KR102769880B1 - β-락타마제 억제제 및 그 용도 - Google Patents

β-락타마제 억제제 및 그 용도 Download PDF

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KR102769880B1
KR102769880B1 KR1020207024397A KR20207024397A KR102769880B1 KR 102769880 B1 KR102769880 B1 KR 102769880B1 KR 1020207024397 A KR1020207024397 A KR 1020207024397A KR 20207024397 A KR20207024397 A KR 20207024397A KR 102769880 B1 KR102769880 B1 KR 102769880B1
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octane
diazaspiro
bicyclo
cyclopropane
oxo
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KR20200113247A (ko
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유추안 우
샤오치앙 후앙
시 첸
용한 후
시아오 리우
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쑤저우 시노벤트 파마슈티칼즈 씨오., 엘티디.
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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
    • C07D471/10—Spiro-condensed 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
    • C07D471/08—Bridged 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)
KR1020207024397A 2018-01-25 2019-01-24 β-락타마제 억제제 및 그 용도 Active KR102769880B1 (ko)

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

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KR20200113247A KR20200113247A (ko) 2020-10-06
KR102769880B1 true KR102769880B1 (ko) 2025-02-20

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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 (1)

* Cited by examiner, † Cited by third party
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WO2014141132A1 (en) * 2013-03-14 2014-09-18 Naeja Pharmaceutical Inc. NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS

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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
JP5038509B2 (ja) * 2008-01-18 2012-10-03 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
CN103649088B (zh) * 2011-08-30 2016-05-11 沃克哈特有限公司 1, 6- 二氮杂双环[3, 2, 1]辛- 7- 酮衍生物及其在治疗细菌感染中的用途
TW201343645A (zh) 2012-03-30 2013-11-01 Cubist Pharm Inc １，３，４－□二唑及１，３，４－噻二唑β－內醯胺酶抑制劑
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
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

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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
JP7273420B2 (ja) 2023-05-15
EP3744722A4 (en) 2021-11-03
EP3744722A1 (en) 2020-12-02

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