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    • 3. 发明授权
    • Anxiolytic aroyl piperidinyl and piperazinylacyl pyrroles
    • 溶血性芳酰基哌啶基和哌嗪基酰基吡咯
    • US5565456A
    • 1996-10-15
    • US403966
    • 1995-03-15
    • Richard J. CarmosinJohn R. CarsonPhilip Pitis
    • Richard J. CarmosinJohn R. CarsonPhilip Pitis
    • C07D207/32C07D207/335C07D401/06C07D403/12A61K31/445A61K31/505C07D401/14
    • C07D207/335C07D401/06C07D403/12
    • Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5; R1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.
    • 下式的芳酰基(哌啶基和哌嗪基)酰基吡咯具有抗焦虑活性:p由N,CH或COH组成; A1选自 + TR ,n是1至5的整数; R 1选自H和C 1-4烷基; R2和R3选自H和C1-4烷基; R 4选自卤素,C 1-4烷基,羟基,C 1-4烷氧基,硝基,氨基,C 1-4酰氨基,氰基,三卤代C 1-4烷基,C 1-4烷基磺酰基,C 1-4烷基亚磺酰基和C 1-4酰基; R 5选自卤素,C 1-4烷基,羟基,C 1-4烷氧基,硝基,氨基,C 1-4酰氨基,氰基,三卤代C 1-4烷基,C 1-4烷基磺酰基,C 1-4烷基亚磺酰基和C 1-4酰基; 及其酸加成盐。