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EA200200366A1 - Замещенное производное тетрациклина (варианты) и способ его получения (варианты), реакционноспособный химический комплекс тетрациклина - Google Patents

Замещенное производное тетрациклина (варианты) и способ его получения (варианты), реакционноспособный химический комплекс тетрациклина

Info

Publication number
EA200200366A1
EA200200366A1 EA200200366A EA200200366A EA200200366A1 EA 200200366 A1 EA200200366 A1 EA 200200366A1 EA 200200366 A EA200200366 A EA 200200366A EA 200200366 A EA200200366 A EA 200200366A EA 200200366 A1 EA200200366 A1 EA 200200366A1
Authority
EA
Eurasian Patent Office
Prior art keywords
tetracycline
substituted
options
derivative
organic substituent
Prior art date
Application number
EA200200366A
Other languages
English (en)
Other versions
EA005118B1 (ru
Inventor
Дэррелл Дж. Коуза
Марк Л. Нельсон
Глен Ренни
Original Assignee
Трастис Оф Тафтс Коллидж
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Трастис Оф Тафтс Коллидж filed Critical Трастис Оф Тафтс Коллидж
Publication of EA200200366A1 publication Critical patent/EA200200366A1/ru
Publication of EA005118B1 publication Critical patent/EA005118B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C07C237/26—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
    • 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
    • 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
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings
    • C07C2603/44—Naphthacenes; Hydrogenated naphthacenes
    • C07C2603/46—1,4,4a,5,5a,6,11,12a- Octahydronaphthacenes, e.g. tetracyclines

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Настоящее изобретение относится к новым способам синтеза, которые позволяют получать ранее недоступные замещенные производные тетрациклина, которые обладают высокой антибактериальной активностью. В способах, описанных в настоящем изобретении, используются реакционноспособные предшественники тетрациклина, реакционноспособные предшественники органического заместителя и катализаторы на основе переходных металлов в условиях, при которых образуется замещенное производное тетрациклина, содержащее требуемый органический заместитель. В одном из вариантов воплощения изобретения замещенное производное тетрациклина может быть получено путем смешивания реакционноспособного предшественника тетрациклина, такого как арендиазониевая соль тетрациклина, и реакционноспособного предшественника органического заместителя, например алкенов, замещенных алкенов, виниловых мономеров, ароматических и гетероароматических соединений, в присутствии катализатора на основе переходного металла, такого как хлорид палладия, в условиях, при которых образуется производное тетрациклина, замещенное органическим заместителем. Такие замещенные производные по выбору могут быть использованы в качестве промежуточных производных для получения других соединений, например при гидрировании ненасыщенных групп заместителя.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200200366A 1999-09-14 2000-09-13 Замещенный аналог тетрациклина (варианты) и способ его получения (варианты) EA005118B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15470199P 1999-09-14 1999-09-14
US23209100P 2000-09-12 2000-09-12
PCT/US2000/025040 WO2001019784A1 (en) 1999-09-14 2000-09-13 Methods of preparing substituted tetracyclines with transition metal-based chemistries

Publications (2)

Publication Number Publication Date
EA200200366A1 true EA200200366A1 (ru) 2002-10-31
EA005118B1 EA005118B1 (ru) 2004-10-28

Family

ID=26851695

Family Applications (3)

Application Number Title Priority Date Filing Date
EA200400944A EA012203B1 (ru) 1999-09-14 2000-09-13 Замещенные производные тетрациклина, фармацевтическая композиция и способ лечения субъекта с их использованием
EA200200366A EA005118B1 (ru) 1999-09-14 2000-09-13 Замещенный аналог тетрациклина (варианты) и способ его получения (варианты)
EA200900632A EA016099B1 (ru) 1999-09-14 2000-09-13 Замещенный аналог тетрациклина (варианты) и способ получения замещенного аналога тетрациклина

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA200400944A EA012203B1 (ru) 1999-09-14 2000-09-13 Замещенные производные тетрациклина, фармацевтическая композиция и способ лечения субъекта с их использованием

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA200900632A EA016099B1 (ru) 1999-09-14 2000-09-13 Замещенный аналог тетрациклина (варианты) и способ получения замещенного аналога тетрациклина

Country Status (21)

Country Link
US (3) US6617318B1 (ru)
EP (5) EP2327687A3 (ru)
JP (2) JP5093953B2 (ru)
KR (1) KR100764992B1 (ru)
CN (2) CN1399627A (ru)
AT (2) ATE523485T1 (ru)
AU (3) AU781439C (ru)
BR (1) BR0013993A (ru)
CA (2) CA2383364C (ru)
CY (1) CY1105094T1 (ru)
CZ (1) CZ301835B6 (ru)
DE (1) DE60027465T2 (ru)
DK (1) DK1240133T3 (ru)
EA (3) EA012203B1 (ru)
ES (1) ES2260051T3 (ru)
HR (1) HRP20020322B1 (ru)
HU (1) HUP0202798A3 (ru)
IL (4) IL148482A0 (ru)
MX (1) MXPA02002595A (ru)
PT (1) PT1240133E (ru)
WO (1) WO2001019784A1 (ru)

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