EA202190167A1 - Замещенные фенилоксазолидиноны для антимикробной терапии - Google Patents

Замещенные фенилоксазолидиноны для антимикробной терапии

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Publication number
EA202190167A1
EA202190167A1 EA202190167A EA202190167A EA202190167A1 EA 202190167 A1 EA202190167 A1 EA 202190167A1 EA 202190167 A EA202190167 A EA 202190167A EA 202190167 A EA202190167 A EA 202190167A EA 202190167 A1 EA202190167 A1 EA 202190167A1
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EA
Eurasian Patent Office
Prior art keywords
antimicrobial therapy
substituted phenyloxazolidinones
phenyloxazolidinones
substituted
spirocyclic
Prior art date
Application number
EA202190167A
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English (en)
Inventor
Кристофер Б. Купер
Хайхун Хуан
Дунфэн Чжан
Надер Фотухи
Такуси Канеко
Original Assignee
Зе Глобал Эллайенс Фо Тб Драг Девелопмент, Инк.
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Application filed by Зе Глобал Эллайенс Фо Тб Драг Девелопмент, Инк. filed Critical Зе Глобал Эллайенс Фо Тб Драг Девелопмент, Инк.
Publication of EA202190167A1 publication Critical patent/EA202190167A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/554Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
    • 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
    • A61P31/06Antibacterial agents for tuberculosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18Oxygen atoms
    • C07D263/20Oxygen atoms attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18Oxygen atoms
    • C07D263/20Oxygen atoms attached in position 2
    • C07D263/24Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/10Heterocyclic 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 two hetero rings linked by a carbon chain containing aromatic rings
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    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
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    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems
    • C07D491/107Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08Bridged systems
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/10Spiro-condensed systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08Bridged systems

Abstract

Изобретение относится к новым оксазолидинонам (формула I)или их фармацевтически приемлемым солям, содержащим кольцо А, характеризующееся N-содержащими моноциклическими, бициклическими или спироциклическими заместителями, к их получению и их применению в качестве лекарственных средств для лечения Mycobacterium tuberculosis и других микробных инфекций, отдельно или в комбинации с другими противоинфекционными средствами лечения.
EA202190167A 2015-07-17 2016-07-15 Замещенные фенилоксазолидиноны для антимикробной терапии EA202190167A1 (ru)

Applications Claiming Priority (1)

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US201562193963P 2015-07-17 2015-07-17

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EA202190167A1 true EA202190167A1 (ru) 2021-07-30

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EA202190167A EA202190167A1 (ru) 2015-07-17 2016-07-15 Замещенные фенилоксазолидиноны для антимикробной терапии
EA201792566A EA037643B1 (ru) 2015-07-17 2016-07-15 Замещенные фенилоксазолидиноны для антимикробной терапии

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US (2) US10550092B2 (ru)
EP (2) EP3932917A3 (ru)
JP (4) JP6786598B2 (ru)
KR (1) KR102511898B1 (ru)
CN (2) CN108348507B (ru)
AU (3) AU2016295165B2 (ru)
BR (1) BR112018000991A2 (ru)
CA (1) CA2990260A1 (ru)
EA (2) EA202190167A1 (ru)
ES (1) ES2897973T3 (ru)
HK (1) HK1255105A1 (ru)
WO (1) WO2017015106A1 (ru)
ZA (1) ZA201800189B (ru)

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KR102511898B1 (ko) * 2015-07-17 2023-03-20 더 글로벌 얼라이언스 포 티비 드러그 디벨롭먼트, 잉크. 항미생물 요법을 위한 치환된 페닐옥사졸리디논
CN108727406B (zh) * 2017-03-28 2021-12-07 北京协和制药二厂 含氮杂环取代的苯并噁嗪噁唑烷酮类化合物及其制备方法和用途
CN112543756A (zh) 2018-07-25 2021-03-23 卡迪拉保健有限公司 用于治疗哺乳动物感染的经取代噁唑烷酮类
WO2020147504A1 (en) * 2019-01-18 2020-07-23 Merck Sharp & Dohme Corp. Oxazolidinone compounds and methods of use thereof as antibacterial agents
WO2020234636A1 (en) 2019-05-17 2020-11-26 Cadila Healthcare Limited Novel compounds for the treatment of mammalian infections
CN110922411B (zh) * 2019-11-27 2021-06-04 合肥远志医药科技开发有限公司 一种药物中间体的合成方法
WO2021184339A1 (en) * 2020-03-20 2021-09-23 Merck Sharp & Dohme Corp. Oxazolidinone compound and methods of use thereof as an antibacterial agent
CN113999152B (zh) * 2021-07-14 2023-05-09 上海凌富药物研究有限公司 一种顺式-1-苄基-2,4-二烷氧基羰基氮杂环丁烷的合成方法
WO2024035618A1 (en) * 2022-08-10 2024-02-15 Merck Sharp & Dohme Llc Processes for preparing oxazolidinone compounds

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NZ738702A (en) 2023-09-29
JP6786598B2 (ja) 2020-11-18
KR102511898B1 (ko) 2023-03-20
AU2021205116B2 (en) 2022-11-10
ES2897973T3 (es) 2022-03-03
EP3307268A1 (en) 2018-04-18
US20200148651A1 (en) 2020-05-14
CN108348507A (zh) 2018-07-31
US10550092B2 (en) 2020-02-04
JP2020122016A (ja) 2020-08-13
AU2016295165B2 (en) 2021-04-22
EP3932917A3 (en) 2022-03-30
EA037643B1 (ru) 2021-04-26
JP7232212B2 (ja) 2023-03-02
CA2990260A1 (en) 2017-01-26
US11964949B2 (en) 2024-04-23
US20180179168A1 (en) 2018-06-28
KR20180026491A (ko) 2018-03-12
AU2022268387A1 (en) 2022-12-15
AU2021205116A1 (en) 2021-08-12
AU2016295165A1 (en) 2018-01-25
EP3307268B1 (en) 2021-09-01
JP2018524406A (ja) 2018-08-30
JP2021183647A (ja) 2021-12-02
EP3307268A4 (en) 2019-01-09
BR112018000991A2 (pt) 2018-12-04
CN108348507B (zh) 2021-10-08
CN113603683A (zh) 2021-11-05
JP2023133610A (ja) 2023-09-22
EA201792566A1 (ru) 2018-10-31
WO2017015106A1 (en) 2017-01-26
HK1255105A1 (zh) 2019-08-02
EP3932917A2 (en) 2022-01-05
ZA201800189B (en) 2019-06-26

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