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发明授权
CN1794997B 作为γ-分泌酶抑制剂、用于治疗阿尔茨海默病的2,3,4,5-四氢苯并[f][1,4]噁吖庚因-5-甲酸酰胺衍生物 失效 - 权利终止

作为γ-分泌酶抑制剂、用于治疗阿尔茨海默病的2,3,4,5-四氢苯并[f][1,4]噁吖庚因-5-甲酸酰胺衍生物
摘要：
本发明涉及式(I)的苯并噁吖庚因酮衍生物及其药学上适合的酸加成盐，其中R1为氢、低级烷氧基、卤素或-NR′R″；n为1或2；R′、R″彼此独立地为氢或低级烷基；R2为氢、低级烷基、-(CH2)m-环烷基、-(CH2)m-苯基或-(CH2)m-O-低级烷基；m为0、1或2；R3为低级烷基、-(CH2)m-C(O)O-低级烷基、环烷基或-(CH2)m-苯基，其未被取代或被一个或两个取代基取代，所述取代基选自卤素或低级烷基；R4为-(CH2)o-苯基，其未被取代或被一个或两个取代基取代，所述取代基选自卤素、三氟甲基、-NR′R″、硝基或-SO2NH2；或为-环烷基，未被取代或被苯基取代；或为选自如权利要求1中所定义的-(CR′R″)o-杂环基，且o为1或2。这些化合物为良好的用于治疗阿尔茨海默病的γ-分泌酶抑制剂。
摘要（英）：

The invention relates to benzoxazepinone derivatives of formula (I), wherein R<1> is hydrogen, lower alkoxy, halogen or -NR'R''; n is 1 or 2; R',R'' are independently from each other hydrogen or loweralkyl; R<2> is hydrogen, lower alkyl, -(CH2)m-cycloalkyl, -(CH2)m-phenyl or -(CH2)m-O-lower alkyl; m is 0,1or 2; R<3> is lower alkyl, -(CH2)m-C(O)O-lower alkyl, cycloalkyl or -(CH2)m-phenyl, which isunsusbtituted or substituted by one or two substituents, selected from the group consisting of halogen or lower alkyl; R<4> is -(CH2)omicron-phenyl, which is unsusbtituted or substituted by one or two substituents, selected from the group consisting of halogen, trifluoromethyl, -NR'R'', nitro or -SO2NH2, or is - cycloalkyl, unsubstituted or substituted by phenyl, or is - (CR'R'')omicron-heterocyclyl, selected from the group defined in claim 1 and o is 1 or 2; and to pharmaceutically suitable acid addition salts thereof. These compounds are good gamma-secretase inhibitors for the treatment ofAlzheimer's disease.

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