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公开(公告)号：EP1255752B1
公开(公告)日：2007-08-08
申请号：EP01914376.7
申请日：2001-02-15
发明人： TANG, Peng, Cho , MILLER, Todd , LI, Xiaoyuan , SUN, Li , WEI, Chung, Chen , SHIRAZIAN, Shahrzad , LIANG, Congxin , VOJKOVSKY, Tomas , NEMATALLA, Asaad, S. , HAWLEY, Michael
IPC分类号： C07D403/06 , A61K31/404 , A61P43/00 , C07D403/14 , C07D401/14
CPC分类号： C07D233/56 , C07D207/33 , C07D209/44 , C07D231/12 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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公开(公告)号：EP1644362A2
公开(公告)日：2006-04-12
申请号：EP04754107.3
申请日：2004-06-25
申请人： Sugen, Inc.
发明人： KOENIG, Marcel , CUI, Jingrong , WEI, Chung, Chen , DO, Steven, Huy , ZHANG, Fang-Jie , VOJKOVSKY, Tomas , RAMPHAL, John , YANG, Guang , MATTSON, Matthew , NELSON, Christopher , TANG, Peng Cho
IPC分类号： C07D403/12
CPC分类号： C07D209/40 , C07D209/34 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D471/04
摘要： The present invention relates to compounds of the formulae (I) - (XII), wherein R1 - R71, A, B, X, Y, G, L and Z are defined herein, and their pharmaceutically acceptable salts. These compounds modulate the activity of c-Met and are therefore expected to be useful in the prevention and treatment of c-Met related disorders such as cancer.
摘要翻译： 本发明涉及式（I） - （XII）的化合物及其药学上可接受的盐，其中R 1 -R 71，A，B，X，Y，G，L和Z如本文所定义。 这些化合物调节c-Met的活性，因此预计可用于预防和治疗c-Met相关病症如癌症。
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3.发明授权3-(4-AMIDOPYRROL-2-YLMETHYLIDENE)-2-INDOLINONE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权3-（4-氨基吡咯-2-基）甲基）-2-吲哚啉衍生物ALS蛋白激酶抑制剂
公开(公告)号：EP1370554B1
公开(公告)日：2005-10-19
申请号：EP02714897.2
申请日：2002-02-15
发明人： GUAN, Huiping , LIANG, Congxin , SUN, Li , TANG, Peng, Cho , WEI, Chung, Chen , MAURAGIS, Michael, A. , VOJKOVSKY, Tomas , JIN, Qingwu , HERRINTON, Paul, Matthew
IPC分类号： C07D403/06 , C07D403/14 , C07D471/04 , A61K31/404 , A61K31/4166 , A61K31/437 , A61K31/5377 , A61K31/541 , A61P35/00
CPC分类号： C07D403/06 , C07D403/14 , C07D471/04
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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4.发明公开PHOSPHATE MIMICS AND METHODS OF TREATMENT USING PHOSPHATASE INHIBITORS 有权PHOSPHAT-MIMETIKA SOWIE BEHANDLUNGSMETHODEN UNTER VERWENDUNG VON PHOSPHATASE-INHIBITOREN
公开(公告)号：EP1212296A1
公开(公告)日：2002-06-12
申请号：EP00961360.5
申请日：2000-08-25
申请人： Sugen, Inc.
发明人： HUANG, Ping , WEI, Chung, Chen , TANG, Peng, Cho , LIANG, Chris , RAMPHAL, John , JALLAL, Bahija , BILTZ, John , LI, Sharon , MATTSON, Matthew, Neil , MCMAHON, Gerald , KOENIG, Marcel
IPC分类号： C07C317/14 , C07C311/09 , C07D231/24 , C07D235/16 , C07D235/18 , C07D295/096 , C07D209/42 , A61K31/10 , A61K31/18 , A61K31/415 , A61K31/535 , A61K31/416 , A61K31/404
CPC分类号： C07C311/09 , C07C317/14 , C07C317/22 , C07C317/32 , C07C317/40 , C07C317/44 , C07C317/50 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D231/24 , C07D235/16 , C07D235/18 , C07D295/096
摘要： The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.
摘要翻译： 本发明涉及三氟甲磺酰基和三氟甲磺酰氨基化合物及其生理上可接受的盐及其前药。 预期这些化合物可调节与细胞信号转导相关的蛋白质酪氨酸酶的活性，特别是蛋白酪氨酸磷酸酶，因此预期可用于预防和治疗与异常蛋白酪氨酸酶相关的细胞信号相关的病症 转导，如癌症，糖尿病，免疫调节，神经退行性疾病，骨质疏松症和感染性疾病。 本发明还涉及含有氟甲基磺酰基的化合物作为磷酸酯模拟物的用途。 这些模拟物可用于抑制，调节或调节细胞中磷酸结合蛋白的活性。
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5.发明授权4-SUBSTITUTED 7-AZA-INDOLIN-2-ONES AND THEIR USE AS PROTEIN KINASE INHIBITORS 有权4-取代的7-氮杂二氢吲哚-2-酮和它们作为蛋白激酶抑制剂的
公开(公告)号：EP1244672B1
公开(公告)日：2005-07-20
申请号：EP00990229.7
申请日：2000-12-21
申请人： Sugen, Inc.
