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1. WO2021091059 - INHIBITOR FOR CARBAPENEM HYDROLYSIS CLASS D BETA-LACTAMASE (CHDL) AND PREPARATION METHOD THEREOF

Publication Number WO/2021/091059
Publication Date 14.05.2021
International Application No. PCT/KR2020/011575
International Filing Date 28.08.2020
IPC
C07F 5/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
FACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
5Compounds containing elements of Groups 3 or 13 of the Periodic System
02Boron compounds
A61K 31/69 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
69Boron compounds
A61P 31/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
CPC
A61K 31/69
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
69Boron compounds
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants
  • 명지대학교 산학협력단 MYONGJI UNIVERSITY INDUSTRY AND ACADEMIA COOPERATION FOUNDATION [KR]/[KR]
Inventors
  • 이상희 LEE, Sang Hee
  • 이정훈 LEE, Jung Hun
  • 전정호 JEON, Jeong Ho
Agents
  • 윤여강 YOON, Yuh-Gang
Priority Data
16/677,97608.11.2019US
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) INHIBITOR FOR CARBAPENEM HYDROLYSIS CLASS D BETA-LACTAMASE (CHDL) AND PREPARATION METHOD THEREOF
(FR) INHIBITEUR POUR LA BÊTA-LACTAMASE DE CLASSE D D'HYDROLYSE DE CARBAPÉNÈME (CHDL) ET SON PROCÉDÉ DE PRÉPARATION
(KO) 카바페넴 가수 분해 클래스 D 베타-락타마제 저해제 및 이의 제조방법
Abstract
(EN)
The present invention relates to an inhibitor for carbapenem hydrolysis class D beta-lactamase and a preparation method thereof and, more particularly, to [3-(2-phenylethoxy)phenyl]boronic acid or a pharmaceutically acceptable salt thereof for inhibiting CHDL, and a preparation method thereof. [3-(2-phenylethoxy)phenyl]boronic acid or a pharmaceutically acceptable salt thereof according to the present invention inhibits all six clinically important subgroups of CHDL and four newly emerging CHDL subgroups. Accordingly, the compound according to the present invention inhibits a wide variety of CHDLs such that when used together with beta-lactam antibiotics, the compound is effective for treatment of infections caused by bacteria that develop antibiotic resistance due to various CHDLs.
(FR)
La présente invention concerne un inhibiteur pour la bêta-lactamase de classe D d'hydrolyse de carbapénème et son procédé de préparation et, plus particulièrement, l'acide [3-(2-phényléthoxy)phényl]boronique ou un sel pharmaceutiquement acceptable de celui-ci pour inhiber CHDL, et son procédé de préparation. L'acide [3-(2-phényléthoxy)phényl]boronique ou un sel pharmaceutiquement acceptable de celui-ci selon la présente invention inhibe tous les six sous-groupes cliniquement importants de CHDL et quatre sous-groupes CHDL nouvellement émergents. En conséquence, le composé selon la présente invention inhibe une grande variété de CHDL de telle sorte que lorsqu'il est utilisé conjointement avec des antibiotiques bêta-lactame, le composé est efficace pour le traitement d'infections provoquées par des bactéries qui développent une résistance aux antibiotiques due à diverses CHDL.
(KO)
본 발명은 카바페넴 가수 분해 클래스 D 베타-락타마제 저해제 및 이의 제조방법에 대한 것으로 보다 구체적으로는 CHDL(카바페넴 가수 분해 클래스 D 베타-락타마제)을 저해하기 위한 [3-(2-페닐에톡시)페닐]보론산 또는 이의 약학적 허용 가능한 염 및 이의 제조방법에 대한 것이다. 본 발명에 따른 [3-(2-페닐에톡시)페닐]보론산 또는 이의 약학적 허용 가능한 염은 CHDL(카바페넴 가수 분해 클래스 D 베타-락타마제) 중 6개의 임상적으로 중요한 서브그룹 모두 및 새롭게 등장하는 4개의 CHDL 서브그룹들을 저해한다. 따라서, 본 발명에 따른 화합물은 넓은 범위에 걸친 다양한 CHDL을 저해하여, 베타-락탐 항생제와 함께 사용될 때 다양한 CHDL에 의해 항생제 내성이 생기는 세균의 감염 및 치료에 효과적이다.
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