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1. WO2020138499 - ALKYL-SUBSTITUTED COMPOUND

Publication Number WO/2020/138499
Publication Date 02.07.2020
International Application No. PCT/JP2019/051620
International Filing Date 27.12.2019
IPC
A61K 31/407 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4196 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61K 31/427 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
A61K 31/546 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame
542ortho- or peri-condensed with heterocyclic ring systems
545Compounds containing 5-thia-1-azabicyclo octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine
546containing further heterocyclic rings, e.g. cephalothin
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
A61K 45/00 2006.01
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/-A61K41/132
CPC
A61K 31/407
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/4196
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41961,2,4-Triazoles
A61K 31/427
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
425Thiazoles
427not condensed and containing further heterocyclic rings
A61K 31/546
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
54having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
542ortho- or peri-condensed with heterocyclic ring systems
545Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula: , e.g. cephalosporins, ; cefaclor, or cephalexine
546containing further heterocyclic rings, e.g. cephalothin
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 45/00
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
Applicants
  • 大日本住友製薬株式会社 SUMITOMO DAINIPPON PHARMA CO., LTD. [JP]/[JP]
  • 学校法人北里研究所 THE KITASATO INSTITUTE [JP]/[JP]
Inventors
  • 小池 祥子 KOIKE Sachiko
  • 井熊 洋平 IKUMA Yohei
  • 上杉 惇一郎 UESUGI Shunichiro
  • 深谷 孝幸 FUKAYA Takayuki
  • 水上 雄貴 MIZUKAMI Yuki
  • 福田 展久 FUKUDA Nobuhisa
  • 砂塚 敏明 SUNAZUKA Toshiaki
  • 野口 吉彦 NOGUCHI Yoshihiko
  • 花木 秀明 HANAKI Hideaki
  • 君嶋 葵 KIMISHIMA Aoi
Agents
  • 山本 秀策 YAMAMOTO Shusaku
  • 森下 夏樹 MORISHITA Natsuki
  • ▲駒▼谷 剛志 KOMATANI Takeshi
  • 飯田 貴敏 IIDA Takatoshi
  • 石川 大輔 ISHIKAWA Daisuke
  • 山本 健策 YAMAMOTO Kensaku
Priority Data
2018-24795128.12.2018JP
2019-15870730.08.2019JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) ALKYL-SUBSTITUTED COMPOUND
(FR) COMPOSÉ SUBSTITUÉ PAR UN ALKYLE
(JA) アルキル置換化合物
Abstract
(EN)
The purpose of the present invention is to provide a novel compound that has an excellent β-lactamase inhibitory activity. The present invention provides: a compound that has an excellent β-lactamase inhibitory activity and is represented by formula (1a), (1b) or (11); or a pharmaceutically acceptable salt thereof. The compound provides a prophylactic or therapeutic agent that is useful for bacterial infection when used in combination with a β-lactam drug or used alone. The present invention also provides a prophylactic or therapeutic agent that is useful for treating a variety of diseases in combination with a β-lactam drug.
(FR)
L’objectif de la présente invention est de décrire un nouveau composé qui possède une excellente activité inhibitrice de la β-lactamase. La présente invention concerne : un composé qui possède une excellente activité inhibitrice de la β-lactamase et qui est représenté par la formule (1a), (1b) ou (11) ; ou un sel pharmaceutiquement acceptable de celui-ci. Le composé fournit un agent prophylactique ou thérapeutique qui est utile en cas d'infection bactérienne lorsqu'il est utilisé en combinaison avec un médicament β-lactame ou utilisé seul. La présente invention concerne également un agent prophylactique ou thérapeutique qui est utile pour traiter une variété de maladies en combinaison avec un médicament β-lactame.
(JA)
優れたβ-ラクタマーゼ阻害作用を有する新規な化合物を提供すること。 本発明は、優れたβ-ラクタマーゼ阻害作用を有する式(1a)、(1b)または(11)で表される化合物、またはその製薬学的に許容される塩を提供する。この化合物は、β-ラクタム系薬剤との併用もしくは単剤にて細菌感染症の有用な予防または治療剤を提供する。本発明はまた、種々の疾患のβ-ラクタム系薬剤との併用による治療のために有用な予防または治療剤を提供する。
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