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US 4,797,406 AGranted
Amides and esters containing bridged piperidines and use as serotonin M antagonists
AssigneeSandoz Ltd.
InventorsBrian P. Richardson, Gunter Engel, Rudolf K. A. Giger, Andrea Vasella
Life of this patent
Estimating the term…
Abstract
The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
Claims9
A compound of formula A-B-C-D wherein A is a group of formula (a) ##STR17## wherein the free valence is attached to either of the fused rings, Z 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, (C.sub.1-4)alkyl, (C.sub.3-5)alkenyl, unsubstituted phenyl, phenyl mono- or polysubstituted by (C.sub.1-4)alkyl, halogen, hydroxy or (C.sub.1-4)alkoxy, or unsubstituted phenyl (C.sub.1-4)alkyl;
- B is --CO-- or --SO.sub.2 --;
- C is --O-- or --NH--;
- and
- D is a group of formula (f) ##STR18## where R.sub.8 is hydrogen, (C.sub.1-7)alkyl, (C.sub.3-5)alkenyl unsubstituted phenyl(C.sub.1 -4)alkyl/mono- or poly-substituted on the phenyl moiety thereof by (C.sub.1-4)alkyl, halogen, hydroxy or (C.sub.1-4)alkoxy;
- and n=2, 3 or 4 or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof.
4 more elements
Dependencies are inferred from the claim text.