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WO1999023056A1 - Nouveaux medicaments anti-convulsions - Google Patents

Nouveaux medicaments anti-convulsions Download PDF

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Publication number
WO1999023056A1
WO1999023056A1 PCT/RU1997/000350 RU9700350W WO9923056A1 WO 1999023056 A1 WO1999023056 A1 WO 1999023056A1 RU 9700350 W RU9700350 W RU 9700350W WO 9923056 A1 WO9923056 A1 WO 9923056A1
Authority
WO
WIPO (PCT)
Prior art keywords
acid
bicyclo
kabonovic
salts
salt
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/RU1997/000350
Other languages
English (en)
Russian (ru)
Inventor
Susanna Askanazovna Saakian
Inessa Ivanovna Kritskaya
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 AU64254/98A priority Critical patent/AU6425498A/en
Priority to PCT/RU1997/000350 priority patent/WO1999023056A1/fr
Publication of WO1999023056A1 publication Critical patent/WO1999023056A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C61/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C61/12—Saturated polycyclic compounds
    • C07C61/125—Saturated polycyclic compounds having a carboxyl group bound to a condensed ring system
    • C07C61/13—Saturated polycyclic compounds having a carboxyl group bound to a condensed ring system having two rings

Definitions

  • the invention is available for the manufacture of new medicinal devices that are equipped with a proprietary vessel.
  • Advantageous activities may have a bearing on various substances that weaken the excitation process or enhance the process of mediation in the central non-payload system.
  • One of the best known ship ships of 25 is a phenobital.
  • diphenin, hexamidine, diazepam, clones, etoxusimide and others are also used.
  • the present invention is subject to 0 new derivatives of bicycles [2, 2, 2] of oxo-2-carboxylic acid I.
  • the resulting salts are 5 non-toxic compounds that are well-disposed in water and reasonably moderate in ethanol, are stable in emergency and in disinfectant. They are not hygienic, do not have stable crystalline hydrates, and aqueous products have a neutral reaction.
  • the structure and composition of the obtained 0 salts are confirmed by the data of elemental analysis, as well as by the methods of research and experimentation.
  • the invention also includes methods of practical use of the declared compounds by introducing the principle of compounds of the formula I in the 5th used for the consolidated use. Ways to get rid of the therapeutic, pharmacological and pharmaceutical use.
  • 10 is used in its general sense, which includes exclusion, restraint, mitigation of the severity of the disease or symptom, or its consequence.
  • compositions of a predominantly 5 exist in the form of accrued units calculated for the receipt of the desired therapeutic effect. They can be administered orally in the form of tablets, capsules, or powders, in the form of generic, internal or external injections, and are used internally.
  • the declared salts are converted to the corresponding products with 0 use of pharmaceuticals or diluents.
  • the inventive invention is illustrated by the communication methods and data on the pharmaceutical activity of the claimed compounds.
  • a solution of 0.18 mol ⁇ or ⁇ or 0.9 mol 25 in water contains 0.2 ml of bicyclic acid [2, 2, 2] acid 2 with ⁇ . ⁇ l. 84-86 ° C, 1 hour ⁇ e ⁇ emeshivayu ⁇ ⁇ i ⁇ mna ⁇ n ⁇ y ⁇ em ⁇ e ⁇ a ⁇ u ⁇ e, izby ⁇ ⁇ isl ⁇ y ⁇ il ⁇ vyvayu ⁇ or izvle ⁇ ayu ⁇ ⁇ ganiches ⁇ im ⁇ as ⁇ v ⁇ i ⁇ elem, v ⁇ dny ⁇ as ⁇ v ⁇ 30 u ⁇ a ⁇ ivayu ⁇ in va ⁇ uume d ⁇ su ⁇ a ⁇ i 120-140 ° C ⁇ luchayu ⁇ na ⁇ ievuyu s ⁇ l, vy ⁇ d 93 ⁇ . ⁇ l.
  • STRUCTURAL-CHARACTERISTIC are 0 areas of valency vibrations of large anion-doubles at 1570-1554 and 1420-1411 cm ⁇ 1 in oil; a multiplet of 2.42 ppm, corresponding to ⁇ -negative, in the case of a direct magnetic resonance (200.13 MHz, ⁇ ⁇ ⁇ ); Nine 5 signals at 21.72, 23.71 ( ⁇ 4 ), 24.75, 24.96, 26.03, 27.71 ( ⁇ ), 29.03, 44.22 and 185.65 ( ⁇ -) ppm in a carbon-magnetic resonance spectrum (50.31 MHz, ⁇ ⁇ ⁇ ). Obtained by this method, the sodium salt is not active in the optical activity. 0
  • magnesium salt is bicyclic [2, 2, 2]
  • 35 is apt to be optically inactive.
  • the hazardous substance (propylene oxide) - the testing agent - is one of the most dispersed shipping agents that cause personal injury.
  • the studied drug was alive in 15-25 minutes. before testing in a dose of 200 mg / kg, and
  • the latent process was detected before the occurrence of motor excitation and all subsequent stages, the strength and duration of the motor reactions and the actual shipping phase.
  • the claimed compounds are distinguished by the design of all of the known medical devices received by us.
  • phenoben 20 frames of the same method with well-known standards from different classes of courthouse products: phenoben, diphenin and konvuleksom (table 4). Reacted in doses of 15-30 mg / kg, weakening the severity of seizure, causes depression of a total of 25 motor activity, attack, dormancy, i.e. genealogy transmission. Diphenin at a dose of 20 mg / kg slightly weakens the severity of the seizure without pronounced “ acute” effect and slightly lengthens the latent foods, not
  • 35 may be attributed to low-dose drugs of the 4th group. .
  • the first dose was 29 mg / kg
  • the second dose was 200 mg / kg
  • the dose was 600 mg / kg each dose.
  • Sacracin did not have a noticeable effect on livelihoods and on conditionally-reflexive activity, i.e. on memory processes (fig. 1).
  • 20 sensitivities of a cholinergic patient is a neuropsychiatric one.
  • the dose of the drug before the start of the drug is founded on founded on a dose of the drug before the start of the drug.
  • Sensitization - Solution Medium Medium, mg / kg mg / kg live (+) -analysis.

