5,6-dihydro-N-[(imidazol-4(or 5)-yl)methyl]-4H-pyrrolo[3,2,1-IJ]

Details 5,6-dihydro-N-[(imidazol-4(or 5)-yl)methyl]-4H-pyrrolo[3,2,1-IJ] 5,6-dihydro-N-[(imidazol-4(or 5)-yl)methyl]-4H-pyrrolo[3,2,1-IJ]

1990-06-13

1992-05-19

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546 94, C07D45114, A61K 3144

Patent

active

051149508

ABSTRACT:
The invention provides amide derivatives of the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, where m represents 2, 3 or 4 or a group --X(CH.sub.2).sub.p, where p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.5, where R.sup.5 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof.
The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.

REFERENCES:
patent: 4015005 (1977-03-01), Goetz
patent: 4151282 (1979-04-01), Welstead et al.
patent: 4567177 (1986-01-01), Bigg et al.
patent: 4619941 (1986-10-01), Wright et al.
patent: 4808581 (1989-02-01), Oxford et al.
patent: 4963546 (1990-10-01), North et al.

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