6-HETEROCYCLIC-4-AMINO-1`,3,4,5-TETRAHYDROBENZ/CD/INDOLES

摘要

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