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RU2008102251A - ANALOGUES OF THIOCOLCHICOSIDE WITH MYORELAXANT AND ANTI-INFLAMMATORY ACTIVITY - Google Patents

ANALOGUES OF THIOCOLCHICOSIDE WITH MYORELAXANT AND ANTI-INFLAMMATORY ACTIVITY Download PDF

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Publication number
RU2008102251A
RU2008102251A RU2008102251/04A RU2008102251A RU2008102251A RU 2008102251 A RU2008102251 A RU 2008102251A RU 2008102251/04 A RU2008102251/04 A RU 2008102251/04A RU 2008102251 A RU2008102251 A RU 2008102251A RU 2008102251 A RU2008102251 A RU 2008102251A
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RU
Russia
Prior art keywords
aminothiocolchicine
demethoxy
compounds
inflammatory activity
medicines
Prior art date
Application number
RU2008102251/04A
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Russian (ru)
Inventor
Габриеле ФОНТАНА (IT)
Габриеле ФОНТАНА
Эцио БОМБАРДЕЛЛИ (IT)
Эцио БОМБАРДЕЛЛИ
Антонелла РИВА (IT)
Антонелла РИВА
Паоло МОРАЦЦОНИ (IT)
Паоло МОРАЦЦОНИ
Донато ПОКАР (IT)
Донато ПОКАР
Мари Луиза ДЖЕЛЬМИ (IT)
Мари Луиза ДЖЕЛЬМИ
Гвидо ПОНТРЕМОЛИ (IT)
Гвидо ПОНТРЕМОЛИ
Original Assignee
Индена С.П.А. (It)
Индена С.П.А.
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 Индена С.П.А. (It), Индена С.П.А. filed Critical Индена С.П.А. (It)
Publication of RU2008102251A publication Critical patent/RU2008102251A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/24—Condensed ring systems having three or more rings
    • C07H15/248—Colchicine radicals, e.g. colchicosides
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40—Y being a hydrogen or a carbon atom
    • C07C323/41—Y being a hydrogen or an acyclic carbon atom

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

1. Соединения общей формулы (I) ! ! где ! R представляет водород, метил или гидроксиметил. ! 2. Соединение, выбранное из: ! 3-N-D-ксилопиранозил-3-О-деметокси-3-аминотиоколхицина; ! 3-N-D-глюкопиранозил-3-О-деметокси-3-аминотиоколхицина; ! 3-N-D-маннопиранозил-3-О-деметокси-3-аминотиоколхицина; ! 3-N-D-арабинопиранозил-3-О-деметокси-3-аминотиоколхицина; ! 3-N-D-ликсопиранозил-3-О-деметокси-3-аминотиоколхицина; ! 3-N-L-рамнопиранозил-3-О-деметокси-3-аминотиоколхицина; ! 3-N-L-фукопиранозил-3-О-деметокси-3-аминотиоколхицина. ! 3. Фармацевтические композиции, включающие соединение по п.1 или 2 в смеси с приемлемыми носителями и/или наполнителями. ! 4. Применение соединений по пп.1 и 2 для изготовления лекарственных средств с миорелаксантной и противовоспалительной активностью. ! 5. Применение соединения формулы (II) ! ! для изготовления лекарственных средств с миорелаксантной активностью.1. Compounds of the general formula (I)! ! where! R represents hydrogen, methyl or hydroxymethyl. ! 2. A compound selected from:! 3-N-D-xylopyranosyl-3-O-demethoxy-3-aminothiocolchicine; ! 3-N-D-glucopyranosyl-3-O-demethoxy-3-aminothiocolchicine; ! 3-N-D-mannopyranosyl-3-O-demethoxy-3-aminothiocolchicine; ! 3-N-D-arabinopyranosyl-3-O-demethoxy-3-aminothiocolchicine; ! 3-N-D-lixopyranosyl-3-O-demethoxy-3-aminothiocolchicine; ! 3-N-L-ramnopyranosyl-3-O-demethoxy-3-aminothiocolchicine; ! 3-N-L-fucopyranosyl-3-O-demethoxy-3-aminothiocolchicine. ! 3. Pharmaceutical compositions comprising a compound according to claim 1 or 2 in admixture with acceptable carriers and / or excipients. ! 4. The use of compounds according to claims 1 and 2 for the manufacture of medicines with muscle relaxant and anti-inflammatory activity. ! 5. The use of the compounds of formula (II)! ! for the manufacture of medicines with muscle relaxant activity.

