AU2016371600B2 - Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections - Google Patents

Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections Download PDF

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Publication number
AU2016371600B2
AU2016371600B2 AU2016371600A AU2016371600A AU2016371600B2 AU 2016371600 B2 AU2016371600 B2 AU 2016371600B2 AU 2016371600 A AU2016371600 A AU 2016371600A AU 2016371600 A AU2016371600 A AU 2016371600A AU 2016371600 B2 AU2016371600 B2 AU 2016371600B2
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tert
mmol
amino
alkyl
optionally substituted
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AU2016371600A1 (en
Inventor
Tesfaye Biftu
Linda Brockunier
Helen Chen
Fa-Xiang Ding
Yan Guo
Xianhai Huang
Jinlong Jiang
Weiguo Liu
Rudrajit MAL
Anthony Ogawa
Weidong Pan
Min Park
Christopher W. Plummer
Wanying Sun
Haifeng Tang
Hongwu Wang
Yi Zang
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Merck Sharp & Dohme LLC
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Merck Sharp & Dohme LLC
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Assigned to MERCK SHARP & DOHME LLC reassignment MERCK SHARP & DOHME LLC Request to Amend Deed and Register Assignors: MERCK SHARP & DOHME CORP.
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    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic 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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • A61K31/41—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (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)
AU2016371600A 2015-12-15 2016-12-12 Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections Active AU2016371600B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562267855P 2015-12-15 2015-12-15
US62/267,855 2015-12-15
PCT/US2016/066064 WO2017106064A1 (en) 2015-12-15 2016-12-12 Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

Publications (2)

Publication Number Publication Date
AU2016371600A1 AU2016371600A1 (en) 2018-05-10
AU2016371600B2 true AU2016371600B2 (en) 2021-02-18

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AU2016371600A Active AU2016371600B2 (en) 2015-12-15 2016-12-12 Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

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US (2) US20180339983A1 (enExample)
EP (2) EP3390357B1 (enExample)
JP (1) JP7184646B2 (enExample)
KR (1) KR20180093925A (enExample)
CN (1) CN108368040B (enExample)
AU (1) AU2016371600B2 (enExample)
CA (1) CA3008006C (enExample)
MA (1) MA44083A (enExample)
MX (1) MX385731B (enExample)
RU (1) RU2746129C2 (enExample)
WO (1) WO2017106064A1 (enExample)

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AU2012340107B2 (en) 2011-11-18 2017-06-15 Regeneron Pharmaceuticals, Inc. Polymer protein microparticles
KR102722949B1 (ko) 2015-06-15 2024-10-28 엔엠디 파마 에이/에스 신경근 장애의 치료에 사용하기 위한 화합물
AU2016371600B2 (en) 2015-12-15 2021-02-18 Merck Sharp & Dohme Llc Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
GEAP202215303A (en) * 2017-10-02 2022-04-11 Merck Sharp & Dohme Chromane monobactam compounds for the treatment of bacterial infections
US10385028B2 (en) 2017-12-14 2019-08-20 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US11730714B2 (en) 2017-12-14 2023-08-22 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US12440477B2 (en) 2017-12-14 2025-10-14 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US11147788B2 (en) 2017-12-14 2021-10-19 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
US11591284B2 (en) 2017-12-14 2023-02-28 Nmd Pharma A/S Compounds for the treatment of neuromuscular disorders
CN108362789B (zh) * 2018-01-19 2020-09-01 珠海优润医药科技有限公司 一种阿维巴坦钠光学异构体的高效液相色谱检测方法
EP3747883A4 (en) * 2018-01-29 2020-12-16 Medshine Discovery Inc. MONOCYCLIC B-LACTAM COMPOUND FOR TREATING BACTERIAL INFECTION
WO2020048827A1 (en) 2018-09-03 2020-03-12 Bayer Aktiengesellschaft 1, 3, 9-triazaspiro[5.5] undecan-2-one compounds
WO2020048828A1 (en) 2018-09-03 2020-03-12 Bayer Pharma Aktiengesellschaft 5-heteroaryl-3,9-diazaspiro[5.5]undecane compounds
US20220002288A1 (en) * 2018-11-13 2022-01-06 Nanjing Sanhome Pharmaceutical Co., Ltd. Monobactam compounds and use therefor
AU2019387370A1 (en) 2018-11-30 2021-06-10 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
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
US12516048B2 (en) 2020-08-06 2026-01-06 Ningxia Academy Of Agriculture And Forestry Sciences B-lactam compounds, their preparation and use as antibacterial agents
CN112661667B (zh) * 2020-12-28 2023-02-03 浦拉司科技（上海）有限责任公司 一种三氟乙脒的制备方法
CN113975396B (zh) * 2021-11-09 2022-11-29 中国医学科学院医药生物技术研究所 包含β-内酰胺类化合物的药物组合物及其用途
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
JP7671398B2 (ja) * 2021-11-18 2025-05-01 メルク・シャープ・アンド・ドーム・エルエルシー クロマンアミジンモノバクタム抗生物質
CR20240212A (es) 2021-11-18 2024-07-01 Merck Sharp & Dohme Llc Compuestos monobactámicos de cromano amidina para tratar las infecciones bacterianas
CN114671910B (zh) * 2022-04-06 2025-03-21 河南师范大学 一种西多福韦的绿色合成方法

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US20150045340A1 (en) * 2012-01-24 2015-02-12 Aicuris Gmbh & Co. Kg Amidine substituted beta-lactam compounds, their preparation and use as antibacterial agents

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WO2015103583A1 (en) 2014-01-06 2015-07-09 President And Fellows Of Harvard College Monobactams and methods of their synthesis and use
HUE042134T2 (hu) * 2014-03-24 2019-06-28 Novartis Ag Monobaktám szerves vegyületek bakteriális fertõzések kezelésére
AU2016371600B2 (en) 2015-12-15 2021-02-18 Merck Sharp & Dohme Llc Biaryl monobactam compounds and methods of use thereof for the treatment of bacterial infections

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Also Published As

Publication number Publication date
JP7184646B2 (ja) 2022-12-06
EP3390357B1 (en) 2021-11-10
EP3978472B1 (en) 2024-10-16
MA44083A (fr) 2021-06-02
AU2016371600A1 (en) 2018-05-10
CN108368040B (zh) 2024-08-23
CN108368040A (zh) 2018-08-03
JP2018537483A (ja) 2018-12-20
RU2746129C2 (ru) 2021-04-07
WO2017106064A1 (en) 2017-06-22
EP3390357A4 (en) 2019-06-12
MX2018005382A (es) 2018-08-16
BR112018010962A8 (pt) 2023-04-11
CA3008006A1 (en) 2017-06-22
US20200361928A1 (en) 2020-11-19
MX385731B (es) 2025-03-18
KR20180093925A (ko) 2018-08-22
EP3978472A1 (en) 2022-04-06
BR112018010962A2 (pt) 2018-12-04
EP3390357A1 (en) 2018-10-24
RU2018123484A (ru) 2020-01-17
US20180339983A1 (en) 2018-11-29
RU2018123484A3 (enExample) 2020-03-26
US11230543B2 (en) 2022-01-25
CA3008006C (en) 2024-04-09

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