发明名称 NK 1 ANTAGONISTS
摘要 A compound having the general structure shown in Formula I:;;or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
申请公布号 US2017029403(A1) 申请公布日期 2017.02.02
申请号 US201615293962 申请日期 2016.10.14
申请人 OPKO Health, Inc. 发明人 Palani Anandan;Huang Xianhai;Xiao Dong;Paliwal Sunil;Tsui Hon-Chung;Wrobleski Michelle Laci;Rao Ashwin U.;Wang Cheng;Shah Sapna S.;Shih Neng-Yang
分类号 C07D401/04;A61K45/06;A61K31/4178;C07D211/56;A61K31/4545;A61K31/454;C07D417/04;A61K31/451;C07D413/04;A61K31/573 主分类号 C07D401/04
代理机构 代理人
主权项 1. A compound of Formula I: or pharmaceutically acceptable salts and/or solvates thereof, wherein: R1 and R2 are each independently selected from the group consisting of H, alkyl, haloalkyl, alkyl substituted with one or more hydroxyl groups, —CN, alkynyl, —N(R6)2, —N(R6)—S(O2)-alkyl, —N(R6)—C(O)—N(R9)2, -alkylene-CN, -cycloalkylene-CN, -alkylene-O-alkyl, —C(O)-alkyl, —C(═N—OR5)-alkyl, —C(O)—N(R9)2, —C(O)—O-alkyl, -alkylene-C(O)-alkyl, -alkylene-C(O)—O-alkyl, -alkylene-C(O)—N(R9)2, with the proviso that at least one of R1 and R2 is —CN, W is ═C(R8)— or ═N—; X is —C(O)— or —S(O2)—; Y is selected from the group consisting of —CH2—, —O—, and —N(R6)—C(O)—, with the proviso that: (a) the nitrogen atom of —N(R6)—C(O)— is bonded to X, and(b) if R1 and/or R2 isand Y is —O—, X is not —S(O2)—; Z is —C(R7)2—, —N(R6)—, or —O—; R3 is selected from the group consisting of H, —CH2OR5, and alkyl; R4 is selected from the group consisting of H, alkyl, cycloalkyl, heterocycloalkyl, heteroaryl, aryl, acyl, aroyl, alkylsulfonyl, and arylsulfonyl; R5 is H or alkyl; R6 is selected from the group consisting of H, alkyl, cycloalkyl, and aryl; each R7 is independently H or alkyl; or each R7, together with the ring carbon to which they are shown attached, form a cycloalkylene ring; R8 is selected from the group consisting of H, alkyl, alkyl substituted with one or more hydroxyl groups, —N(R6)2, —N(R6)—S(O2)-alkyl, —N(R6)—S(O2)-aryl, —N(R6)—C(O)-alkyl, —N(R6)—C(O)-aryl, alkylene-O-alkyl, and —CN; R9 is selected from the group consisting of H, alkyl, and aryl, or each R9, together with the nitrogen to which they are shown attached, form a heterocycloalkyl ring; Ar1 and Ar2 are each independently selected from the group consisting of unsubstituted aryl and aryl substituted with 0 to 3 substituents selected from the group consisting of halogen, alkyl, alkoxy, haloalkyl, haloalkoxy, —CN, —OH, and —NO2; n is 0, 1, or 2; and m is 1, 2, or 3.
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