[(Imidazol-4(and 5)-yl)methyl] tetracyclic ketones having 5-HT.sub.3 antagonist activity
US5045545A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 26, 1989 |
| Grant date | Sep 3, 1991 |
| Priority date | — |
| Expiry date | May 26, 2009 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention relates to tetracyclic ketones of the general formula (I) ##STR1## wherein n represents 1, 2 or 3; PA1 Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3 -7cycloalkyl, 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; PA1 Y represents a group --(CH.sub.2)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.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof. The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.