Heterocyclic carboxylic acid amides and esters
OwnerPeter Donatsch, Gunter Engel +6inventors
InventorsPeter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Hildegard R. Stadler, Brigitte M. Stadler, Sigrid A. Stadler, Gerald Breuleux
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Abstract
The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
Claims34
A compound of formula I:
- A--CO--B--D I
- wherein
- A is a group of formula II ##STR7## wherein the free valence is attached to the fused ring X;
- X is --CH.sub.2 --, --NR.sub.3 --, --O-- or --S--;
- R.sub.1 and R.sub.2, independently, are hydrogen, halogen, (C
- .sub.1-4)alkyl, (C.sub.1-4)alkoxy, hydroxy, amino, (C.sub.1-4)alkylamino, di-(C.sub.1-4)alkylamino, mercapto or (C.sub.1-4)alkylthio;
- R.sub.3 is hydrogen or (C.sub.1-4)alkyl;
- B is --O-- or --NH--;
- and
- D is a group of formula IV ##STR8## wherein n is 2, 3, or 4, and
- R.sub.8 is hydrogen, (C.sub.1-7)alkyl, (C.sub.3-5)alkenyl or unsubstituted phenyl (C.sub.1-4)alkyl;
- or D is a group of formula V ##STR9## or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
A compound according to claim 1 of formula I wherein A, X, R.sub.1, R.sub.2, R.sub.3, B, D, n and R.sub.8 are as defined in claim 13, or a pharmaceutically acceptable acid addition salt thereof.
A compound according to claim 3 of formula I wherein R.sub.1, R.sub.2 and R.sub.8 are as defined in claim 15, or a pharmaceutically acceptable acid addition salt thereof.
Dependencies are inferred from the claim text.