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Cette invention concerne une préparation anti-épileptique d'une grande efficacité qui consiste en un des nouveaux dérivés d'acide carboxylique alicyclique. Dans un même aspect, cette invention concerne également des sels de métaux alcalins ou alcalino-terreux d'acide bicyclo-[2,2,2]octan-carboxylique, lesquels sels possèdent une action anti-convulsions. Ces composés ne sont pas toxiques, n'ont aucun effet adverse et permettent de prévenir et de traiter l'épilepsie grâce à leur action sélective à l'égard des réactions convulsives chez les mammifères. Le sel le plus efficace parmi ceux proposés consiste en un sel de Na dudit acide, dénommé sacricine. Cette préparation est de préférence administrée par voie intra-nasale dans l'organisme. Cette invention concerne en outre des compositions pharmaceutiques contenant les sels susmentionnés, ainsi que leur utilisation dans la production de médicaments qui permettent de soigner ou de prévenir et même d'interrompre des états convulsifs chez les mammifères, y compris chez l'homme.
PCT/RU1997/000350 1997-11-05 1997-11-05 Nouveaux medicaments anti-convulsions Ceased WO1999023056A1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU64254/98A AU6425498A (en) 1997-11-05 1997-11-05 New anticonvulsant drugs
PCT/RU1997/000350 WO1999023056A1 (fr) 1997-11-05 1997-11-05 Nouveaux medicaments anti-convulsions

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/RU1997/000350 WO1999023056A1 (fr) 1997-11-05 1997-11-05 Nouveaux medicaments anti-convulsions

Publications (1)

Publication Number Publication Date
WO1999023056A1 true WO1999023056A1 (fr) 1999-05-14

Family

ID=20130159

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU1997/000350 Ceased WO1999023056A1 (fr) 1997-11-05 1997-11-05 Nouveaux medicaments anti-convulsions

Country Status (2)

Country Link
AU (1) AU6425498A (fr)
WO (1) WO1999023056A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010071872A2 (fr) 2008-12-20 2010-06-24 Ase Pharmaceuticals, Llc Dérivés bicycliques (2.2.2) et leurs procédés d'utilisation

