首页> 外国专利> 1,3,4,16b-tetrahydro-2H,10H-indolo 2,1-c!pyrazino- 1,2-a! 1, 4!benzodiazepines useful as serotonin-2 receptor antagonists

1,3,4,16b-tetrahydro-2H,10H-indolo 2,1-c!pyrazino- 1,2-a! 1, 4!benzodiazepines useful as serotonin-2 receptor antagonists

机译:1,3,4,16b-四氢-2H,10H-吲哚2,1-c!吡嗪诺-1,2-a! 1,4!苯二氮卓类化合物可用作5-羟色胺2受体拮抗剂

摘要

The invention relates to 1,3,4,16b-tetrahydro-2H,10H-indolo[2,1-c]pyrazino[1,2-a][1,4]benzodiaz epine derivatives of the formula I, IMAGE (I) wherein R1 is hydrogen, lower alkyl, C3-7-alkenyl, C3-7-alkynyl, 3 to 7 ring-membered cycloalkyl, C2-7-alkyl substituted by a substituent selected from hydroxy, amino, N-mono-lower alkyl-amino and N,N-di-lower alkyl-amino; or R1 is lower alkyl substituted by a substituent selected from 3 to 7 ring-membered cycloalkyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl and lower alkanoyl; or R1 is lower alkyl substituted by either phenyl or benzoyl each of said phenyl or benzoyl radicals being unsubstituted or substituted by up to three members selected from lower alkyl, lower alkoxy, lower alkylthio, halogen and trifluoromethyl; R2 and R3 represent hydrogen, lower alkyl, hydroxy, lowr alkoxy, halogen or trifluoromethyl; and R4 represents hydrogen, lower alkyl, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono- or N,N-di-lower alkyl-carbamoyl, or formyl; salts and 2N-oxides; which are useful as serotonin-2 receptor antagonists.
机译:本发明涉及式I的1,3,4,16b-四氢-2H,10H-吲哚并[2,1-c]吡嗪并[1,2-a] [1,4]苯并二氮杂e品肾上腺素衍生物,<图像> (I)其中R 1是氢,低级烷基,C 3-7-烯基,C 3-7-炔基,3至7个环元环烷基,C 2-7-烷基被选自羟基,氨基,N-单-取代基的取代基取代低级烷基氨基和N,N-二低级烷基氨基;或R 1是被选自3至7个环元环烷基,羧基,低级烷氧羰基,氨基甲酰基,N-单-低级烷基氨基甲酰基,N,N-二-低级烷基氨基甲酰基和低级烷酰基的取代基取代的低级烷基;或R1是被苯基或苯甲酰基取代的低级烷基,所述苯基或苯甲酰基中的每一个未被取代或被至多三个选自低级烷基,低级烷氧基,低级烷硫基,卤素和三氟甲基的成员取代; R2和R3代表氢,低级烷基,羟基,低级烷氧基,卤素或三氟甲基; R 4表示氢,低级烷基,羟基-低级烷基,羧基,低级烷氧羰基,氨基甲酰基,N-单或N,N-二低级烷基氨基甲酰基或甲酰基;盐和2N氧化物;可用作5-羟色胺2受体拮抗剂。

著录项

  • 公开/公告号NO166186C

    专利类型

  • 公开/公告日1991-06-12

    原文格式PDF

  • 申请/专利权人 CIBA-GEIGY AG;

    申请/专利号NO19870004111

  • 发明设计人 WASLEY JAN W. F.;

    申请日1987-09-30

  • 分类号C07D487/14;

  • 国家 NO

  • 入库时间 2022-08-22 05:58:03

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