发明名称 CERTAIN DIPEPTIDYL PEPTIDASE INHIBITORS
摘要 Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
申请公布号 US2015284385(A1) 申请公布日期 2015.10.08
申请号 US201314443984 申请日期 2013.11.18
申请人 SHANGHAI FOCHON PHARMACEUTICAL CO LTD 发明人 Wang Weibo;Zhao Xingdong;Zhang Huajie;Fang Bo;Rong Yue;Yuan Quan;Tian Qiang;Fu JieMin;Deng Jie;Zeng Fanxin;Lin Min;Jiang Lihua;Sun Jing;Liu Yanxin
分类号 C07D471/04 主分类号 C07D471/04
代理机构 代理人
主权项 1. At least one compound of formula (I):and/or at least one pharmaceutically acceptable salt thereof,wherein:Ar is aryl unsubstituted or substituted with one to five R1 substituents;each R1 is independently selected from: halogen, cyano, hydroxy, C1-6 alkoxy, wherein alkoxy is unsubstituted or substituted with one to five halogens, and C1-6 alkyl, wherein alkyl is unsubstituted or substituted with one to five halogens;Q is selected from aryl, heteroaryl, and heterocyclyl, wherein aryl, heteroaryl, and heterocyclyl are each unsubstituted or independently substituted with at least one substituent, such as one, two, three, four or five substituents, independently selected from R2;each R2 is independently selected from: halogen, cyano, hydroxy C1-10 alkoxy, wherein alkoxy is optionally substituted with one to five substituents independently selected from fluorine and hydroxy, C1-10 alkyl, wherein alkyl is optionally substituted with one to five substituents independently selected from fluorine and hydroxy, C2-10 alkenyl, wherein alkenyl is optionally substituted with one to five substituents independently selected from fluorine and hydroxy, C2-10 alkynyl, wherein alkynyl is optionally substituted with one to five substituents independently selected from fluorine and hydroxy, (CH2)n-aryl, wherein aryl is optionally substituted with one to five substituents independently selected hydroxy, halogen, cyano, nitro, CO2H, C1-6 alkyloxycarbonyl, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines, (CH2)n-heteroaryl, wherein heteroaryl is optionally substituted with one to three substituents independently selected from hydroxy, halogen, cyano, nitro, CO2H, C1-6 alkyloxycarbonyl, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines, (CH2)n-heterocyclyl, wherein heterocycyl is optionally substituted with one to three substituents independently selected from oxo, hydroxy, halogen, cyano, nitro, CO2H, C1-6 alkyloxycarbonyl, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines, (CH2)n—C3-6 cycloalkyl, wherein cycloalkyl is optionally substituted with one to three substituents independently selected from halogen, hydroxy, cyano, nitro, CO2H, C1-6 alkyloxycarbonyl, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines, (CH2)n—COOH, (CH2)n—COOC1-6 alkyl, (CH2)n—NR4R5, (CH2)n—CONR4R5, (CH2)n—OCONR4R5, (CH2)n—SO2NR4R5, (CH2)n—SO2R6, (CH2)n—NR7SO2R6, (CH2)n—NR7CONR4R5, (CH2)n—NR7COR7, and (CH2)n—NR7CO2R6, wherein the individual methylene (CH2) in each of the above (CH2) is optionally substituted with one to two substituents independently selected from fluorine, hydroxy, C1-4 alkyl, and C1-4 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines;each R3 is independently selected from: halogen, cyano, hydroxy, C1-6 alkyl, wherein alkyl is unsubstituted or substituted with one to five halogens, and C1-6 alkoxy, wherein alkoxy is unsubstituted or substituted with one to five halogens;R4 and R5 are each independently selected from: hydrogen, (CH2)p-phenyl, wherein phenyl is optionally substituted with one to five substituents independently selected from halogen, hydroxy, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines, (CH2)p—C3-6 cycloalkyl, wherein cycloalkyl is optionally substituted with one to five substituents independently selected from halogen, hydroxy, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines, and C1-6 alkyl, wherein alkyl is optionally substituted with one to five substituents independently selected from fluorine and hydroxy, wherein the individual methylene (CH2) in each of the above (CH2)p is optionally substituted with one to two substituents independently selected from fluorine, hydroxy, C1-4 alkyl, and C1-4 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines; orR4 and R5 together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein said heterocyclic ring is optionally substituted with one to three substituents independently selected from halogen, hydroxy, C1-6 alkyl, and C1-6 alkoxy, wherein alkyl and alkoxy are optionally substituted with one to five fluorines;each R6 is independently C1-6 alkyl, wherein alkyl is optionally substituted with one to five substituents independently selected from fluorine and hydroxyl;R7 is hydrogen or R6;each m is independently 0, 1, 2, or 3;each n is independently 0, 1, 2, or 3; andeach p is independently 0, 1, or 2.
地址 Shanghai CN