-11-21

申请号：TR200101395

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：TR200101186T2

公开(公告)日：2001-10-22

申请号：TR200101186

申请日：1999-09-17

Applicant: BASF AG

Inventor： HIRST GAVIN C ,  CALDERWOOD DAVID ,  MUNSCHAUER RAINER ,  ARNOLD LEE D ,  JOHNSTON DAVID N ,  RAFFERTY 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：NZ337529A

公开(公告)日：2000-10-27

申请号：NZ33752998

申请日：1998-03-09

Applicant: BASF AG

Inventor： CALDERWOOD DAVID JOHN ,  JOHNSTON DAVID NORMAN ,  RAFFERTY PAUL ,  TWIGGER HELEN LOUISE ,  MUNSCHAUER RAINER ,  ARNOLD LEE

IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

Abstract: The pyrrolo[2,3-d]pyrimidin-4-ylamine derivatives or pharmaceutically acceptable salts have the formula I wherein: R1 is H, 2-phenyl-1,3-dioxan-5-yl, optionally substituted phenylalkyl or ORA substituted alkyl, cycloalkyl or cycloalkenyl; R2 is H, alkyl, cycloalkyl, halo, hydroxy, R4 or optionally substituted phenylalkyl or phenyl; R3 is an AR5 substituted phenyl that can be further substituted; A is NH, O, NHSO2, SO2NH, alkylene, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p or A is absent and R5 is attached directly to the phenyl ring; p is 0 to 2; R5 is optionally substituted phenyl or when A is absent R5 is optionally substituted phthalimido, pyrazolyl or phenyl; R4 is optionally substituted thienyl, benzo(b)thienyl, pyridyl, pyrazolyl, isoxazolyl, thiadiazolyl, indazolyl or oxadiazolyl. A pharmaceutical composition thereof is useful for treating benign and neoplastic proliferative diseases and disorders and disorders of the immune system.

公开(公告)号：AU4037800A

公开(公告)日：2000-10-23

申请号：AU4037800

申请日：2000-03-28

Applicant: BASF AG

Inventor： DOYLE KEVIN J ,  RAFFERTY PAUL ,  STEELE ROBERT W ,  TURNER ALLYSON ,  WILKINS DAVID J ,  ARNOLD LEE D

IPC: A61K31/416 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/5377 ,  A61P1/04 ,  A61P3/10 ,  A61P7/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/14 ,  A61P11/00 ,  A61P15/18 ,  A61P17/02 ,  A61P17/06 ,  A61P19/00 ,  A61P19/02 ,  A61P27/02 ,  A61P27/06 ,  A61P29/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D231/54 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D495/04 ,  C07D521/00

Abstract: This invention relates to compounds formula (I) and pharmaceutically acceptable salts thereof which are inhibitors of protein kinase activity, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.