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公开(公告)号:AU5179000A
公开(公告)日:2000-12-28
申请号:AU5179000
申请日:2000-06-02
Applicant: BASF AG
Inventor: RAFFERTY PAUL , CALDERWOOD DAVID , ARNOLD LEE D , PASCUAL BEATRIZ GONZALEZ , MATINEZ JOSE L ORTEGO , VEGA MARIA J PEREZ DE , 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
Abstract: Q is -N=or CR 2 X is S, O or NOR 3 Y is -O-, -S-, -SO- or -SO 2 - R and R 1 are each, independently, H, a substituted or unsubstituted aliphatic, aromatic, heteroaromatic or aralkyl group R 2 is H or a substituent R 3 is H, or -C(O)R 4 R 4 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.
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公开(公告)号:NO994509L
公开(公告)日:1999-09-17
申请号:NO994509
申请日:1999-09-17
Applicant: BASF AG
Inventor: CALDERWOOD DAVID JOHN , JOHNSTON DAVID NORMAN , RAFFERTY PAUL , TWIGGER HELEN LOUISE , MUNSCHAUER RAINER , ARNOLD LEO
IPC: A61K31/519 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/04 , A61K31/505
Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.
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公开(公告)号:NO994509A
公开(公告)日:1999-09-17
申请号:NO994509
申请日:1999-09-17
Applicant: BASF AG
Inventor: CALDERWOOD DAVID JOHN , JOHNSTON DAVID NORMAN , RAFFERTY PAUL , TWIGGER HELEN LOUISE , MUNSCHAUER RAINER , ARNOLD LEO
IPC: A61K31/519 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/04 , A61K31/505
CPC classification number: C07D487/04
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公开(公告)号:CZ20011563A3
公开(公告)日:2003-02-12
申请号:CZ20011563
申请日:1999-11-04
Applicant: BASF 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 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/10 , A61K31/44 , A61K31/445 , A61K31/4965 , A61K31/505
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.
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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.
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公开(公告)号:NO20012219A
公开(公告)日:2001-06-13
申请号:NO20012219
申请日:2001-05-04
Applicant: BASF AG
Inventor: DOYLE KEVIN J , RAFFERTY PAUL , STEELE ROBERT WILLIAM , WILKINS DAVID J , HOCKLEY MICHAEL , ARNOLD LEE DANIEL , 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
CPC classification number: C07D403/12 , C07D231/54 , C07D401/04 , C07D401/12 , C07D409/04 , C07D417/12 , C07D491/04 , C07D495/04
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公开(公告)号:AU6388900A
公开(公告)日:2001-02-19
申请号:AU6388900
申请日:2000-07-28
Applicant: BASF AG
Inventor: MOSET MARINA M , BERLANGA JOSE MARIA CASTELLANO , FERNANDEZ ISABEL F , CALDERWOOD DAVID J , RAFFERTY PAUL , ARNOLD LEE
IPC: A61K31/4152 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/10 , A61P3/12 , A61P5/14 , A61P5/16 , A61P7/00 , A61P7/10 , A61P9/10 , A61P9/14 , A61P11/00 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P37/08 , A61P43/00 , C07D231/20 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D403/00
Abstract: 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.
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公开(公告)号:CA2380644A1
公开(公告)日:2001-02-08
申请号:CA2380644
申请日:2000-07-28
Applicant: BASF AG
Inventor: CALDERWOOD DAVID J , ARNOLD LEE , RAFFERTY PAUL , FERNANDEZ ISABEL F , MOSET MARINA M , BERLANGA JOSE MARIA CASTELLANO
IPC: A61K31/4152 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/4709 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/10 , A61P3/12 , A61P5/14 , A61P5/16 , A61P7/00 , A61P7/10 , A61P9/10 , A61P9/14 , A61P11/00 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P37/08 , A61P43/00 , C07D231/20 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: Chemical compounds having structural formula (I) and physiologically acceptable salts thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibite d by these chemical compounds, are involved in angiogenic processes. Thus, the se 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.
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公开(公告)号:CA2350235A1
公开(公告)日:2000-05-18
申请号:CA2350235
申请日:1999-11-04
Applicant: BASF AG
Inventor: STEELE ROBERT W , RAFFERTY PAUL , DOYLE KEVIN J , ERICSSON ANNA M , WILKINS DAVID J , ARNOLD LEE D , HOCKLEY MICHAEL
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 , C07D231/00 , C07D307/00 , C07D333/00 , A61P29/00 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/53
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 activit y, of which some are novel compounds, to pharmaceutical compositions containing these pyrazoles and to processes for preparing these pyrazoles.
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公开(公告)号:TR199902301T2
公开(公告)日:1999-12-21
申请号:TR9902301
申请日:1998-03-09
Applicant: BASF AG
Inventor: CALDERWOOD DAVID JOHN , JOHNSTON DAVID NORMAN , RAFFERTY PAUL , TWIGGER HELEN LOUISE , MUNSCHAUER DR RAINER , ARNOLD LEE
IPC: A61K31/519 , A61P35/00 , A61P37/02 , A61P43/00 , C07D487/04
Abstract: Compounds of formula I including pharmaceutically acceptable salts thereof in which R1 represents hydrogen, 2-phenyl-1,3-dioxan-5-yl, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C5-7 cycloalkenyl group or an (optionally substituted phenyl)C1-6 alkyl group wherein the alkyl, cycloalkyl and cycloalkenyl groups are optionally substituted by one or more groups of formula ORA in which RA represents H or a C1-6 alkyl group provided that a group of formula ORA is not located on the carbon attached to nitrogen; R2 represents hydrogen, a C1-6 alkyl group, a C3-8 cycloalkyl group, halo, hydroxy, an (optionally substituted phenyl)C1-6 alkyl group, optionally substituted phenyl or R4; and R3 represents a group of formula (a) in which the phenyl ring is additionally optionally substituted and A represents NH, O, NHSO2, SO2NH, a C1-4 alkylene chain, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p in which p is 0, 1 or 2, or A is absent and R5 is attached directly to the phenyl ring; and R5 represents optionally substituted phenyl and, additionally, when A is absent R5 represents a) a phthalimido group optionally substituted by halo or b) a pyrazolylamino group in which the pyrazole ring is optionally substituted by one or more of the following: hydroxy or optionally substituted phenyl; R4 represents a heterocyclic group; are described which are useful in treating proliferative diseases and disorders of the immune system in mammals. Processes to prepare these compounds and pharmaceutical compositions containing these compound are also described.
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