Patent ID: 8242087
Filing Date: 2012-08-14
Classification: A61P,C07H,C12P

Abstract:
1. A phosphate-modified nucleoside represented by the structural formula (I) wherein B is a pyrimidine or purine base, or an analogue thereof, optionally substituted with one or two substituents independently selected from the group consisting of halogen, hydroxyl, sulfhydryl, methyl, ethyl, amino and methylamino; R R W is O or S; and R wherein n is 0 Z is selected from the group consisting of O, S, NH and NCH each of R R m is 0 or 1; and dotted lines represent the point of attachment of Z to the phosphorous atom of formula (I); or the structural formula (I′): wherein B is a pyrimidine or purine base, or an analogue thereof, optionally substituted with one or two substituents independently selected from the group consisting of halogen, hydroxyl, sulfhydryl, methyl, ethyl, isopropyl, amino, methylamino, ethylamino, trifluoromethyl and cyano; R R W is O; and R wherein dotted lines represent the point of attachment of Z to the phosphorous atom of formula (I′); n is 0, 1 or 2; Z is selected from the group consisting of O, S, NH and NCH Ar is an aryl group; and stereoisomers, enantiomers and pharmaceutically acceptable salts thereof, provided that said phosphate-modified nucleoside is not: N-5′-adenylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, N-5′-uridylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, N-5′-thimidylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, N-5′-adenylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, monoammonium salt, N-5′-guanylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, monoammonium salt, N-5′-uridylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, monoammonium salt, N-5′-thymidylylphosphoramidate L-aspartic acid 1,4-dimethyl ester, monoammonium salt, N-5′-citidylylphosphoramidate L-aspartic acid disodium salt, N-5′-uridylylphosphoramidate L-histidine, N-5′-uridylylphosphoramidate L-histidine 1-methyl ester, N-5′-adenylylphosphoramidate L-histidine 1-methyl ester, N-5′-cytidylylphosphoramidate L-histidine 1-methyl ester, or N-5′-uridylylphosphoramidate L-aspartic acid.