KR102771577B1 - 3α-에티닐-3β-하이드록시안드로스탄-17-온 옥심의 약학적 제형 - Google Patents

3α-에티닐-3β-하이드록시안드로스탄-17-온 옥심의 약학적 제형 Download PDF

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KR102771577B1
KR102771577B1 KR1020207018543A KR20207018543A KR102771577B1 KR 102771577 B1 KR102771577 B1 KR 102771577B1 KR 1020207018543 A KR1020207018543 A KR 1020207018543A KR 20207018543 A KR20207018543 A KR 20207018543A KR 102771577 B1 KR102771577 B1 KR 102771577B1
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propylene glycol
pharmaceutical formulation
glycerol
oxime
hydroxyandrostan
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KR20200093008A (ko
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폴 알헤디프
마그누스 도버스코그
마야 요한손
토마스 마이어
니콜라스 시퍼
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유메크린 코그니션 에이비
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/569Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7016Disaccharides, e.g. lactose, lactulose

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (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)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020207018543A 2017-11-27 2018-11-27 3α-에티닐-3β-하이드록시안드로스탄-17-온 옥심의 약학적 제형 Active KR102771577B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762590757P 2017-11-27 2017-11-27
US62/590,757 2017-11-27
PCT/EP2018/082727 WO2019102040A1 (en) 2017-11-27 2018-11-27 PHARMACEUTICAL FORMULATION OF 3α-ETHYNYL-3β-HYDROXYANDROSTAN-17-ONE OXIME

Publications (2)

Publication Number Publication Date
KR20200093008A KR20200093008A (ko) 2020-08-04
KR102771577B1 true KR102771577B1 (ko) 2025-02-20

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US (2) US10603326B2 (https=)
EP (1) EP3716954A1 (https=)
JP (1) JP7314459B2 (https=)
KR (1) KR102771577B1 (https=)
CN (1) CN111432805B (https=)
AU (1) AU2018374029B2 (https=)
BR (1) BR112020010519A2 (https=)
CA (1) CA3083555A1 (https=)
IL (1) IL274893B2 (https=)
MX (1) MX391097B (https=)
UA (1) UA128186C2 (https=)
WO (1) WO2019102040A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3716954A1 (en) 2017-11-27 2020-10-07 Umecrine Cognition AB Pharmaceutical formulation of 3 -ethynyl-3 -hydroxyandrostan-17-one oxime
EP4079307A1 (en) 2021-04-20 2022-10-26 Umecrine Cognition AB New medical use
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

Citations (2)

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WO2015114308A1 (en) 2014-01-29 2015-08-06 Umecrine Cognition Ab Steroid compound for use in the treatment of hepatic encephalopathy
WO2016033556A1 (en) * 2014-08-28 2016-03-03 Lipocine Inc. BIOAVAILABLE SOLID STATE (17-β)-HYDROXY-4-ANDROSTEN-3-ONE ESTERS

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GB9608719D0 (en) 1996-04-26 1996-07-03 Scherer Ltd R P Pharmaceutical compositions
SE511313C2 (sv) 1997-01-13 1999-09-06 Gs Dev Ab Komposition med reglerad frisättning innefattande fettsyraester av diacylglycerol
GB9907715D0 (en) 1999-04-01 1999-05-26 Scherer Corp R P Pharmaceutical compositions
KR20010100194A (ko) * 2000-03-13 2001-11-14 박호군 여러 가지 물질의 가용화용 조성물과 제형 및 그들의제조방법
US20040191207A1 (en) 2003-03-31 2004-09-30 Lipari John M. Alpha-hydroxy acid ester drug delivery compositions and methods of use
US20100209496A1 (en) 2006-09-06 2010-08-19 Eleni Dokou Liquid and semi-solid pharmaceutical formulations for oral administration of a substituted amide
DK2792681T3 (en) 2006-11-21 2017-01-23 Umecrine Ab Use of Pregnancy and Androstan Steroids in the Preparation of a Pharmaceutical Composition for the Treatment of CNS Disorders.
RU2012133627A (ru) 2010-01-14 2014-04-20 Умекрине Муд Аб Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, с улучшенными свойствами хранения и растворимости
US9034858B2 (en) 2010-11-30 2015-05-19 Lipocine Inc. High-strength testosterone undecanoate compositions
US8951996B2 (en) 2011-07-28 2015-02-10 Lipocine Inc. 17-hydroxyprogesterone ester-containing oral compositions and related methods
US9801819B2 (en) 2012-06-28 2017-10-31 Johnson & Johnson Consumer Inc. Racecadotril compositions
HK1223300A1 (zh) * 2013-06-03 2017-07-28 Tolmar, Inc. 皮质类固醇组合物
WO2015193224A1 (en) 2014-06-17 2015-12-23 Merck Sharp & Dohme B.V. Stable formulations of testosterone undecanoate
KR101679992B1 (ko) 2015-12-31 2016-11-28 주식회사 유유제약 프로필렌글리콜 모노라우레이트를 포함하는 두타스테리드의 약학적 조성물 및 이의 제조 방법
KR101716878B1 (ko) 2016-05-12 2017-03-15 주식회사 유유제약 글리세롤 지방산에스테르유도체 또는 프로필렌글리콜 지방산에스테르유도체를 함유한 두타스테리드와 타다라필의 복합 캡슐제제 조성물 및 이의 제조방법
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EP3716954A1 (en) 2017-11-27 2020-10-07 Umecrine Cognition AB Pharmaceutical formulation of 3 -ethynyl-3 -hydroxyandrostan-17-one oxime

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WO2015114308A1 (en) 2014-01-29 2015-08-06 Umecrine Cognition Ab Steroid compound for use in the treatment of hepatic encephalopathy
WO2016033556A1 (en) * 2014-08-28 2016-03-03 Lipocine Inc. BIOAVAILABLE SOLID STATE (17-β)-HYDROXY-4-ANDROSTEN-3-ONE ESTERS

Also Published As

Publication number Publication date
IL274893B1 (en) 2024-04-01
KR20200093008A (ko) 2020-08-04
EP3716954A1 (en) 2020-10-07
US20190358244A1 (en) 2019-11-28
CN111432805B (zh) 2023-02-17
MX2020005442A (es) 2022-03-30
US11123351B2 (en) 2021-09-21
RU2020121142A3 (https=) 2022-03-28
AU2018374029B2 (en) 2024-01-11
IL274893B2 (en) 2024-08-01
US20200297737A1 (en) 2020-09-24
IL274893A (en) 2020-07-30
CN111432805A (zh) 2020-07-17
UA128186C2 (uk) 2024-05-01
NZ764901A (en) 2025-05-02
US10603326B2 (en) 2020-03-31
CA3083555A1 (en) 2019-05-31
MX391097B (es) 2025-03-21
WO2019102040A1 (en) 2019-05-31
AU2018374029A1 (en) 2020-06-18
BR112020010519A2 (pt) 2020-10-20
JP7314459B2 (ja) 2023-07-26
RU2020121142A (ru) 2021-12-29
JP2021504468A (ja) 2021-02-15

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