JP7273420B2 - β－ラクタマーゼ阻害剤及びその用途 - Google Patents

β－ラクタマーゼ阻害剤及びその用途 Download PDF

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Publication number
JP7273420B2
JP7273420B2 JP2020540565A JP2020540565A JP7273420B2 JP 7273420 B2 JP7273420 B2 JP 7273420B2 JP 2020540565 A JP2020540565 A JP 2020540565A JP 2020540565 A JP2020540565 A JP 2020540565A JP 7273420 B2 JP7273420 B2 JP 7273420B2
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octane
diazaspiro
bicyclo
oxo
cyclopropan
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JP2021511351A (ja
JP2021511351A5 (enExample
Inventor
ウー、ユチュアン
ホアン、シャオチャン
チェン、シー
フー、ヨンハン
リウ、シャオ
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Evopoint Biosciences Co Ltd
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Evopoint Biosciences Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2020540565A 2018-01-25 2019-01-24 β－ラクタマーゼ阻害剤及びその用途 Active JP7273420B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2018/074185 2018-01-25
CN2018074185 2018-01-25
PCT/CN2019/073000 WO2019144912A1 (zh) 2018-01-25 2019-01-24 β-内酰胺酶抑制剂及其用途

Publications (3)

Publication Number Publication Date
JP2021511351A JP2021511351A (ja) 2021-05-06
JP2021511351A5 JP2021511351A5 (enExample) 2023-03-13
JP7273420B2 true JP7273420B2 (ja) 2023-05-15

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US (1) US11078202B2 (enExample)
EP (1) EP3744722A4 (enExample)
JP (1) JP7273420B2 (enExample)
KR (1) KR102769880B1 (enExample)
CN (1) CN111670187B (enExample)
AU (1) AU2019211693B2 (enExample)
CA (1) CA3089150A1 (enExample)
WO (1) WO2019144912A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102769880B1 (ko) 2018-01-25 2025-02-20 쑤저우 시노벤트 파마슈티칼즈 씨오., 엘티디. β-락타마제 억제제 및 그 용도
CA3238268A1 (en) 2021-11-17 2023-05-25 Xufan WANG ?-lactamase inhibitor intermediate and preparation method therefor
CN117186107A (zh) * 2022-05-31 2023-12-08 成都先导药物开发股份有限公司 一种制备2-取代-5,7-二羰基-2,6-二氮杂螺[3,4]辛烷中间体的方法
WO2024160247A1 (zh) 2023-02-02 2024-08-08 苏州信诺维医药科技股份有限公司 含β-内酰胺酶抑制剂的药物组合物及其应用
CN116730941B (zh) * 2023-06-15 2024-07-02 广东省科学院微生物研究所(广东省微生物分析检测中心) 5-苯基-1,3,4-恶二唑类化合物及其制备方法和应用
CN118453513B (zh) * 2024-05-23 2025-06-17 苏州信诺维医药科技股份有限公司 一种β-内酰胺酶抑制剂液体制剂的制备工艺

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011510012A (ja) 2008-01-18 2011-03-31 メルク・シャープ・エンド・ドーム・コーポレイション β−ラクタマーゼ阻害剤
WO2014141132A1 (en) 2013-03-14 2014-09-18 Naeja Pharmaceutical Inc. NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS
JP2014525434A (ja) 2011-08-30 2014-09-29 ウォックハート リミテッド １，６−ジアザビシクロ［３，２，１］オクタン−７−オン誘導体および細菌感染の処置におけるそれらの使用
JP2015512419A (ja) 2012-03-30 2015-04-27 キュービスト ファーマシューティカルズ， インコーポレイテッド イソオキザゾールβ−ラクタマーゼ阻害剤
JP2015514095A (ja) 2012-03-30 2015-05-18 キュービスト ファーマシューティカルズ， インコーポレイテッド １，３，４−オキサジアゾールおよび１，３，４−チアジアゾールβ−ラクタマーゼ阻害剤

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US1098129A (en) 1910-04-05 1914-05-26 John Thomas Simpson Aeroplane.
US1033000A (en) 1910-12-14 1912-07-16 Joseph Leslie Forster Pneumatic piano-player.
US1337809A (en) 1917-06-22 1920-04-20 Winton Alexander Protecting means for vessels
CN106211771A (zh) 2014-01-21 2016-12-07 沃克哈特有限公司 含氮化合物及其作为抗菌剂的用途
IN2014MU01196A (enExample) 2014-03-29 2015-10-02 Wockhardt Ltd
EP3131583A1 (en) 2014-04-18 2017-02-22 The Wockhardt Limited Pharmaceutical compositions comprising antibacterial agents
WO2015173663A1 (en) 2014-05-14 2015-11-19 Wockhardt Limited A process for preparation of trans-sulfuric acid mono-{2-[5-(2-methylamino-ethyl)-[1,3,4]-oxadiazol-2-yl]-7-oxo-1,6-diaza-bicyclo [3.2.1]oct-6-yl} ester
WO2015173665A1 (en) 2014-05-14 2015-11-19 Wockhardt Limited A process for preparation of trans-sulfuric acid mono-{2-[5-(3-azetidinylamino)-methyl-[1,3,4]- oxadiazol-2-yl]-7-oxo-1,6-diazabicyclo[3.2.1] oct-6-yl} ester trifluoroacetate
CN108137567A (zh) 2015-10-02 2018-06-08 乐高化学生物科学股份有限公司 用于抑制β-内酰胺酶的组合物和方法
KR102769880B1 (ko) 2018-01-25 2025-02-20 쑤저우 시노벤트 파마슈티칼즈 씨오., 엘티디. β-락타마제 억제제 및 그 용도

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011510012A (ja) 2008-01-18 2011-03-31 メルク・シャープ・エンド・ドーム・コーポレイション β−ラクタマーゼ阻害剤
JP2014525434A (ja) 2011-08-30 2014-09-29 ウォックハート リミテッド １，６−ジアザビシクロ［３，２，１］オクタン−７−オン誘導体および細菌感染の処置におけるそれらの使用
JP2015512419A (ja) 2012-03-30 2015-04-27 キュービスト ファーマシューティカルズ， インコーポレイテッド イソオキザゾールβ−ラクタマーゼ阻害剤
JP2015514095A (ja) 2012-03-30 2015-05-18 キュービスト ファーマシューティカルズ， インコーポレイテッド １，３，４−オキサジアゾールおよび１，３，４−チアジアゾールβ−ラクタマーゼ阻害剤
WO2014141132A1 (en) 2013-03-14 2014-09-18 Naeja Pharmaceutical Inc. NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS

Also Published As

Publication number Publication date
KR20200113247A (ko) 2020-10-06
US11078202B2 (en) 2021-08-03
WO2019144912A1 (zh) 2019-08-01
CN111670187A (zh) 2020-09-15
CA3089150A1 (en) 2019-01-24
US20210032260A1 (en) 2021-02-04
AU2019211693A1 (en) 2020-09-03
JP2021511351A (ja) 2021-05-06
CN111670187B (zh) 2021-04-16
AU2019211693B2 (en) 2023-12-21
EP3744722A4 (en) 2021-11-03
EP3744722A1 (en) 2020-12-02
KR102769880B1 (ko) 2025-02-20

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