发明名称 AMIDE DERIVATIVE
摘要 The present invention provides a useful medicament for the treatment and/or prophylaxis of a disease associated with the enhancement of OPN production including cancer, which comprises a compound of formula:;;wherein R1, R2, R3, R4, R5, R6, R7, m, n, p, X, and Y are as defined in the specification, a pharmaceutically acceptable salt thereof.
申请公布号 US2016368860(A1) 申请公布日期 2016.12.22
申请号 US201515121687 申请日期 2015.02.27
申请人 TOHOKU UNIVERSITY ;NATIONAL UNIVERSITY CORPORATION GUNMA UNIVERSITY ;FUSO PHARMACEUTICAL INDUSTRIES, LTD. 发明人 Kikuchi Haruhisa;Oshima Yoshiteru;Hattori Toshio;Kubohara Yuzuru;Yamada Osamu;Zhang Jing;Matsushita Yoshihisa;Kida Shinya
分类号 C07C235/50;C07C235/48;C07C233/36;C07C233/78;C07C233/62;C07D309/08;C07D471/04;C07C237/34;C07C237/42;C07C235/60;C07C237/22;C07D205/04;C07D207/16;C07D211/60;C07D333/38;C07D213/81;C07D209/14 主分类号 C07C235/50
代理机构 代理人
主权项 1. A compound of formula:wherein R1 and R3 are independently hydrogen atom, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 heterocycloalkyl, C6-10 aryl, or 5- to 10-membered heteroaryl wherein the C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 heterocycloalkyl, C6-10 aryl, and 5- to 10-membered heteroaryl independently may be optionally substituted with one group or the same or different two or more groups selected independently from the group consisting of halogen, hydroxy, mercapto, cyano, nitro, amino, mono- or di-C1-6 alkylamino, C1-4 acyl, C1-4 acylamino, C1-4 alkylsulfonyl, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C2-6 alkenyl, C2-6 alkynyl, and —OR5 at any replaceable positions; R2 is hydrogen atom, amino, amino substituted with one or two independently-selected C1-6 alkyl, hydroxy, or C1-6 alkoxy; R4 is hydrogen atom, halogen, amino, amino substituted with one or two independently-selected C1-6 alkyl, C1-6 alkyl, or C1-6 haloalkyl; R5 is C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 heterocycloalkyl, C6-10 aryl, or 5- to 10-membered heteroaryl wherein the C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 heterocycloalkyl, C6-10 aryl, and 5- to 10-membered heteroaryl may be optionally substituted with one group or the same or different two or more groups selected independently from the group consisting of halogen, hydroxy, mercapto, cyano, nitro, amino, mono- or di-C1-6 alkylamino, C1-4 acyl, C1-4 acylamino, C1-4 alkylsulfoxy, C1-6 alkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, C2-6 alkenyl, and C2-6 alkynyl at any replaceable positions; R6 and R7 are independently hydrogen atom or C1-4 alkyl; n is 0 to 4, provided that when n is 1 to 4 and R6 is C1-4 alkyl, the terminal carbon atom of R6 may be combined with any one carbon atom of the alkylene group in the parenthesis for n to form a 4- to 6-membered ring; m is 0 or 1; p is 0 or 1; X is O, or when p is 0 and R2 is amino or substituted amino which is linked at the 2-position of the benzene ring, X may be CH connecting the nitrogen atom in R2 to form a pyrrole ring; and Y is CH2 or NH;or a pharmaceutically acceptable salt thereof, provided that the following compound is excluded:N-(3-(2-amino-3-(4-hydroxyphenoxy)phenyl)-3-oxopropyl)-4-hydroxybenzamide.
地址 Sendai-shi, Miyagi JP