EA200870564A1 - Новые производные бензотиазинона и их применение в качестве антибактериальных средств - Google Patents

Новые производные бензотиазинона и их применение в качестве антибактериальных средств

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Publication number
EA200870564A1
EA200870564A1 EA200870564A EA200870564A EA200870564A1 EA 200870564 A1 EA200870564 A1 EA 200870564A1 EA 200870564 A EA200870564 A EA 200870564A EA 200870564 A EA200870564 A EA 200870564A EA 200870564 A1 EA200870564 A1 EA 200870564A1
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Eurasian Patent Office
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saturated
independently
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application
halogenated
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EA200870564A
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EA015910B1 (ru
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Вадим А. Макаров
Стюарт Т. Коул
Уте Мелльманн
Original Assignee
Ляйбниц Инститьют Фор Нэчерал Продакт Ресерч Энд Инфекшн Байолоджи Э. Ф. Ханс-Кнелль-Институт (Хки)
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Application filed by Ляйбниц Инститьют Фор Нэчерал Продакт Ресерч Энд Инфекшн Байолоджи Э. Ф. Ханс-Кнелль-Институт (Хки) filed Critical Ляйбниц Инститьют Фор Нэчерал Продакт Ресерч Энд Инфекшн Байолоджи Э. Ф. Ханс-Кнелль-Институт (Хки)
Publication of EA200870564A1 publication Critical patent/EA200870564A1/ru
Publication of EA015910B1 publication Critical patent/EA015910B1/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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • 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
    • 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
    • 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
    • A61P31/08Antibacterial agents for leprosy
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D491/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D491/10Spiro-condensed systems
    • C07D491/113Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pulmonology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Новые производные бензотиазина формулы (I) и их применение в качестве антибактериальных средств при инфекционных заболеваниях, вызванных бактериями, особенно туберкулеза (ТВ) и проказы, вызванных микобактериями, где Rи Rявляются, независимо друг от друга, NO, CN, CONRR, COOR, CHO, галогеном, NRR, SONRR, SR, OCF, моно-, ди- или трифторметилом; Rи Rявляются, независимо друг от друга, Н, насыщенным или ненасыщенным, линейным или разветвленным алифатическим радикалом, имеющим 1-7 членов цепи, циклоалкилом, имеющим 3-6 атомов углерода, бензилом, SR, OR; Rи Rявляются, независимо друг от друга, насыщенным или ненасыщенным, галогенированным или негалогенированным, линейным или разветвленным алифатическим радикалом, имеющим 1-8 членов цепи, циклоалкилом, имеющим 3-6 атомов углерода, фенилом, или Rи Rвместе представляют собой двухвалентные радикалы: формула (II) или (III), где m равно 1-4, или представляют собой двухвалентные радикалы, насыщенные или ненасыщенные моно- или полигетероциклы с гетероатомами N, S, О и замещенные группой (R10)x, где х равно 1-4.
EA200870564A 2006-05-24 2006-05-24 Производные бензотиазинона и их применение в качестве антибактериальных средств EA015910B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2006/004942 WO2007134625A1 (en) 2006-05-24 2006-05-24 New benzothiazinone derivatives and their use as antibacterial agents

Publications (2)

Publication Number Publication Date
EA200870564A1 true EA200870564A1 (ru) 2009-06-30
EA015910B1 EA015910B1 (ru) 2011-12-30

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EA200870564A EA015910B1 (ru) 2006-05-24 2006-05-24 Производные бензотиазинона и их применение в качестве антибактериальных средств

Country Status (24)

Country Link
US (2) US7863268B2 (ru)
EP (1) EP2029583B1 (ru)
JP (1) JP5068813B2 (ru)
KR (1) KR101314999B1 (ru)
CN (1) CN101472922B (ru)
AP (1) AP2444A (ru)
AT (1) ATE470667T1 (ru)
AU (1) AU2006343832B2 (ru)
BR (1) BRPI0621693B8 (ru)
CA (1) CA2652841C (ru)
CR (1) CR10519A (ru)
CY (1) CY1110769T1 (ru)
DE (1) DE602006014885D1 (ru)
DK (1) DK2029583T3 (ru)
EA (1) EA015910B1 (ru)
ES (1) ES2345902T3 (ru)
IL (1) IL195453A (ru)
MX (1) MX2008014958A (ru)
NZ (1) NZ573833A (ru)
PL (1) PL2029583T3 (ru)
PT (1) PT2029583E (ru)
SI (1) SI2029583T1 (ru)
TN (1) TNSN08474A1 (ru)
WO (1) WO2007134625A1 (ru)

