RU2771275C2 - Нейро-аттенуирующие кетаминовые и норкетаминовые соединения, их производные и способы их получения - Google Patents

Нейро-аттенуирующие кетаминовые и норкетаминовые соединения, их производные и способы их получения Download PDF

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RU2771275C2
RU2771275C2 RU2017119222A RU2017119222A RU2771275C2 RU 2771275 C2 RU2771275 C2 RU 2771275C2 RU 2017119222 A RU2017119222 A RU 2017119222A RU 2017119222 A RU2017119222 A RU 2017119222A RU 2771275 C2 RU2771275 C2 RU 2771275C2
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pharmaceutically acceptable
ketamine
acceptable salt
norketamine
compound
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RU2017119222A
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Russian (ru)
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RU2017119222A3 (enExample
RU2017119222A (ru
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Алекс НИВОРОЖКИН
Нельсон ЛАНДРАУ
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Аморса Терапьютикс, Инк.
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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
    • A61K31/13—Amines
    • A61K31/133—Amines having hydroxy groups, e.g. sphingosine
    • 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
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
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    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/001—Acyclic or carbocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/20—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
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  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
RU2017119222A 2014-11-04 2015-11-04 Нейро-аттенуирующие кетаминовые и норкетаминовые соединения, их производные и способы их получения RU2771275C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462074645P 2014-11-04 2014-11-04
US62/074,645 2014-11-04
PCT/US2015/059113 WO2016073653A1 (en) 2014-11-04 2015-11-04 Neuro-attenuating ketamine and norketamine compounds, derivatives thereof, and methods

Publications (3)

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RU2017119222A RU2017119222A (ru) 2018-12-06
RU2017119222A3 RU2017119222A3 (enExample) 2019-06-07
RU2771275C2 true RU2771275C2 (ru) 2022-04-29

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RU2017119222A RU2771275C2 (ru) 2014-11-04 2015-11-04 Нейро-аттенуирующие кетаминовые и норкетаминовые соединения, их производные и способы их получения

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US (6) US10252982B2 (enExample)
EP (2) EP4393487A3 (enExample)
JP (2) JP6882180B2 (enExample)
KR (1) KR102604397B1 (enExample)
CN (2) CN115521217A (enExample)
AU (1) AU2015343083B2 (enExample)
CA (1) CA2966737A1 (enExample)
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RS (1) RS65411B1 (enExample)
RU (1) RU2771275C2 (enExample)
SI (1) SI3215147T1 (enExample)
WO (1) WO2016073653A1 (enExample)

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WO2016186968A1 (en) * 2015-05-15 2016-11-24 The Arizona Board Of Regents On Behalf Of The University Of Arizona Compositions and methods for treating motor disorders
AU2016288188B2 (en) 2015-06-27 2021-08-05 Shenox Pharmaceuticals, Llc Ketamine transdermal delivery system
WO2017180589A1 (en) * 2016-04-11 2017-10-19 Auspex Pharmaceuticals, Inc. Deuterated ketamine derivatives
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US20190240184A1 (en) * 2016-10-27 2019-08-08 National University Corporation Chiba University Pharmaceutical applications for (s)-norketamine and salts thereof
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WO2018234568A2 (en) * 2017-06-23 2018-12-27 Develco Pharma Schweiz Ag HYDROXYNORKETAMINE FOR USE IN TREATING DEPRESSION
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US10869838B2 (en) 2017-10-10 2020-12-22 Douglas Pharmaceuticals, Ltd. Extended release pharmaceutical formulation
WO2019073408A1 (en) * 2017-10-10 2019-04-18 Douglas Pharmaceuticals Ltd. PROLONGED RELEASE PHARMACEUTICAL FORMULATION AND TREATMENT METHODS
US11471415B2 (en) 2017-10-10 2022-10-18 Douglas Pharmaceuticals, Ltd. Extended release pharmaceutical formulation and methods of treatment
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PL3505157T3 (pl) 2017-12-29 2022-04-11 Celon Pharma S.A. Kompozycja ketaminy w postaci suchego proszku do podawania dopłucnego w leczeniu depresji opornej na leczenie
CN118453559A (zh) 2018-02-15 2024-08-09 国立大学法人千叶大学 炎症性疾病或骨病的预防或治疗剂及医药组合物
CA3099293A1 (en) 2018-05-04 2019-11-07 Perception Neuroscience, Inc. Methods of treating substance abuse
BR112020023882A2 (pt) 2018-06-27 2021-02-09 Clexio Biosciences Ltd. método para tratar transtorno depressivo maior
US11865088B2 (en) 2018-10-05 2024-01-09 Clexio Biosciences Ltd. Method of treating major depressive disorder
EP3863617A1 (en) 2018-10-11 2021-08-18 Clexio Biosciences Ltd. Esketamine for use in treating major depressive disorder
CN113939286A (zh) * 2019-03-25 2022-01-14 道格拉斯制药有限公司 缓释药物制剂
US12589083B2 (en) 2019-05-07 2026-03-31 Clexio Biosciences Ltd. Abuse-deterrent dosage forms containing esketamine
EP3965733A4 (en) 2019-05-07 2023-01-11 Clexio Biosciences Ltd. ABUSE DETERRENT DOSAGE FORMS CONTAINING ESKETAMINE
CN114302721B (zh) * 2019-08-06 2025-07-18 加利福尼亚大学董事会 聚酮的可规模化制备
US12186280B2 (en) 2019-10-11 2025-01-07 Pike Therapeutics Inc. Pharmaceutical composition and method for treating seizure disorders
WO2021137148A1 (en) * 2019-12-30 2021-07-08 Clexio Biosciences Ltd. Dosage regime with esketamine for treating neuropsychiatric or neurological conditions
US12268658B2 (en) 2019-12-30 2025-04-08 Clexio Biosciences Ltd. Dosage regime with esketamine for treating major depressive disorder
US12478592B2 (en) 2019-12-30 2025-11-25 Clexio Biosciences Ltd. Dosage regime with esketamine for treating neuropsychiatric or neurological conditions
MX2022014599A (es) 2020-05-20 2022-12-16 Certego Therapeutics Inc Gaboxadol deuterado en anillo y su uso para el tratamiento de trastornos psiquiatricos.
CA3190204A1 (en) * 2020-09-24 2022-03-31 Paul William Glue Extended release pharmaceutical formulation
CN114524737B (zh) * 2020-11-23 2024-10-22 江苏恒瑞医药股份有限公司 一种取代的环己酮类化合物
GB202019952D0 (en) * 2020-12-17 2021-02-03 Neurocentrx Pharma Ltd Novel compositions
JP2024515891A (ja) * 2021-04-30 2024-04-10 プログレッシブ セラピューティクス インコーポレーテッド 情緒障害の処置のためのケタミン及びカンナビス
CN116730853A (zh) * 2022-03-04 2023-09-12 上海致根医药科技有限公司 新型氨基酮类化合物及其制备方法和用途

