Amide derivatives and methods for using the same as selective neuropeptide Y receptor antagonists
First Claim
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1. A compound having the formula:
- or pharmaceutically acceptable salts thereof wherein R1-R5 are each individually selected from the group of substituents including hydrogen, halogen, hydroxyl, thiol lower alkyl, substituted lower alkyl, alkenyl, alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, acyl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, and cyano and wherein the compound is not a compound selected from the group consisting of N-(2,6-Dibromo-4-ethyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2-Amino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2,4-Difluoro-benzyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 5-Chloro-2-{2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzoic acid methyl ester, 5-Amino-2-{2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzamide, N-(2-Amino-4-benzenesulfonyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Diethylamino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-N-(4-phenylamino-phenyl)-acetamide, N-(3-Dimethylamino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2-Amino-4-propylsulfanyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(7-Hydroxy-naphthalen-1-yl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Chloro-3-nitro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Bromo-3-chloro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(7-Butoxy-naphthalen-2-yl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(1H-Indazol-6-yl)-2-[4-(2-oxo-2,3-dihydro-benzoidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Hydroxy-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Ethoxy-naphthalen-1-yl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4Ethoxy-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2-Chloro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1yl]-N-(4-phenylazo-phenyl)-acetamide 4-{2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzamide, N-(4-Acetylamino-phenyl)-2-[4-(2-oxo-2.3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-N-(4-phenoxy-phenyl)-acetamide, N-(4-Dimethylamino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl]-piperidin-1-yl-acetamide, N-(4-Acetyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Nitro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3dihydro-benzoidazol-1-yl)-piperidin-1-yl]-N-(4-trifluoromethyl-phenyl)-acetamide, N-(3-Chloro-4-nitro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Chloro-phenyl)-2-[4-(2-oxo-2,3dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-N-p-tolyl-acetamide, 4-{2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzoic acid methy, ester, N-(4-Methoxy-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoidazol-1-yl)-piperidin-1-yl]-acetamide, and N-(4-Cyclohexyl-phenyl)-2-morpholin-4-yl-acetamide.
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Abstract
Amide derivatives and methods of administering the compositions to mammals to treat disorders such as obesity that are mediated by NPY and especially those mediated by NPY via the Y5 receptor.
59 Citations
8 Claims
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1. A compound having the formula:
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or pharmaceutically acceptable salts thereof wherein R1-R5 are each individually selected from the group of substituents including hydrogen, halogen, hydroxyl, thiol lower alkyl, substituted lower alkyl, alkenyl, alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, acyl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, nitro, and cyano and wherein the compound is not a compound selected from the group consisting of N-(2,6-Dibromo-4-ethyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2-Amino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2,4-Difluoro-benzyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 5-Chloro-2-{2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzoic acid methyl ester, 5-Amino-2-{2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzamide, N-(2-Amino-4-benzenesulfonyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Diethylamino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-N-(4-phenylamino-phenyl)-acetamide, N-(3-Dimethylamino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2-Amino-4-propylsulfanyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(7-Hydroxy-naphthalen-1-yl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Chloro-3-nitro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Bromo-3-chloro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(7-Butoxy-naphthalen-2-yl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(1H-Indazol-6-yl)-2-[4-(2-oxo-2,3-dihydro-benzoidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Hydroxy-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Ethoxy-naphthalen-1-yl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4Ethoxy-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(2-Chloro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1yl]-N-(4-phenylazo-phenyl)-acetamide 4-{2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzamide, N-(4-Acetylamino-phenyl)-2-[4-(2-oxo-2.3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-N-(4-phenoxy-phenyl)-acetamide, N-(4-Dimethylamino-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl]-piperidin-1-yl-acetamide, N-(4-Acetyl-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Nitro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3dihydro-benzoidazol-1-yl)-piperidin-1-yl]-N-(4-trifluoromethyl-phenyl)-acetamide, N-(3-Chloro-4-nitro-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoidazol-1-yl)-piperidin-1-yl]-acetamide, N-(4-Chloro-phenyl)-2-[4-(2-oxo-2,3dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetamide, 2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-N-p-tolyl-acetamide, 4-{2-[4-(2-Oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-acetylamino}-benzoic acid methy, ester, N-(4-Methoxy-phenyl)-2-[4-(2-oxo-2,3-dihydro-benzoidazol-1-yl)-piperidin-1-yl]-acetamide, and N-(4-Cyclohexyl-phenyl)-2-morpholin-4-yl-acetamide. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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Specification