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 US2016137652(A1) 申请公布日期 2016.05.19
申请号 US201514933863 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.;Cherney Emily Charlotte;Shan Weifang;Huang Audris
分类号 C07D487/04;A61K31/47;C07D231/56;A61K31/416;C07D215/233;C07D471/04;A61K31/437;C07D239/74;A61K31/517;A61K31/4375;C07D217/04;C07D405/08;A61K31/4709;C07D417/08;C07D401/12;C07D401/14;A61K31/506;A61K31/496;A61K31/519;A61K45/06;C07D215/06 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; the subscript p is 1 or 0;the ring designated as A is phenyl, 5- or 6-membered heteroaryl, or C5-7 cycloalkyl;Z is O;B is N, C(OR5a), or C(R3a);each X is independently NR5a, O, CHR5, C(O), or CH(OR5a);Q is N, C(CN), or CR6;D is a bond, 0, C(R5)2, or NR5a;E is an optionally substituted 9- or 10-membered fused bicyclic heteroaryl;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, R3a and R4 are independently hydrogen, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C1-C6 haloalkyl, optionally substituted C3-C6 cycloalkyl-C1-C4 alkyl, optionally substituted aryl-C1-C6 alkyl, fluorine, OH, CN, CO2H, C(O)NH2, N(R5)2, optionally substituted —O—C1-C6 alkyl, —(CR5R5)m—OH, —(CR5R5)m—CO2H, —(CR5R5)m—C(O)NH2, —(CR5R5)m—C(O)NHR5, —(CR5R5)mN(R5)2, —NH(CR5R5)mCO2H or —NH(CR5R5)m—C(O)NH2;each R5 is independently H, F, OH, or optionally substituted 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
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