CN111432805B - 3α-乙炔基-3β-羟基雄甾烷-17-酮肟的药物制剂 - Google Patents

3α-乙炔基-3β-羟基雄甾烷-17-酮肟的药物制剂 Download PDF

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CN111432805B
CN111432805B CN201880076423.8A CN201880076423A CN111432805B CN 111432805 B CN111432805 B CN 111432805B CN 201880076423 A CN201880076423 A CN 201880076423A CN 111432805 B CN111432805 B CN 111432805B
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propylene glycol
pharmaceutical formulation
ethynyl
oxime
amount
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CN111432805A (zh
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P·阿赫德夫
M·多夫斯科格
M·约翰逊
T·梅耶尔
N·施佩尔
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Umecrine Cognition AB
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Umecrine Cognition AB
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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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds 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
    • A61K31/568—Compounds 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
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds 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
    • A61K31/568—Compounds 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
    • A61K31/569—Compounds 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
    • 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
    • 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
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • 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
    • 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
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7016—Disaccharides, e.g. lactose, lactulose

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (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)
CN201880076423.8A 2017-11-27 2018-11-27 3α-乙炔基-3β-羟基雄甾烷-17-酮肟的药物制剂 Active CN111432805B (zh)

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

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CN111432805A CN111432805A (zh) 2020-07-17
CN111432805B true CN111432805B (zh) 2023-02-17

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

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA128186C2 (uk) 2017-11-27 2024-05-01 Умекрайн Когнішн Аб ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ 3<font face="Symbol">a</font>-ЕТИНІЛ-3<font face="Symbol">b</font>-ГІДРОКСІАНДРОСТАН-17-ОНУ ОКСИМУ
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

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9405304D0 (en) 1994-03-16 1994-04-27 Scherer Ltd R P Delivery systems for hydrophobic drugs
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
JP2010502703A (ja) 2006-09-06 2010-01-28 メルク エンド カムパニー インコーポレーテッド 置換アミドの経口投与のための液体及び半固体の医薬製剤
EP2711372A1 (en) 2006-11-21 2014-03-26 Umecrine AB The use of pregnane and androstane steroids for the manufacture of a pharmaceutical composition for the treatment of CNS disorders
JP5687287B2 (ja) 2010-01-14 2015-03-18 ウメクライン ムード エービー 改善された保存性及び溶解特性を有する３−ベータ−ヒドロキシ−５−アルファ−プレグナン−２０−オンを含有する薬学的組成物
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
CN106163528A (zh) * 2014-01-29 2016-11-23 梅克芳识别有限公司 用于治疗肝脑病的甾族化合物
WO2015193224A1 (en) 2014-06-17 2015-12-23 Merck Sharp & Dohme B.V. Stable formulations of testosterone undecanoate
US9498485B2 (en) * 2014-08-28 2016-11-22 Lipocine Inc. Bioavailable solid state (17-β)-hydroxy-4-androsten-3-one esters
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
US10278977B2 (en) 2016-06-06 2019-05-07 Umecrine Cognition Ab Methods for treating hypersomnolence
UA128186C2 (uk) 2017-11-27 2024-05-01 Умекрайн Когнішн Аб ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ 3<font face="Symbol">a</font>-ЕТИНІЛ-3<font face="Symbol">b</font>-ГІДРОКСІАНДРОСТАН-17-ОНУ ОКСИМУ

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US11123351B2 (en) 2021-09-21
AU2018374029B2 (en) 2024-01-11
JP7314459B2 (ja) 2023-07-26
JP2021504468A (ja) 2021-02-15
IL274893B1 (en) 2024-04-01
US20200297737A1 (en) 2020-09-24
KR20200093008A (ko) 2020-08-04
US10603326B2 (en) 2020-03-31
EP3716954A1 (en) 2020-10-07
UA128186C2 (uk) 2024-05-01
BR112020010519A2 (pt) 2020-10-20
IL274893B2 (en) 2024-08-01
MX2020005442A (es) 2022-03-30
RU2020121142A3 (enExample) 2022-03-28
CA3083555A1 (en) 2019-05-31
CN111432805A (zh) 2020-07-17
MX391097B (es) 2025-03-21
AU2018374029A1 (en) 2020-06-18
US20190358244A1 (en) 2019-11-28
NZ764901A (en) 2025-05-02
WO2019102040A1 (en) 2019-05-31
RU2020121142A (ru) 2021-12-29
KR102771577B1 (ko) 2025-02-20
IL274893A (en) 2020-07-30

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