RU2458065C2 - Новые стероидные соединения, обладающие повышенной растворимостью в воде и устойчивостью к метаболизму, и способы их приготовления - Google Patents

Новые стероидные соединения, обладающие повышенной растворимостью в воде и устойчивостью к метаболизму, и способы их приготовления Download PDF

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RU2458065C2
RU2458065C2 RU2009107537/04A RU2009107537A RU2458065C2 RU 2458065 C2 RU2458065 C2 RU 2458065C2 RU 2009107537/04 A RU2009107537/04 A RU 2009107537/04A RU 2009107537 A RU2009107537 A RU 2009107537A RU 2458065 C2 RU2458065 C2 RU 2458065C2
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pregnan
ethynyl
hydroxy
fluoro
oxime
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RU2009107537/04A
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Russian (ru)
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RU2009107537A (ru
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Торбьёрн БЭКСТРЁМ (SE)
Торбьёрн БЭКСТРЁМ
Джинна РАГАГНИН (SE)
Джинна РАГАГНИН
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Юмекрайн Аб
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by only one oxygen atom doubly bound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0016—Oximes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C07J7/007—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified not substituted in position 17 alfa

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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
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  • Rheumatology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
RU2009107537/04A 2006-11-21 2007-11-20 Новые стероидные соединения, обладающие повышенной растворимостью в воде и устойчивостью к метаболизму, и способы их приготовления RU2458065C2 (ru)

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US86065806P 2006-11-21 2006-11-21
US60/860,658 2006-11-21

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RU2009107537A RU2009107537A (ru) 2010-12-27
RU2458065C2 true RU2458065C2 (ru) 2012-08-10

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US (9) US8580983B2 (oth)
EP (4) EP2792681B1 (oth)
JP (5) JP5386362B2 (oth)
AU (1) AU2007322423C1 (oth)
BR (2) BR122013033954B8 (oth)
CA (2) CA2664126C (oth)
DK (3) DK2792681T3 (oth)
ES (3) ES2662500T3 (oth)
HU (3) HUE026961T2 (oth)
IN (1) IN2014DN02014A (oth)
MX (1) MX2009005335A (oth)
PL (3) PL2792681T3 (oth)
PT (1) PT2097437E (oth)
RU (1) RU2458065C2 (oth)
SI (1) SI2097437T1 (oth)
WO (1) WO2008063128A1 (oth)

Cited By (13)

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RU2667065C2 (ru) * 2012-11-28 2018-09-14 Энсэрм (Энститю Насьональ Де Ля Санте Э Де Ля Решерш Медикаль) Производные прегненолона
RU2712786C2 (ru) * 2015-01-12 2020-01-31 Умекрин Когнишн Аб 3α-ЭТИНИЛ,3β-ГИДРОКСИ,5α-ПРЕГНАН-20-ОКСИМ ДЛЯ ПРИМЕНЕНИЯ ПРИ ЛЕЧЕНИИ РАССТРОЙСТВ ЦНС
US11613556B2 (en) 2016-10-18 2023-03-28 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
RU2797408C2 (ru) * 2018-02-11 2023-06-05 Цзянсу Хэнсох Фармасьютикал Груп Ко., Лтд. Регуляторы-производные стероидов, способы их получения и их применение
US11732000B2 (en) 2015-07-06 2023-08-22 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US11851457B2 (en) 2016-10-18 2023-12-26 Sage Therapeutics Oxysterols and methods of use thereof
US11878995B2 (en) 2016-05-06 2024-01-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US11884697B2 (en) 2016-04-01 2024-01-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US11905309B2 (en) 2013-03-13 2024-02-20 Sage Therapeutics, Inc. Neuroactive steroids and methods of use thereof
US12129275B2 (en) 2011-09-08 2024-10-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
US12129276B2 (en) 2014-06-18 2024-10-29 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US12268697B2 (en) 2015-07-06 2025-04-08 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US12415830B2 (en) 2019-01-08 2025-09-16 Chengdu kanghong pharmaceutical co ltd Steroid compound, and use thereof and preparation method therefor

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IN2014DN02014A (oth) 2006-11-21 2015-07-10 Umecrine Ab
CN101585862B (zh) * 2008-05-20 2014-12-17 梅克芳股份公司 甾族化合物
CA2786330C (en) 2010-01-14 2013-11-19 Umecrine Mood Ab A pharmaceutical composition comprising 3-beta-hydroxy-5-alpha-pregnan-20-one with improved storage and solubility properties
WO2011138460A1 (en) * 2010-05-07 2011-11-10 Institut National De La Sante Et De La Recherche Medicale (Inserm) Progesterone receptor antagonists and uses thereof
CA2935015C (en) 2014-01-29 2022-05-31 Umecrine Cognition Ab Steroid compound for use in the treatment of hepatic encephalopathy
US10774108B2 (en) * 2014-11-27 2020-09-15 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
DE102015120587A1 (de) 2015-11-26 2017-06-01 Brandenburgische Technische Universität Cottbus-Senftenberg Verfahren zur selektiven Oxygenierung von Testosteron und Testosteron-ähnlichen Steroiden
US10278977B2 (en) 2016-06-06 2019-05-07 Umecrine Cognition Ab Methods for treating hypersomnolence
WO2018147792A1 (en) 2017-02-10 2018-08-16 Asarina Pharma Ab 3-beta-hydroxy-5-alpha-pregnan-20-one for use in medical treatment
EP3579842A4 (en) 2017-02-10 2020-12-23 Asarina Pharma AB 3-BETA-HYDROXY-5-ALPHA-PRÉGNAN-20-ONE FOR USE IN THE TREATMENT OF ESSENTIAL TREMMENTS
CN111432805B (zh) 2017-11-27 2023-02-17 梅克里内科尼蒂翁公司 3α-乙炔基-3β-羟基雄甾烷-17-酮肟的药物制剂
CA3094026A1 (en) 2018-04-05 2019-10-10 Asarina Pharma Aps Gaba-a antagonists for treating substance withdrawal disorders
CN112457362B (zh) * 2019-09-06 2023-09-19 上海青东生物科技有限公司 一种卤代四环三萜衍生物及其制备与应用
EP4079307A1 (en) 2021-04-20 2022-10-26 Umecrine Cognition AB New medical use
CN118251403A (zh) 2021-11-10 2024-06-25 梅克芳股份公司 用于调节GABA-A受体的α-3亚型的3.α.取代的3.β.-羟基17-肟化的雄甾烷化合物
EP4430056A1 (en) 2021-11-10 2024-09-18 Umecrine AB 3.beta.-hydroxy, 3.alpha.-ethyl steroids for modulation of the alpha-3 subtype of the gaba-a receptor
EP4429669A1 (en) 2021-11-10 2024-09-18 Umecrine AB Steroid as a modulator of gabaa receptor
EP4389129A1 (en) 2022-12-22 2024-06-26 Umecrine Cognition AB 3a-ethynyl-3beta hydroxyandrostan 17-one oxime for treating parkinson's disease and l-dopa-induced dyskinesia
WO2025252725A1 (en) 2024-06-04 2025-12-11 Umecrine Cognition Ab Novel pharmaceutical formulation of golexanolone
WO2025252724A1 (en) 2024-06-04 2025-12-11 Umecrine Cognition Ab Novel pharmaceutical formulation of golexanolone

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US5120723A (en) * 1987-08-25 1992-06-09 University Of Southern California Method, compositions, and compounds for modulating brain excitability
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