发明名称 Glucopyranosyl derivatives and their uses in medicine
摘要 Disclosed are glucopyranosyl derivatives used as sodium dependent glucose cotransporters (SGLTs) inhibitors, intermediates or preparation processes thereof, and pharmaceutical uses thereof, especially glucopyranosyl derivatives represented by Formula (I), or pharmaceutically acceptable salts or all stereoisomers thereof, pharmaceutical compositions containing these derivatives and their uses for treatment of diabetes and diabetes-related diseases.;
申请公布号 US9394329(B2) 申请公布日期 2016.07.19
申请号 US201414435730 申请日期 2014.09.26
申请人 SUNSHINE LAKE PHARMA CO., LTD. 发明人 Wei Yonggang;Wen Jiaping;Zhu Guozhi;Lu Yonghua;Wang Heran;Wang Yincai;Yuan Mingyun;Gu Zheng;Wu Wuyong;Kang Panpan;Zhang Zongyuan;Chen Gang;Tang Pengcho
分类号 C07H15/00;C07H15/04;C07H9/04;C07H7/04;A61K45/06;A61K31/7034;A61K31/7048 主分类号 C07H15/00
代理机构 Squire Patton Boggs (US) LLP 代理人 Law Kam W.;Squire Patton Boggs (US) LLP
主权项 1. A compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, a racemate, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein each of R1, R2 and R3 is OH; wherein R6 is —OR6a or —OC(═O)R6b; and each of R4 and R5 is independently —H, alkyl, alkylamino, alkynyl, alkenyl, cyano, cycloalkyl or heterocyclyl, and wherein optionally each of the alkyl, alkylamino, alkynyl, alkenyl, cycloalkyl and heterocyclyl is substituted by one or more substituents independently selected from —H, —F, —Cl, —Br, —I, hydroxy, cyano, amino, alkynyl, alkenyl, carboxy, mercapto, alkylamino, —SR13, —C(═O)R13, —C(═O)OR13, —OC(═O)R13, —OC(═O)OR13, —NHC(═O)R13, —C(═O)NHR13, trifluoromethyl, —S(═O)2R13, —S(═O)R13, aryl, heteroaryl, arylalkyl, heteroarylalkyl, arylalkoxy and heteroarylalkoxy, or R4 and R5, together with the carbon atom to which they are attached, form a ring A, wherein the ring A is a saturated or unsaturated, 3- to 8-membered ring, and wherein the ring A optionally contains one or more atoms or atomic groups independently selected from —NH—, —O—, —S—, —C(═O)— and —S(═O)—, and wherein the ring A is optionally substituted by one or more substituents independently selected from —H, —F, —Cl, —Br and —I; or wherein R4 is —H; and R5and R6, together with the carbon atom to which they are attached, form a ring B, wherein the ring B is a saturated or unsaturated, 3- to 8-membered ring, and wherein the ring B optionally contains one or more atoms or atomic groups independently selected from —NH—, —O—, —S—, —C(═O)— and —S(═O)—, and wherein the ring B is optionally substituted by one or more substituents independently selected from —H, —F, —Cl, —Br and —I; wherein R6a is —H, alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl, and wherein optionally each of the alkyl, cycloalkyl, heterocyclyl, aryl, heteroaryl, arylalkyl and heteroarylalkyl is substituted by one or more substituents independently selected from —H, —F, —Cl, —Br, —I, hydroxy, cyano, amino, alkynyl, alkenyl, carboxy, mercapto, trifluoromethyl, —SR14, —C(═O)R14, —C(═O)OR14, —OC(═O)R14, —OC(═O)OR14, —NHC(═O)R14, —S(═O)2R14 and —S(═O)R14; wherein R6b is alkyl, alkoxy, arylalkoxy or heteroarylalkoxy, and wherein optionally each of the alkoxy, arylalkoxy or heteroarylalkoxy is substituted by one or more substituents independently selected from —H, —F, —Cl, —Br, —I, hydroxy, cyano, amino, alkynyl, alkenyl, carboxy and mercapto; wherein R7 is —H, alkyl, alkylamino, alkynyl or alkenyl; wherein R8 is —H, alkylamino, alkynyl or alkenyl; wherein at least one of R4, R5, R7 and R8 is not H; wherein R9 is —H, —F, —Cl, —Br, —I or C1-6 alkyl; wherein R10 is C1-6 alkoxy or C1-6 haloalkoxy; wherein Y is methylene, which is optionally substituted by one or more substituents independently selected from —H, —F, —Cl, —Br and hydroxy; wherein each R11 is independently —H, —F, —Cl, —Br, —I or C1-6 alkoxy; wherein n is 1, 2 or 3; wherein each R12 is independently —H, —F, —Cl or —I; wherein m is 1, 2, 3 or 4; and wherein each R13 and R14 is independently —H, alkyl, aryl, heteroaryl, cycloalkyl or heterocyclyl, and wherein optionally each of the alkyl, aryl, heteroaryl, cycloalkyl and heterocyclyl is substituted by one or more substituents independently selected from —H, —F, —Cl, —Br, —I, hydroxy, amino, cyano, alkyl, alkoxy, alkylamino, hydroxyalkyl, cycloalkoxy, aryloxy, heteroaryloxy, heterocycloalkoxy, trifluoromethyl, carboxy and —C(═O)O-alkyl.
地址 Dongguan, Guangdong CN