发明名称 N-Aryl Unsaturated Fused Ring Tertiary Amine Compounds, Preparation Method and Anti-Tumor Applications Thereof
摘要 The present invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, its preparation method, a pharmaceutical composition comprising the compound, and its use in manufacture of a medicament for treatment of a disease or disorder, wherein R1, R2, R5, R6, X, Y, Q, W, n1 and n2 are defined as those stated in the description.;
申请公布号 US2015141407(A1) 申请公布日期 2015.05.21
申请号 US201314403750 申请日期 2013.05.30
申请人 Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China 发明人 Xie Lan;Wang Xiaofeng;Lee Kuo-Hsiung
分类号 C07D473/40;C07D403/04;C07D473/32;C07D215/20;C07D473/00;C07D401/04;C07D413/04 主分类号 C07D473/40
代理机构 代理人
主权项 1. A compound of Formula I or a pharmaceutically acceptable salt thereof: wherein, X and Y each independently are —O—, —S—, —S(O)—, —S(O)2—, —C(O)—, —NR′—, —CHOR′—, —CHNHR′—, —CHNR′R″— or —CR′R″—; or X and Y together form —CH═CH—; wherein R′ and R″ each independently are H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C1-6 alkoxyl, C1-6 alkylamino, hydroxyl C1-6 alkyl, C1-6 halogenated alkyl, hydroxyl, acyl, aryl or heteroaryl; and when R′ and R″ form a chiral center at substitution site, the compound of Formula I can be a single R or S configuration or a racemate; R1 represents 1, 2, 3 or 4 substituents optionally existing on the benzene ring, independently being H, alkyl, alkoxyl, halogen, acyl, alkenyl, alkynyl, hydroxyl, cyano, amino, alkylamino, dialkylamino, cyano alkyl, hydroxyl alkyl, halogenated alkyl, acylamino, alkylthio, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; R2 is alkyl, alkoxyl, halogen, acyl, alkenyl, alkynyl, hydroxyl, cyano, amino, alkylamino, dialkylamino, acylamino, alkylthio, cycloalkyl, hydroxyl alkyl, halogenated alkyl, cyano alkyl, heterocycloalkyl, aryl or heteroaryl; Q and W each independently are N or CR; wherein R is H, halogen (e.g., fluorine, chlorine, bromine, iodine), cyano, amino, hydroxyl, C1-6 alkyl, C1-6 alkoxyl, hydroxyl C1-6 alkyl, C1-6 halogenated alkyl, cyano C1-6 alkyl, C1-6 alkylamino, C1-6dialkylamino, C2-6 alkenyl or conjugated alkenyl, C2-6 alkynyl or conjugated alkynyl, acyl, acylamino, alkylthio, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; R5 and R6 together with carbon atoms linked to them form 5- or 6-membered saturated, partially unsaturated carbocyclic ring or heterocyclic ring, or aromatic ring or aromatic heterocyclic ring forming a conjugated system, wherein the heterocyclic ring or aromatic heterocyclic ring optionally contains 1, 2, 3 or 4 heteroatoms independently selected from N, O or S; the ring is optionally substituted with 1, 2, 3 or 4 R3; or R5 and R6 each independently are H, alkyl, alkoxyl, hydroxyl alkyl, halogen, halogenated alkyl, carboxyl, ester group, acyl, alkenyl, alkynyl, hydroxyl, cyano, amino, alkylamino, dialkylamino, acylamino, alkylthio, cycloalkyl, heterocycloalkyl, aryl or heteroaryl, which are optionally substituted with 1, 2, 3 or 4 R3; R3 independently is H, C1-6 alkyl, C1-6 alkoxyl, fluorine, chlorine, bromine, iodine, acyl, C2-6 alkenyl, C2-6 alkynyl, hydroxyl, cyano, amino, C1-6 alkylamino, acylamino, C1-6alkylthio, C3-6 cycloalkyl, heterocycloalkyl, C5-10aryl or heteroaryl; n1=0, 1 or 2; and n2=0 or 1.
地址 Beijing CN