EA030850B1 - Органические соединения, являющиеся монобактамами, для лечения бактериальных инфекций - Google Patents

Органические соединения, являющиеся монобактамами, для лечения бактериальных инфекций Download PDF

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Publication number
EA030850B1
EA030850B1 EA201691766A EA201691766A EA030850B1 EA 030850 B1 EA030850 B1 EA 030850B1 EA 201691766 A EA201691766 A EA 201691766A EA 201691766 A EA201691766 A EA 201691766A EA 030850 B1 EA030850 B1 EA 030850B1
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Eurasian Patent Office
Prior art keywords
amino
mmol
methyl
tert
alkyl
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EA201691766A
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English (en)
Russian (ru)
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EA201691766A1 (ru
Inventor
Вирендер Сингх Аулакх
Энтони Казаре
Сяодун Лин
Мика Линдвалль
Глен Макинрой
Хейнц Эрнст Моузер
Фолькерт Рек
Меилиана Тжандра
Роберт Лоуэлл Симмонс
Арегахегн Йифру
Цинмин Чжу
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Новартис Аг
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Publication of EA201691766A1 publication Critical patent/EA201691766A1/ru
Publication of EA030850B1 publication Critical patent/EA030850B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/433Thidiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EA201691766A 2014-03-24 2015-03-23 Органические соединения, являющиеся монобактамами, для лечения бактериальных инфекций EA030850B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461969735P 2014-03-24 2014-03-24
US201462088304P 2014-12-05 2014-12-05
PCT/US2015/022011 WO2015148379A1 (en) 2014-03-24 2015-03-23 Monobactam organic compounds for the treatment of bacterial infections

Publications (2)

Publication Number Publication Date
EA201691766A1 EA201691766A1 (ru) 2016-12-30
EA030850B1 true EA030850B1 (ru) 2018-10-31

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US (4) US9174978B2 (cg-RX-API-DMAC7.html)
EP (2) EP3511328B1 (cg-RX-API-DMAC7.html)
JP (1) JP6153674B2 (cg-RX-API-DMAC7.html)
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US10919887B2 (en) 2015-09-23 2021-02-16 Novartis Ag Salts and solid forms of a monobactam antibiotic
US11414411B2 (en) 2017-08-02 2022-08-16 Novartis Ag Chemical process for manufacturing monobactam antibiotic and intermediates thereof

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US20180282331A1 (en) 2015-11-09 2018-10-04 Wockhardt Limited 7-Oxo -6-(sulfooxy)- 1,6-diazabicyclo [3.2.1] octane containing compounds and their use in treatment of bacterial infections (changed by PCT to: 7-OXO -6-(SULFOOXY)- 1,6-DIAZABICYCLO [3.2.1] OCTANE CONTAINING COMPOUNDS AND THEIR USE IN TREATMENT OF BACTERIAL INFECTIONS
JP7184646B2 (ja) * 2015-12-15 2022-12-06 メルク・シャープ・アンド・ドーム・エルエルシー ビアリールモノバクタム化合物および細菌感染治療のためのそれの使用方法
MX2018010878A (es) 2016-03-07 2018-11-09 Merck Sharp & Dohme Compuestos de aril-monobactam biciclicos y metodos de uso de los mismos para el tratamiento de infecciones bacterianas.
IL269390B (en) 2017-03-20 2022-08-01 Broad Inst Inc Compounds and methods for the treatment of parasitic diseases
WO2019058346A1 (en) * 2017-09-22 2019-03-28 Novartis Ag MONOBACTAM ADMINISTRATION IN ASSOCIATION WITH ANTIBIOTIC AGENT FOR THE TREATMENT OF COMPLICATED INTRA-ABDOMINAL INFECTION
KR102455390B1 (ko) * 2017-10-02 2022-10-17 아릭사 파마슈티컬스 인코포레이티드 아즈트레오남 유도체 및 이의 용도
MX2020003581A (es) 2017-10-02 2020-07-22 Merck Sharp & Dohme Compuestos monobactamicos cromanos para el tratamiento de infecciones bacterianas.
WO2019092180A1 (en) * 2017-11-10 2019-05-16 Novartis Ag Administration of monobactam for the treatment of urinary tract infection
JP7280273B2 (ja) 2018-01-29 2023-05-23 メッドシャイン ディスカバリー インコーポレイテッド 細菌感染を治療するための単環β-ラクタム化合物
KR102017784B1 (ko) * 2018-04-11 2019-09-03 전북대학교산학협력단 민감성 및 선택성을 개선한 캠필로박터 검출용 배지 조성물 및 이를 이용한 캠필로박터 검출방법
KR102017785B1 (ko) * 2018-05-17 2019-09-03 전북대학교산학협력단 민감성 및 선택성을 개선한 캠필로박터 선택증균용 배지 조성물 및 이를 이용한 캠필로박터 검출방법
US11905286B2 (en) 2018-08-09 2024-02-20 Antabio Sas Diazabicyclooctanones as inhibitors of serine beta-lactamases
FI3833665T3 (fi) 2018-08-09 2023-10-09 Antabio Sas Diatsabisyklo-oktanoneja seriini-beeta-laktamaasien inhibiittoreina
US20220002288A1 (en) 2018-11-13 2022-01-06 Nanjing Sanhome Pharmaceutical Co., Ltd. Monobactam compounds and use therefor
US12310948B2 (en) 2018-12-18 2025-05-27 Shenzhen Optimum Biological Technology Co., Ltd Application of monocyclic β-lactam compound in pharmacy
CN114787158B (zh) * 2019-11-22 2023-10-24 苏州二叶制药有限公司 磺酰脲环取代的单环β-内酰胺类抗生素
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
WO2021121387A1 (zh) 2019-12-19 2021-06-24 南京明德新药研发有限公司 化合物在制药中的应用
EP3838266A1 (en) 2019-12-20 2021-06-23 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Microfluidic production of biofunctionalized giant unilamellar vesicles for targeted intracellular cargo delivery
CN113754651B (zh) * 2020-06-02 2023-04-18 中国医学科学院医药生物技术研究所 一种β-内酰胺化合物、其用途及其制备方法
CN115210231B (zh) * 2020-07-16 2024-10-08 宁夏农林科学院 单环内酰胺类化合物、其制备方法及其作为抗菌药的用途
WO2022185240A1 (en) 2021-03-04 2022-09-09 Bp Asset Vi, Inc. Formulation of a monobactam antibiotic
WO2022185241A1 (en) 2021-03-04 2022-09-09 Bp Asset Vi, Inc. Process for manufacturing a monobactam antibiotic
KR20240105442A (ko) * 2021-11-18 2024-07-05 머크 샤프 앤드 돔 엘엘씨 크로만 아미딘 모노박탐 항생제
CN115304594B (zh) 2022-10-12 2023-02-14 苏州二叶制药有限公司 磺酰脲环取代的化合物的盐型及其晶型

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