发明名称 Novel Dihydropyridin-2(1H)-One Compounds as S-Nitrosoglutathione Reductase Inhibitors and Neurokinin-3 Receptor Antagonists
摘要 The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
申请公布号 US2015157616(A1) 申请公布日期 2015.06.11
申请号 US201514598202 申请日期 2015.01.15
申请人 N30 Pharmaceuticals, Inc. 发明人 Sun Xicheng;Qiu Jian
分类号 A61K31/4412;A61K31/4439;A61K31/4436;A61K31/444 主分类号 A61K31/4412
代理机构 代理人
主权项 1. A method of treatment of a disease or condition which comprises administering a therapeutically effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof to a patient in need wherein X is selected from the group consisting of phenyl, substituted phenyl, thiophen-yl, substituted thiophen-yl, thiazol-yl, substituted thiazol-yl, pyrazin-yl, substituted pyrazin-yl, pyridin-yl, and substituted pyridin-yl, cyclohexyl, substituted cyclohexyl; Y is selected from the group consisting of phenyl, substituted phenyl, thiophen-yl, substituted thiophen-yl, thiazol-yl, substituted thiazol-yl, pyrazin-yl, substituted pyrazin-yl, pyridin-yl, substituted pyridin-yl, furan-yl, substituted furan-yl, benzo[d][1,3]dioxol-yl, substituted benzo[d][1,3]dioxol-yl, imidazol-yl, substituted imidazol-yl, naphthalen-yl, substituted naphthalen-yl, pyrrol-yl, substituted pyrrol-yl, pyrazol-yl, substituted pyrazol-yl, tetrahydrofuran-yl, substituted tetrahydrofuran-yl, cyclopentyl, substituted cyclopentyl, cyclohexyl, and substituted cyclohexyl; Z is selected from the group consisting of O, S, and NR7; R1 and 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 hydroxyl, carboxyl, and tetrazol-5-yl; 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; and R6 is selected from the group consisting of hydrogen and hydroxyl.
地址 Boulder CO US