发明名称 Piperazine derivatives and methods of use
摘要 The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
申请公布号 US8946227(B2) 申请公布日期 2015.02.03
申请号 US201313754345 申请日期 2013.01.30
申请人 Merck Serono SA 发明人 Magar Sharad;Goutopoulos Andreas;Liao Yihua;Schwarz Matthias;Thomas Russell J.
分类号 A61K31/4965;C07D295/00;C07D409/14;A61K31/496;C07D401/14;C07D403/12;C07D487/04;C07D471/04 主分类号 A61K31/4965
代理机构 Morgan, Lewis & Bockius LLP 代理人 Morgan, Lewis & Bockius LLP
主权项 1. A method for treating infertility in a human female, comprising administering to a human female suffering from or suspected of suffering from infertility a therapeutically effective amount of a compound of Formula I:wherein R1 is H; R2 is selected from aryl and heteroaryl; R3 is selected from C1-C16-alkyl, C2-C16-alkenyl, C2-C16-alkynyl, monocyclic aryl, monocyclic heteroaryl, 3-8-membered monocyclic cycloalkyl, monocyclic heterocycloalkyl, acyl, C1-C16-alkyl aryl, C1-C16-alkyl heteroaryl, C2-C16-alkenyl aryl, C2-C16-alkenyl heteroaryl, C2-C16-alkynyl aryl, C2-C16-alkynyl heteroaryl, C1-C16-alkyl cycloalkyl, C1-C16-alkyl heterocycloalkyl, C2-C16-alkenyl cycloalkyl, C2-C16-alkenyl heterocycloalkyl, C2-C16-alkynyl cycloalkyl, C2-C16-alkynyl heterocycloalkyl, alkoxycarbonyl, aminocarbonyl, C1-C16-alkyl carboxy, C1-C16-alkyl acyl, aryl acyl, heteroaryl acyl, C3-C8-(hetero)cycloalkyl acyl, C1-C16-alkyl acyloxy, C1-C16-alkyl alkoxy, C1-C16-alkyl alkoxycarbonyl, C1-C16-alkyl aminocarbonyl, C1-C16-alkyl acylamino, acylamino, sulfmyl, C1-C16-alkyl sulfanyl, C1-C16-alkyl ureido, C1-C16-alkyl carbamate, C1-C16-alkyl amino, and C1-C16-alkyl ammonium; R4 is selected from C1-C12-alkyl, C2-C12-alkenyl, C2-C12-alkynyl, aryl, heteroaryl, 3-8-membered cycloalkyl, heterocycloalkyl, and amino; and pharmaceutically acceptable salts thereof.
地址 Coinsins, Vaud CH