发明名称 KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
摘要 Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
申请公布号 US2014329795(A1) 申请公布日期 2014.11.06
申请号 US201214241699 申请日期 2012.08.28
申请人 Courtney Stephen Martin;Prime Michael;Mitchell William;Brown Christopher John;De Aguiar Pena Paula C.;Johnson Peter;Dominguez Celia;Toledo-Sherman Leticia M.;Munoz Ignacio 发明人 Courtney Stephen Martin;Prime Michael;Mitchell William;Brown Christopher John;De Aguiar Pena Paula C.;Johnson Peter;Dominguez Celia;Toledo-Sherman Leticia M.;Munoz Ignacio
分类号 C07D239/28;C07D401/12;C07D403/06;C07D417/12;C07D239/42;C07D403/12;C07D471/04;C07D405/12;C07D487/04;C07D401/04;C07D413/12 主分类号 C07D239/28
代理机构 代理人
主权项 1. At least one chemical entity chosen from compounds of Formula I and pharmaceutically acceptable salts and prodrugs thereof wherein: X and Y are independently chosen from —N— and —CH—, provided that at least one of X and Y is —N—;R1 is chosen from optionally substituted aryl and optionally substituted heteroaryl;R2 is chosen from hydrogen and optionally substituted lower alkyl;R3 is chosen from hydrogen, halo, optionally substituted lower alkyl, hydroxyl, optionally substituted lower alkoxy, and optionally substituted amino, or R1 and R3, taken together with intervening atoms form a bicyclic ring of the formula which is optionally substituted where m is 0 or 1 and n is 0 or 1, provided that at least one of m and n is 1 and W is —O—, or —N(R8)— where R8 is hydrogen or lower alkyl;L is chosen from —C(O)O—, —C(O)N(R4)—, —N(R4)S(O)2—, —S(O)2N(R4)—, —C(O)N(R4)S(O)2—, —C(O)—, and —C(═N)—OR7 where R7 is hydrogen or lower alkyl, provided that if L is —C(O)N(R4)—, then R5 also can be lower alkoxy; andR4 and R5 taken together with the nitrogen to which they are bound form an optionally substituted 4- to 7-membered heterocycloalkyl ring, which is optionally fused to an optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl ring.
地址 Oxfordshire GB