Patent ID: 8158642
Filing Date: 2012-04-17
Classification: A61P,C07D

Abstract:
1. A method for treating a disease selected from the group consisting of asthma, inflammatory bowel disease, ulcerative colitis, Crohn's disease, multiple sclerosis, rheumatoid arthritis, graft versus host disease, and organ or graft rejection in a human or animal subject comprising administering to the human or animal subject a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of formula I: wherein: Ar is selected from the group consisting of aryl, heteroaryl, substituted aryl, and substituted heteroaryl; n is an integer from 1 to 4; X is S or O; T is selected from the group consisting of a bond, —O—, —S—, —S(O)—, —S(O) R R or R wherein W is selected from the group consisting of alkylene and substituted alkylene, and wherein one or more of the carbon atoms in the alkylene chain may be replaced by —C(O)—, —C(S)—, —O— or —N(R 10 )— where R 10 is hydrogen, C 1 to C 4 alkyl, or substituted C 1 to C 4 alkyl; R provided that when one of R R R R Y is N or CH; or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof, with the proviso excluding the following compounds as well as their pharmaceutically acceptable salt or ester thereof: N-[2-diethylamino-5-{N-ethyl-N-(trifluoro acetyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(iso-propylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(t-butylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(furan-2-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(piperidin-1-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(N-ethyl-N-iso-propylaminocarbonyl)amino}-pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(thien-3-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(thien-2-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(furan-3-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(3-thiapyrrolidin-1-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}phenylalanine; N-[2-diethylamino-5-{N-ethyl-N-(thien-2-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}-phenylalanine t-butyl ester; N-[2-diethylamino-5-{N-ethyl-N-(trifluoromethylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}-phenylalanine t-butyl ester; N-[2-diethylamino-5-{N-ethyl-N-(t-butylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}-phenylalanine t-butyl ester; and N-[2-diethylamino-5-{N-ethyl-N-(furan-3-ylcarbonyl)amino}pyrimidin-4-yl]-L-4′-{(pyrrolidin-1-yl)carbonyloxy}-phenylalanine t-butyl ester.