Patent ID: 7304057
Filing Date: 2007-12-04
Classification: A61P,C07D

Abstract:
1. A compound of formula (I): or a pharmaceutically acceptable salt or a hydrate thereof, wherein X is S, SO or SO Y is O or S; Z is CR R R Ar wherein the relative configuration of group —SO 2 R 1 to group —CYZR 2 is a trans-configuration; and wherein said compound is selected from the group consisting of: 2-{[(3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carbonyl]amino}-3-phenyl-propionic acid benzyl ester, 2-{[(3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carbonyl]amino}-3-methyl-butyric acid benzyl ester, 2-{[(3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carbonyl]amino}-4-methyl-pentanoic acid benzyl ester, 2-{[(3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carbonyl]amino}-4-methyl-pentanoic acid ethyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [3-(pyridin-3-yl)]-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [N-methyl-N-(pyridin-2-yl)]-ethyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid phenyipropyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (2-trifluoromethyl)-phenylethyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (N-methyl-N-benzyl)-ethyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (3-phenyl)-allyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (3-cyclohexyl)-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (1,3-diphenyl)-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (1-p-methoxyphenyl-3-phenyl)-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (1-p-fluorophenyl-3-phenyl)-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [3-phenyl-1-(thiophen-2-yl)]-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [3-(6-methyl-pyridin-2-yl)]-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [N-ethyl-N-3-(3-methyl)phenyl]-ethyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (1,3-diphenylmethyloxy)-isopropyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (thiophen-2-yl)-ethyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (3-phenoxy)-propyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [1-phenyl-1-(3-tolyl)]-methyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid [1-methyl-1-(3-trifluoromethylphenyl)]-methyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid 4-nitrobenzyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid 2-methoxybenzyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid (3-ethoxy-2-methoxy)-benzyl ester, (3R)-4-(4-toluenesulfonyl)thiomorpholine-3-carboxylic acid 4-phenylbenzyl ester, and 2-{[(3R)-1,1-dioxo-4-(4-toluenesulfonyl)thiomorpholine-3-carbonyl]amino}-4-methyl-pentanoic acid ethyl ester.