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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.
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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.
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公开(公告)号：CZ20010960A3
公开(公告)日：2001-10-17
申请号：CZ20010960
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
CPC classification number: C07D487/04 , C07F9/6561 , C07F9/65842
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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.
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公开(公告)号：AU1908000A
公开(公告)日：2000-05-29
申请号：AU1908000
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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Patent Agency Ranking
公开(公告)号：CA2344262A1
公开(公告)日：2000-03-30
申请号：CA2344262
申请日：1999-09-17
Applicant: BASF AG
Inventor： CALDERWOOD DAVID , ARNOLD LEE D , DENG BOJUAN B , MAZDIYASNI HORMOZ , HIRST GAVIN , RAFFERTY PAUL , JOHNSTON DAVID N , TOMETZKI GERALD B , MUNSCHAUER RAINER , TWIGGER HELEN L
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：AU9691198A
公开(公告)日：1999-04-27
申请号：AU9691198
申请日：1998-10-06
Applicant: BASF AG
Inventor： ARNOLD LEE D , XU YAJUN , BARLOZZARI TERESA
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 indeno[1,2-c]-, naphtho[1,2-c]- and benzo[6,7]cyclohepta[1,2-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：AU762992B2
公开(公告)日：2003-07-10
申请号：AU1909100
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：AU753555B2
公开(公告)日：2002-10-24
申请号：AU6048499
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：CZ20011564A3
公开(公告)日：2002-04-17
申请号：CZ20011564
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 , A61K31/4439
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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