CN111670187B - β-内酰胺酶抑制剂及其用途 - Google Patents

β-内酰胺酶抑制剂及其用途 Download PDF

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Publication number
CN111670187B
CN111670187B CN201980010129.1A CN201980010129A CN111670187B CN 111670187 B CN111670187 B CN 111670187B CN 201980010129 A CN201980010129 A CN 201980010129A CN 111670187 B CN111670187 B CN 111670187B
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octane
cyclopropane
oxo
bicyclo
diazaspiro
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Chinese (zh)
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CN111670187A (zh
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吴予川
黄少强
陈曦
胡永韩
刘霄
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Suzhou Sinoway Pharmaceutical Technology Co ltd
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Suzhou Sinovent Pharmaceuticals 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
    • 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
    • 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

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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)
CN201980010129.1A 2018-01-25 2019-01-24 β-内酰胺酶抑制剂及其用途 Active CN111670187B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2018074185 2018-01-25
CNPCT/CN2018/074185 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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CN111670187A CN111670187A (zh) 2020-09-15
CN111670187B true CN111670187B (zh) 2021-04-16

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

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
EP4659750A1 (en) 2023-02-02 2025-12-10 Evopoint Biosciences Co., Ltd. PHARMACEUTICAL COMPOSITION CONTAINING ß-LACTAMASE INHIBITOR AND USE THEREOF
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
CN101918407A (zh) * 2008-01-18 2010-12-15 默沙东公司 β-内酰胺酶抑制剂
CN103649088A (zh) * 2011-08-30 2014-03-19 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
WO2014141132A1 (en) * 2013-03-14 2014-09-18 Naeja Pharmaceutical Inc. NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS
CN104334555A (zh) * 2012-03-30 2015-02-04 丘比斯特药物股份有限公司 异噁唑β-内酰胺酶抑制剂
WO2015150890A1 (en) * 2014-03-29 2015-10-08 Wockhardt Limited A process for preparation of trans-sulfuric acid mono-{2-(5-(3-amino-propyl)-[1,3,4]oxadiazol-2-yl]-7-oxo-1,6-diazabicyclo [3.2.1] oct-6-yl}ester

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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
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
US9822115B2 (en) 2014-01-21 2017-11-21 Wockhardt Limited Nitrogen containing compounds and their use as antibacterial agents
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
CA3000087A1 (en) 2015-10-02 2017-04-06 Legochem Biosciences, Inc. Compositions and methods for inhibiting beta-lactamase
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
CN101918407A (zh) * 2008-01-18 2010-12-15 默沙东公司 β-内酰胺酶抑制剂
CN103649088A (zh) * 2011-08-30 2014-03-19 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
CN104334555A (zh) * 2012-03-30 2015-02-04 丘比斯特药物股份有限公司 异噁唑β-内酰胺酶抑制剂
WO2014141132A1 (en) * 2013-03-14 2014-09-18 Naeja Pharmaceutical Inc. NEW HETEROCYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND β-LACTAMASE INHIBITORS
WO2015150890A1 (en) * 2014-03-29 2015-10-08 Wockhardt Limited A process for preparation of trans-sulfuric acid mono-{2-(5-(3-amino-propyl)-[1,3,4]oxadiazol-2-yl]-7-oxo-1,6-diazabicyclo [3.2.1] oct-6-yl}ester

Also Published As

Publication number Publication date
AU2019211693A1 (en) 2020-09-03
AU2019211693B2 (en) 2023-12-21
EP3744722A1 (en) 2020-12-02
KR102769880B1 (ko) 2025-02-20
WO2019144912A1 (zh) 2019-08-01
CN111670187A (zh) 2020-09-15
CA3089150A1 (en) 2019-01-24
US20210032260A1 (en) 2021-02-04
JP7273420B2 (ja) 2023-05-15
JP2021511351A (ja) 2021-05-06
KR20200113247A (ko) 2020-10-06
EP3744722A4 (en) 2021-11-03
US11078202B2 (en) 2021-08-03

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Address after: 215127 building 22, area B, phase II, bio Industrial Park, 218 Sangtian street, Suzhou Industrial Park, Suzhou City, Jiangsu Province

Patentee after: Suzhou Sinoway Pharmaceutical Technology Co.,Ltd.

Address before: 215127 building 22, area B, phase II, bio Industrial Park, 218 Sangtian street, Suzhou Industrial Park, Suzhou City, Jiangsu Province

Patentee before: Suzhou Sinovent Pharmaceuticals Co.,Ltd.