Patent ID: 8367688
Filing Date: 2013-02-05
Classification: A61P,C07D

Abstract:
1. A method for inhibiting tumor metastasis wherein the tumor metastasis is selected from the group consisting of metastasis of lymphoma, melanoma and renal cell carcinoma in a human or animal subject comprising administering to the human or animal subject a pharmaceutical composition of comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of one or more of a compound of formula I: wherein: Ar is selected from the group consisting of aryl, heteroaryl, substituted aryl, and substitutedheteroaryl; 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 or 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-(trifluoroacetyl)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-(trifluoromethylcarbony)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.