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WO2011081567A1 - Produits médicamenteux pour traiter la sclérose en plaques - Google Patents

Produits médicamenteux pour traiter la sclérose en plaques Download PDF

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Publication number
WO2011081567A1
WO2011081567A1 PCT/RU2010/000784 RU2010000784W WO2011081567A1 WO 2011081567 A1 WO2011081567 A1 WO 2011081567A1 RU 2010000784 W RU2010000784 W RU 2010000784W WO 2011081567 A1 WO2011081567 A1 WO 2011081567A1
Authority
WO
WIPO (PCT)
Prior art keywords
multiple sclerosis
triiodide
treatment
animals
experimental
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/RU2010/000784
Other languages
English (en)
Russian (ru)
Inventor
Геннадий Алексеевич ВИЛКОВ
Борис Витальевич СТРАДОМСКИЙ
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.)
SOLODUNOV YURIY YURYEVICH
Original Assignee
SOLODUNOV YURIY YURYEVICH
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 SOLODUNOV YURIY YURYEVICH filed Critical SOLODUNOV YURIY YURYEVICH
Publication of WO2011081567A1 publication Critical patent/WO2011081567A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/13—Amines
    • A61K31/14—Quaternary ammonium compounds, e.g. edrophonium, choline
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Definitions

  • the invention relates to the field of psychoneurology, in particular to means for the treatment of multiple sclerosis.
  • Betaferon - recombinant human interferon beta-lb (Mashkovsky MD 2003. Medicines. M: New Wave, p. 324-325).
  • Betaferon is the only drug whose effectiveness has been shown in a long-term (5 years) placebo-controlled study (Totolyan NA 2005. Betaferon in the treatment of multiple sclerosis: a standard of evidence of effectiveness // Journal of Neurology and Psychiatry. 7: p. 68 -71).
  • the disadvantage of this drug is the rather low efficiency of its use - a decrease in the frequency of exacerbations of the disease and their severity by only 30%, the presence of such side effects as increased depressive symptoms (Sokolova E.S., Totolyan N.A., Klimenko V.M. 2003. Psycho-emotional changes in the treatment of patients with multiple sclerosis with betaferone // "Stress and Behavior” VII Interdisciplinary Conference on Biological Psychiatry, Novosibirsk), as well as the very high cost of pharmacotherapy with Betaferon.
  • the objective of the invention which determines its purpose, is the creation of new drugs with pronounced pharmacological activity for the treatment of multiple sclerosis, with high therapeutic efficacy, while reducing unwanted side effects, reducing the cost of treatment.
  • the technical result of the claimed invention which can be achieved by its implementation, is the creation of a group of compounds with high activity in the treatment of multiple sclerosis.
  • R 2 methyl (Met), ethyl (Et), propyl (Pro).
  • the method of producing 1,3-dialkylbenzimidazolium triiodides for the treatment of multiple sclerosis is safe for individuals involved in the process.
  • Example 2 1,3-diethylbenzimidazolium triiodide triiodide: 59 g (0.5 M) of benzimidazole and 68 g (0.5 M) of sodium trihydride are placed in 160 ml of 96% ethyl alcohol, 156 g (1 M) of ethyl iodide are added and boil the reaction mixture for 3 hours. 127 g (0.5 M) of crystalline iodine are added, cooled on ice, the resulting crystalline product is washed with 96% ethyl alcohol and ice water, filtered and dried for 24 hours at + 55 ° C.
  • Example 3 1,3-dipropylbenzimidazolium triiodide triiodide: 59 g (0.5 M) of benzimidazole and 68 g (0.5 M) of sodium trihydrate are placed in 160 ml of 96% ethyl alcohol, 170 g (1 M) of propyl iodide are added and boil the reaction mixture for 3 hours. 127 g (0.5 M) of crystalline iodine are added, cooled on ice, the resulting crystalline product is washed with ethyl alcohol 96% and ice water, filtered and dried for 48 hours at + 30 ° C.
  • EAE Experimental allergic encephalomyelitis
  • an encephalitogenic emulsion is prepared (homologous brain of animals in complete Freund's adjuvant), which is introduced into the pads of the hind legs of guinea pigs (Abdurasulova I.N., Serdyuk S.E., Gmiro V.E. 2007. // Neuroimmunology. V, N 1. P. 4-10 )
  • mice were used as controls, i.e. only encephalitogenic emulsion was administered to them.
  • the animals were orally administered 4 mg of 100% 1,3-diethylbenzimidazolium triiodide in suspension in water for injection in a volume of 4 ml.
  • 1,3-diethylbenzimidazolium (mixture with polyvinylpyrrolidone in a ratio of 1: 1000, the content of 1,3-diethylbenzimidazolium triiodide in the administered mixture is 4 mg per animal).
  • the animals were orally administered 4 mg of 100% 1,3-dimethylbenzimidazolium triiodide in suspension in water for injection in a volume of 4 ml.
  • 1,3-dipropylbenzimidazolium (mixture with polyvinylpyrrolidone in a ratio of 1: 1000, the content of triiodide 1,3- dipropylbenzimidazolium in the injected mixture is 4 mg per animal).
  • the clinical index (CI) was determined by the severity and prevalence of neurological manifestations: muscle weakness of one limb - 0.5 points, paresis - 1 point, paralysis - 1.5. With the defeat of several limbs, the points were summarized. In the presence of additional symptoms (paresis of sphincters), another 1 point was added for each symptom. The absence of visible violations was taken as 0 points, in case of death - 6 points.
  • the claimed funds can be used as medicines for the treatment of multiple sclerosis in medicine.