Claims (5)

1. Соединения общей формулы (I)1. Compounds of General Formula ( I )
Figure 00000001
Figure 00000001
 гдеWhere R представляет водород, метил или гидроксиметил.R represents hydrogen, methyl or hydroxymethyl. 2. Соединение, выбранное из:2. A compound selected from: 3-N-D-ксилопиранозил-3-О-деметокси-3-аминотиоколхицина;3-N-D-xylopyranosyl-3-O-demethoxy-3-aminothiocolchicine; 3-N-D-глюкопиранозил-3-О-деметокси-3-аминотиоколхицина;3-N-D-glucopyranosyl-3-O-demethoxy-3-aminothiocolchicine; 3-N-D-маннопиранозил-3-О-деметокси-3-аминотиоколхицина;3-N-D-mannopyranosyl-3-O-demethoxy-3-aminothiocolchicine; 3-N-D-арабинопиранозил-3-О-деметокси-3-аминотиоколхицина;3-N-D-arabinopyranosyl-3-O-demethoxy-3-aminothiocolchicine; 3-N-D-ликсопиранозил-3-О-деметокси-3-аминотиоколхицина;3-N-D-lixopyranosyl-3-O-demethoxy-3-aminothiocolchicine; 3-N-L-рамнопиранозил-3-О-деметокси-3-аминотиоколхицина;3-N-L-ramnopyranosyl-3-O-demethoxy-3-aminothiocolchicine; 3-N-L-фукопиранозил-3-О-деметокси-3-аминотиоколхицина.3-N-L-fucopyranosyl-3-O-demethoxy-3-aminothiocolchicine. 3. Фармацевтические композиции, включающие соединение по п.1 или 2 в смеси с приемлемыми носителями и/или наполнителями.3. Pharmaceutical compositions comprising a compound according to claim 1 or 2 in a mixture with acceptable carriers and / or excipients. 4. Применение соединений по пп.1 и 2 для изготовления лекарственных средств с миорелаксантной и противовоспалительной активностью.4. The use of compounds according to claims 1 and 2 for the manufacture of medicines with muscle relaxant and anti-inflammatory activity. 5. Применение соединения формулы (II)5. The use of the compounds of formula ( II )
Figure 00000002
Figure 00000002
 для изготовления лекарственных средств с миорелаксантной активностью. for the manufacture of medicines with muscle relaxant activity.
RU2008102251/04A 2005-07-22 2006-07-20 ANALOGUES OF THIOCOLCHICOSIDE WITH MYORELAXANT AND ANTI-INFLAMMATORY ACTIVITY RU2008102251A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT001418A ITMI20051418A1 (en) 2005-07-22 2005-07-22 ANALOGUES OF THIOILCYCOSIDE WITH HYDRO-LASER ACTIVITY AND ANTI-INFLAMMATORY
ITMI2005A001418 2005-07-22

Publications (1)

Publication Number Publication Date
RU2008102251A true RU2008102251A (en) 2009-07-27

Family

ID=37420844

Family Applications (1)

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RU2008102251/04A RU2008102251A (en) 2005-07-22 2006-07-20 ANALOGUES OF THIOCOLCHICOSIDE WITH MYORELAXANT AND ANTI-INFLAMMATORY ACTIVITY

Country Status (14)

Country Link
EP (1) EP1907405A1 (en)
JP (1) JP2009502755A (en)
KR (1) KR20080036585A (en)
CN (1) CN101228175A (en)
AU (1) AU2006271923A1 (en)
BR (1) BRPI0613680A2 (en)
CA (1) CA2615860A1 (en)
IL (1) IL188900A0 (en)
IT (1) ITMI20051418A1 (en)
MX (1) MX2008000968A (en)
NO (1) NO20080377L (en)
NZ (1) NZ565265A (en)
RU (1) RU2008102251A (en)
WO (1) WO2007009772A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8421747B2 (en) * 2008-09-24 2013-04-16 Microsoft Corporation Object detection and user settings
CN102448930A (en) * 2009-05-27 2012-05-09 共有药物有限公司 Thiocolchicine derivatives, method of making and methods of use thereof
US20110184061A1 (en) * 2010-01-22 2011-07-28 Nielsen Kurt R Thiocolchicine and colchicine analogs, methods of making and methods of use thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1291550B1 (en) * 1997-04-11 1999-01-11 Indena Spa DERIVATIVES OF COLCHICINE AND THIOCOLCHICINE WITH ANTI-INFLAMMATORY AND MYORELAXING ACTIVITIES
ITMI20031144A1 (en) * 2003-06-06 2004-12-07 Indena Spa COLCHICOSIDE ANALOGUES.

Also Published As

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ITMI20051418A1 (en) 2007-01-23
AU2006271923A1 (en) 2007-01-25
BRPI0613680A2 (en) 2011-01-25
CA2615860A1 (en) 2007-01-25
EP1907405A1 (en) 2008-04-09
KR20080036585A (en) 2008-04-28
JP2009502755A (en) 2009-01-29
NZ565265A (en) 2010-01-29
WO2007009772A1 (en) 2007-01-25
NO20080377L (en) 2008-02-01
CN101228175A (en) 2008-07-23
IL188900A0 (en) 2008-04-13
MX2008000968A (en) 2008-03-26

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Effective date: 20100401