Dihydropyridine npy antagonists: piperazine derivatives
AssigneeBristol-Myers Squibb Company
InventorsGraham S. Poindexter, Marc Bruce, Graham Johnson, Michael Kozlowski, Karen LeBoulluec, Ivo Monkovic, Ramakrishna Seethala, Charles P. Sloan
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Abstract
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperazine and homopiperazine 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.
Claims10
A compound of Formula (I) or its pharmaceutically acceptable ##STR12## 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 ##STR13## R.sup.5 is selected from hydrogen, halogen, hydroxy, lower alkyl, lower alkenyloxy, and lower alkoxy;
- B is --NH-- or a covalent bond except when R.sup.4 is cyano;
- n is an integer selected from 2 to 5;
- and
- Z is ##STR14## in which m is the integer 2 or 3;
- R.sup.6 is selected from formyl, lower alkyl, phenyl-lower-alkyl, ##STR15## with R.sup.7 and R.sup.8 being independently selected from hydrogen, lower alkyl, C.sub.3-7 cycloalkyl, lower alkoxy, hydroxy, phenoxy, NH.sub.2, NHCOR.sup.1, CO.sub.2 R.sup.1, NO.sub.2, trifluoromethyl, and phenyl.
Dependencies are inferred from the claim text.