发明名称 Tetrazolones as inhibitors of fatty acid synthase
摘要 Provided herein are tetrazolone FASN inhibitors of the formula (I):; or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. ;Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
申请公布号 US9346769(B2) 申请公布日期 2016.05.24
申请号 US201313975236 申请日期 2013.08.23
申请人 Infinity Pharmaceuticals, Inc. 发明人 Bahadoor Adilah;Castro Alfredo C.;Chan Lawrence K.;Keaney Gregg F.;Nevalainen Marta;Nevalainen Vesa;Peluso Stephane;Snyder Daniel A.;Tibbitts Thomas T.
分类号 A61K31/7056;A61K31/497;A61K31/5377;A61K31/4439;A61K31/454;A61K31/428;A61K31/4184;A61K31/4709;A61K31/5415;A61K31/55;A61K31/41;A61K38/21;A61K45/06;C07D257/04;C07D401/06;C07D401/12;C07D403/06;C07D403/12;C07D407/12;C07D413/06;C07D413/12;C07D417/04;C07D417/06;C07D295/185;C07D295/205;C07D401/14;C07D403/04;C07D405/12 主分类号 A61K31/7056
代理机构 Jones Day 代理人 Jones Day
主权项 1. A method of inhibiting fatty acid synthase (FASN) in a subject, wherein the subject has a FASN-mediated disorder selected from hyperproliferative disorders, inflammatory disorders, obesity related disorders, Type II diabetes mellitus, fatty liver disease, microbial infections, viral infections, bacterial infections, fungal infections, parasitic infections, and protozoal infections comprising administering to a subject a therapeutically effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, tautomer, stereoisomer and/or polymorph thereof; wherein: RA is selected from C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl and 5-14 membered heteroaryl; RB is selected from C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, 3-14 membered heteroaliphatic, 3-14 membered heterocyclyl, C6-14 aryl and 5-14 membered heteroaryl; RC is selected from hydrogen, —OH, —ORC1, —ON(RC2)2, —N(RC2)2, —C(═O)RC1, —CHO, —CO2RC1, —C(═O)N(RC2)2, —C(═NRC2)ORC1, —C(═NRC2)N(RC2)2, —SO2RC1, —S(═O)RC1, —Si(RC1)3, C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, 3-14 membered heteroaliphatic, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl; each instance of RC1 is, independently, selected from C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, 3-14 membered heteroaliphatic, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl; and each instance of RC2 is, independently, selected from hydrogen, —OH, —ORC1, —CN, —C(═O)RC1, —CO2RC1, —SO2RC1, —P(═O)2RC1, —P(═O)(RC1)2, C1-10 alkyl, C1-10 perhaloalkyl, C2-10 alkenyl, C2-10 alkynyl, 3-14 membered heteroaliphatic, C3-10 carbocyclyl, 3-14 membered heterocyclyl, C6-14 aryl, and 5-14 membered heteroaryl, or two RC2 groups are joined to form a 3-14 membered heterocyclyl or 5-14 membered heteroaryl ring; or RB and RC together with the nitrogen (N) atom to which each is attached are joined to form a 5-14 membered ring.
地址 Cambridge MA US