首页> 外国专利> 1-substituted-3- (1-oecyan or carbamoylaa-1,1-diphenylmethyl) piperidine compounds, process for their preparation and the use of the compounds for the manufacture of a medicament for the treatment of diseases associated with altered motility and / or tone of smooth muscle, as well as Similar to the 1-position unsubstituted compounds for use as intermediates in the procedures set

1-substituted-3- (1-oecyan or carbamoylaa-1,1-diphenylmethyl) piperidine compounds, process for their preparation and the use of the compounds for the manufacture of a medicament for the treatment of diseases associated with altered motility and / or tone of smooth muscle, as well as Similar to the 1-position unsubstituted compounds for use as intermediates in the procedures set

机译:1-取代的3-(1-喹啉或氨基甲酰基aa-1,1-二苯基甲基)哌啶化合物,其制备方法以及该化合物在制备用于治疗与运动性和/或改变有关的疾病的药物中的用途平滑肌的音调,以及与1位未取代的化合物相似的中间体

摘要

A compound of the formula:- CHEM or a pharmaceutically acceptable salt thereof, wherein Y is a direct link, -CH2, -(CH2)2-, -CH2O- or -CH2S-; R is -CN or -CONH2; and R1 is a group of the formula:- CHEM where R2 and R3 are each independently H, C1-C4 alkyl, C1-C4 alkoxy, -(CH2)nOH, halo, trifluoromethyl, cyano, -(CH2)nNR4R5, -CO(C1-C4 alkyl), -OCO(C1-C4 alkyl), -CH(OH)(C1-C4 alkyl), -C(OH)(C1-C4 alkyl)2, -SO2NH2, -(CH2)nCONR4R5 or -(CH2)nCOO(C1-C4 alkyl); R4 and R5 are each independently H or C1-C4 alkyl; n is 0, 1 or 2; X and X1 are each independently O or CH2; m is 1, 2 or 3; and "Het" is pyridyl, pyrazinyl or thienyl. The compounds are muscarinic receptor antagonists useful in the treatment of diseases associated with the altered motility and/or tone of smooth muscle, especially irritable bowel syndrome.
机译:式:-的化合物或其药学上可接受的盐,其中Y是直接连接基,-CH 2,-(CH 2)2-,-CH 2 O-或-CH 2 S-; R为-CN或-CONH2; R 1为下式的基团:-CHEM>,其中R 2和R 3各自独立地为H,C1-C4烷基,C1-C4烷氧基,-(CH2)nOH,卤素,三氟甲基,氰基,-(CH 2)nNR 4 R 5,-CO(C 1 -C 4烷基),-OCO(C 1 -C 4烷基),-CH(OH)(C 1 -C 4烷基),-C(OH) )(C 1 -C 4烷基)2,-SO 2 NH 2,-(CH 2)n CONR 4 R 5或-(CH 2)n COO(C 1 -C 4烷基); R 4和R 5各自独立地为H或C 1 -C 4烷基。 n为0、1或2; X和X 1各自独立地为O或CH 2; m为1、2或3; “ Het”是吡啶基,吡嗪基或噻吩基。该化合物是毒蕈碱受体拮抗剂,可用于治疗与平滑肌的运动性和/或音调改变有关的疾病,特别是肠易激综合症。

著录项

  • 公开/公告号DK79991A

    专利类型

  • 公开/公告日1991-06-28

    原文格式PDF

  • 申请/专利权人 PFIZER INC.;

    申请/专利号DK19910000799

  • 申请日1991-04-30

  • 分类号C07D211/34;C07D405/06;

  • 国家 DK

  • 入库时间 2022-08-22 05:58:58

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