Benzimidazoline-2-oxo-1-carboxylic acid compounds useful as 5-HT

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546126, C07D45112, A61K 3146

Patent

active

052235114

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.

REFERENCES:
patent: 4871744 (1989-10-01), King et al.

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