首页> 外国专利> Indole Derivatives as Steroid 5 Alpha-Reductase Inhibitors as Steroid 5 Alpha-Reductase Inhibitors

Indole Derivatives as Steroid 5 Alpha-Reductase Inhibitors as Steroid 5 Alpha-Reductase Inhibitors

机译:吲哚衍生物作为甾体5α-还原酶抑制剂作为甾体5α-还原酶抑制剂

摘要

The present invention provides compounds of the general formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing such compounds, their use, methods and intermediates used in their preparation.;Wherein X is O, NH, N (COne-C4Alkyl), direct bond, COne-C4Alkylene, C2-C4Alkenylene or C2-C4Alkynylene wherein the alkylene, alkenylene and alkynylene are COne-C4/RTI is optionally substituted by alkyl or aryl; Y is methylene; 0 /RTI 2-C6Alkylene; C2-C6Alkenylene or C2-C6Alkynylene wherein all of these groups are COne-C6Or a group of the general formula (II) wherein m and n are each independently selected from integers of 0 and 1 to 5, wherein the sum of m and n is not more than 5 And p is an integer from 2 to 6; R is H, OH, halo, COne-C4Alkyl or COne-C4Alkoxy; ROne, R2, R3And R4Are each independently H, COne-C4Alkyl, COne-C4Alkoxy, OH, halo,-CF3,-CO2(COne-C4Alkyl),-CONH2,-CONH (COne-C4Alkyl) and-CON (COne-C4Alkyl)2/RTI R5Is-COOH,-COOR7,-CONR8R9Or tetrazol-5-yl; R6Is a group of the above general formula (III) or (IV).
机译:本发明提供了通式(I)的化合物,其药学上可接受的盐以及包含此类化合物的药物组合物,它们的用途,方法以及在其制备中使用的中间体。其中X是O,NH,N(C 一个 -C 4 烷基),直接键,C 一个 -C 4 亚烷基,C 2 -C 4 亚链烯基或C 2 -C 4 亚链烯基,其中亚烷基,亚烯基和亚炔基为C One -C 4 任选地被烷基或芳基取代; Y为亚甲基; 0 2 -C 6 亚烷基; C 2 -C 6 亚烯基或C 2 -C 6 亚炔基,其中所有这些基团均为C 一个 -C 6 或通式(II)的基团,其中m和n各自独立地选自0和1至5的整数,其中m和n的总和不大于5且p为2至6的整数; R为H,OH,卤素,C One -C 4 烷基或C One -C 4 烷氧基; R 1 ,R 2 ,R 3 和R 4 分别独立为H,C One < / Sub> -C 4 烷基,C 1 -C 4 烷氧基,OH,卤素,-CF 3 ,-CO 2 (C 一个 -C 4 烷基),-CONH 2 ,-CONH(C < Sub>一个 -C 4 烷基)和-CON(C 一个 -C 4 烷基) 2 R 5 是-COOH,-COOR 7 ,-CONR 8 R 9 或四唑-5-基; R 6 是上述通式(III)或(IV)的基团。

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