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    6-Heterocyclyl-4-amino-1,2,2a,3,4,5-hexahydrobenz CD indoles for treating motion sickness and vomiting
    3.
    发明公开
    6-Heterocyclyl-4-amino-1,2,2a,3,4,5-hexahydrobenz CD indoles for treating motion sickness and vomiting 失效
    6-杂环基-4-氨基-1,2,2a，3,4,5-六氢化苯并（CD）吲哚的制备方法，用于在Behandlung von Reisekrankheit und Erbrechen。

    公开(公告)号：EP0590970A1

    公开(公告)日：1994-04-06

    申请号：EP93307745.5

    申请日：1993-09-29

    申请人： ELI LILLY AND COMPANY

    发明人： Booher, Richard Nolan ,  Flaugh, Michael Edward ,  Lawhorn, David Ernest ,  Martinelli, Michael John ,  Paget, Charles Johnson, Jr. ,  Schaus, John Mehnert

    IPC分类号： C07D403/04 ,  A61K31/40

    CPC分类号： C07D401/04 ,  A61K31/40 ,  C07D209/90 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  Y02P20/55

    摘要： The use of a compound, or a pharmaceutically acceptable salt thereof, of the formula

    wherein:
       R¹ is hydrogen, C₁-C₄ alkyl, C₃-C₄ alkenyl, cyclopropylmethyl, aryl (C₁-C₄ alkyl), -(CH₂) n S(C₁-C₄ alkyl), -C(O)R⁴ or -(CH₂) n C(O)NR⁵R⁶;
       R² is hydrogen, C₁-C₄ alkyl, cyclopropylmethyl or C₃-C₄ alkenyl;
       R³ is hydrogen, C₁-C₄ alkyl or an amino blocking group;
       n is 1-4;
       R⁴ is hydrogen, C₁-C₄ alkyl, C₁-C₄ haloalkyl, C₁-C₄ alkoxy or phenyl;
       R⁵ and R⁶ are independently hydrogen, C₁-C₄ alkyl, or C₅-C₈ cycloalkyl with the proviso that when one of R⁵ or R⁶ is a cycloalkyl the other is hydrogen;
       HET is a tetrazolyl ring, a substituted tetrazolyl ring or an aromatic 5- or 6-membered heterocyclic ring, said ring having from one to three heteroatoms which are the same or different and which are selected from the group consisting of sulfur, oxygen, and nitrogen with the proviso that the 6-membered heterocyclic ring can only contain carbon and nitrogen and with the further proviso that the 5-membered ring contains no more than one oxygen or one sulfur but not both oxygen and sulfur; to prepare a medicament for treating emesis or motion sickness; and a compound of the formula above wherein HET is an optionally substituted tetrazolyl ring.

    摘要翻译： 其中：R 1是氢，C 1 -C 4烷基，C 3 -C 4烯基，环丙基甲基，芳基（C 1 -C 4烷基）， - （ CH2）nS（C1-C4烷基），-C（O）R4或 - （CH2）nC（O）NR5R6; R 2是氢，C 1 -C 4烷基，环丙基甲基或C 3 -C 4烯基; R 3是氢，C 1 -C 4烷基或氨基封端基; n为1-4; R 4是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 1 -C 4烷氧基或苯基; R 5和R 6独立地是氢，C 1 -C 4烷基或C 5 -C 8环烷基，条件是当R 5或R 6中的一个是环烷基时，另一个是氢; HET是四唑基环，取代的四唑基环或芳族5-或6-元杂环，所述环具有一至三个相同或不同的杂原子，并且选自硫，氧和 氮，条件是6元杂环只能含有碳和氮，另外条件是5元环含有不超过一个氧或一个硫，但不含氧和硫; 制备用于治疗呕吐或运动病的药物; 和上式的化合物，其中HET是任选取代的四唑基环。