发明名称 NOVEL ESTROGEN RECEPTOR LIGANDS
摘要 Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.;
申请公布号 US2014323518(A1) 申请公布日期 2014.10.30
申请号 US201214234916 申请日期 2012.08.02
申请人 KARO BIO AB 发明人 Cheng Aiping;Garg Neeraj;Krüger Lars;Löfstedt Joakim;Koch Eva;Koehler Konrad;Hagberg Lars;Nöteberg Daniel
分类号 C07C251/48;A61K31/381;C07D261/08;A61K31/42;C07D307/54;A61K31/341;A61K31/155;C07D215/14;A61K31/47;C07D217/16;A61K31/472;C07D409/10;A61K31/416;C07D213/58;A61K31/4418;C07D333/24 主分类号 C07C251/48
代理机构 代理人
主权项 1. A compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 is selected from the group consisting of optionally substituted 5-10 membered heterocyclyl, optionally substituted phenyl, optionally substituted naphthyl, optionally substituted C3-8cycloalkyl, optionally substituted C5-6cycloalkenyl, optionally substituted phenylC2-4alkenyl, C2-8alkenyl, haloC2-8alkenyl, dihaloC2-8alkenyl, trihaloC2-8alkenyl, and C3-8cycloalkylC2-4alkenyl, wherein when said heterocyclyl, phenyl or naphthyl group or part of group is substituted, it is substituted with from 1 to 5 substituents, each substituent being independently selected from the group consisting of ORA, N(RB)2, halogen, cyano, nitro, —C(O)C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6 alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl, and when said C3-8cycloalkyl or C5-6cycloalkenyl group is substituted, it is substituted with 1, 2 or 3 substituents selected from C1-5alkyl, C1-5alkenyl, C1-5alkynyl, C1-5alkyl substituted with up to 3 halogen atoms, —CO—C1-5alkyl, and halogen; R2 is selected from the group consisting of —C(NH2)═N—OH, —C(O)N(RC)2, cyano, —CHO, —CH═N—OH, —C(O)NH—OH, —C(CO2H)═N—OH, —C(O—C1-4alkyl)=NH, —C(NH2)═N—NH2, —C(O)—C(O)—NH2, —C(O)CO2H, —CO2H, —CH2—CO2H, —CH(OH)CO2H, —C H2NH—CONH2, C1-6alkyl-NH2, C1-6alkyl-OH, —CH2SO3H, —NH—C(NH2)═NH, —NH—C(O)NH2, —N═C(—NH—CH2CH2—NH—), N(RB)2, N(OH)2, NHSO2RD, —S—CN, —S—C(NH2)═NH, —S—C(NH2)═N—OH, SO2N(RE)2, SO3H, cyanoC1-6alkyl, and optionally substituted 5-10 membered heterocyclyl containing from one to three nitrogen atoms, wherein when said heterocyclyl group is substituted, it is substituted with from 1 to 3 substituents, each substituent being independently selected from the group consisting of ORA, N(RB)2, halogen, cyano, nitro, —C(O)C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6 alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl; R3 is selected from the group consisting of hydrogen, halogen, cyano, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, haloC1-6alkyl, dihaloC1-6alkyl, trihaloC1-6alkyl, optionally substituted phenyl, optionally substituted phenylC1-4alkyl, optionally substituted 5-10 membered heterocyclyl, and optionally substituted 5-10 membered heterocyclylC1-4alkyl, wherein when said phenyl or heterocyclyl group or part of group is substituted, it is substituted with from 1 to 5 substituents, each substituent being independently selected from the group consisting of ORA, N(RB)2, halogen cyano, nitro, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl; R4 is selected from the group consisting of hydrogen, halogen, cyano, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, and haloC1-6alkyl, dihaloC1-6alkyl, and trihaloC1-6alkyl; each of R5, R6, R8 and R9 is independently selected from the group consisting of hydrogen, ORA, N(RB)2, halogen, cyano, nitro, —C(O)C1-4alkyl, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6 alkyl, dihaloC1-6alkyl and trihaloC1-6alkyl; R7 is ORA; or R6 and R7 may, together with the atoms they are attached to, form a 5-, 6- or 7-membered cyclic group optionally containing one to three heteroatoms selected from O, N and S, said 5-, 6- or 7-membered cyclic group being optionally substituted with one of more groups selected from ORA, cyano, nitro, C1-6 alkyl, C2-6alkenyl, C2-6alkynyl, halo C1-6 alkyl, dihalo C1-6 alkyl and trihalo C1-6 alkyl; and each RA, each RB, each RC, each RD and each RE is independently selected from the group consisting of hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-8cycloalkyl and C3-8cycloalkylC1-6alkyl; each optionally substituted by from 1 to 3 halogen atoms.
地址 Huddinge SE