Patent Number: 6,166,209

Title: Piperidine derivatives

Abstract: The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na.sup.+ excretion and arterial blood pressure disorders and metabolic disorders such as obesity.

Inventors: Adam; Geo (Schopfheim, DE), Cesura; Andrea (Basel, CH), Galley; Guido (Rheinfelden, DE), Jenck; Fran.cedilla.ois (Riedisheim, FR), Rover; Stephan (Inzlingen, DE), Wichmann; Jurgen (Steinen, DE)

Assignee: Hoffmann-La Roche Inc.

International Classification: C07D 471/10 (20060101); C07D 491/10 (20060101); C07D 471/00 (20060101); C07D 221/00 (20060101); C07D 221/20 (20060101); C07D 491/00 (20060101); C07D 491/20 (20060101); A61K 031/438 (); A61K 031/40 (); C07D 405/04 ()

Expiration Date: 12/26/2013