EA201101327A1 - Замещенные 8-сульфонил-2,3,4,5-тетрагидро-1н-гамма-карболины, лиганды, фармацевтическая композиция, способ их получения и применения - Google Patents

Замещенные 8-сульфонил-2,3,4,5-тетрагидро-1н-гамма-карболины, лиганды, фармацевтическая композиция, способ их получения и применения

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Publication number
EA201101327A1
EA201101327A1 EA201101327A EA201101327A EA201101327A1 EA 201101327 A1 EA201101327 A1 EA 201101327A1 EA 201101327 A EA201101327 A EA 201101327A EA 201101327 A EA201101327 A EA 201101327A EA 201101327 A1 EA201101327 A1 EA 201101327A1
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EA
Eurasian Patent Office
Prior art keywords
receptors
optionally substituted
substituted
tetrahydro
general formula
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EA201101327A
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English (en)
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EA018944B1 (ru
Inventor
Андрей Александрович ИВАЩЕНКО
Александр Васильевич ИВАЩЕНКО
Володимир Михайлович КИСИЛЬ
Олег Дмитриевич МИТЬКИН
Николай Филиппович САВЧУК
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Андрей Александрович ИВАЩЕНКО
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Publication of EA201101327A1 publication Critical patent/EA201101327A1/ru
Publication of EA018944B1 publication Critical patent/EA018944B1/ru

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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Данное изобретение относится к новым замещенным 8-сульфонил-2,3,4,5-тетрагидро-1H-γ-карболинам общей формулы 1 и их фармацевтически приемлемым солям-лигандам, обладающим биологической активностью одновременно в отношении альфа-адреноцепторов, допаминовых рецепторов, гистаминовых рецепторов, имидазолиновых рецепторов, сигма рецепторов, норепинефриневых рецепторов, серотониновых рецепторов, к активным компонентам, фармацевтическим композициям, содержащим в качестве активного компонента новые лиганды, к новым лекарственным средствам, применяемым для лечения болезней и состояний центральной нервной системы. В общей формуле 1R1 представляет собой заместитель, выбранный из водорода, необязательно замещенного С-Салкила или C-Cалкилоксикарбонила; R2 представляет собой заместитель циклической системы, в том числе атом водорода, необязательно замещенный C-Салкил, необязательно замещенный С-Салкенил или замещенный сульфонил; R3 представляет собой необязательно замещенный арил или замещенную аминогруппу.
EA201101327A 2009-05-22 2010-04-30 Замещенные 8-сульфонил-2,3,4,5-тетрагидро-1н-гамма-карболины, лиганды, фармацевтическая композиция, способ их получения и применения EA018944B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2009119369/04A RU2404180C1 (ru) 2009-05-22 2009-05-22 Замещенные 8-сульфонил-2,3,4,5-тетрагидро-1н-гамма-карболины, лиганды, фармацевтическая композиция, способ их получения и применения
PCT/RU2010/000216 WO2010134846A1 (ru) 2009-05-22 2010-04-30 Замещенные 8-cульфohил-2,3,4,5-tetpaгидpo-1h-гamma- карболины, лиганды, фармацевтическая композиция, способ их получения и применения

Publications (2)

Publication Number Publication Date
EA201101327A1 true EA201101327A1 (ru) 2012-04-30
EA018944B1 EA018944B1 (ru) 2013-11-29

Family

ID=43126357

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201101327A EA018944B1 (ru) 2009-05-22 2010-04-30 Замещенные 8-сульфонил-2,3,4,5-тетрагидро-1н-гамма-карболины, лиганды, фармацевтическая композиция, способ их получения и применения

Country Status (6)

Country Link
US (1) US20120071493A1 (ru)
EP (1) EP2433939A1 (ru)
KR (1) KR20120028335A (ru)
EA (1) EA018944B1 (ru)
RU (1) RU2404180C1 (ru)
WO (1) WO2010134846A1 (ru)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111892593B (zh) * 2020-08-19 2021-11-16 南通大学 一种8-甲氧基-5H-吡啶并[4,3-b]吲哚及其合成方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2329044C1 (ru) * 2006-11-16 2008-07-20 Андрей Александрович Иващенко Лиганды 5-ht6 рецепторов, фармацевтическая композиция, способ ее получения и лекарственное средство

Also Published As

Publication number Publication date
WO2010134846A8 (ru) 2012-01-05
WO2010134846A1 (ru) 2010-11-25
RU2404180C1 (ru) 2010-11-20
EA018944B1 (ru) 2013-11-29
KR20120028335A (ko) 2012-03-22
US20120071493A1 (en) 2012-03-22
EP2433939A1 (en) 2012-03-28

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KG MD TJ TM RU

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

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