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公开(公告)号:PL346700A1
公开(公告)日:2002-02-25
申请号:PL34670099
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.
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公开(公告)号:BG105481A
公开(公告)日:2001-12-31
申请号:BG10548101
申请日:2001-04-27
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 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/53 , A61P29/00
Abstract: The invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion of formula 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. 77 claims
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公开(公告)号:AU8726801A
公开(公告)日:2001-10-08
申请号:AU8726801
申请日:2001-03-20
Applicant: BASF AG
Inventor: BUMP NANCY J , ARNOLD LEE D , DIXON RICHARD W , HOEFFKEN HANS WOLFGANG , ALLEN KAREN , BELLAMACINA CORNELIA
IPC: G01N33/48 , A61K38/00 , A61K45/00 , A61P1/00 , A61P1/04 , A61P1/16 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/12 , A61P15/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61P43/00 , C07K14/71 , C12N9/12 , C12N9/99 , C12N15/09 , G01N33/15 , G01N33/50 , G01N33/68 , C07K14/00
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公开(公告)号:BR9915139A
公开(公告)日:2001-08-07
申请号:BR9915139
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:BR9915132A
公开(公告)日:2001-08-07
申请号:BR9915132
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 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/505 , A61K31/53 , A61P29/00
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:ID29063A
公开(公告)日:2001-07-26
申请号:ID20011000
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:ID29028A
公开(公告)日:2001-07-26
申请号:ID20010652
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 , ARNOLD LEE D
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.
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公开(公告)号:CA2304466A1
公开(公告)日:1999-04-15
申请号:CA2304466
申请日:1998-10-06
Applicant: BASF AG
Inventor: HOCKLEY MICHAEL , ARNOLD LEE D , TURNER ALLYSON , BARLOZZARI TERESA , RAFFERTY PAUL , XU YAJUN
IPC: C07D231/54 , A61K31/415 , A61K31/416 , A61K31/4427 , A61K31/4439 , A61P1/02 , A61P1/04 , A61P9/00 , A61P9/10 , A61P15/00 , A61P17/06 , A61P19/00 , A61P19/02 , A61P27/02 , A61P35/00 , A61P43/00 , C07D401/04 , C07D403/04
Abstract: Chemical compounds that are derivatives of indeno1,2-c!pyrazole are inhibitors of tyrosine kinase activity. Several of the tyrosine kinases, whose activity is inhibited by these chemical compounds, are involved in angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell proliferation is a factor. Compounds of this invention also inhibit the induction of vascular hyperpermeability and the associated formation of edema, ascites, and exudates.
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19.
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.
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公开(公告)号:PL348210A1
公开(公告)日:2002-05-06
申请号:PL34821099
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 , A61K31/415
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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