CN108778273B - 二环芳基单环β-内酰胺化合物及其用于治疗细菌感染的用途的方法 - Google Patents

二环芳基单环β-内酰胺化合物及其用于治疗细菌感染的用途的方法 Download PDF

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CN108778273B
CN108778273B CN201780015430.2A CN201780015430A CN108778273B CN 108778273 B CN108778273 B CN 108778273B CN 201780015430 A CN201780015430 A CN 201780015430A CN 108778273 B CN108778273 B CN 108778273B
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tert
amino
mmol
compound
pharmaceutically acceptable
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CN108778273A (zh
Inventor
刘卫国
F-X.丁
孙万莺
R.K.德吉泽斯
唐海峰
X.黄
J.简
郭燕
H.王
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Merck Sharp & Dohme BV
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Merck Sharp & Dohme LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
    • C07C53/16—Halogenated acetic acids
    • C07C53/18—Halogenated acetic acids containing fluorine
    • 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
    • C07D471/04—Ortho-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
    • A61K31/431—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 containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201780015430.2A 2016-03-07 2017-03-02 二环芳基单环β-内酰胺化合物及其用于治疗细菌感染的用途的方法 Active CN108778273B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662304447P 2016-03-07 2016-03-07
US62/304447 2016-03-07
PCT/US2017/020303 WO2017155765A1 (en) 2016-03-07 2017-03-02 Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

Publications (2)

Publication Number Publication Date
CN108778273A CN108778273A (zh) 2018-11-09
CN108778273B true CN108778273B (zh) 2022-06-17

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Country Link
US (1) US10407421B2 (enExample)
EP (1) EP3426248B1 (enExample)
JP (1) JP7034929B2 (enExample)
KR (1) KR102408800B1 (enExample)
CN (1) CN108778273B (enExample)
AU (1) AU2017228870B2 (enExample)
BR (1) BR112018067930B1 (enExample)
CA (1) CA3016341A1 (enExample)
MA (1) MA43811A (enExample)
MX (1) MX2018010878A (enExample)
RU (1) RU2733402C2 (enExample)
WO (1) WO2017155765A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10407421B2 (en) 2016-03-07 2019-09-10 Merck Sharp & Dohme Corp Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
MX2019010302A (es) 2017-03-30 2019-11-21 Hoffmann La Roche Isoquinolinas como inhibidores de hpk1.
GEAP202215303A (en) * 2017-10-02 2022-04-11 Merck Sharp & Dohme Chromane monobactam compounds for the treatment of bacterial infections
EP3747883A4 (en) * 2018-01-29 2020-12-16 Medshine Discovery Inc. MONOCYCLIC B-LACTAM COMPOUND FOR TREATING BACTERIAL INFECTION
JP7386841B2 (ja) 2018-07-24 2023-11-27 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト イソキノリン化合物及びその使用
TW202024053A (zh) 2018-10-02 2020-07-01 美商建南德克公司 異喹啉化合物及其用途
TW202023558A (zh) 2018-10-03 2020-07-01 美商建南德克公司 8-胺基異喹啉化合物及其用途
US20220002288A1 (en) * 2018-11-13 2022-01-06 Nanjing Sanhome Pharmaceutical Co., Ltd. Monobactam compounds and use therefor
WO2020125670A1 (zh) * 2018-12-18 2020-06-25 南京明德新药研发有限公司 单环β-内酰胺化合物在制药中的应用
CN110963967B (zh) * 2019-11-25 2021-02-12 武汉智顿科技发展有限公司 一种2-甲基-4-氨基喹啉的制备方法
CN111018777B (zh) * 2019-11-25 2021-02-12 武汉智顿科技发展有限公司 一种地喹氯铵的制备方法
CN111303144B (zh) * 2019-12-13 2020-11-27 苏州信诺维医药科技有限公司 一种治疗细菌感染的化合物
US12491180B2 (en) 2019-12-19 2025-12-09 Shenzhen Optimum Biological Technology Co., Ltd Application of compound in treating pneumonia
WO2022047603A1 (en) 2020-09-01 2022-03-10 Ningxia Academy Of Agriculture And Forestry Sciences Beta-lactamase inhibitors and their preparation
US11780832B2 (en) 2021-03-31 2023-10-10 Fedora Pharmaceuticals Inc. Lactivicin compounds, their preparation and use as antibacterial agents
US12410166B2 (en) 2021-05-07 2025-09-09 Ningxia Academy Of Agriculture And Forestry Sciences Sulfonylamidine substituted compounds and their use as beta-lactamase inhibitors
US20240390335A1 (en) * 2021-11-09 2024-11-28 Institute Of Medicinal Biotechnology, Chinese Academy Of Medical Sciences Pharmaceutical composition containing beta-lactam compound and use thereof
KR20250093507A (ko) * 2022-11-07 2025-06-24 고쿠리츠 다이가쿠 호진 교토 다이가쿠 퀴나졸린 유도체
CN121955228A (zh) * 2025-12-31 2026-05-01 北京大学人民医院 同时检测亚胺培南、雷利巴坦和西司他丁的方法及其应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0531976A1 (en) * 1991-09-09 1993-03-17 E.R. SQUIBB & SONS, INC. Heteroaryl derivatives of monocyclic beta-lactam antibiotics
WO2013110643A1 (en) * 2012-01-24 2013-08-01 Aicuris Gmbh & Co. Kg Amidine substituted beta - lactam compounds, their preparation and use as antibacterial agents

