首页> 外国专利> 1-Aryl-1-hydroxy-1-substituted-3- (4-substituted-1-piperazinyl) -2-propanone and its use in the treatment of bladder disorders of neurological origin.

1-Aryl-1-hydroxy-1-substituted-3- (4-substituted-1-piperazinyl) -2-propanone and its use in the treatment of bladder disorders of neurological origin.

机译:1-芳基-1-羟基-1-取代-3-(4-取代-1-哌嗪基)-2-丙酮及其在治疗神经源性膀胱疾病中的应用。

摘要

Compounds are disclosed having the formula (I): CHEM in which R1 is a C1 to C12 alkyl, said alkyl being straight or branched chain, saturated or unsaturated, monosubstituted or unsubstituted, said substituents being selected from piperidine, pyrrolidine, morpholine, thiomorpholine or cycloalkyl of 3 to 7 carbons, a cycloalkyl of 3 to 9 carbons, a lower alkylcycloalkyl of 4 to 9 carbons, or a polycycloalkyl of 2 to 3 rings containing 7 to 12 carbons; R2 is hydrogen, phenyl, phenyl singly or multiply substituted with halogen, hydroxy, lower alkoxy, methylene dioxy, nitro, lower alkyl or trifluoromethyl, lower alkyl, said alkyl being branched chain or straight, saturated, unsaturated, or cyclic and substituted or unsubstituted, said substituents being selected from thienyl, pyrrolyl, pyridyl, furanyl, hydroxy, lower alkoxy, or acetoxyalkyl wherein the alkyl group has 1 to 3 carbons, phenyl, phenyl substituted with halogen, hydroxy, lower alkoxy, lower alkyl, nitro, methylene dioxy or trifluoromethyl, Ph is phenyl or phenyl para-substituted by halogen, lower alkyl, lower alkoxy or trifluoromethyl; and the pharmaceutically acceptable nontoxic salts thereof. The preparation of the compounds, pharmaceutical compositions containing them and their use in the treatment of neurogenic bladder disorder are also enclosed.
机译:公开了具有式(I)的化合物:其中R 1为C 1 -C 12烷基,所述烷基为直链或支链,饱和或不饱和,单取代或未取代的基团,所述取代基选自哌啶,吡咯烷,吗啉, 3至7个碳的硫代吗啉或环烷基,3至9个碳的环烷基,4至9个碳的低级烷基环烷基,或2至3个含7至12个碳的环的多环烷基; R 2是氢,苯基,被卤素,羟基,低级烷氧基,亚甲基二氧基,硝基,低级烷基或三氟甲基,低级烷基取代的一个或多个苯基,所述烷基为支链或直链,饱和,不饱和或环状的,且被取代或未被取代的,所述取代基选自噻吩基,吡咯基,吡啶基,呋喃基,羟基,低级烷氧基或乙酰氧基烷基,其中烷基具有1-3个碳,苯基,被卤素取代的苯基,羟基,低级烷氧基,低级烷基,硝基,亚甲基二氧基或三氟甲基,Ph是被卤素,低级烷基,低级烷氧基或三氟甲基对位取代的苯基或苯基;及其药学上可接受的无毒盐。还包括了化合物的制备,包含它们的药物组合物及其在治疗神经性膀胱疾病中的用途。

著录项

  • 公开/公告号DE69022058T2

    专利类型

  • 公开/公告日1996-04-25

    原文格式PDF

  • 申请/专利权人 MARION MERRELL DOW INC US;

    申请/专利号DE19906022058T

  • 申请日1990-11-20

  • 分类号C07D295/108;C07D333/20;A61K31/495;C07D307/52;C07D317/58;

  • 国家 DE

  • 入库时间 2022-08-22 03:41:45

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