发明名称 DIARYLALKYLAMINE REV-ERB ANTAGONISTS AND THEIR USE AS MEDICAMENTS
摘要 The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses as anti-proliferative and pro-apoptotic agents for cancer therapy.;
申请公布号 US2016237057(A1) 申请公布日期 2016.08.18
申请号 US201415027951 申请日期 2014.10.09
申请人 FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA 发明人 Grimaldi Benedetto;Torrente Esther;Scarpelli Rita;Bottegoni Giovanni;Bandiera Tiziano;Veronesi Marina
分类号 C07D333/20;C07D309/14;C07D211/58;C07D295/08;C07D295/16 主分类号 C07D333/20
代理机构 代理人
主权项 1. A compound of Formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein Ar and Ar′ are independently selected from the group consisting of a 5- to 10-membered aromatic and heteroaromatic single or fused rings comprising up to 3 heteroatoms selected from N, O and S; R is selected from the group consisting of hydrogen, a linear or branched unsubstituted or substituted C1-6 alkyl and an unsubstituted or substituted aryl C1-6 alkyl; R1, R2, R3 and R4 are independently selected from the group consisting of H, halogen, linear or branched, unsubstituted or substituted C1-6 alkyl, C1-6alkoxy, hydroxy C1-6 alkyl, OH, CN, fluoro C1-6 alkyl and fluoro C1-6 alkoxy; R1, R2, R3 and R4 can be attached to any position of Ar and Ar′ group, respectively; Y is selected from the group consisting of N and CH; X is selected from the group consisting of CH and N; R5 and R6 are independently selected from the group consisting of H, halogen, unsubstituted or substituted linear or branched C1-6 alkyl, ═O, unsubstituted or substituted aryl, unsubstituted or substituted aryl C1-6 alkyl, hydroxy C1-6 alkyl, C1-6 alkylCO, unsubstituted or substituted arylCO, unsubstituted or substituted aryl C1-6 alkylCO, COOR7, CONR8R9 and SO2R10 wherein R7, R8, R9, and R10 are independently selected from the group consisting of hydrogen and linear or branched C1-6 alkyl; R5 and R6 can be attached to any carbon atom of the ring to which they are connected and they may be connected to the same carbon atom or to different carbon atoms of the ring; and R11 is selected from the group consisting of H, linear or branched C1-6 alkyl, C1-6 alkylCO, aryl and aryl C1-6 alkyl; or R5 and R6, or R5 and R11 or R6 and R11 are linked together to form an unsubstituted or substituted 4- to 10-membered ring, saturated or unsaturated, and containing up to two nitrogen atoms; q and p are, independently, 0 or an integer from 1 to 2 with the proviso that when both Y and X are N, neither q and p are 0; R12 and R13 are independently selected from the group consisting of H, F, C1-6 alkyl, C1-6 alkyl-OH, ═O, OH, COOH, CO2Me, CONH2, CONHMe and CONMe2 and can be attached to any position of the ring to which they are connected and they may be connected to the same carbon atom or to different carbon atoms of the ring; W is selected from the group consisting of a bond and a heteroatom selected from the group consisting of O, S and NR14, wherein R14 is selected from the group consisting of H, linear or branched C1-6 alkyl, C1-6 alkylCO, unsubstituted or substituted aryl, unsubstituted or substituted aryl C1-6 alkyl, unsubstituted or substituted arylCO, SO2R15, CONR16R17 and COOR18, wherein R15, R16, R17 and R18 are independently selected from the group consisting of H and linear or branched C1-6 alkyl; m is an integer from 1 to 3, n is 0 or an integer from 1 to 3 with the proviso that when W is bond, n is not 0;provided that the compound of Formula (I) is not: 4-[[[1-(4-methoxyphenyl)cyclopentyl]amino]methyl]-2-[(4-methyl-1-piperazinyl)methyl]-phenol; 4-[[[1-(2-fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methyl-1-piperazinyl)methyl]-phenol or 4-[[[1-(2-methoxyphenyl)cyclopentyl]amino]methyl]-2-[(4-methyl-1-piperazinyl)methyl]-phenol.
地址 Genova IT