TWI907333B - 用於治療cns病症之組合物及方法 - Google Patents

用於治療cns病症之組合物及方法

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Publication number
TWI907333B
TWI907333B TW107146684A TW107146684A TWI907333B TW I907333 B TWI907333 B TW I907333B TW 107146684 A TW107146684 A TW 107146684A TW 107146684 A TW107146684 A TW 107146684A TW I907333 B TWI907333 B TW I907333B
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Taiwan
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substituted
unsubstituted
group
alkyl
compound
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TW107146684A
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Chinese (zh)
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TW201938172A (zh
Inventor
艾伯特 J 羅比喬德
法藍西司科 G 薩突羅
佩拉杜 馬利亞 耶稣 巴蘭可
丹尼爾 拉
柏伊德 L 哈里森
Original Assignee
美商賽吉醫療有限責任公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/002Expansion of ring A by one atom, e.g. A homo steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/19Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a saturated carbon skeleton containing rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C307/02Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/385Saturated compounds containing a keto group being part of a ring
    • C07C49/487Saturated compounds containing a keto group being part of a ring containing hydroxy groups
    • C07C49/507Saturated compounds containing a keto group being part of a ring containing hydroxy groups polycyclic
    • C07C49/513Saturated compounds containing a keto group being part of a ring containing hydroxy groups polycyclic a keto group being part of a condensed ring system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J61/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by contraction of only one ring by one or two atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/004Expansion of ring B by one atom, e.g. B homo steroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/006Expansion of ring C by one atom, e.g. C homo steroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion of ring D by one atom, e.g. D homo steroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/40Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/40Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42Ortho- or ortho- and peri-condensed systems containing four condensed rings containing only six-membered rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW107146684A 2017-12-22 2018-12-22 用於治療cns病症之組合物及方法 TWI907333B (zh)

Applications Claiming Priority (18)

Application Number Priority Date Filing Date Title
US201762610067P 2017-12-22 2017-12-22
US62/610,067 2017-12-22
US201762611977P 2017-12-29 2017-12-29
US201762612164P 2017-12-29 2017-12-29
US201762612067P 2017-12-29 2017-12-29
US201762612070P 2017-12-29 2017-12-29
US62/612,067 2017-12-29
US62/611,977 2017-12-29
US62/612,070 2017-12-29
US62/612,164 2017-12-29
US201862765164P 2018-08-17 2018-08-17
US62/765,164 2018-08-17
US201862728499P 2018-09-07 2018-09-07
US62/728,499 2018-09-07
US201862737559P 2018-09-27 2018-09-27
US62/737,559 2018-09-27
US201862754977P 2018-11-02 2018-11-02
US62/754,977 2018-11-02

Publications (2)

Publication Number Publication Date
TW201938172A TW201938172A (zh) 2019-10-01
TWI907333B true TWI907333B (zh) 2025-12-11

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US (2) US20220315621A1 (https=)
EP (1) EP3728285B1 (https=)
JP (3) JP2021506904A (https=)
KR (1) KR20200104349A (https=)
CN (3) CN118085004A (https=)
AR (1) AR114044A1 (https=)
AU (2) AU2018392093B2 (https=)
BR (1) BR112020012761A2 (https=)
CA (1) CA3086189A1 (https=)
IL (2) IL275506A (https=)
MA (1) MA51316A (https=)
MX (3) MX2020006608A (https=)
TW (1) TWI907333B (https=)
WO (1) WO2019126761A1 (https=)

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EP2806877B2 (en) 2012-01-23 2025-01-29 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
CA2882708A1 (en) 2012-08-21 2014-02-27 Sage Therapeutics, Inc. Methods of treating epilepsy or status epilepticus
KR102396328B1 (ko) 2013-04-17 2022-05-10 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
EP3504189A1 (en) 2016-08-23 2019-07-03 Sage Therapeutics, Inc. A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid
MA51046A (fr) 2017-12-08 2021-03-17 Sage Therapeutics Inc Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc
BR112020012761A2 (pt) 2017-12-22 2021-02-17 Sage Therapeutics, Inc. composições e métodos para o tratamento de distúrbios do snc
TW201930269A (zh) 2018-01-12 2019-08-01 美商賽吉醫療公司 用於治療cns病症之組合物及方法
EP3750909B1 (en) * 2018-02-11 2025-03-05 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Steroid derivative regulators, method for preparing the same, and uses thereof
EP4321519B1 (en) 2018-10-12 2026-04-08 Sage Therapeutics, LLC Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
KR20250174100A (ko) 2018-12-05 2025-12-11 세이지 테라퓨틱스, 인크. 신경활성 스테로이드 및 이의 사용 방법
CN115651054B (zh) * 2019-01-08 2024-06-21 成都康弘药业集团股份有限公司 甾体类化合物、用途及其制备方法
SG11202112391UA (en) 2019-05-31 2021-12-30 Sage Therapeutics Inc Neuroactive steroids and compositions thereof
JP7754725B2 (ja) * 2019-06-27 2025-10-15 セージ セラピューティクス, インコーポレイテッド Cns障害を治療するための組成物及び方法
CN114729000A (zh) * 2019-06-27 2022-07-08 萨奇治疗股份有限公司 用于治疗cns病症的化合物
CA3143509A1 (en) * 2019-06-27 2020-12-30 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
WO2022246634A1 (en) * 2021-05-25 2022-12-01 Zhejiang Jiachi Development Pharmaceuticals Ltd. Compositions for treating insomnia and uses thereof
WO2025016311A1 (zh) * 2023-07-14 2025-01-23 成都康弘药业集团股份有限公司 一种甾体类化合物的晶型及其用途
CN119529013B (zh) * 2024-11-25 2025-11-07 湖南新合新生物医药有限公司 一种祖拉诺龙中间体的合成方法

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CN111741965A (zh) 2020-10-02
AU2018392093B2 (en) 2024-02-01
RU2020123930A (ru) 2022-01-26
CN118085004A (zh) 2024-05-28
JP2023119042A (ja) 2023-08-25
CN118772223A (zh) 2024-10-15
AU2023285947A1 (en) 2024-01-25
TW201938172A (zh) 2019-10-01
US20220315621A1 (en) 2022-10-06
EP3728285B1 (en) 2026-04-08
IL323780A (en) 2025-12-01
MX2023002004A (es) 2023-02-27
EP3728285A1 (en) 2020-10-28
US20250171492A1 (en) 2025-05-29
CN111741965B (zh) 2024-06-25
JP2025078783A (ja) 2025-05-20
JP7689160B2 (ja) 2025-06-05
JP2021506904A (ja) 2021-02-22
CA3086189A1 (en) 2019-06-27
AR114044A1 (es) 2020-07-15
BR112020012761A2 (pt) 2021-02-17
IL275506A (en) 2020-08-31
MX2020006608A (es) 2020-11-06
WO2019126761A1 (en) 2019-06-27
MX2023002006A (es) 2023-02-27
MA51316A (fr) 2020-10-28
AU2018392093A1 (en) 2020-07-09
KR20200104349A (ko) 2020-09-03

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