WO2002074311A1 - Preparation medicinale antitumorale, antivirale, antibacterienne, antiparasitaire, anti-inflammatoire, antifongique et immunomodulatrice, procede de fabrication et formes de medicaments - Google Patents

Preparation medicinale antitumorale, antivirale, antibacterienne, antiparasitaire, anti-inflammatoire, antifongique et immunomodulatrice, procede de fabrication et formes de medicaments Download PDF

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Publication number
WO2002074311A1
WO2002074311A1 PCT/RU2002/000117 RU0200117W WO02074311A1 WO 2002074311 A1 WO2002074311 A1 WO 2002074311A1 RU 0200117 W RU0200117 W RU 0200117W WO 02074311 A1 WO02074311 A1 WO 02074311A1
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WO
WIPO (PCT)
Prior art keywords
carrier
τεμ
active part
pharmaceutical
biologically active
Prior art date
Application number
PCT/RU2002/000117
Other languages
English (en)
Russian (ru)
Inventor
Oleg Viktorovich Travkin
Elena Vladimirovna Yakovleva
Original Assignee
Oleg Viktorovich Travkin
Elena Vladimirovna Yakovleva
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 Oleg Viktorovich Travkin, Elena Vladimirovna Yakovleva filed Critical Oleg Viktorovich Travkin
Priority to EA200301035A priority Critical patent/EA005929B1/ru
Publication of WO2002074311A1 publication Critical patent/WO2002074311A1/fr

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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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders

