Substituted 3,4-annelated benzimidazol-2(1H)-ones
AssigneeDuphar International Research B.V.
InventorsIneke Van Wijngaarden, Derk Hamminga, Wouter Wouters
Life of this patent
Estimating the term…
Loading patent…
AssigneeDuphar International Research B.V.
InventorsIneke Van Wijngaarden, Derk Hamminga, Wouter Wouters
Estimating the term…
The present invention is concerned with compounds of formula 1 ##STR1## wherein R.sub.0 is alkyl, alkoxy or alkylthio having 1-4 carbon atoms, hydroxy, halogen, Z, together with the carbon atom and the nitrogen atom and the intermediate carbon atom, constitutes a heterocyclic group which consists of 5-8 ring atoms, in which, besides the already present nitrogen atom, a second hetero atom from the group N, O, or S may be present, which ring may be substituted with 1-4 methyl group, or which ring may be annelated with a phenyl group optionally substituted with fluorine, or a methyl or methoxy group; A is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.3, R.sub.4 and R.sub.5 is hydrogen, alkyl having 1-6 carbon atoms, cycloalkyl having 3-7 carbon atoms, alkenyl having 2-6 carbon atoms or phenyl alkyl having 1-3 carbon atoms in the alkyl group, and the two other groups independently of each other are hydrogen or alkyl having 1-4 carbon atoms, or wherein A is a polycyclic ring system in which one carbon atom is replaced by a tertiary nitrogen atom, for example, a ring system of formula 4, 5 or 6, ##STR3## wherein p is an integer having the value 1 or 2, q is an integer having the value 2, 3 or 4, r is an integer having the value 1, 2 or 3, and R.sub.6 is alkyl having 1-4 carbon atoms, cycloalkyl having 3-6 carbon atoms, cyclopropylmethyl, allyl, propargyl or benzyl, and B is an oxygen atom or a group .dbd.N--R, wherein R is hydrogen, alkyl having 1-6 carbon atoms or benzyl, or wherein B-A represents a group of formula 7 ##STR4## wherein R.sub.3 and R.sub.5 having the meanings defined above, and the pharmaceutically acceptable acid addition salts thereof, which are pharmaceutically active as 5-HT receptor antagonists, and pharmaceutical products containing these compounds.
A 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivative of formula (1):
Dependencies are inferred from the claim text.