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2065104A (en) * 1979-10-26 1981-06-24 Secr Defence Liquid Crystal Bicyclo-octane Compounds
FR2547814A1 (fr) * 1983-06-22 1984-12-28 Sanofi Sa Derives de l'acide bicyclo (3.2.1.) octane carboxylique, leur procede de preparation et leur application therapeutique
EP0132964A2 (fr) * 1983-06-29 1985-02-13 Richter Gedeon Vegyeszeti Gyar R.T. Dérivés de 2-azabicyclo[2,2,2]-octane
US4826866A (en) * 1987-11-02 1989-05-02 A. H. Robins Company, Incorporated 3-amino-5-methyl-1H-pyrazole-4-carboxylic acids and esters thereof as anticonvulsants, muscle relaxants and anxiolytics
US4956124A (en) * 1987-05-11 1990-09-11 Henkel Kommanditgesellschaft Auf Aktien Bicyclic decanedioic acids, a process for their production, and their use as flotation aids
RU2091366C1 (ru) * 1992-06-16 1997-09-27 Инесса Ивановна Крицкая Натриевая соль бицикло(2.2.2.)октан -2-карбоновой кислоты, проявляющая противосудорожную активность

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2065104A (en) * 1979-10-26 1981-06-24 Secr Defence Liquid Crystal Bicyclo-octane Compounds
FR2547814A1 (fr) * 1983-06-22 1984-12-28 Sanofi Sa Derives de l'acide bicyclo (3.2.1.) octane carboxylique, leur procede de preparation et leur application therapeutique
EP0132964A2 (fr) * 1983-06-29 1985-02-13 Richter Gedeon Vegyeszeti Gyar R.T. Dérivés de 2-azabicyclo[2,2,2]-octane
US4956124A (en) * 1987-05-11 1990-09-11 Henkel Kommanditgesellschaft Auf Aktien Bicyclic decanedioic acids, a process for their production, and their use as flotation aids
US4826866A (en) * 1987-11-02 1989-05-02 A. H. Robins Company, Incorporated 3-amino-5-methyl-1H-pyrazole-4-carboxylic acids and esters thereof as anticonvulsants, muscle relaxants and anxiolytics
RU2091366C1 (ru) * 1992-06-16 1997-09-27 Инесса Ивановна Крицкая Натриевая соль бицикло(2.2.2.)октан -2-карбоновой кислоты, проявляющая противосудорожную активность

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
MASHKOVSKY M.D., Lekarstvennye Sredstva, Chast II, Moscow, MEDITSINA, 1993, pages 111-112. *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010071872A2 (fr) 2008-12-20 2010-06-24 Ase Pharmaceuticals, Llc Dérivés bicycliques (2.2.2) et leurs procédés d'utilisation
WO2010071872A3 (fr) * 2008-12-20 2010-11-25 Ase Pharmaceuticals, Llc Dérivés bicycliques (2.2.2) et leurs procédés d'utilisation
CN102300573A (zh) * 2008-12-20 2011-12-28 苏珊娜·A·萨基扬 [2.2.2]双环衍生物及其使用方法
JP2012512913A (ja) * 2008-12-20 2012-06-07 サアキアン，スザンナ，エイ． ［２．２．２］二環式誘導体及び使用方法
AU2009327316B2 (en) * 2008-12-20 2015-06-04 Ase Pharmaceuticals, Llc [2.2.2] bicyclic derivatives and methods of use
US20170000750A1 (en) * 2008-12-20 2017-01-05 Ase Pharmaceuticals, Llc [2.2.2] bicyclic derivatives and methods of use
CN106309418A (zh) * 2008-12-20 2017-01-11 艾思益制药有限责任公司 [2.2.2]双环衍生物及其使用方法
KR101840178B1 (ko) * 2008-12-20 2018-03-19 에이에스이 파마수티컬스, 엘엘씨. 〔２.２.２〕비시클릭 유도체 및 사용방법
US9943493B2 (en) * 2008-12-20 2018-04-17 Ase Pharmaceuticals, Llc [2.2.2] bicyclic derivatives and methods of use
RU2691406C2 (ru) * 2008-12-20 2019-06-13 ЭйЭсИ Фармасьютикалз, ЭлЭлСи [2.2.2]-бициклические производные и способы применения
US10966944B2 (en) * 2008-12-20 2021-04-06 Ase Pharmaceuticals, Llc [2.2.2] bicyclic derivatives and methods of use

Also Published As

Publication number Publication date
AU6425498A (en) 1999-05-24

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