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公开(公告)号：EP1448523B1
公开(公告)日：2007-08-22
申请号：EP02787747.1
申请日：2002-11-20
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BACH, Andrew, Thomas , KAPA, Prasad, Koteswara , LEE, George, Tien-San , LOESER, Eric, M. , SABIO, Michael, Lloyd , STANTON, James, Lawrence , VEDANANDA, Thalaththani, Ralalage
IPC分类号： C07D209/12 , C07D413/12 , C07D205/04 , C07D405/12 , C07D207/48 , C07D403/12 , C07D401/12 , C07D417/12 , A61K31/40 , A61K31/395 , A61P3/04 , A61P3/06 , A61P3/10 , A61P25/28 , A61P11/00 , A61P1/04
CPC分类号： C07D205/04 , C07D207/16 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula (I) provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARa and PPARy receptors.
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公开(公告)号：EP1635835B1
公开(公告)日：2010-01-06
申请号：EP04739809.4
申请日：2004-06-11
申请人： Novartis AG , Novartis Pharma GmbH
IPC分类号： A61K31/505 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , A61K31/506 , A61P35/00
CPC分类号： C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04
摘要： This application discloses compounds that inhibit Raf kinase having the formula (I), wherein R1 is a phenyl radical or a heteroaryl radical; and R2 is a phenyl radical; or an N-oxide or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of proliferative diseases, such as cancer.
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公开(公告)号：EP1635835A1
公开(公告)日：2006-03-22
申请号：EP04739809.4
申请日：2004-06-11
申请人： Novartis AG , Novartis Pharma GmbH
IPC分类号： A61K31/505 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , A61K31/506 , A61P35/00
CPC分类号： C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04
摘要： This application discloses compounds that inhibit Raf kinase having the formula (I), wherein R1 is a phenyl radical or a heteroaryl radical; and R2 is a phenyl radical; or an N-oxide or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of proliferative diseases, such as cancer.
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公开(公告)号：EP1448523A1
公开(公告)日：2004-08-25
申请号：EP02787747.1
申请日：2002-11-20
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BACH, Andrew, Thomas , KAPA, Prasad, Koteswara , LEE, George, Tien-San , LOESER, Eric, M. , SABIO, Michael, Lloyd , STANTON, James, Lawrence , VEDANANDA, Thalaththani, Ralalage
IPC分类号： C07D209/12 , C07D413/12 , C07D205/04 , C07D405/12 , C07D207/48 , C07D403/12 , C07D401/12 , C07D417/12 , A61K31/40 , A61K31/395 , A61P3/04 , A61P3/06 , A61P3/10 , A61P25/28 , A61P11/00 , A61P1/04
CPC分类号： C07D205/04 , C07D207/16 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the formula (I) provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPARa and PPARy receptors.
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5.发明公开
公开(公告)号：EP1345957A2
公开(公告)日：2003-09-24
申请号：EP01985424.9
申请日：2001-12-19
申请人： Novartis AG , Novartis Pharma GmbH
发明人： BAIR, Kenneth, Walter , CHEN, Ying-Nan, Pan , RAMSEY, Timothy, Michael , SABIO, Michael, Lloyd , SHARMA, Sushil, Kumar
摘要： The novel compounds of this invention have the general structural formula la-d: The compounds of this invention relate to 8-mer, 7-mer, 6-mer and 5-mer peptides having the following amino acid sequences, and referred to collectively as having 'formula la-d': or a pharmaceutically acceptable salt or ester thereof, that inhibit the interaction of the transcription factor E2F-1 to Cyclin A. As an antagonist of the E2F-1/Cyclin A interaction, the compounds of the present invention may be used in the treatment of cancer.
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6.发明公开1,4-DISUBSTITUTED ISOQUINOLINE DERIVATIVES AS RAF-KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES 审中-公开1,4-二取代的异喹啉AS Raf激酶抑制剂，其增殖性疾病治疗是合适的
公开(公告)号：EP1667980A1
公开(公告)日：2006-06-14
申请号：EP04765544.4
申请日：2004-09-23
申请人： Novartis AG , Novartis Pharma GmbH
发明人： FINK, Cynthia, Anne , PEREZ, Lawrence, Blas , RAMSEY, Timothy, Michael , YUSUFF, Naeem , VERSACE, Richard, William , BATT, David, Bryant , SABIO, Michael, Lloyd , KIM, Sunkyu
IPC分类号： C07D217/22 , C07D401/04 , C07D405/04 , C07D405/14 , C07D401/14 , C07D413/14 , C07D409/14 , C07D413/04 , C07D413/10 , C07D417/14 , A61K31/4725 , A61P35/00
CPC分类号： C07D401/04 , C07D217/22 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/10 , C07D413/14 , C07D417/14 , C07D491/10 , C07D491/113
摘要： This invention relates to compounds of formula (I) wherein the variable substituents are described herein. The compounds are useful for the treatment of conditions and diseases characterized by an aberrant MAP kinase signaling pathway, such as cancer.
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7.发明公开CERTAIN SUBSTITUTED POLYKETIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE IN TREATING TUMORS 审中-公开某些取代聚酮化合物含药物组合物及其用于肿瘤的治疗
公开(公告)号：EP1417195A1
公开(公告)日：2004-05-12
申请号：EP02794555.9
申请日：2002-08-05
申请人： Novartis AG , Novartis Pharma GmbH
发明人： KINDER, Frederick, Ray, Jr. , BAIR, Kenneth, Walter , RAMSEY, Timothy, Michael , SABIO, Michael, Lloyd
IPC分类号： C07D309/30 , C07C271/12
CPC分类号： C07D309/30
摘要： The present invention relates to certain substituted polyketides of formula (I), wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.
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8.发明公开USE OF ISOQUINOLINE DERIVATIVES FOR TREATING CANCER AND MAP KINASE RELATED DISEASES 有权异喹啉衍生物对癌症的治疗和疾病相关的地图激酶USE
公开(公告)号：EP1603566A1
公开(公告)日：2005-12-14
申请号：EP04718960.0
申请日：2004-03-10
申请人： Novartis AG
发明人： BATT, David, Bryant , BOLD, Guido , KIM, Sunkyu , RAMSEY, Timothy, Michael , SABIO, Michael, Lloyd
IPC分类号： A61K31/4725 , A61K31/472 , A61P35/00
CPC分类号： A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/4725
摘要： This invention relates to the treatment of a disease that is characterized by an aberrant MAP kinase signaling pathway by administering a compound of the formula (I) wherein the variable substituents are defined herein, to a patient in need of such treatment. The inventive method is especially useful for the treatment of cancers that have a mutated RAF kinase, especially melanoma.
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9.发明授权USE OF ISOQUINOLINE DERIVATIVES FOR TREATING CANCER AND MAP KINASE RELATED DISEASES 有权异喹啉衍生物对癌症的治疗和疾病相关的地图激酶USE
公开(公告)号：EP1603566B1
公开(公告)日：2009-01-21
申请号：EP04718960.0
申请日：2004-03-10
申请人： NOVARTIS AG
发明人： BATT, David, Bryant , BOLD, Guido , KIM, Sunkyu , RAMSEY, Timothy, Michael , SABIO, Michael, Lloyd
IPC分类号： A61K31/4725 , A61P35/00
CPC分类号： A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/4725
摘要： This invention relates to the treatment of a disease that is characterized by an aberrant MAP kinase signaling pathway by administering a compound of the formula (I) wherein the variable substituents are defined herein, to a patient in need of such treatment. The inventive method is especially useful for the treatment of cancers that have a mutated RAF kinase, especially melanoma.
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