首页> 外国专利> 6-ARYL-S-TRIAZOLO(4,3-A)-(OR TETRAZOLO(1,5-A)PYRIDO(2,3-F)-DIAZEPINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

6-ARYL-S-TRIAZOLO(4,3-A)-(OR TETRAZOLO(1,5-A)PYRIDO(2,3-F)-DIAZEPINES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:6-ARYL-S-三唑(4,3-A)-(或四唑(1,5-A)吡咯并(2,3-F)-二氮杂二苯并噻吩,它们的制备和药物组合物

摘要

The present invention provides 6-aryl-s-triazolo- (4,3-a)-pyrido-(2,3-f)-(1,4)-diazepines of the formula I where R1 is a hydrogen atom, a halogen atom, an alkyl group with 1-6 C atoms, a mercapto group, an alkylmercapto group with 1-6 C atoms, an amino group, a monoalkylamino group with 1-6 C atoms or a dialkylamino group with alkyl residues from 1-6 C atoms, which alkyl residues together with the N atom to whiah they are attached may also form a pyrollidine ring, R2 is a hydrogen atom, an alkyl group with 1-6 C atoms, a hydroxy group, an acyloxy group with 2-6 C atoms, or an alkoxy group with 1-6 C atoms, R3 is hydrogen, an alkyl group with 1-6 C atoms, an alkoxy group with 1-6 C atoms or a halogen atom, the grouping A-B-represents the group -N=N-, -CO-NR4, C(SR5)=N-, -C(OR5)=N-, or -CR6=N-, R4 is hydrogen, an alkenyl group with 2 to 6 C atoms, an alkinyl group with 2-6 C atoms, a hydroxyalkyl group with 1-6 C atoms, a ketoalkyl group with 1-6 C atoms, a cyanoalky group with 1-6 C atoms or an alkyl group with 1-6 C atoms which may also contain an alkoxy group with 1-6 C atoms or a dialkylamino group with alkyl residues from 1-6 C atoms, R5 is hydrogen or an alkyl group with 1-6 C atoms, R6 is hydrogen or an alkyl group with 1-6 C atoms or a haloalkyl group with 1-6 C atoms and -Y-Z-stands for the groupings ?C=N-, ?C=N(?O)-, ?CH-NH- or ?CH-N(OH)-, and where R6 is other than an alkyl group when R1 is chlorine, R2 is hydrogen, R3 is hydrogen or a halogen and Y-Z is the grouping ?C=N- its optical isomers and its pharmaceutically acceptable salts. The compounds of formula I are pharmacodynamically active. In particular, they possess anxiolytic, spasmolytic and sedative properties. Some are also antiphlogistic and protect against ulcers.
机译:本发明提供了式I的6-芳基-s-三唑-(4,3-a)-吡啶-(2,3-f)-(1,4)-二氮杂pine,其中R 1是氢原子,卤素原子,具有1-6个碳原子的烷基,巯基,具有1-6个碳原子的烷基巯基,氨基,具有1-6个碳原子的单烷基氨基或具有1-6个烷基残基的二烷基氨基烷基残基与N原子相连的C原子也可能形成吡咯烷环,R2是氢原子,C 1-6的烷基,羟基,2-6的酰氧基C 3为C原子或1-6个C原子的烷氧基,R3为氢,C 1-6原子的烷基,1-6 C原子的烷氧基或卤素原子,基团AB-表示基团- N = N-,-CO-NR4,C(SR5)= N-,-C(OR5)= N-或-CR6 = N-,R4是氢,具有2至6个碳原子的烯基,炔基具有2-6个碳原子的基团,具有1-6个碳原子的羟烷基,具有1-6个碳原子的酮烷基,具有1-6个碳原子的氰基烷基oms或具有1-6 C原子的烷基,也可以包含具有1-6 C原子的烷氧基或具有1-6 C原子的烷基残基的二烷基氨基,R5是氢或具有1-6 C的烷基R 6是氢或具有1-6个碳原子的烷基或具有1-6个碳原子的卤代烷基,并且-YZ代表基团?C = N-、? C = N(?O)-、? CH-NH-或?CH-N(OH)-,并且当R1为氯,R2为氢,R3为氢或卤素且YZ为基团?C = N-时,R6为烷基以外的R6时,异构体及其药学上可接受的盐。式I化合物具有药效学活性。特别是,它们具有抗焦虑,解痉和镇静作用。有些还具有消炎作用,可以预防溃疡。

著录项

  • 公开/公告号IL50816A

    专利类型

  • 公开/公告日1980-09-16

    原文格式PDF

  • 申请/专利权人 DEGUSSA AG;

    申请/专利号IL19760050816

  • 发明设计人

    申请日1976-11-02

  • 分类号C07D471/14;A61K31/55;

  • 国家 IL

  • 入库时间 2022-08-22 18:31:19

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