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BENZIMIDAZOLE DERIVATIVES AND THEIR APPLICATION FOR MODULATION OF THE RECEPTOR COMPLEX OF GAMMA-AMINOBUT ACID (GABA)

机译:苯并咪唑衍生物及其在调制γ-氨基乙酸(GABA)受体复合物中的应用

摘要

1. The compound of General formula (I):! ! or its N-oxide, any of its isomers, or any mixture of its isomers,! or a pharmaceutically acceptable salt thereof,! where! Ra, Rb and Rc independently of one another are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, hydroxy, alkoxy, alkoxyalkyl, arylalkyl, formyl, alkylcarbonyl or alkoxyalkylcarbonyl; ! Rd represents a heteroaryl group; ! where the heteroaryl group is optionally substituted with one or more substituents independently selected from the group consisting of:! halo, hydroxy, R′R ″ N—, R′R ″ N-alkyl, cyano, nitro, trifluoromethyl, trifluoromethoxy, hydrazino, alkoxy, cycloalkoxy, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl and alkynyl groups; ! where R ′ and R ″ independently of one another are hydrogen or alkyl. ! 2. The compound according to claim 1, where Ra is hydrogen, alkyl or arylalkyl. ! 3. The compound according to claim 1, where Rb represents hydrogen, alkyl, alkoxy, arylalkyl, formyl or alkylcarbonyl. ! 4. The compound according to claim 1, where Rb represents hydrogen or alkyl. ! 5. The compound according to any one of claims 1 to 4, where Rd is a heteroaryl group selected from thiazolyl, pyridyl, pyrimidyl and pyrazinyl; ! wherein the heteroaryl group is optionally substituted with one or more substituents independently selected from the group consisting of halo, hydrazino and alkoxy. ! 6. The compound according to claim 1, representing! C- [1- (3-Thiazol-2-ylphenyl) -1H-benzimidazol-5-yl] methylamine; ! C- [1- (3-Pyridin-3-ylphenyl) -1H-benzimidazol-5-yl] methylamine; ! C- [1- (3- [6-Fluoropyridin-3-yl] phenyl) -1H-benzimidazol-5-yl] methylamine; ! C- [1- (3- [Pyridin-2-yl] phenyl) -1H-benzimidazol-5-yl] methylamine; ! C- [1- (3-Pyrazin-2-ylphenyl) -1H-benzimidazol-5-yl] me
机译:1.通式(I)的化合物: !或其N-氧化物,其任何异构体或任何异构体混合物!或其药学上可接受的盐!哪里! Ra,Rb和Rc彼此独立地是氢,烷基,环烷基,环烷基烷基,烯基,炔基,羟基,烷氧基,烷氧基烷基,芳基烷基,甲酰基,烷基羰基或烷氧基烷基羰基; ! Rd表示杂芳基。 !其中杂芳基任选地被一个或多个独立地选自以下的取代基取代:卤素,羟基,R'R''N-,R'R''N-烷基,氰基,硝基,三氟甲基,三氟甲氧基,肼基,烷氧基,环烷氧基,烷基,环烷基,环烷基烷基,烯基和炔基; !其中R'和R''彼此独立地是氢或烷基。 ! 2.根据权利要求1的化合物,其中R a为氢,烷基或芳基烷基。 ! 3.根据权利要求1的化合物,其中Rb代表氢,烷基,烷氧基,芳基烷基,甲酰基或烷基羰基。 ! 4.根据权利要求1的化合物,其中Rb代表氢或烷基。 ! 5.根据权利要求1-4中任一项的化合物,其中Rd是选自噻唑基,吡啶基,嘧啶基和吡嗪基的杂芳基; !其中杂芳基任选地被一个或多个独立地选自卤素,肼基和烷氧基的取代基取代。 ! 6.根据权利要求1的化合物,其代表! C- [1-(3-噻唑-2-基苯基)-1H-苯并咪唑-5-基]甲胺; ! C- [1-(3-吡啶-3-基苯基)-1H-苯并咪唑-5-基]甲胺; ! C- [1-(3- [6-氟吡啶啶-3-基]苯基)-1H-苯并咪唑-5-基]甲胺; ! C- [1-(3- [吡啶-2-基]苯基] -1H-苯并咪唑-5-基]甲胺; ! C- [1-(3-吡嗪-2-基苯基)-1H-苯并咪唑-5-基] me

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