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1. 发明授权

EP1255752B1 PYRROLE SUBSTITUTED 2-INDOLINONE PROTEIN KINASE INHIBITORS 有权转让
标题翻译：吡咯取代的吲哚啉-2- ON蛋白激酶抑制剂
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
申请人： Sugen, Inc. , Pharmacia & Upjohn Company LLC
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.

2. 发明授权

EP1301507B1 MANNICH BASE PRODRUGS OF 3 - (PYRROL-2-YLMETHYLIDENE)-2-INDOLINONE DERIVATIVES AND THEIR USE AS MODULATORS OF PROTEIN KINASES 有权
标题翻译：的3-（吡咯-2-基亚甲基）-2-二氢吲哚酮衍生物的曼尼希碱的前体药物以及它们作为蛋白激酶抑制剂的
公开(公告)号：EP1301507B1
公开(公告)日：2006-07-19
申请号：EP01939357.8
申请日：2001-05-24
申请人： Sugen, Inc. , Pharmacia & Upjohn Company LLC
发明人： MOON, Malcolm, Wilson , MOROZOWICH, Walter , GAO, Ping , TANG, Peng, Cho
IPC分类号： C07D403/06 , A61K31/404 , A61P43/00 , C07D403/14
CPC分类号： C07D403/06 , C07D403/14 , C07F9/5728 , C07F9/65583
摘要： The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives of formula (I): that modulate the activity of protein kinases ('PKs'). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.

3. 发明授权

EP1370554B1 3-(4-AMIDOPYRROL-2-YLMETHYLIDENE)-2-INDOLINONE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
标题翻译： 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
申请人： Pharmacia & Upjohn Company LLC , Sugen, Inc.
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.

4. 发明公开

EP1218342A2 MONO- AND BIS-INDOLYLQUINONES AND PROPHYLACTIC AND THERAPEUTIC USES THEREOF 审中-公开
标题翻译：单和双indolylquinone衍生物及其癌症和糖尿病的治疗
公开(公告)号：EP1218342A2
公开(公告)日：2002-07-03
申请号：EP00965395.7
申请日：2000-09-25
申请人： Sugen, Inc.
发明人： TANG, Peng, Cho , MCMAHON, Gerald , HARRIS, G. Davis, Jr. , LIPSON, Ken
IPC分类号： C07D209/12 , C07D209/42 , A61K31/404 , A61P3/10 , A61P35/00
CPC分类号： A61K31/404 , A61K31/4045 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/42
摘要： The present invention relates to a class of indolylquinone compounds that inhibit GRB-2 adaptor protein function, pharmaceutical compositions comprising these compounds, and methods for ameliorating the symptoms of cell proliferative disorders associated with GRB-2 adaptor protein function using these compounds. The present invention further relates to methods for treating insulin-related disorders, such as diabetes, insulin resistance, insulin deficiency and insulin allergy, and for ameliorating the symptoms of insulin-related disorders, using certain indolylquinone compounds and pharmaceutical compositions thereof. The present invention also relates to novel synthetic methods for the preparation of mono- and bis-indolylquinone compounds.

5. 发明公开

EP1139754A1 3-HETEROARYLIDENYL-2-INDOLINONE COMPOUNDS FOR MODULATING PROTEIN KINASE ACTIVITY AND FOR USE IN CANCER CHEMOTHERAPY 审中-公开
标题翻译： 3- HETEROARYLALKYLIDENYL -2-吲哚满酮进行调制的蛋白激酶活性和FOR USE IN癌症化疗
公开(公告)号：EP1139754A1
公开(公告)日：2001-10-10
申请号：EP99966725.6
申请日：1999-12-30
申请人： Sugen, Inc.
发明人： LANGECKER, Peter, J. , SHAWVER, Laura, Kay , TANG, Peng, Cho , SUN, Li
IPC分类号： A01N43/38 , A61K31/40
CPC分类号： A61K31/404 , A61K31/505 , A61K2300/00
摘要： The present invention relates to 3-heteroarylidenyl-2-indolinone compounds that modulate the enzymatic 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. Furthermore, these compounds are expected to enhance the efficacy of other chemotherapeutic agents, in particular, fluorinated pyrimidines, in the treatment of cancer.

