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US 5,668,151 AGranted
Dihydropyridine NPY antagonists: piperidine derivatives
AssigneeBristol-Myers Squibb Company
InventorsGraham S. Poindexter, Marc Bruce, Graham Johnson, Karen LeBoulluec, Charles P. Sloan
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Abstract
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperidine and tetrahydropyridine derivatives of 4-phenyl-1,4-dihydropyridines of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Claims15
A compound of Formula I and its pharmaceutically acceptable ##STR20## acid addition salts or hydrates thereof, wherein R.sup.1 is lower alkyl;
- R.sup.2 and R.sup.3 are independently selected from cyano and lower alkyl;
- R.sup.4 is selected from --CO.sub.2 R.sup.1, cyano and ##STR21## R.sup.5 is selected from hydrogen, halogen, hydroxy, lower alkyl, lower alkenyloxy, and lower alkoxy;
- B is --NH--, --NR.sup.1 --, --O-- or a covalent bond except when R.sup.4 is cyano;
- n is an integer selected from 2 to 5;
- and
- Z is ##STR22## R.sup.6 is hydrogen, hydroxy or cyano;
- and R.sup.7 is C.sub.3-7 cycloalkyl, ##STR23## with m being zero or an integer from 1 to 4;
- and R.sup.8 and R.sup.9 being independently selected from hydrogen, lower alkyl, C.sub.3-7 cycloalkyl, lower alkoxy, lower alkenyloxy, lower alkynyloxy, hydroxy, phenyl, phenoxy, NH.sub.2, NHCOR.sup.1, CO.sub.2 R.sup.1, NO.sub.2 and trifluoromethyl.
5 more elements
Dependencies are inferred from the claim text.