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发明授权
CN101238106B 氟取代的2-氧代氮杂环庚烷衍生物 失效 - 权利终止

氟取代的2-氧代氮杂环庚烷衍生物
摘要：
本发明涉及通式(I)的化合物及其可药用酸加成盐、旋光纯对映体、外消旋体或其非对映体混合物，其中R1是被卤素取代的低级烷基、或未取代的、或被卤素取代的芳基或杂芳基；R2是杂环烷基、芳基或杂芳基，其是未取代的或被一个或多个选自卤素、低级烷氧基、被卤素取代的低级烷基、被卤素取代的O-低级烷基所取代，或被C(O)-NR”2、(CR2)m-C(O)-R’、杂芳基或S(O)2-低级烷基所取代；R3/R3’、R4/R4’和R5/R5’彼此独立地是氢或氟，其中R4/R4’或R5/R5’中至少一个总是氟；R’是芳基或羟基；R”是氢、环烷基或是杂环烷基；R是氢或低级烷基；m是0、1、2或3。已经发现通式(I)化合物为γ-分泌酶抑制剂，并且相关化合物可用于治疗阿尔茨海默病或包括但不限于宫颈癌和乳腺癌和造血系统恶变的常见癌症。
摘要（英）：

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, (CR2)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 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.

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