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US 6,444,675 B2Granted
4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists
AssigneeBristol-Myers Squibb Company
InventorSing-Yuen Sit
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Abstract
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I. As antagonists of NPY-induced behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
Claims14
A compound of Formula (I) or its pharmaceutically acceptable acid addition salts or hydrates thereof
- wherein
- R1 and R4 are independently selected from lower alkyl and CO2R5, cyano and
- where R5 is a lower alkyl;
- R2 and R3 are independently selected from hydrogen, cyano and lower alkyl;
- A is lower alkyl or C5-6cycloalkyl;
- X is —NH— or a covalent bond;
- n is an integer selected from 2 to 5;
- in which R6 and R7 are independently selected from lower alkyl and lower alkanol;
- the solid and broken line denote a single or double covalent bond;
- R8 is selected from hydrogen, lower alkyl, —CO2R1, —(CH2)mR10, hydroxy, cyano, —(CH2)nNR11R12, wherein
- m is zero or an integer from 1 to 3;
- R10 is C3-7 cycloalkyl, naphthyl,
- with R13 being lower alkyl, lower alkenyl, C3-7 cycloalkyl, lower alkoxy, hydrogen, halogen, hydroxy, dialkylamino, phenoxy, amino, —NHCOR1, —CO2R1, NO2, trifluoromethyl, phenyl, and R11 and R12 are lower alkyl or are taken together as a C3-5 alkylene chain or an ethyl-oxy-ethyl chain.
10 more elements
Dependencies are inferred from the claim text.