公开(公告)号：US11608319B2

公开(公告)日：2023-03-21

申请号：US17117615

申请日：2020-12-10

Applicant: Industrial Technology Research Institute

Inventor： Chih-Wei Fu ,  Chih-Peng Liu ,  Yi-Hsun Chen ,  Chia-Mu Tu ,  Chiu-Lien Hung

IPC: C07D231/12 ,  C07D403/12 ,  A61P27/06

Abstract: A compound represented by Formula (I), a pharmaceutically acceptable salt or ester, hydrate, solvate or crystalline form thereof is provided: The compound represented by Formula (I) is a β-amino acid derivative, and in Formula (I) X is a single bond or O; Y is NH or C═O; Z is C═O, C═S, NH, W is C or N; A is a single bond, O, OH, OCH2, a heterocycle or N3; R1 is H or F; R2 is H, F, OH, CF3, CH2OH, CHO or R3 is H; n is 0 or 1; and m is 0 or 1.

公开(公告)号：US10696638B2

公开(公告)日：2020-06-30

申请号：US16206000

申请日：2018-11-30

Applicant: Industrial Technology Research Institute

Inventor： Chih-Hung Chen ,  Yi-Hsun Chen ,  Jui-Wen Huang ,  Kuo-Kuei Huang ,  Chih-Peng Liu ,  Chrong-Shiong Hwang

IPC: C07D217/02 ,  A61K31/472 ,  A61P27/02 ,  A61K31/4725 ,  A61K9/08 ,  A61K9/00

Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof is provided. In formula (I), Ar is indazole, 5-isoquinoline, 6-isoquinoline, or their N-oxide. X is —C(═Z)—, wherein Z is N—CN, NH, NR4, NCOR4, NCONR4R5, NCO-aryl, S, or O. Y and J are independently H, alkyl, aryl, aminoalkyl, —NH2, —CN, —OH, —O-alkyl, —O-aryl, —COOH, —COOR4, —CONHR4, —CONHCH2-aryl, —CONR4CH2-aryl, —NHCOR4, halogen, halogened alkyl, -alkyl-OR4, -alkyl-ONO2, alkyl-ONO2, —OCOOR4, —O(C═O)-aryl, —CHR4OH, —CH2OH, —CH2O(C═O)-aryl, —CH2O(C═O)—R4, —CHR4O(C═O)-aryl, —CHR4O(C═O)—R4, unsaturated carboxylic ester, substituted alkynyl, —NHSO2R4, —SO2R4, —SO2NHR4, or —SO2NR4R5, or Y and J bond together to form a carbocylic or aromatic ring, wherein R4 and R5 are independently H, substituted C1-C6 alkyl, substituted aryl, cycloalkyl, alkylaryl, -alkyl-NR6R7, —S(O)0-2-(alkyl-NR6R7). R1, R2 and R3 are H, C1-C6 alkyl, cycloalkyl, aryl, alkylaryl, alkylheteroaryl, alkylheterocycle, wherein any one thereof is optionally substituted with one or more of OH, NO2, or NR8R9.