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US 5,326,768 AGranted
3,4-annelated benzimidazol-2-(1H)-one 1-carboxylic acid derivatives
AssigneeDuphar International Research B.V.
InventorsIneke Van Wijngaarden, Derk Hamminga, Wouter Wouters
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Abstract
The present invention concerns 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivatives of the formula ##STR1## wherein R.sub.0, Z, A, B and C are as defined herein. Such derivatives are useful in the treatment of symptoms which are caused by over-excitation of 5-hydroxytryptamine receptors.
Claims6
A 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivative of formula (1):
- ##STR17## wherein R.sub.0 is hydrogen, alkyl, alkoxy or alkylthio having 1-4 carbon atoms, hydroxy, or halogen;
- Z may be ethylene, trimethylene or tetramethylene which may optionally be substituted with 1-3 methyl groups;
- A is a group of the formula (5):
- ##STR18## wherein q is 2 or 3 , and R.sub.6 is alkyl having 1-4 carbon atoms, cycloalkyl having 3-6 C-atoms, cyclopropyl methyl, allyl, proparyl or benzyl, and
- B is an oxygen atom or a group --N(R)--, wherein R is hydrogen, alkyl having 1-6 carbon atoms or benzyl;
- or a pharmaceutically acceptable acid addition salt thereof.
3 more elements
N-(end o-9-methyl-9-azabicyclo[3,3,1]non-3-yl)-5,6-dihydro-4H-imidazo[4,5,1-ij]qui nolin-2(1H)-one 1-carboxamide having the formula:
- ##STR19##
Dependencies are inferred from the claim text.