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WO2002028868A1 - Derives de thiazine - Google Patents

Derives de thiazine Download PDF

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Publication number
WO2002028868A1
WO2002028868A1 PCT/RU2000/000395 RU0000395W WO0228868A1 WO 2002028868 A1 WO2002028868 A1 WO 2002028868A1 RU 0000395 W RU0000395 W RU 0000395W WO 0228868 A1 WO0228868 A1 WO 0228868A1
Authority
WO
WIPO (PCT)
Prior art keywords
compounds
phenyl
cooh
thiazine derivatives
thiazin
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/RU2000/000395
Other languages
English (en)
Russian (ru)
Other versions
WO2002028868A8 (fr
Inventor
Elena Alexandrovna Izakson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to PCT/RU2000/000395 priority Critical patent/WO2002028868A1/fr
Priority to AU2001225605A priority patent/AU2001225605A1/en
Publication of WO2002028868A1 publication Critical patent/WO2002028868A1/fr
Publication of WO2002028868A8 publication Critical patent/WO2002028868A8/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • 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
    • A61K31/54—Heterocyclic 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
    • 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
    • A61K31/54—Heterocyclic 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
    • A61K31/542—Heterocyclic 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 heterocyclic ring systems
    • 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
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
    • C07D279/06—1,3-Thiazines; Hydrogenated 1,3-thiazines not condensed with other rings

Definitions

  • the invention is available in medicine, in part - in the form of pharmaceuticals and is intended for use in the market of inadequate and non-compliant medical products.
  • the claimed compounds are obtained by the following method.
  • the minimum inhibitory concentration was determined by the use of serial dilutions in a liquid medium [6 .. Testing was carried out with a consumable test.
  • the data obtained indicate the presence of antimicrobial activity in respect to gamma-positive and gross-negative bacteria.
  • the cultivars were cultivated on a cultivar with an ⁇ / jack cage (sowing dose - 10 FID50 / ml) in an Ebunculus plate at 37 ° C in a C0 2 incubator.
  • the tested compounds were distributed in ⁇ . After the daily incubation, the virus was removed, the environment was changed. The final result was taken into account after 36 hours of incubation at 37 ° ⁇ in the ⁇ 2 atmosphere due to the presence of a cytopathic effect.
  • the tested compounds tested in Guinea 80 introduced white nonlinear mice weighing 18–20 g with a gastric probe (300 mg / kg) or an internal (100 mg / kg) probe. Each test group included 3 males and 3 females. The state of the animals was observed for 72 hours.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne le domaine de la médecine, et plus particulièrement la pharmacologie, et peut être utilisée comme nouveaux agents antibactériens et antimicrobiens qui sont notamment efficaces contre les microbactéries. Le principe de base de cette invention réside dans la synthèse et la définition d'une activité biologique puissante des dérivés de thiazine ayant la formule générale (1) dans laquelle X = OH ou O, Ar est sélectionné parmi C6H5, 4-C6H5NO2, 4-C6H4CH3, 4-C6H4OH, 4-C6H4Cl, 3,4-(CH 3)O2C6H3, Y est sélectionné dans la formule (2) et Z est une liaison chimique ou CH2-CH2.
PCT/RU2000/000395 2000-10-03 2000-10-03 Derives de thiazine Ceased WO2002028868A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
PCT/RU2000/000395 WO2002028868A1 (fr) 2000-10-03 2000-10-03 Derives de thiazine
AU2001225605A AU2001225605A1 (en) 2000-10-03 2000-10-03 Thiazine derivatives

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/RU2000/000395 WO2002028868A1 (fr) 2000-10-03 2000-10-03 Derives de thiazine

Publications (2)

Publication Number Publication Date
WO2002028868A1 true WO2002028868A1 (fr) 2002-04-11
WO2002028868A8 WO2002028868A8 (fr) 2002-05-10

Family

ID=20129555

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2000/000395 Ceased WO2002028868A1 (fr) 2000-10-03 2000-10-03 Derives de thiazine

Country Status (2)

Country Link
AU (1) AU2001225605A1 (fr)
WO (1) WO2002028868A1 (fr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3962223A (en) * 1971-12-31 1976-06-08 Roussel-Uclaf Substituted cephene-4-carboxylates and their method of preparation
US4016158A (en) * 1971-12-31 1977-04-05 Roussel-Uclaf Cephalosporin derivatives
RU95110049A (ru) * 1992-10-29 1997-01-10 Смитклайн Бичам Плс (Gb) 6-(замещенные метилен)пенемы, способ их получения, промежуточные продукты, фармкомпозиция, способ лечения

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3962223A (en) * 1971-12-31 1976-06-08 Roussel-Uclaf Substituted cephene-4-carboxylates and their method of preparation
US4016158A (en) * 1971-12-31 1977-04-05 Roussel-Uclaf Cephalosporin derivatives
RU95110049A (ru) * 1992-10-29 1997-01-10 Смитклайн Бичам Плс (Gb) 6-(замещенные метилен)пенемы, способ их получения, промежуточные продукты, фармкомпозиция, способ лечения

Also Published As

Publication number Publication date
AU2001225605A1 (en) 2002-04-15
WO2002028868A8 (fr) 2002-05-10

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