Definitions

  • ⁇ nas ⁇ yaschee v ⁇ emya shi ⁇ is ⁇ lzuyu ⁇ sya ⁇ iv ⁇ vi ⁇ usnye le ⁇ a ⁇ s ⁇ vennye ⁇ e ⁇ a ⁇ a ⁇ y dvu ⁇ ⁇ sn ⁇ vny ⁇ g ⁇ u ⁇ : ⁇ e ⁇ a ⁇ a ⁇ y on ⁇ sn ⁇ ve an ⁇ malny ⁇ nu ⁇ le ⁇ z ⁇ d ⁇ v (na ⁇ ime ⁇ , atsi ⁇ l ⁇ vi ⁇ , vi ⁇ az ⁇ l) and ⁇ a ⁇ zhe in ⁇ e ⁇ e ⁇ ny or i ⁇ indu ⁇ y [5 -9].
  • the group of pharmaceutical products is supplied with salicylate drugs (asparty), phenylpropylene
  • ⁇ antiparasitic drugs are not effective in the treatment of simple and helminthic drugs, such as quinine, carynecine, and erythema.
  • ⁇ s ⁇ b ⁇ e value ⁇ a ⁇ iches ⁇ y medicine imeyu ⁇ ⁇ e ⁇ a ⁇ a ⁇ y- immun ⁇ s ⁇ imulya ⁇ y, na ⁇ ime ⁇ , levamiz ⁇ l, ⁇ imalin, ami ⁇ sin and ⁇ a ⁇ zhe ⁇ e ⁇ a ⁇ e ⁇ in (ami ⁇ il ⁇ z) s ⁇ zdanny on ⁇ sn ⁇ ve m ⁇ n ⁇ zameschenn ⁇ g ⁇ e ⁇ i ⁇ a m ⁇ n ⁇ sa ⁇ a ⁇ ida - immun ⁇ m ⁇ dulya ⁇ , ⁇ bladayuschy vy ⁇ azhennym ⁇ iv ⁇ v ⁇ s ⁇ ali ⁇ elnym deys ⁇ viem [11-13].
  • Immunomodulating medication is known to be in the form of hydrophobic derivatives of Acidic Acid [19]; however, there is a lack of treatment for it.
  • the main active principle of these drugs is the available salts of ⁇ -acid acid.
  • the efficacy of these drugs is harmful to the patient. This, in turn, significantly weakens the effect of this medication on internal drugs. Otherwise, these drugs have a limited and limited therapeutic effect.
  • HEALTH OF IZB ⁇ IA Tasks iz ⁇ b ⁇ e ⁇ eny yavlyae ⁇ sya ⁇ az ⁇ ab ⁇ a n ⁇ v ⁇ g ⁇ le ⁇ a ⁇ s ⁇ venn ⁇ g ⁇ ⁇ e ⁇ a ⁇ a ⁇ a, ⁇ bladayuscheg ⁇ vys ⁇ y a ⁇ ivn ⁇ s ⁇ yu and shi ⁇ im s ⁇ e ⁇ m nes ⁇ etsi ⁇ iches ⁇ g ⁇ ⁇ a ⁇ ma ⁇ l ⁇ giches ⁇ g ⁇ deys ⁇ viya - immun ⁇ m ⁇ duli ⁇ uyuscheg ⁇ , ⁇ iv ⁇ a ⁇ azi ⁇ a ⁇ n ⁇ g ⁇ , ⁇ iv ⁇ vi ⁇ usn ⁇ g ⁇ , ⁇ iv ⁇ ba ⁇ e ⁇ ialn ⁇ g ⁇ , ⁇ iv ⁇ - g ⁇ ib ⁇ v ⁇ g ⁇ , ⁇ iv ⁇ v ⁇ s ⁇ ali ⁇ el
  • the biologically active part of the drug contains a mixture of acid and its acid or its total total formula (1)
  • the group may be in the hemiacetal or hemicetal form, in the ⁇ or ⁇ configuration ⁇ .
  • ⁇ ⁇ , ⁇ , -C ⁇ 2- ⁇
  • X, ⁇ are selected from the group: ⁇ , ⁇ , alkyl, hydroxyalkyl, alkoxy, alkoxyalkyl.
  • ⁇ , ⁇ ⁇ 2, ⁇ are selected from the group: ⁇ , alkyl, aryl, alkenyl.
  • ⁇ and 0 ⁇ 2, ⁇ ⁇ ⁇ / 1 and ⁇ , ⁇ ⁇ ⁇ 2 and ⁇ - are selected from the group: alkyl, aryl, benzyl, alkenyl.
  • ⁇ ? 3, ⁇ ? 4 - are selected from the group: gleich, alkyl, aryl, or ⁇ 3 and cartedaleatty Arts.4 together with the nitrogen atom, form a morphine, pyridine or pyridine heterocycle, 1-6.
  • a medicinal product in a medicinal form of ointment or cream or in stock or gel or liniment in the form of a pharmaceutical drug is fatty or non-oily or fatty. %, the biological active part of 0.1 - 50 of the base ointment 50 - 99.9.
  • the biologically active part is 0.1–50%, a stabilizer and, or an intermediate, 50–99.9.
  • the medicinal product in the medicinal form is available in the pharmaceutical form as a pharmaceutically acceptable carrier, which contains 5 and / or peripheral arteries. %, biologically active part 0.1 - 50 diluent, conservative and / or flavoring agent 50 - 99.9.
  • the medicinal product in the pharmaceutical form of the aerosol consumes the propellant, the propellant and the oxygen source.
  • % biologically active part 0.1 - 50 gas propellant, reagent and oxygen 50 - 99.9.
  • ⁇ ⁇ ezul ⁇ a ⁇ e se ⁇ ii is ⁇ y ⁇ any and issled ⁇ vany e ⁇ s ⁇ e ⁇ imen ⁇ aln ⁇ us ⁇ an ⁇ vlen ⁇ , ch ⁇ n ⁇ vye le ⁇ a ⁇ stvennye ⁇ my zayavlyaem ⁇ g ⁇ le ⁇ a ⁇ s ⁇ venn ⁇ g ⁇ ⁇ e ⁇ a ⁇ a ⁇ bladayu ⁇ vy ⁇ azhennym immun ⁇ m ⁇ duli ⁇ uyuschim, ⁇ iv ⁇ a ⁇ azi ⁇ a ⁇ nym, ⁇ iv ⁇ vi ⁇ usnym, ⁇ iv ⁇ ba ⁇ e ⁇ ialnym, ⁇ iv ⁇ g ⁇ ib ⁇ vym, ⁇ iv ⁇ v ⁇ s ⁇ ali ⁇ elnym and ⁇ iv ⁇ u ⁇ levym action niz ⁇ y ⁇ sichn ⁇ s ⁇ yu, vys ⁇ im inde ⁇ s ⁇ m ⁇ e ⁇ a ⁇ ev ⁇
  • the group contains a new, not well-known material, which is previously significant.
  • PAN 2 4.5 g of 3-chloro-10-methylene oxide-9-acid and 5.5 g of 1,2; 3,4-d-i- ⁇ -isopropyl idene 6- ⁇ ( ⁇ , ⁇ -d had an amylamine ) - ⁇ , ⁇ -galacto-pyranoses participate in heating up to 90-100 ⁇ in 0, 4 liters of anhydrous water.
  • the resulting solution cools, brings up to 500 ml of glycerin, and filters through a bacterial filter. Pour 5 ml of flasks, cover with rubber rubbers, compress with hard bags, and sterilize. ⁇ regulate 97%.
  • the drug is intended for the treatment of severe immune, viral and bacterial diseases, as well as an effective medical treatment.
  • the resulting medicinal product of ⁇ D ⁇ currently has a resolution of the Ministry of Health ⁇ ⁇ ° 269/2000 for the use of medicine in the form of a pharmaceutical product.
  • FSC 42-3686-00 has been approved for a 10% stable solution for injections.
  • the pills are effective in the quality of both the preventative and the therapeutic agents and the different types of diseases.
  • Supplements containing 200 mg of the active substance used for administration to the body, in the form of rectal (suppositories) and vaginal, are produced.
  • Manufacturing activity (on the model of prosthetic disease) is claimed to be a medicinal product.
  • mice weighing 18 -22 g, were infected with a dose of 10 W 50. After 1 hour after infection, they administered drugs, 100 mg / kg, internally.
  • the leukemia ⁇ -388 was mimicked internally by male mice, line D, in the amount of 10 6 cells. Starting 2 days after chewing, the mice were injected with 0.1 ml of the compound, and the lively drugs were administered with 16 mg of the drug, 100 mg / day.
  • PRACTICAL ACTIVITY (on the model of leukemia kot-388) is claimed by the medicinal product.
  • the proposed medicinal product does not only have the unique advantage that it does not have any good Gest ⁇ ⁇ and ⁇ ⁇ ' ⁇ do not detect mutagenic activity.
  • the ingredients used for the production of the biological active part of the product are: 18 a) and its a ⁇ id ⁇ nu ⁇ susnaya ⁇ isl ⁇ a ⁇ izv ⁇ dnye imeyu ⁇ znachi ⁇ eln ⁇ smaller a ⁇ ivn ⁇ s ⁇ , barter znachi ⁇ eln ⁇ ⁇ ⁇ y ⁇ e ⁇ a ⁇ ev ⁇ iches ⁇ y inde ⁇ s and imee ⁇ ⁇ l ⁇ ⁇ iv ⁇ vi ⁇ usnuyu and immun ⁇ m ⁇ duli ⁇ uyuschuyu a ⁇ ivn ⁇ sti, mal ⁇ ⁇ as ⁇ v ⁇ imy in gid ⁇ bny ⁇ ⁇ as ⁇ v ⁇ i ⁇ elya ⁇ , ⁇ ichem chas ⁇ gig ⁇ s ⁇ ichny and ⁇ e ⁇ mu ⁇ l ⁇ ⁇ anya ⁇ sya.

