发明名称 6-Heterocyclic-4-amino-1,3,4,5-tetrahydrobenz [cd]indoles for treating motion sickness and vomiting.
摘要 The use of a compound, or pharmaceutically acceptable salt thereof, of the formula <CHEM> wherein: R<1> is hydrogen, C1-C4 alkyl, C3-C4 alkenyl, cyclopropylmethyl, aryl(C1-C4 alkyl), -(CH2)nS(C1-C4 alkyl), -C(O)R<4>, or -(CH2)nC(O)NR<5>R<6>; R<2> is hydrogen, C1-C4 alkyl, cyclopropylmethyl or C3-C4 alkenyl; R<3> is hydrogen, C1-C4 alkyl or an amino blocking group; n is 1-4; R<4> is hydrogen, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy or phenyl; R<5> and R<6> are independently hydrogen, C1-C4 alkyl, or C5-C8 cycloalkyl with the proviso that when one of R<5> or R<6> 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.
申请公布号 ZA9307153(B) 申请公布日期 1995.03.27
申请号 ZA19930007153 申请日期 1993.09.27
申请人 ELI LILLY AND COMPANY 发明人 RICHARD NOLAN BOOHER;DAVID ERNEST LAWHORN;JOHN MEHNERT SCHAUS;MICHAEL EDWARD FLAUGH;CHARLES JOHNSON PAGET JR
分类号 A61K31/40;A61K31/4025;A61K31/403;A61K31/404;A61K31/41;A61K31/415;A61K31/42;A61K31/422;A61K31/4245;A61K31/425;A61K31/427;A61K31/435;A61K31/44;A61K31/4427;A61K31/443;A61K31/4433;A61K31/4439;A61K31/445;A61K31/495;A61K31/497;A61K31/50;A61K31/505;A61K31/53;A61P1/00;A61P1/04;A61P1/06;A61P1/08;A61P9/02;A61P9/12;A61P13/02;A61P15/00;A61P25/00;A61P25/04;A61P25/20;A61P25/24;A61P25/26;A61P25/28;A61P25/30;A61P43/00;C07D209/00;C07D209/40;C07D401/04;C07D401/10;C07D403/04;C07D403/10;C07D405/04;C07D405/10;C07D409/04;C07D409/10;C07D413/04;C07D413/10;C07D417/04;C07D417/10;C07D419/04 主分类号 A61K31/40
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