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4684722A (en) 1986-01-06 1987-08-04 E. R. Squibb & Sons, Inc. Monosulfactams
MY127641A (en) 1995-10-12 2006-12-29 Essential Therapeutics Inc Cephalosporin antibiotics
RU2269525C2 (ru) * 2000-08-10 2006-02-10 Бритиш Биотех Фармасьютикалс Лимитед Антибактериальные агенты
KR101403164B1 (ko) 2005-12-07 2014-06-03 바실리어 파마슈티카 아게 베타-락타마아제 저해제 및 모노박탐 항생물질의 유용한조합
CA2691987C (en) 2007-06-12 2016-08-16 Achaogen, Inc. Antibacterial agents
JP5777725B2 (ja) 2010-11-29 2015-09-09 ファイザー・インク モノバクタム
US20140275007A1 (en) 2013-03-14 2014-09-18 Rempex Pharmaceuticals, Inc. Oxamazin antibiotics
HUE042134T2 (hu) 2014-03-24 2019-06-28 Novartis Ag Monobaktám szerves vegyületek bakteriális fertõzések kezelésére
US10407421B2 (en) 2016-03-07 2019-09-10 Merck Sharp & Dohme Corp Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0531976A1 (en) * 1991-09-09 1993-03-17 E.R. SQUIBB & SONS, INC. Heteroaryl derivatives of monocyclic beta-lactam antibiotics
WO2013110643A1 (en) * 2012-01-24 2013-08-01 Aicuris Gmbh & Co. Kg Amidine substituted beta - lactam compounds, their preparation and use as antibacterial agents
CN104203237A (zh) * 2012-01-24 2014-12-10 艾库里斯有限及两合公司 脒取代的β-内酰胺化合物、其制备和作为抗菌剂的用途

Also Published As

Publication number Publication date
MX2018010878A (es) 2018-11-09
WO2017155765A1 (en) 2017-09-14
KR20180121948A (ko) 2018-11-09
US10407421B2 (en) 2019-09-10
CA3016341A1 (en) 2017-09-14
JP2019507768A (ja) 2019-03-22
MA43811A (fr) 2018-11-28
EP3426248A1 (en) 2019-01-16
RU2018134948A (ru) 2020-04-08
RU2733402C2 (ru) 2020-10-01
BR112018067930A2 (pt) 2019-01-22
EP3426248A4 (en) 2019-07-10
RU2018134948A3 (enExample) 2020-04-08
US20190071436A1 (en) 2019-03-07
JP7034929B2 (ja) 2022-03-14
AU2017228870B2 (en) 2021-02-18
BR112018067930A8 (pt) 2023-04-11
KR102408800B1 (ko) 2022-06-13
BR112018067930B1 (pt) 2024-02-15
EP3426248B1 (en) 2023-11-15
CN108778273A (zh) 2018-11-09
AU2017228870A1 (en) 2018-09-06

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Patentee before: MERCK SHARP & DOHME Corp.