首页> 外国专利> PROPARGYLAMINO INDAN DERIVATIVES AND PROPARGYLAMINOTETRALIN DERIVATIVES AS BRAIN SELECTIVE MAO INHIBITORS

PROPARGYLAMINO INDAN DERIVATIVES AND PROPARGYLAMINOTETRALIN DERIVATIVES AS BRAIN SELECTIVE MAO INHIBITORS

机译:作为脑选择性毛抑制剂的前炔丙基茚满衍生物和炔丙基戊四烯酸衍生物

摘要

The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure:, wherein R1 is OC (O) R9 and R2 is H, wherein R9 i s branched or unbranched C1 to C6 alkyl, aryl, or aralkyl, or R1 is OC (O) R4 and R2 is OC (O) R4, wherein R4 is branched or unbranched C1 to C6 alkyl, aryl, aralkyl or NR5R6, wherein R5 and R6 are each independently H, C1 to C8 alkyl, C6 to C12 aryl, C6 to C12 aralkyl or C6 to C12 cycloalkyl, each optionally substituted; wherein R3 is H or C1 to C6 alkyl; wherein n is 0 or 1; and wherein m is 1 or 2, or a pharmaceutically acceptable salt thereof. Additionally, the subject invention provides methods of treating neurological disorders using these compounds, uses of these compounds for the manufacture of medicaments for treating neurological disorders and processes for synthesis of these compounds.
机译:本发明提供选择性地抑制脑中单胺氧化酶(MAO)的炔丙基氨基茚满(PAI)和炔丙基氨基四氢萘的衍生物,其具有以下结构:其中R1是OC(O)R9和R2是H,其中R9是支链或直链的C 1至C 6烷基,芳基或芳烷基,或R 1为OC(O)R 4且R 2为OC(O)R 4,其中R 4为支链或直链的C 1至C 6烷基,芳基,芳烷基或NR 5 R 6,其中R 5和R 6各自为独立地为H,C 1至C 8烷基,C 6至C 12芳基,C 6至C 12芳烷基或C 6至C 12环烷基,各自任选地被取代;其中R3为H或C1-C6烷基;其中n为0或1;其中m为1或2,或其药学上可接受的盐。另外,本发明提供了使用这些化合物治疗神经系统疾病的方法,这些化合物在制备用于治疗神经系统疾病的药物中的用途以及这些化合物的合成方法。

著录项

  • 公开/公告号IL163341A

    专利类型

  • 公开/公告日2005-11-20

    原文格式PDF

  • 申请/专利权人 TEVA PHARMACEUTICAL INDUSTRIES LTD.;

    申请/专利号IL163341

  • 发明设计人

    申请日2004-08-03

  • 分类号

  • 国家 IL

  • 入库时间 2022-08-21 21:39:19

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