发明名称 IMMUNOREGULATORY AGENTS
摘要 Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided.
申请公布号 US2016137653(A1) 申请公布日期 2016.05.19
申请号 US201514933879 申请日期 2015.11.05
申请人 Flexus Biosciences, Inc. 发明人 Beck Hilary Plake;Jaen Juan Carlos;Osipov Maksim;Powers Jay Patrick;Reilly Maureen Kay;Shunatona Hunter Paul;Walker James Ross;Zibinsky Mikhail;Balog James Aaron;Williams David K.;Markwalder Jay A.;Seitz Steven P.;Cherney Emily Charlotte;Zhang Liping;Shan Weifang;Guo Weiwei;Huang Audris
分类号 C07D487/04;A61K31/277;C07C233/65;A61K31/166;C07D211/08;A61K31/445;C07C211/45;A61K31/136;C07D215/04;A61K31/47;A61K31/4709;C07D215/233;C07D213/68;A61K31/4412;A61K31/496;A61K31/519;A61K31/5377;A61K45/06;C07C255/50 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound having the formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein, the subscript n is 1 or 0; A is —C(O)—, —NH—, —SO2—, —CH2—, or —CHR3—; B is a bond, —C(O)—, —NH—, —CH2—, or —CHR3—; T is a bond, —CH2—, —NH—, —O—, —OCH2—, —C(O)CH2—, or —CR3R4—; wherein when A is —NH— and B is —C(O)—, then T is other than —C(R3)(R4)—; D is N or C(R5); E is N or C(R6); V is a bond, —O—, or —C(R5a)2; G is an optionally substituted aryl, optionally substituted heteroaryl, or an optionally substituted 9- or 10-membered fused bicyclic heteroaryl; J1 is CH, N or C(R2), when R2 is attached to the ring vertex identified as J1; R1 and R2 are independently hydrogen, halogen, optionally substituted C1-C4 haloalkyl, optionally substituted C3-C6 cycloalkyl, optionally substituted 3- to 6-membered cycloheteroalkyl, optionally substituted phenyl, optionally substituted heteroaryl, optionally substituted C1-C4 alkyl, optionally substituted C1-C4 alkoxy, CN, SO2NH2, NHSO2CH3, NHSO2CF3, OCF3, SO2CH3, SO2CF3, or CONH2, and when R1 and R2 are on adjacent vertices of a phenyl ring they may be joined together to form a 5- or 6-membered cycloheteroalkyl ring having one or two ring vertices independently selected from O, N and S, wherein said cycloheteroalkyl ring is optionally substituted with from one to three members selected from fluoro and C1-C3 alkyl; R3 and R4 are independently hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C1-C6 haloalkyl, fluorine, OH, CN, CO2H, C(O)NH2, N(R5a)2, optionally substituted —O—C1-C6 alkyl, —(CR5R5)m—OH, —(CR5R5)m—CO2H, —(CR5R5)m—C(O)NH2, —(CR5R5)m—C(O)NHR5a, —(CR5R5)mN(R5a)2, —NH(CR5R5)mCO2H or —NH(CR5R5)m—C(O)NH2; each R5 is independently H, F, OH, optionally substituted C1-C6 alkyl or optionally substituted —O—C1-C6 alkyl; each R5a is independently H, or optionally substituted C1-C6 alkyl; R6 is H, OH, F, optionally substituted C1-C6 alkyl, optionally substituted —O—C1-C6 alkyl, or —N(R5a)2; and each m is independently 1, 2, or 3.
地址 Princeton NJ US