Ketone derivatives which are antagonists of 5-HT at 5-HT.sub.3 receptors, compositions containing them, and method of use
US4963546A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jan 31, 1989 |
| Grant date | Oct 16, 1990 |
| Priority date | — |
| Expiry date | Jan 31, 2009 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/06
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene chain and R.sup.3 is a hydrogen atom; or PA0 R.sup.1 and R.sup.3 together form a C.sub.2-4 alkylene chain and R.sup.2 is a hydrogen atom; PA0 A-B represents the group R.sup.4 R.sup.5 C--CH.sub.2 or R.sup.4 C.dbd.CH; PA0 R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or a C.sub.1-6 alkyl group; and PA0 Im represents an imidazolyl group of formula: ##STR2## wherein one of the groups represented by R.sup.6, R.sup.7 and R.sup.8 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 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.