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KR101314999B1 (ko) 2006-05-24 2013-10-04 라이브니츠 인스티튜트 포 내추럴 프로덕트 리서치 앤드 인펙션 바이올로지 이.브이. 한스-크뇔-인스티튜트 (에이치케이아이) 신규한 벤조티아지논 유도체 및 그의 항균제로서의 용도
EP2020406A1 (en) * 2007-07-16 2009-02-04 Leibniz-Institut für Naturstoff-Forschung und Infektionsbiologie e.V. Hans-Knöll-Institut New antimicrobial compounds, their synthesis and their use for treatment of mammalian infection
WO2009100731A1 (en) 2008-02-13 2009-08-20 Universita' Degli Studi Di Pavia An effective new drug target for the treatment of tuberculosis
EP2380886A1 (en) 2010-04-23 2011-10-26 Vadim A. Makarov Process for the preparation of 2-aminosubstituted 1,3-benzothiazine-4-ones
WO2012066518A1 (en) * 2010-11-19 2012-05-24 Ecole Polytechnique Federale De Lausanne (Epfl) 2-piperazin-1-yl-4h-1,3-benzothiazin-4-one derivatives and their use for the treatment of mammalian infections
EP2468746A1 (en) 2010-12-23 2012-06-27 The University of Queensland Benzothiazinone compounds and their use as anti-tuberculosis agents
US8486717B2 (en) 2011-01-18 2013-07-16 Symbolics, Llc Lateral flow assays using two dimensional features
CN102276598B (zh) * 2011-05-27 2014-11-05 四川大学 苯并噻嗪硫酮衍生物及其制备方法和用途
CN102367239B (zh) * 2011-07-20 2015-10-28 沈阳药科大学 2-芳基-2,3-二氢-4h-1,3-苯并噻嗪-4-酮衍生物及其用途
EP2570413A1 (en) 2011-09-15 2013-03-20 The University Of Queensland Benzothiazinone derivatives as anti-tuberculosis agents
CN103508980B (zh) * 2012-06-14 2016-07-06 四川大学 苯并噻嗪-4-酮衍生物及其制备方法和用途
US9874556B2 (en) 2012-07-18 2018-01-23 Symbolics, Llc Lateral flow assays using two dimensional features
CN104211708B (zh) * 2013-05-29 2018-08-24 中国医学科学院药物研究所 苯并噁嗪酮衍生物及其作为抗菌剂的应用
CN108051590B (zh) 2013-09-13 2020-12-11 Symbolics有限责任公司 运用二维试验和对照信号读出模式的侧向层析检测
CN105705486B (zh) 2013-11-18 2019-03-01 格里洛工厂股份有限公司 用于自烷烃和发烟硫酸制备烷基磺酸的新型引发剂
DE102014012546A1 (de) * 2014-09-26 2016-03-31 Martin-Luther-Universität Halle-Wittenberg Antimykobakteriell wirksame Substanzen, Verfahren zu ihrer Herstellung und deren Verwendung
EP3072889A1 (en) 2015-03-23 2016-09-28 Ecole Polytechnique Federale De Lausanne (Epfl) 2-Homopiperazine-1-yl-4H-1,3-benzothiazine-4-one derivatives and process for the preparation of 2-(homo)piperazine 1,3-benzothiazine-4-one hydrochlorides
CN105622596B (zh) * 2016-02-19 2018-10-30 浙江司太立制药股份有限公司 含有烷氧亚胺基氮杂环片段的苯并噻嗪-4-酮类化合物及其制备方法
CN105669664B (zh) * 2016-02-19 2019-05-10 浙江司太立制药股份有限公司 含有碱性氮杂环片段的苯并噻嗪-4-酮类化合物及其制备方法
CN110312725B (zh) * 2016-09-22 2022-03-11 莱比尼兹自然研究和感染生物学研究所协会汉斯诺尔研究所(Hki) 新型抗菌化合物,其在哺乳动物感染治疗中的应用及新的代谢机制
RU2663848C1 (ru) * 2018-03-23 2018-08-10 Федеральное государственное бюджетное учреждение науки Институт органического синтеза им. И.Я. Постовского Уральского отделения Российской академии наук (ИОС УрО РАН) 5-Фтор-2-(4-этоксикарбонилпиперазин-1-ил)-1,3-бензотиазин-4-он, обладающий противотуберкулезной активностью
CN111269197A (zh) * 2020-04-08 2020-06-12 苏州大学 苯并噻嗪酮化合物及其制备方法与作为抗结核药物的应用
CN113121521B (zh) * 2021-03-26 2022-11-04 苏州大学 6-位三氟甲基取代的苯并噻嗪酮衍生物及其制备方法与应用

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Also Published As

Publication number Publication date
IL195453A (en) 2013-01-31
ES2345902T3 (es) 2010-10-05
PL2029583T3 (pl) 2010-10-29
US20090239851A1 (en) 2009-09-24
JP2009537576A (ja) 2009-10-29
AP2444A (en) 2012-08-31
EP2029583A1 (en) 2009-03-04
NZ573833A (en) 2010-10-29
CA2652841A1 (en) 2007-11-29
PT2029583E (pt) 2010-08-12
AP2008004723A0 (en) 2008-12-31
AU2006343832B2 (en) 2011-07-21
ATE470667T1 (de) 2010-06-15
WO2007134625A1 (en) 2007-11-29
KR20090029736A (ko) 2009-03-23
IL195453A0 (en) 2009-08-03
DK2029583T3 (da) 2010-09-27
AU2006343832A1 (en) 2007-11-29
EP2029583B1 (en) 2010-06-09
CA2652841C (en) 2015-01-27
SI2029583T1 (sl) 2010-09-30
MX2008014958A (es) 2009-04-15
KR101314999B1 (ko) 2013-10-04
BRPI0621693A2 (pt) 2011-12-20
BRPI0621693B1 (pt) 2020-11-17
US20110160193A1 (en) 2011-06-30
DE602006014885D1 (de) 2010-07-22
EA015910B1 (ru) 2011-12-30
BRPI0621693B8 (pt) 2021-05-25
CN101472922B (zh) 2012-05-30
CY1110769T1 (el) 2015-06-10
CR10519A (es) 2009-04-14
JP5068813B2 (ja) 2012-11-07
TNSN08474A1 (en) 2010-04-14
US7863268B2 (en) 2011-01-04
CN101472922A (zh) 2009-07-01

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