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    • 2. 发明申请
    • HISTONE DEMETHYLASE INHIBITORS AND USES THEREOF FOR TREATMENT O F CANCER
    • HISTONE DEMETHYLASE抑制剂及其用于治疗的用途
    • WO2012071469A2
    • 2012-05-31
    • PCT/US2011061954
    • 2011-11-22
    • NEVADA CANCER INSTSHENZHEN GRADUATE SCHOOL OF PEKING UNIVERSITYZHANG HUIYE TAOQUAN JUNMINWANG JING
    • ZHANG HUIYE TAOQUAN JUNMINWANG JING
    • C07D403/02A61K31/496
    • C07D295/215A61K31/496C07D211/46C07D211/58C07D211/62
    • A compound of formula I: or a pharmaceutically acceptable salt, Ri is an optionally substituted heterocyclic group; R and R' are independently H, CH3, NO2, SO2N(CH3)2, SO2N((CH3)SO2), COOH, COOCH3, CO(N(CH3)), alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, heteroaryl, heterocycloalkyl, alkoxy, alkylcarbonyloxy, arylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, carboxylate, alkylcarbonyl, alkylaminocarbonyl, aralkylaminocarbonyl, alkenylaminocarbonyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkenylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylthiocarbonyl, trifluoromethyl, pentafluoroethyl, halogen, cyano, thio, amido, ether, ester, hydroxyl, hydroxyalkyl, saturated or unsaturated fatty acids, azido, phosphonamido, sulfonamido, lactam, phosphate, phosphonato, phosphinato, amino, acylamino, amidino, imino, guanidino, sulfhydryl, alkylthio, arylthio, thiocarboxylate, sulfates, alkylsulfinyl, sulfonato, sulfamoyl, sulfonamido, nitro, cyano, or azido; m and n are independently integers from 1 to 4; T, U, V, and Z are independently CH, N, or CR; L is NH, CH2, O, S, or SO2; X is N or CH; Y and Y' are independently O or S; and R3 is an optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group.
    • 式I化合物或其药学上可接受的盐,R 1是任选取代的杂环基; R和R'独立地是H,CH 3,NO 2,SO 2 N(CH 3)2,SO 2 N((CH 3)SO 2),COOH,COOCH 3,CO(N(CH 3)),烷基,烯基,炔基,芳基,芳烷基,环烷基, 杂芳基,杂环烷基,烷氧基,烷基羰基氧基,芳基羰基氧基,烷氧基羰基氧基,芳氧基羰基氧基,羧酸酯,烷基羰基,烷基氨基羰基,芳烷基氨基羰基,烯基氨基羰基,烷基羰基,芳基羰基,芳烷基羰基,烯基羰基,烷氧羰基,氨基羰基,烷硫基羰基,三氟甲基,五氟乙基,卤素,氰基, 醚,酯,羟基,羟基烷基,饱和或不饱和脂肪酸,叠氮基,酰基氨基,亚磺酰氨基,内酰胺,磷酸酯,膦酰基,次膦酸酯基,氨基,酰氨基,脒基,亚氨基,胍基,巯基,烷硫基,芳硫基,硫代羧酸酯,硫酸酯,烷基亚磺酰基, 磺酸基,氨磺酰基,亚磺酰氨基,硝基,氰基或叠氮基; m和n独立地为1至4的整数; T,U,V和Z独立地为CH,N或CR; L是NH,CH 2,O,S或SO 2; X为N或CH; Y和Y'独立地为O或S; 并且R 3是任选取代的芳基,杂芳基,环烷基或杂环烷基。