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
    • 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
    • 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
    • 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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)

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

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US (6) US10252982B2 (enExample)
EP (2) EP3215147B1 (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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PT (1) PT3215147T (enExample)
RS (1) RS65411B1 (enExample)
RU (1) RU2771275C2 (enExample)
SI (1) SI3215147T1 (enExample)
WO (1) WO2016073653A1 (enExample)

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US11426366B2 (en) * 2015-05-15 2022-08-30 Arizona Board Of Regents On Behalf Of The Universsity Of Arizona Compositions and methods for treating motor disorders
CN107847469A (zh) 2015-06-27 2018-03-27 美国神农制药责任有限公司 氯胺酮透皮递送系统
AU2017250086A1 (en) * 2016-04-11 2018-09-20 Clexio Biosciences Ltd. Deuterated ketamine derivatives
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WO2018079693A1 (ja) * 2016-10-27 2018-05-03 国立大学法人 千葉大学 （ｓ）－ノルケタミンおよびその塩の医薬品としての応用
MX2019012285A (es) 2017-04-13 2020-11-06 Ovid Therapeutics Inc Metodos de tratamiento de encefalopatias del desarrollo.
EP3641742B1 (en) * 2017-06-23 2026-03-25 Ketabon GmbH Hydroxynorketamine for the use in the treatment of depression
CN111201217A (zh) 2017-07-31 2020-05-26 斯玛尔药物有限公司 羟基去甲氯胺酮的晶型
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US12090123B2 (en) 2017-10-10 2024-09-17 Douglas Pharmaceuticals Ltd. Extended release pharmaceutical formulation
US11471415B2 (en) 2017-10-10 2022-10-18 Douglas Pharmaceuticals, Ltd. Extended release pharmaceutical formulation and methods of treatment
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EP3501503A1 (en) * 2017-12-22 2019-06-26 Cosmo Technologies Ltd. Solid delivery composition
DK3505157T3 (da) 2017-12-29 2022-02-28 Celon Pharma Sa Tørpulver-ketaminsammensætning til pulmonal indgivelse ved behandlingsresistent depression
WO2019160057A1 (ja) 2018-02-15 2019-08-22 国立大学法人千葉大学 炎症性疾患若しくは骨疾患の予防又は治療剤及び医薬組成物
CN118121577A (zh) 2018-05-04 2024-06-04 感知神经科学公司 治疗物质滥用的方法
CA3103440A1 (en) 2018-06-27 2020-01-02 Clexio Biosciences Ltd. Method of treating major depressive disorder
WO2020070706A1 (en) 2018-10-05 2020-04-09 Clexio Biosciences Ltd. Dosage regime of esketamine for treating major depressive disorder
WO2020075134A1 (en) 2018-10-11 2020-04-16 Clexio Biosciences Ltd. Esketamine for use in treating major depressive disorder
KR20220002905A (ko) * 2019-03-25 2022-01-07 더글라스 파머수티클스 리미티드 서방형 약학 제제
US11324707B2 (en) 2019-05-07 2022-05-10 Clexio Biosciences Ltd. Abuse-deterrent dosage forms containing esketamine
US12589083B2 (en) 2019-05-07 2026-03-31 Clexio Biosciences Ltd. Abuse-deterrent dosage forms containing esketamine
EP4009966A4 (en) * 2019-08-06 2023-12-13 The Regents of the University of California PREPARATION OF SCALABLE POLYKETIDES
US12186280B2 (en) 2019-10-11 2025-01-07 Pike Therapeutics Inc. Pharmaceutical composition and method for treating seizure disorders
WO2021137147A1 (en) 2019-12-30 2021-07-08 Clexio Biosciences Ltd. Dosage regime with esketamine for treating major depressive disorder
JP2023507926A (ja) * 2019-12-30 2023-02-28 クレキシオ バイオサイエンシーズ エルティーディー． 神経精神状態または神経学的状態を治療するためのエスケタミンを用いた投与計画
IL298334A (en) * 2020-05-20 2023-01-01 Certego Therapeutics Inc Ring deuterated gaboxadol and its use for the treatment of psychiatric disorders
JP2023543211A (ja) * 2020-09-24 2023-10-13 ダグラス ファーマシューティカルズ エルティーディー． 徐放性医薬製剤
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
US20240207338A1 (en) * 2021-04-30 2024-06-27 Progressive Therapeutics Inc Ketamine and cannabis for the treatment of emotional disorders
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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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
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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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US10981859B2 (en) 2021-04-20
RU2017119222A3 (enExample) 2019-06-07
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EP3215147B1 (en) 2024-02-28
US20230192593A1 (en) 2023-06-22
WO2016073653A1 (en) 2016-05-12
LT3215147T (lt) 2024-04-25
EP4393487A3 (en) 2024-08-21
AU2015343083A1 (en) 2017-06-08
PT3215147T (pt) 2024-04-18
SI3215147T1 (sl) 2024-05-31
CN115521217A (zh) 2022-12-27
RU2017119222A (ru) 2018-12-06
US20190263749A1 (en) 2019-08-29
JP2021120389A (ja) 2021-08-19
US12466783B2 (en) 2025-11-11
US20170355663A1 (en) 2017-12-14
US11613515B2 (en) 2023-03-28
HUE066468T2 (hu) 2024-08-28
KR20170083575A (ko) 2017-07-18
EP3215147A4 (en) 2018-05-30
RS65411B1 (sr) 2024-05-31
PL3215147T3 (pl) 2024-06-24
FI3215147T3 (fi) 2024-04-18
ES2977383T3 (es) 2024-08-22
US20260109663A1 (en) 2026-04-23
US10252982B2 (en) 2019-04-09
US20220106258A1 (en) 2022-04-07
KR102604397B1 (ko) 2023-11-21
CN107106529A (zh) 2017-08-29
DK3215147T3 (da) 2024-04-02
JP2018501299A (ja) 2018-01-18
JP6882180B2 (ja) 2021-06-02
US20220402863A1 (en) 2022-12-22
US11603348B2 (en) 2023-03-14
CA2966737A1 (en) 2016-05-12
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