发明名称 NUCLEAR RECEPTOR BINDING AGENTS
摘要 The present application relates to methods of treating, preventing, delaying the onset of, reducing the incidence of, or reducing the severity of fibrosis, obesity and conditions associated with post-menopausal obesity.
申请公布号 US2017014401(A1) 申请公布日期 2017.01.19
申请号 US201615019923 申请日期 2016.02.09
申请人 GTx, Inc. 发明人 Dalton James T.;Narayanan Ramesh;Yepuru Muralimohan
分类号 A61K31/472;A61K31/4725 主分类号 A61K31/472
代理机构 代理人
主权项 1. A method for treating, delaying onset, reducing the incidence of, or reducing the severity of a fibrosis in a subject, comprising administering a compound, or its optical isomer, pharmaceutically acceptable salt, pharmaceutical product, N-oxide, hydrate or any combination thereof, represented by the structure of Formula XI:Wherein R1, R2, and R3 are each, independently, hydrogen, aldehyde, COOH, —C(═NH)—OH, CHNOH, CH═CHCO2H, CH═CHCO2R, —CH═CH2, hydroxyalkyl, halogen, hydroxyl, alkoxy, cyano, nitro, CF3, NH2, 4-methoxyphenyl, 4-hydroxyphenyl, SH, COR, COOR, OCOR, alkenyl, allyl, 2-methylallyl, alkynyl, propargyl, OSO2CF3, OSO2CH3, NHR, NHCOR, N(R)2, sulfonamide, SO2R, alkyl, cycloalkyl, haloalkyl, aryl, phenyl, benzyl, protected hydroxyl, OCH2CH2NR4R5, Z-Alk-Q, Z-Alk-NR4R5, Z-Alk-heterocycle or OCH2CH2-heterocycle in which the heterocycle is a 3-7 membered saturated or unsaturated, substituted or unsubstituted heterocyclic ring; R is alkyl, cycloalkyl, hydrogen, haloalkyl, dihaloalkyl, trihaloalkyl, CH2F, CHF2, CF3, CF2CF3, aryl, phenyl, benzyl, -Ph-CF3, -Ph-CH2F, -Ph-CHF2, -Ph-CF2CF3, halogen, alkenyl, CN, NO2 or OH; R′ is hydrogen, Alk or COR; R″ is hydrogen, Alk or COR; R4 and R5 are independently hydrogen, phenyl, benzyl, an alkyl group of 1 to 6 carbon atoms, a 3 to 7 member cycloalkyl, heterocycloalkyl, aryl or heteroaryl group; Z is O, NH, CH2 or Q is SO3H, CO2H, CO2R, NO2, tetrazole, SO2NH2 or SO2NHR; h is 0, 1, 2 or 3; i is 0, 1, 2, 3 or 4; n is 1, 2, 3 or 4; m is 1 or 2; p is 0, 1, 2, 3, 4 or 5; and Alk is a linear alkyl of 1-7 carbons, branched alkyl of 1-7 carbons, or cycloalkyl of 3-8 carbons.
地址 Memphis TN US