Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT receptor antagonists
US5223511A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 4, 1992 |
| Grant date | Jun 29, 1993 |
| Priority date | — |
| Expiry date | Mar 4, 2012 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/08
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula: ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sub.1 is hydrogen; R.sub.2 is hydrogen, halogen or C.sub.1-6 alkoxy; Y is oxygen or N--R.sub.3 in which R.sub.3 is hydrogen; A is a group selected from: ##STR2## wherein p is 1; r is 0, 2 or 3: R.sub.4 is hydrogen; R.sub.5 is hydrogen, C.sub.1-6 alkyl, or R.sub.5 is a group of the formula --CR.sub.6 =N--R.sub.7 wherein R.sub.6 is hydrogen, C.sub.1-4 alkyl or amino and R.sub.7 is hydrogen or C.sub.1-6 alkyl; or a pharmaceutically acceptable acid addition salt thereof. The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions contained in them are also described.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.