6. 发明公开

EP0954315A2 USE OF QUINAZOLINE DERIVATIVES FOR THE MANUFACTURE OF A MEDICAMENT IN THE TREATMENT OF HYPERPROLIFERATIVE SKIN DISORDERS 失效
标题翻译： QUINAZOLINDERIVATE用于生产药物来治疗疾病增殖性皮肤使用
公开(公告)号：EP0954315A2
公开(公告)日：1999-11-10
申请号：EP97941542.0
申请日：1997-09-11
申请人： Sugen, Inc.
发明人： McMAHON, Gerald , SHAWVER, Laura, Kay , NAROG, Blair , TANG, Peng, Cho , HIRTH, Klaus, Peter
IPC分类号： A61K9 , A61K31 , A61K47 , C07D239
CPC分类号： A61K9/0014 , A61K31/517 , A61K47/06 , A61K47/10 , A61K47/12 , A61K47/14 , C07D239/94
摘要： This invention is directed to methods and compositions for treating hyperproliferative skin disorders utilizing a quinazoline derivative as an active ingredient.

7. 发明公开

EP0832073A1 QUINAZOLINES AND PHARMACEUTICAL COMPOSITIONS 失效
标题翻译：喹唑啉和FARMAZEUTISCHE组合物
公开(公告)号：EP0832073A1
公开(公告)日：1998-04-01
申请号：EP96917174.0
申请日：1996-06-04
申请人： Sugen, Inc.
发明人： TANG, Peng, Cho , McMAHON, Gerald
IPC分类号： A61K31 , A61P35 , A61P43 , C07D239
CPC分类号： C07D239/74
摘要： The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities. The present invention also provides pharmaceutical compositions and methods for inhibiting cell proliferation of differentiation and related disorders. Examples of such disorders include cancers, blood vessel proliferative disorders, psoriasis, hyperimmune response and fibrotic disorders. Example ofother disorders include the HER2 disorders, EGF disorders, IGFR disorders, PDGFR disorders, met disorders, SrC disorders, and KDR/FLK-1 disorders described herein. It is to be understood that compounds which are effective for diseases related to one TK will also likely be effective for diseases related to other TK's, especially those from the same family. Thus, for example, compounds shown to have good effect against Her2 are likely to also have good effect against other members of the Her family, i.e., EGFR, Her3,and Her4.

8. 发明公开

EP1212296A1 PHOSPHATE MIMICS AND METHODS OF TREATMENT USING PHOSPHATASE INHIBITORS 有权
标题翻译： 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。

9. 发明公开

EP1082305A1 PYRROLE SUBSTITUTED 2-INDOLINONE PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：吡咯取代的2-吲哚酮蛋白激酶抑制剂
公开(公告)号：EP1082305A1
公开(公告)日：2001-03-14
申请号：EP99927120.8
申请日：1999-05-28
申请人： Sugen, Inc.
发明人： TANG, Peng, Cho , SUN, Li , McMAHON, Gerald
IPC分类号： C07D209/04 , C07D413/06 , A61K31/40 , A61K31/535
CPC分类号： C07D403/06 , C07D209/34
摘要： The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof 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.
摘要翻译：本发明涉及新的吡咯取代的2-吲哚满酮化合物及其生理上可接受的盐和前药，它们调节蛋白激酶的活性，因此预计可用于预防和治疗与蛋白激酶有关的细胞紊乱如癌症。

10. 发明公开

EP1012150A1 HETEROARYLCARBOXAMIDE COMPOUNDS ACTIVE AGAINST PROTEIN TYROSINE KINASE RELATED DISORDERS 失效
标题翻译： Heteroarylcarboxamide化合物对由蛋白酪氨酸激酶引起的疾病是有效的
公开(公告)号：EP1012150A1
公开(公告)日：2000-06-28
申请号：EP98924794.5
申请日：1998-05-18
申请人： Sugen, Inc.
发明人： McMAHON, Gerald , TANG, Peng, Cho , SHAWVER, Laura, Kay , HIRTH, Klaus, Peter
IPC分类号： C07D413/02 , C07D231/12 , C07D261/18 , C07D261/08
CPC分类号： C07D277/32 , C07D261/18 , C07D401/12 , C07D413/12
摘要： The present invention relates to novel heteroarylcarboxamides which modulate the activity of protein tyrosine kinases and are expected to be useful in the treatment of abnormal protein tyrosine kinase activity driven disorders, to methods for the treatment of inappropriate FGFR activity related disorders with the heteroarylcarboxamide, N-(4-trifluoromethyl-phenyl)-5-methylisoxazole-4-carboxamide, and to the treatment of solid tumor cancers, especially glioblastoma and astrocytoma, with a combination of a nitrosourea, preferably BCNU (carmustin) and N-(4-trifluoromethyl-phenyl)-5-methylisoxazole-4-carboxamide.

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