发明人： LIANG, Congxin , SUN, Li , WEI, Chung, Chen , TANG, Peng, Cho , MCMAHON, Gerald , HIRTH, Klaus, Peter , CUI, Jingrong
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of formula (1) and pharmaceuitaclly acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of formula (1) and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.
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6.发明公开3-PYRROLYL-PYRIDOPYRAZOLES AND 3-PYRROLYL-INDAZOLES AS NOVEL KINASE INHIBITORS 审中-公开3-吡咯PYRIDOPYRAZOLE和3-吡咯基吲唑的新激酶抑制剂的
公开(公告)号：EP1545515A1
公开(公告)日：2005-06-29
申请号：EP03785178.9
申请日：2003-08-12
申请人： Sugen, Inc.
发明人： WEI, Chung, Chen , HUANG, Ping , XIA, Yi
IPC分类号： A61K31/416 , A61K31/437 , A61K31/5377 , C07D471/04 , C07D403/04 , C07D413/14
CPC分类号： C07D401/14 , A61K31/416 , A61K31/437 , A61K31/5377 , C07D403/04 , C07D471/04
摘要： Compounds of Formula (I) are useful as mediators of protein kinases and have activity as cell proliferation inhibitors where X, R1-R7 and R9 are as defined herein.
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7.发明公开4-HETEROARYL-3-HETEROARYLIDENYL-2-INDOLINONES AND THEIR USE AS PROTEIN KINASE INHIBITORS 审中-公开4 - 杂芳基-3- heteroarylidenyl -2-吲哚满酮和它们作为蛋白激酶抑制剂的用途
公开(公告)号：EP1296975A1
公开(公告)日：2003-04-02
申请号：EP01948830.3
申请日：2001-06-29
申请人： Sugen, Inc.
发明人： TANG, Peng, Cho , WEI, Chung, Chen , HUANG, Ping , CUI, Jingron
IPC分类号： C07D401/14 , C07D409/14 , C07D401/04 , C07D491/04 , C07D471/04 , C07D403/14 , C07D417/14 , A61K31/40
CPC分类号： C07D401/04 , C07D401/14 , C07D403/06 , C07D403/14 , C07D409/14 , C07D417/14 , C07D491/04
摘要： The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-idolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases ('PKs'), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.
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公开(公告)号：EP1255752A2
公开(公告)日：2002-11-13
申请号：EP01914376.7
申请日：2001-02-15
申请人： Sugen, Inc. , PHARMACIA & UPJOHN COMPANY , Miller, Todd , Li, Xiaoyuan , Sun, Li , Wei, Chung Chen , Shirazian, Shahrzad , Liang, Congxin , Vojkovsky, Tomas , Nematalla, Asaad S. , Tang, Peng Cho
发明人： TANG, Peng, Cho , MILLER, Todd , LI, Xiaoyuan , SUN, Li , WEI, Chung, Chen , SHIRAZIAN, Shahrzad , LIANG, Congxin , VOJKOVSKY, Tomas , NEMATALLA, Asaad, S. , HAWLEY, Michael
IPC分类号： C07D403/06 , A61K31/404 , A61P43/00 , C07D403/14 , C07D401/14
CPC分类号： C07D233/56 , C07D207/33 , C07D209/44 , C07D231/12 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14
摘要： The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
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9.发明公开4-SUBSTITUTED 7-AZA-INDOLIN-2-ONES AND THEIR USE AS PROTEIN KINASE INHIBITORS 有权4-取代的7-氮杂二氢吲哚-2-酮和它们作为蛋白激酶抑制剂的
公开(公告)号：EP1244672A1
公开(公告)日：2002-10-02
申请号：EP00990229.7
申请日：2000-12-21
申请人： Sugen, Inc.
发明人： LIANG, Congxin , SUN, Li , WEI, Chung, Chen , TANG, Peng, Cho , MCMAHON, Gerald , HIRTH, Klaus, Peter , CUI, Jingrong
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention relates to 4-substituted 7-aza-indolin-2-ones and their use as protein kinase inhibitors. Particular 4-substituted 7-aza-indolin-2-ones disclosed herein are of formula (1) and pharmaceuitaclly acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, X, Y, and Z are defined herein. The invention further relates to pharmaceutical compositions and dosage forms comprising compounds of formula (1) and to methods of their use for the treatment and/or prevention of diseases such as, but not limited to, cancer.
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10.发明公开GEOMETRICALLY RESTRICTED 3-CYCLOPENTYLIDENE-1,3-DIHYDROINDOL-2-ONES AS POTENT PROTEIN KINASE INHIBITORS 审中-公开几何LIMITED 3-亚环戊基-1,3-二氢 - 吲哚-2-酮作为有效蛋白激酶抑制剂
公开(公告)号：EP1653946A2
公开(公告)日：2006-05-10
申请号：EP04778023.4
申请日：2004-08-05
申请人： Sugen, Inc.
IPC分类号： A61K31/404 , C07D403/04
CPC分类号： C07D209/34 , C07D209/42 , C07D403/06 , C07D403/14 , C07D471/04
摘要： The present invention relates to certain sulfonamido-substituted geometrically restricted indolinones of the formula (I): wherein R1 - R12 and X are variables defined herein. The sulfonamido-substituted geometrically restricted indolinones of the preferred embodiments of the present invention modulate the activity of protein kinases ('PKs'). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
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