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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EA
Eurasian Patent Office
Prior art keywords
amino
mmol
methyl
tert
alkyl
Prior art date
Application number
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
Original Assignee
Новартис Аг
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Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201691766A1 publication Critical patent/EA201691766A1/ru
Publication of EA030850B1 publication Critical patent/EA030850B1/ru

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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
    • A61K31/425—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • 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
    • A61K31/495—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
    • 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
    • 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • 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)
  • 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)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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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EA201691766A EA030850B1 (ru) 2014-03-24 2015-03-23 Органические соединения, являющиеся монобактамами, для лечения бактериальных инфекций

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US (4) US9174978B2 (enExample)
EP (2) EP3122745B1 (enExample)
JP (1) JP6153674B2 (enExample)
KR (1) KR101733441B1 (enExample)
CN (1) CN106164072B (enExample)
AP (1) AP2016009374A0 (enExample)
AU (1) AU2015236369B2 (enExample)
BR (1) BR112016020333B1 (enExample)
CA (1) CA2939254C (enExample)
CL (1) CL2016002285A1 (enExample)
CU (1) CU24441B1 (enExample)
CY (1) CY1121701T1 (enExample)
DK (2) DK3511328T3 (enExample)
EA (1) EA030850B1 (enExample)
EC (1) ECSP16073620A (enExample)
ES (2) ES2862203T3 (enExample)
GT (1) GT201600183A (enExample)
HR (1) HRP20190501T1 (enExample)
HU (1) HUE042134T2 (enExample)
IL (1) IL247259B (enExample)
LT (1) LT3122745T (enExample)
MA (1) MA39777B1 (enExample)
MX (1) MX373444B (enExample)
MY (1) MY179292A (enExample)
PE (1) PE20161371A1 (enExample)
PH (1) PH12016501577B1 (enExample)
PL (1) PL3122745T3 (enExample)
PT (1) PT3122745T (enExample)
RS (1) RS58509B1 (enExample)
SG (1) SG11201606711UA (enExample)
SI (1) SI3122745T1 (enExample)
SM (1) SMT201900218T1 (enExample)
SV (1) SV2016005274A (enExample)
TW (1) TWI714525B (enExample)
UA (1) UA121383C2 (enExample)
WO (1) WO2015148379A1 (enExample)
ZA (1) ZA201605565B (enExample)

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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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WO2017081615A1 (en) 2015-11-09 2017-05-18 Wockhardt Limited 7-oxo -6-(sulfooxy)- 1,6-diazabicyclo [3.2.1] octane containing compounds and their use in treatment of bacterial infections
MA44083A (fr) 2015-12-15 2021-06-02 Merck Sharp & Dohme Composés de biarylmonobactame pour le traitement d'infections bactériennes
BR112018067930B1 (pt) 2016-03-07 2024-02-15 Merck Sharp & Dohme Llc Composto, sal de ácido trifluoroacético, composição farmacêutica, e, uso de um composto
US11174260B2 (en) 2017-03-20 2021-11-16 The Broad Institute, 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
AU2018345321B2 (en) * 2017-10-02 2021-05-20 Arixa Pharmaceuticals, Inc. Aztreonam derivatives and uses thereof
AU2018345523B2 (en) 2017-10-02 2021-10-21 Merck Sharp & Dohme Llc Chromane monobactam compounds for the treatment of bacterial infections
WO2019092180A1 (en) * 2017-11-10 2019-05-16 Novartis Ag Administration of monobactam for the treatment of urinary tract infection
WO2019144969A1 (zh) 2018-01-29 2019-08-01 南京明德新药研发股份有限公司 用于治疗细菌感染的单环β-内酰胺化合物
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
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US11905286B2 (en) 2018-08-09 2024-02-20 Antabio Sas Diazabicyclooctanones as inhibitors of serine beta-lactamases
WO2020098635A1 (zh) 2018-11-13 2020-05-22 南京圣和药业股份有限公司 单环内酰胺化合物及其应用
US12310948B2 (en) 2018-12-18 2025-05-27 Shenzhen Optimum Biological Technology Co., Ltd Application of monocyclic β-lactam compound in pharmacy
EP4046998B1 (en) * 2019-11-22 2024-02-28 Suzhou Erye Pharmaceutical Co., Ltd. Sulfonylurea ring substituted monocyclic beta-lactam antibiotics
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
EP4079305A4 (en) 2019-12-19 2024-01-10 Shenzhen Optimum Biological Technology Co., Ltd APPLICATION OF A COMPOUND IN THE PREPARATION OF DRUG
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
WO2022011626A1 (en) * 2020-07-16 2022-01-20 Ningxia Academy Of Agriculture And Forestry Sciences Novel monobactam compounds, their preparation and use as antibacterial agents
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
US20250019376A1 (en) 2021-11-18 2025-01-16 Merck Sharp & Dohme Llc Chromane amidine monobactam antibiotics
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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