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US5384331A (en) * 1991-07-18 1995-01-24 Genentech, Inc. Ketamine analogues for treatment of thrombocytopenia
US20040248964A1 (en) * 2002-11-18 2004-12-09 Crooks Peter A. Analgesic uses of norketamine and ketamine/norketamine prodrugs
WO2009131794A1 (en) * 2008-03-27 2009-10-29 University Of Kentucky Research Foundation Opioid-ketamine and norketamine codrug combinations for pain management
US7638651B2 (en) * 2007-04-26 2009-12-29 Auspex Pharmaceuticals Substituted cyclohexanones
WO2010120797A2 (en) * 2009-04-13 2010-10-21 Auspex Pharmaceuticals, Inc. Methods of reduction of interpatient variability
RU2463049C2 (ru) * 2006-07-19 2012-10-10 Уотсон Лабораториес, Инк. Лекарственные формы с контролируемым высвобождением и соответствующие способы

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US5384331A (en) * 1991-07-18 1995-01-24 Genentech, Inc. Ketamine analogues for treatment of thrombocytopenia
US20040248964A1 (en) * 2002-11-18 2004-12-09 Crooks Peter A. Analgesic uses of norketamine and ketamine/norketamine prodrugs
RU2463049C2 (ru) * 2006-07-19 2012-10-10 Уотсон Лабораториес, Инк. Лекарственные формы с контролируемым высвобождением и соответствующие способы
US7638651B2 (en) * 2007-04-26 2009-12-29 Auspex Pharmaceuticals Substituted cyclohexanones
WO2009131794A1 (en) * 2008-03-27 2009-10-29 University Of Kentucky Research Foundation Opioid-ketamine and norketamine codrug combinations for pain management
WO2010120797A2 (en) * 2009-04-13 2010-10-21 Auspex Pharmaceuticals, Inc. Methods of reduction of interpatient variability

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LAI I et al. Ketamine Metabolism. Identification and Synthesis of Deaminated Products, Journal of Pharmaceutical Sciences, 1985, 74(4), p.486-488. Sulake, Rohidas S. et al. Synthesis of deuterium labeled ketamine metabolite dehydronorketamine-d4.Bioorganic & Medicinal Chemistry Letters,2011, 21(19), 5719-5721. *
Sulake, Rohidas S. et al. Synthesis of deuterium labeled ketamine metabolite dehydronorketamine-d4.Bioorganic & Medicinal Chemistry Letters,2011, 21(19), 5719-5721. *

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RU2017119222A3 (enExample) 2019-06-07
WO2016073653A1 (en) 2016-05-12
US11613515B2 (en) 2023-03-28
KR20170083575A (ko) 2017-07-18
EP3215147A1 (en) 2017-09-13
DK3215147T3 (da) 2024-04-02
US20220106258A1 (en) 2022-04-07
US20220402863A1 (en) 2022-12-22
KR102604397B1 (ko) 2023-11-21
AU2015343083A1 (en) 2017-06-08
US10252982B2 (en) 2019-04-09
US20170355663A1 (en) 2017-12-14
LT3215147T (lt) 2024-04-25
JP2021120389A (ja) 2021-08-19
US20260109663A1 (en) 2026-04-23
PL3215147T3 (pl) 2024-06-24
JP6882180B2 (ja) 2021-06-02
RS65411B1 (sr) 2024-05-31
EP3215147A4 (en) 2018-05-30
HUE066468T2 (hu) 2024-08-28
US11603348B2 (en) 2023-03-14
EP3215147B1 (en) 2024-02-28
US10981859B2 (en) 2021-04-20
US20190263749A1 (en) 2019-08-29
EP4393487A3 (en) 2024-08-21
CN107106529A (zh) 2017-08-29
SI3215147T1 (sl) 2024-05-31
FI3215147T3 (fi) 2024-04-18
PT3215147T (pt) 2024-04-18
EP4393487A2 (en) 2024-07-03
US20230192593A1 (en) 2023-06-22
US12466783B2 (en) 2025-11-11
RU2017119222A (ru) 2018-12-06
AU2015343083B2 (en) 2020-07-23
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CA2966737A1 (en) 2016-05-12
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