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1.发明公开SUBSTANTIALLY PURE 2-{¬2-(2-METHYLAMINO-PYRIMIDIN-4-YL)-1H-INDOLE-5-CARBONYL|-AMINO}-3-(PHENYLPYRIDIN-2-YL-AMINO)-PROPIONIC ACID AS AN IKB KINASE INHIBITOR 审中-公开基本上纯的2 - {[2-（2-甲基氨基吡啶-4-基）-1H-吲哚-5-羰基] - 氨基} -3-（苯基 - 吡啶-2-基氨基）丙酸，为IKB - 激酶抑制剂
公开(公告)号：EP1747215A1
公开(公告)日：2007-01-31
申请号：EP05749733.1
申请日：2005-05-11
IPC分类号： C07D401/14 , A61K31/506 , A61P11/06
CPC分类号： C07D401/14
摘要： The present invention is directed to the substantially pure compound of formula (A), or pharmaceutically acceptable salt, or solvate of said compound; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (A), and a pharmaceutically acceptable carrier; and the use of a compound of formula (A) having activity as an inhibitor, preferably a selective inhibitor, of IkB (IKK), particularly IKK-2, and methods related thereto.
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2.发明公开[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(4-BROMO-3-METHYL-5-PROPOXY-THIOPHEN-2-YL)-METHANONE HYDROCHLORIDE AS AN INHIBITOR OF MAST CELL TRYPTASE 审中-公开[4-（5-氨基-2-氟 - 苯基）哌啶-1-基] - （4-甲氧基-3-甲基-5-丙氧基] -2-甲基） - 甲氧基氯化物ALS抑制剂甲醇腈
公开(公告)号：EP1737848A1
公开(公告)日：2007-01-03
申请号：EP05731154.0
申请日：2005-03-24
发明人： GAO, Zhongli , DAVIS, Larry , LEVELL, Julian , CZEKAJ, Mark , SLEDESKI, Adam, W. , HADDAD, El-Bdaoui
IPC分类号： C07D409/06 , A61K31/4535 , A61P11/06
CPC分类号： C07D409/06
摘要： The present invention extends to the compound of formula I, or a prodrug, pharmaceutically acceptable salt, or solvate of said compound. Furthermore, the present invention is directed to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed to the use of a compound of formula I as an inhibitor of tryptase, comprising introducing the compound into a composition comprising tryptase. In addition, the present invention is directed to the use of a compound of formula I for treating a patient suffering from, or subject to, a physiological condition in need of amelioration of an inhibitor of tryptase comprising administering to the patient a therapeutically effective amount of the compound of Claim 1. The present invention is directed also to the preparation of a compound of formula I.
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