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1. 发明申请

WO2007020190A1 FLUORO SUBSTITUTED 2-OXO AZEPAN DERIVATIVES 审中-公开
标题翻译：氟替代2-OXO AZEPAN衍生物
公开(公告)号：WO2007020190A1
公开(公告)日：2007-02-22
申请号：PCT/EP2006/064935
申请日：2006-08-02
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
发明人： FLOHR, Alexander , GALLEY, Guido , JAKOB-ROETNE, Roland , KITAS, Eric Argirios , WOSTL, Wolfgang
IPC分类号： C07D223/12 , C07D413/12 , C07D401/12 , C07D403/12 , C07D409/14 , A61K31/55 , A61P25/28 , A61P35/00
CPC分类号： C07D409/14 , C07D223/12 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The invention relates to compounds of general formula (I), wherein R 1 is lower alkyl substituted by halogen, or is aryl or heteroaryl, unsubstituted or substituted by halogen; R 2 is heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyloxy, lower alkyl substituted by halogen, O-lower alkyl substituted by halogen or are substituted by C(O)-NR" 2 , (CR 2 )m-C(O)-R’ heteroaryl or S(O) 2 -lower alkyl; R 3 /R 3’ , R 4 /R 4’ and R 5 /R5’ are independently from each other hydrogen or fluoro, wherein at least one of R4/R4’ or R 5 /R 5’ is always fluoro; R' is aryl or hydroxy; R" is hydrogen, cycloalkyl or is heterocycloalkyl; R is hydrogen or lower alkyl; m is 0, 1, 2 or 3; and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. It has been found that the compounds of general formula (I) are γ-secretase inhibitors and the related compounds may be useful in the treatment of Alzheimer's disease or common cancers including but not limited to cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1为被卤素取代的低级烷基，或未取代或被卤素取代的芳基或杂芳基; R 2是未取代的或被一个或多个选自以下的取代基取代的杂环烷基，芳基或杂芳基：卤素，低级烷氧基，被卤素取代的低级烷基，被卤素或被C（O）-NR“2取代，（CR 2）m C（O）-R'杂芳基或S（O） /低级烷基; R 3，R 3，R 3，R 4，R 4，R 4， R 5 / R 5'或R 5'或R 5'中的至少一个独立地为氢或氟，其中R 4 / R 4'或R 5' 总是氟; R'是芳基或羟基; R“是氢，环烷基或杂环烷基; R是氢或低级烷基; m为0,1,2或3; 以及药学上合适的酸加成盐，旋光纯对映异构体，外消旋体或非对映体混合物。已经发现通式（I）的化合物是γ-分泌酶抑制剂，相关化合物可用于治疗阿尔茨海默病或常见癌症，包括但不限于宫颈癌和乳腺癌以及造血系统的恶性肿瘤。

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