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

Abstract

L'invention relève de la médecine, de la pharmacologie et de l'industrie chimique et pharmaceutique. Elle vise à créer une nouvelle préparation médicinale ayant une activité élevée et une large gamme d'action pharmacologique non spécifique; l'invention concerne aussi un procédé de fabrication de toutes les formes de médicaments existant à ce jour. La nouveauté consiste en la partie bioactive de la préparation qui contient un mélange d'acide acridone acétique ou de ses dérivés avec des éthers monosubstitués de monosaccharides; la partie bioactive a été traitée thermiquement conjointement avec un excipient pharmaceutiquement acceptable à des températures entre 80 °C et 120 °C. Il a été découvert que l'une des préparations médicinales les plus actives est une préparation contenant de l'Anandine, qui est un mélange d'acide N-acridone acétique (glucoaminopropylcarbacridone) et 3-0 (N,N-diméthylamino-n-propyl)-1,2:5,6- di-O-isopropylidène-α, D-glucofuranose (diméthylaminopropylglucofuranose). La préparation médicinale a été obtenue sous toutes les formes de médicaments connues. L'invention contient 6 séries d'exemples de fabrication de la préparation et de ces formes médicinales ainsi que des informations détaillées sur l'estimation expérimentale de toutes les activités biologiques énumérées dans le titre de l'invention, avec 7 tableaux de mesures comparatives. Les résultats ont montré qu'on a créé une nouvelle préparation facile à fabriquer, stable, adaptée à toutes les formes de médicaments et très efficaces dont l'activité biologique est supérieure à celles des analogues; en outre, sa gamme d'action pharmacologique est non spécifique et étonnamment étendue.
PCT/RU2002/000117 2001-03-20 2002-03-18 Preparation medicinale antitumorale, antivirale, antibacterienne, antiparasitaire, anti-inflammatoire, antifongique et immunomodulatrice, procede de fabrication et formes de medicaments WO2002074311A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EA200301035A EA005929B1 (ru) 2001-03-20 2002-03-18 Противоопухолевый, противовирусный, антибактериальный, противопаразитарный, противовоспалительный, иммуномодулирующий и противогрибковый лекарственный препарат, способ его изготовления и лекарственныеформы

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2001107818/14A RU2197248C2 (ru) 2001-03-20 2001-03-20 Лекарственный препарат, обладающий иммуномоделирующим, иммунокоррегирующим, противопаразитарным, противосклеротическим, противовирусным, противобактериальным, противогрибковым, противовоспалительным и противоопухолевым действием, и способ его приготовления
RU2001107818 2001-03-20

