首页> 外国专利> METMETMETMETMETROROROROROROMANMANMANUFACTACTRESRESPECTIMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREYeah. HAS ADOPTED A RELATED 2-MIMETICAL AND/OR RELATED BLOCKING ACTION.

METMETMETMETMETROROROROROROMANMANMANUFACTACTRESRESPECTIMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREYeah. HAS ADOPTED A RELATED 2-MIMETICAL AND/OR RELATED BLOCKING ACTION.

机译:METMETMETMETMETROROROROROROMANMANMANUFACTACTRESRESPECTIMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANMANPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREPREYeah。已采取相关的2隐式和/或相关的阻止操作。

摘要

Novel aminophenylethanolamines of the accompanying formula I, in which R1 denotes a hydrogen, fluorine, chlorine, bromine or iodine atom or a cyano group; R2 denotes a fluorine atom, a straight-chain or branched alkyl group having 1 to 5 carbon atoms, a hydroxyalkyl, aminoalkyl, dialkylaminoalkyl, trifluoromethyl, alkoxy, nitro, cyano, carboxyl, carbalkoxy or carbamoyl group; R3 and R4, which are identical or different, denote hydrogen atoms, straight-chain or branched alkyl groups having 1 to 6 carbon atoms, hydroxyalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aralkyl groups, are prepared by removing the protective groups from corresponding compounds having protected hydroxy and/or protected amino groups. The novel compounds can be obtained in the form of their racemates or their optically active antipodes. The novel compounds have useful pharmacological properties, in particular ss2-mimetic and/or ss1-blocking actions in addition to an analgesic, uterospasmolytic and an antispastic action on the striated musculature, one or the other action being predominant depending on their substitution. The d-(+) compounds in particular have a selective action on the ss1-receptors and the l-(-) compounds have a preferred action on the ss2-receptors. IMAGE
机译:式I的新型氨基苯基乙醇胺,其中R 1表示氢,氟,氯,溴或碘原子或氰基; R 2表示氟原子,具有1至5个碳原子的直链或支链烷基,羟烷基,氨基烷基,二烷基氨基烷基,三氟甲基,烷氧基,硝基,氰基,羧基,氨基甲氧基或氨基甲酰基; R 3和R 4相同或不同,表示氢原子,具有1-6个碳原子的直链或支链烷基,羟烷基,环烷基,环烷基烷基,烯基,炔基或任选取代的芳烷基,其通过除去保护基而制备。相应的化合物具有保护的羟基和/或保护的氨基。可以以其外消旋物或它们的旋光对映体的形式获得新化合物。除了对横纹肌组织的止痛,宫缩和解痉作用外,该新型化合物还具有有用的药理性质,特别是ss2-模拟和/或ss1-阻断作用,取决于它们的取代,一种或另一种作用是主要的。 d-(+)化合物特别对ss1-受体具有选择性作用,而l-(-)化合物对ss2-受体具有优选作用。 <图像>

著录项

  • 公开/公告号NL7316139A

    专利类型

  • 公开/公告日1974-06-20

    原文格式PDF

  • 申请/专利权人

    申请/专利号NL19730016139

  • 发明设计人

    申请日1973-11-26

  • 分类号C07C91/40;C07C93/14;C07C101/68;C07C121/78;C07D13/10;C07D85/26;C07D51/00;C07B19/00;A61K27/00;

  • 国家 NL

  • 入库时间 2022-08-23 06:09:01

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号