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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.
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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:CA2347916A1
公开(公告)日:2000-05-18
申请号:CA2347916
申请日:1999-11-03
Applicant: BASF AG
Inventor: ARNOLD LEE D , BOUSQUET PETER F
IPC: A61K45/00 , A61K31/7105 , A61K38/00 , A61K38/17 , A61K38/19 , A61K39/395 , A61K48/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/10 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/06 , A61P11/16 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/02 , A61P19/00 , A61P27/00 , A61P27/06 , A61P27/12 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07K14/71 , A61K31/415
Abstract: Vascular hyperpermeability and the subsequent events such as macular edema, retinoblastoma, ocular ischemia, ocular inflammatory disease or infection, choroidal melanoma, edematous side-effects induced by iron chelation therapy , pulmonary edema, myocardial infarction, rheumatoid diseases, anaphylaxis, allergies, hypersensitive reactions, cerebral edema, brain tumor fluid-fille d cysts, communicating hydrocephalus, carpal tunnel syndrome, organ damage resulting from a burn, irritation or infection, erythema multiforme, edemato us macules and other disorders, brain tumors, tumor effusions, lung or breast carcinomas, ascites, pleural effusions, pericardial effusions, high altitude "sickness", radioanaphylaxis, radiodermatitis, glaucoma, conjunctivitis, choroidal melanoma, adult respiratory distress syndrome, asthma, bronchitis, ovarian hyperstimulation syndrome, polycystic ovary syndrome, menstrual swelling, menstrual cramps, stroke, head trauma, cerebral infarct or occlusion, hyotension, ulcerations, sprains, fractures, effusions associated with synovitis, diabetic complications, hyperviscosity syndrome, liver cirrhosis, microalbuminuria, proteinuria, oliguria, electrolyte imbalance, nephrotic syndrome, exudates, fibroses, keloid, can be inhibited by the administration of a compound that inhibits the enzyme activity of the VEGF tyrosine kinase receptor known as KDR tyrosine kinase. The preferred compoun d 4,5-dihydro-3-pyridin-4-yl-1(2)H-benzo[g]indazole selectively inhibits the function of KDR tyrosine kinase but do not block the activity of Flt-1 tyrosine kinase which is another VEGE tyrosine kinase receptor.
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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
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公开(公告)号:CA2304565A1
公开(公告)日:1999-04-15
申请号:CA2304565
申请日:1998-10-06
Applicant: BASF AG
Inventor: ARNOLD LEE D , BARLOZZARI TERESA , XU YAJUN
IPC: A61K31/416 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P27/00 , A61P35/00 , A61P43/00 , C07D231/54 , C07D231/56 , C07D401/04 , C07D405/04 , C07D409/04 , A61K31/415 , A61K31/44
Abstract: Chemical compounds that are derivatives of indeno1,2-c!-, naphtho1,2-c!- and benzo6,7!cyclohepta1,2-c!pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in hyperproliferative, angiogenic or in vascular hyperpermeability processes. Thus, these chemical compounds can ameliorate disease states where tumor formation, metastasis, angiogenesis, vascular hyperpermeability or endothelial cell proliferation is a factor.
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公开(公告)号:PL348163A1
公开(公告)日:2002-05-06
申请号:PL34816399
申请日:1999-11-03
Applicant: BASF AG
Inventor: ARNOLD LEE D , BOUSQUET PETER F
IPC: A61K45/00 , A61K31/7105 , A61K38/00 , A61K38/17 , A61K38/19 , A61K39/395 , A61K48/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/10 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/06 , A61P11/16 , A61P13/00 , A61P13/02 , A61P15/00 , A61P17/02 , A61P19/00 , A61P27/00 , A61P27/06 , A61P27/12 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07K14/71
Abstract: Vascular hyperpermeability and the subsequent events such as macular edema, retinoblastoma, ocular ischemia, ocular inflammatory disease or infection, choroidal melanoma, edematous side-effects induced by iron chelation therapy, pulmonary edema, myocardial infarction, rheumatoid diseases, anaphylaxis, allergies, hypersensitive reactions, cerebral edema, brain tumor fluid-filled cysts, communicating hydrocephalus, carpal tunnel syndrome, organ damage resulting from a burn, irritation or infection, erythema multiforme, edematous macules and other disorders, brain tumors, tumor effusions, lung or breast carcinomas, ascites, pleural effusions, pericardial effusions, high altitude "sickness", radioanaphylaxis, radiodermatitis, glaucoma, conjunctivitis, choroidal melanoma, adult respiratory distress syndrome, asthma, bronchitis, ovarian hyperstimulation syndrome, polycystic ovary syndrome, menstrual swelling, menstrual cramps, stroke, head trauma, cerebral infarct or occlusion, hyotension, ulcerations, sprains, fractures, effusions associated with synovitis, diabetic complications, hyperviscosity syndrome, liver cirrhosis, microalbuminuria, proteinuria, oliguria, electrolyte imbalance, nephrotic syndrome, exudates, fibroses, keloid, can be inhibited by the administration of a compound that inhibits the enzyme activity of the VEGF tyrosine kinase receptor known as KDR tyrosine kinase. The preferred compound 4,5-dihydro-3-pyridin-4-yl-1(2)H-benzo[g]indazole selectively inhibits the function of KDR tyrosine kinase but do not block the activity of Flt-1 tyrosine kinase which is another VEGE tyrosine kinase receptor.
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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.
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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
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公开(公告)号:CZ20010959A3
公开(公告)日:2001-12-12
申请号:CZ20010959
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 , A61P35/04
CPC classification number: C07D487/04
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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
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