Landscapes

  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne le domaine de la psycho-neurologie et notamment des produits médicamenteux pour traiter la sclérose en plaques. L'invention propose des substances possédant un degré d'activité élevé lors du traitement de la sclérose en plaques, qui font partie du groupe des compositions tri-iodure 1,3 de dialkylbenzimidazole correspondant à la formule générale (I) dans laquelle R1, R2 = méthyl (met), éthyl (Et), propyl (Pro).
PCT/RU2010/000784 2009-12-29 2010-12-24 Produits médicamenteux pour traiter la sclérose en plaques Ceased WO2011081567A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2009148873 2009-12-29
RU2009148873/15A RU2414899C1 (ru) 2009-12-29 2009-12-29 Средства для лечения рассеянного склероза

Publications (1)

Publication Number Publication Date
WO2011081567A1 true WO2011081567A1 (fr) 2011-07-07

Family

ID=44052725

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU2010/000784 Ceased WO2011081567A1 (fr) 2009-12-29 2010-12-24 Produits médicamenteux pour traiter la sclérose en plaques

Country Status (2)

Country Link
RU (1) RU2414899C1 (fr)
WO (1) WO2011081567A1 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2663931C1 (ru) * 2017-09-25 2018-08-13 Общество с ограниченной ответственностью "Кратос" Биологически активная композиция

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2094047C1 (ru) * 1995-12-25 1997-10-27 Ливицкий Василий Иванович Композиция, обладающая противоопухолевым действием
RU2150274C1 (ru) * 1996-12-26 2000-06-10 Бачин Игорь Валентинович Стабилизированная водорастворимая композиция трийодида 1,2,3-триалкилбензимидазолия
RU2198880C2 (ru) * 2000-10-04 2003-02-20 Ливицкий Василий Иванович Трийодиды 1,2,3-замещенных бензимидазолия и способы их получения

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2033164C1 (ru) * 1992-01-10 1995-04-20 Ливицкий Василий Иванович Антимикробный лечебный препарат
US6166219A (en) * 1995-12-28 2000-12-26 Fujisawa Pharmaceutical Co., Ltd. Benzimidazole derivatives
RU2148578C1 (ru) * 1999-04-20 2000-05-10 Ливицкий Василий Иванович Дийодидхлориды 1,2,3-замещенного бензимидазолия и их водорастворимая композиция
SE0301699D0 (sv) * 2003-06-10 2003-06-10 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
SE0302573D0 (sv) * 2003-09-26 2003-09-26 Astrazeneca Ab Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof
CA2581232C (fr) * 2004-09-24 2015-04-07 Astrazeneca Ab Derives de benzimidazole, compositions contenant ces derives, preparation et utilisations de ces derniers
JP2008518905A (ja) * 2004-11-02 2008-06-05 ファイザー株式会社 スルホニルベンゾイミダゾール誘導体
RU2318817C1 (ru) * 2006-10-10 2008-03-10 Аверин Константин Михайлович 1,3-диалкилбензимидазолия галогениды, обладающие регенерационной, противовоспалительной и противомикробной активностью

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2094047C1 (ru) * 1995-12-25 1997-10-27 Ливицкий Василий Иванович Композиция, обладающая противоопухолевым действием
RU2150274C1 (ru) * 1996-12-26 2000-06-10 Бачин Игорь Валентинович Стабилизированная водорастворимая композиция трийодида 1,2,3-триалкилбензимидазолия
RU2198880C2 (ru) * 2000-10-04 2003-02-20 Ливицкий Василий Иванович Трийодиды 1,2,3-замещенных бензимидазолия и способы их получения

Also Published As

Publication number Publication date
RU2414899C1 (ru) 2011-03-27

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