Publications (1)

Publication Number Publication Date
WO2002074311A1 true WO2002074311A1 (fr) 2002-09-26

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Application Number Title Priority Date Filing Date
PCT/RU2002/000117 WO2002074311A1 (fr) 2001-03-20 2002-03-18 Preparation medicinale antitumorale, antivirale, antibacterienne, antiparasitaire, anti-inflammatoire, antifongique et immunomodulatrice, procede de fabrication et formes de medicaments

Country Status (3)

Country Link
EA (1) EA005929B1 (fr)
RU (1) RU2197248C2 (fr)
WO (1) WO2002074311A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019100061A1 (fr) * 2017-11-20 2019-05-23 Silicon Swat, Inc. Dérivés d'acide oxoacridinyle acétique et procédés d'utilisation
US11414387B2 (en) 2017-11-20 2022-08-16 Stingthera, Inc. Oxoacridinyl acetic acid derivatives and methods of use

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0607254A2 (pt) * 2005-01-28 2009-08-25 Susan Szathmary composições imunologicamente ativa, método in vitro para identificação de peptìdeo ou proteìna, uso da composição e célula dendrìtica
RU2326115C2 (ru) 2005-11-21 2008-06-10 Ефаг АО Соли 1-алкиламино-1-дезоксиполиолов с 9-оксоакридин-10-уксусной кислотой, лекарственные препараты на их основе, применение, способы профилактики и лечения

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0692475A1 (fr) * 1993-04-01 1996-01-17 Limited Liability Partnership "Polysan" N-METHYLE-N-/$g(a),$g(D)-GLUCOPYRANOZIL/AMMONIAC-2-/ACRIDON-9-ON-10-YLE/ACETATE/CYCLOPHERONE DOTEE DE PROPRIETES DE PRODUCTION D'INTERFERON, ANTIVIRALES (Y COMPRIS L'ACTIVITE ANTI-VIH), ANTIPARASITAIRES, ANTI-PROMOTEUR ET RADIOPROTECTRICES
RU2093510C1 (ru) * 1996-09-26 1997-10-20 Олег Викторович Травкин Соли 2-дезокси-2-амино (или 2-метиламино)-d-глюкозы с n-акридонуксусной кислотой, обладающие противомикробной активностью
RU2118532C1 (ru) * 1996-04-10 1998-09-10 Олег Викторович Травкин Противоинфекционное, противовоспалительное и противоопухолевое лекарственное средство

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0692475A1 (fr) * 1993-04-01 1996-01-17 Limited Liability Partnership "Polysan" N-METHYLE-N-/$g(a),$g(D)-GLUCOPYRANOZIL/AMMONIAC-2-/ACRIDON-9-ON-10-YLE/ACETATE/CYCLOPHERONE DOTEE DE PROPRIETES DE PRODUCTION D'INTERFERON, ANTIVIRALES (Y COMPRIS L'ACTIVITE ANTI-VIH), ANTIPARASITAIRES, ANTI-PROMOTEUR ET RADIOPROTECTRICES
RU2118532C1 (ru) * 1996-04-10 1998-09-10 Олег Викторович Травкин Противоинфекционное, противовоспалительное и противоопухолевое лекарственное средство
RU2093510C1 (ru) * 1996-09-26 1997-10-20 Олег Викторович Травкин Соли 2-дезокси-2-амино (или 2-метиламино)-d-глюкозы с n-акридонуксусной кислотой, обладающие противомикробной активностью
WO1998013352A1 (fr) * 1996-09-26 1998-04-02 Oleg Viktorovich Travkin Sels de 2-desoxy-2-amino(ou 2-methylamino)-d-glucose comprenant de l'acide n-arachidonacetique et possedant une activite anti-microbienne

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019100061A1 (fr) * 2017-11-20 2019-05-23 Silicon Swat, Inc. Dérivés d'acide oxoacridinyle acétique et procédés d'utilisation
US10745358B2 (en) 2017-11-20 2020-08-18 Silicon Swat, Inc. Oxoacridinyl acetic acid derivatives and methods of use
CN111630036A (zh) * 2017-11-20 2020-09-04 西利康斯瓦特股份有限公司 氧代吖啶基乙酸衍生物及其使用方法
US11414387B2 (en) 2017-11-20 2022-08-16 Stingthera, Inc. Oxoacridinyl acetic acid derivatives and methods of use

Also Published As

Publication number Publication date
EA200301035A1 (ru) 2004-02-26
EA005929B1 (ru) 2005-08-25
RU2197248C2 (ru) 2003-01-27

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