发明名称 FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME
摘要 Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
申请公布号 US2017066749(A1) 申请公布日期 2017.03.09
申请号 US201615354834 申请日期 2016.11.17
申请人 Zafgen, Inc. 发明人 Vath James E.;Zahler Robert
分类号 C07D405/12;C07D417/14;C07D491/107;C07D491/048;C07D491/08;C07D487/08;A61K9/00;A61K31/5377;A61K31/397;A61K31/4025;A61K31/4523;A61K31/541;A61K31/496;A61K31/4155;A61K31/403;A61K31/5383;A61K31/4427;C07D405/14 主分类号 C07D405/12
代理机构 代理人
主权项 1. A compound represented by: wherein: p is 2; B is RiRjN—; wherein Ri and Rj taken together with the nitrogen to which they are attached form a 4-9 membered monocyclic, bridged bicyclic, fused bicyclic or spirocyclic heterocyclic ring, which may have an additional heteroatom selected from the group consisting of N, O, and S(O)w (wherein w is 0, 1 or 2); wherein the 4-9 membered monocyclic, bridged bicyclic, fused bicyclic or spirocyclic heterocyclic ring may be optionally substituted on carbon by one, two, or more substituents selected from the group consisting of halogen, hydroxyl, oxo, cyano, C1-6alkyl, C1-6alkoxy, and RaRbN-carbonyl-; wherein said C1-6alkyl may optionally be substituted by one, two, or more substituents selected from the group consisting of fluorine and hydroxyl; wherein if said 4-9 membered monocyclic, bridged bicyclic, fused bicyclic or spirocyclic heterocyclic ring contains a —NH moiety, that nitrogen may be optionally substituted by a substituent selected from the group consisting of C1-6alkyl and C1-6alkyl-S(O)2—; wherein C1-6alkyl and C1-6alkyl-S(O)2— may optionally be substituted by one or more fluorines; Ra and Rb are independently selected, for each occurrence, from the group consisting of hydrogen and C1-3alkyl; wherein C1-3alkyl may optionally be substituted by one or more substituents selected from halogen, cyano, oxo and hydroxyl; or a pharmaceutically acceptable salt or stereoisomer thereof.
地址 Boston MA US