发明名称 Dihydropyrimidin-2(1H)-one compounds as neurokinin-3 receptor antagonists
摘要 The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
申请公布号 US8906933(B2) 申请公布日期 2014.12.09
申请号 US201013814316 申请日期 2010.09.24
申请人 N30 Pharmaceuticals, Inc. 发明人 Sun Xicheng;Qiu Jian
分类号 A61K31/505;C07D409/14;C07D413/10;C07D239/22;C07D409/04 主分类号 A61K31/505
代理机构 Swanson & Bratschun, L.L.C. 代理人 Swanson & Bratschun, L.L.C.
主权项 1. A method of attenuating at least one deleterious symptom or effect of schizophrenia characterized by overstimulation of NK3 which comprises administering to a patient in need thereof a therapeutically effective amount of an NK3 receptor antagonist of formula I: wherein X is selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl, each having 6 members or less in the ring; Y is selected from the group consisting of aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl; Z is selected from the group consisting of O, S and NR7; R1, R2 and R7 are independently selected from the group consisting of hydrogen, and C1-C6 alkyl; R3 is selected from the group consisting of hydrogen, nitro, cyano, carboxyl, carbamoyl, methylsulfonamido, fluoro, chloro, bromo, hydroxy, methylsulfonyl, and methylsulfinyl, isoxazol-4-yl, C1-C6 alkoxy, —C(NH)NHOH, sulfonic acid, and acetyl; R4 is selected from the group consisting of hydrogen, hydroxy, methoxy, carboxyl, and tetrazol-5-yl; or optionally R3 and R4, taken together can form a heterocycle; R5 is selected from the group consisting of hydrogen, hydroxyl, carboxy, chloro, fluoro, cyano, —O(CH2)1-6NMe2, C1-C6 alkyl, —O(CH2)1-6OCH3, —O(CH2)1-6OH, acetyl, CF3, and C1-C6 alkoxy; or optionally R4 and R5, taken together can form a heterocycle; and R6 is selected from the group consisting of hydrogen and hydroxyl.
地址 Boulder CO US