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1. (WO2018059331) POLYAMIDE COMPOUND AND USE THEREOF

Pub. No.:    WO/2018/059331    International Application No.:    PCT/CN2017/103027
Publication Date: Fri Apr 06 01:59:59 CEST 2018 International Filing Date: Sat Sep 23 01:59:59 CEST 2017
IPC: C07K 7/06
A61K 38/08
A61P 29/00
A61P 17/00
A61P 7/10
A61P 3/12
A61P 1/00
A61P 11/14
A61P 27/06
Applicants: SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.
四川科伦博泰生物医药股份有限公司
Inventors: CAI, Jiaqiang
蔡家强
TIAN, Qiang
田强
ZHAO, Mingliang
赵明亮
ZENG, Hong
曾宏
SONG, Hongmei
宋宏梅
YU, Nan
郁楠
DENG, Hua
邓华
ZHONG, Wei
钟维
YANG, Long
杨龙
WU, Lei
吴雷
HUANG, Haitao
黄海涛
WU, Yongyong
吴勇勇
SU, Donghai
苏东海
ZHOU, Xin
周信
TAN, Yuting
谭玉婷
WANG, Lichun
王利春
WANG, Jingyi
王晶翼
Title: POLYAMIDE COMPOUND AND USE THEREOF
Abstract:
The present invention relates to a polyamide compound and a use thereof; specifically, the present invention relates to a type of polyamide compound (which preferably contains one or more amide bonds formed by the condensation of same or different L-amino acids or D-amino acids), or stereoisomers thereof, polymorphs thereof, solvates thereof, or metabolites thereof, prodrugs thereof or pharmaceutically acceptable salts or esters thereof, or pharmaceutical compositions thereof, as well as a method for preparing the polyamide compound and a use thereof in the prevention or treatment of diseases associated with a κ-opioid receptor. The polyamide compound of the present invention has excellent κ-opioid receptor agonistic activities and hydrophilic ability, thus having a lesser ability of penetrating the blood-brain barrier and a lowered capacity for entering the brain. The compound of the present invention has higher selectivity for a κ-opioid receptor, lowered addictiveness, improved pharmacokinetic properties, and improved safety (lower toxicity and/or fewer side effects, good patient compliance, and/or a lesser propensity for developing tolerance, among other excellent medicinal properties).