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Azepin dibenzo derivative compounds and benzoazepin substituted gamma secretase Inhibitors, its Synthesis process and Pharmaceutical compositions containing them

机译:阿齐平二苯并衍生物化合物和苯并ze杂取代的γ分泌酶抑制剂,其合成方法和含有它们的药物组合物

摘要

1 - Compuestos de f rmula general en donde R1 es - (CHR) q-arilo o - (CHR) q-heteroarilo que est n sin sustituir o mono di- o tri-sustituidos por alquilo inferior alcoxilo inferior CF3 o hal geno o es or is - (CH2) n-CR2-CF3, where the two radicals R together with the carbon atom form a cycloalkyl ring; R´ is hydrogen or lower alkyl; n is 1, 2 or 3; m is 0 or 1 ; p is 0, 1, 2, 3, 4, 5 or 6; q is 0, 1, 2 or 3; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, -CH2CF2CF3, CH2CF3, (CH2) 2CF3 , CF3, CHF2, CH2F o is aryl, optionally mono, di or tri-substituted by halogen, or is - (CH2) nNR5R6, where R5 and R6 are independently of each other hydrogen or lower alkyl; R4 is one of the following groups where R7 is hydrogen, lower alkyl, - (CH2) n-CF3 or - (CH2) n-cycloalkyl; R8 is hydrogen, lower alkyl, -C (O) -phenyl,-C (O) -lower alkyl, -C (O) O- (CH2) n-cycloalkyl, -C (O) O- (CH2) n-lower alkyl, -C (O) NH- (CH2) n- lower alkyl or -C (O) NH- (CH2) n-cycloalkyl; R9 is hydrogen, lower alkyl, - (CH2) n-cycloalkyl or - (CH2) n-CF3; and to pharmaceutically acceptable acid addition salts, optically enantiomers cigars, racemates or diastereomeric mixtures thereof.
机译:1-通用制表商R1 es-(CHR)q-arilo o-(CHR)q-heteroarilo que est n sin替代品o单二-o-三替代品por alquilo劣质alcoxilo劣质CF3或hal geno o es或者是-(CH 2)n -CR 2 -CF 3,其中两个基团R与碳原子一起形成环烷基环;或R′是氢或低级烷基; n为1、2或3; m为0或1; p为0、1、2、3、4、5或6; q是0、1、2或3; R 2是氢或低级烷基; R 3是氢,低级烷基,-CH 2 CF 2 CF 3,CH 2 CF 3,(CH 2)2 CF 3,CF 3,CHF 2,CH 2 F o是芳基,可选地被卤素单,二或三取代,或者是-(CH 2)nNR 5 R 6,其中R 5和R 6是彼此独立的氢或低级烷基; R4是下列基团之一,其中R7是氢,低级烷基,-(CH2)n-CF3或-(CH2)n-环烷基; R 8是氢,低级烷基,-C(O)-苯基,-C(O)-低级烷基,-C(O)O-(CH2)正环烷基,-C(O)O-(CH2)n-低级烷基,-C(O)NH-(CH 2)正-低级烷基或-C(O)NH-(CH 2)正环烷基; R9是氢,低级烷基,-(CH2)正环烷基或-(CH2)正CF3;对于药学上可接受的酸加成盐,旋光对映体雪茄,外消旋体或非对映体混合物。

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