CA3086189A1 - Compositions and methods for treating cns disorders - Google Patents

Compositions and methods for treating cns disorders Download PDF

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Publication number
CA3086189A1
CA3086189A1 CA3086189A CA3086189A CA3086189A1 CA 3086189 A1 CA3086189 A1 CA 3086189A1 CA 3086189 A CA3086189 A CA 3086189A CA 3086189 A CA3086189 A CA 3086189A CA 3086189 A1 CA3086189 A1 CA 3086189A1
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CA
Canada
Prior art keywords
substituted
unsubstituted
compound
alkyl
independently hydrogen
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CA3086189A
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English (en)
French (fr)
Inventor
Albert Jean Robichaud
Francesco G. Salituro
Maria Jesus Blanco-Pillado
Daniel La
Boyd L. Harrison
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sage Therapeutics Inc
Original Assignee
Sage Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of CA3086189A1 publication Critical patent/CA3086189A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/002—Expansion of ring A by one atom, e.g. A homo steroids
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
    • 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
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic 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
    • C07C233/17—Carboxylic 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
    • C07C233/19—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides 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
    • C07C307/02—Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/385—Saturated compounds containing a keto group being part of a ring
    • C07C49/487—Saturated compounds containing a keto group being part of a ring containing hydroxy groups
    • C07C49/507—Saturated compounds containing a keto group being part of a ring containing hydroxy groups polycyclic
    • C07C49/513—Saturated compounds containing a keto group being part of a ring containing hydroxy groups polycyclic a keto group being part of a condensed ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J61/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by contraction of only one ring by one or two atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/004—Expansion of ring B by one atom, e.g. B homo steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/006—Expansion of ring C by one atom, e.g. C homo steroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/40—Ortho- or ortho- and peri-condensed systems containing four condensed rings
    • C07C2603/42—Ortho- 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)
CA3086189A 2017-12-22 2018-12-21 Compositions and methods for treating cns disorders Pending CA3086189A1 (en)

Applications Claiming Priority (19)

Application Number Priority Date Filing Date Title
US201762610067P 2017-12-22 2017-12-22
US62/610,067 2017-12-22
US201762612067P 2017-12-29 2017-12-29
US201762612070P 2017-12-29 2017-12-29
US201762612164P 2017-12-29 2017-12-29
US201762611977P 2017-12-29 2017-12-29
US62/611,977 2017-12-29
US62/612,164 2017-12-29
US62/612,067 2017-12-29
US62/612,070 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
PCT/US2018/067306 WO2019126761A1 (en) 2017-12-22 2018-12-21 Compositions and methods for treating cns disorders

Publications (1)

Publication Number Publication Date
CA3086189A1 true CA3086189A1 (en) 2019-06-27

Family

ID=65234664

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3086189A Pending CA3086189A1 (en) 2017-12-22 2018-12-21 Compositions and methods for treating cns disorders

Country Status (13)

Country Link
US (2) US20220315621A1 (enExample)
EP (1) EP3728285A1 (enExample)
JP (3) JP2021506904A (enExample)
KR (1) KR20200104349A (enExample)
CN (3) CN118085004A (enExample)
AR (1) AR114044A1 (enExample)
AU (2) AU2018392093B2 (enExample)
BR (1) BR112020012761A2 (enExample)
CA (1) CA3086189A1 (enExample)
IL (1) IL275506A (enExample)
MA (1) MA51316A (enExample)
MX (3) MX2020006608A (enExample)
WO (1) WO2019126761A1 (enExample)

Families Citing this family (22)

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Publication number Priority date Publication date Assignee Title
NZ773177A (en) 2012-01-23 2022-09-30 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders
IL275725B (en) 2012-08-21 2022-08-01 Sage Therapeutics Inc Treatment methods for epilepsy and status epilepticus
AU2014256229B2 (en) 2013-04-17 2018-10-04 Sage Therapeutics, Inc. 19-nor C3,3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof
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
US10774108B2 (en) 2014-11-27 2020-09-15 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
NZ791594A (en) 2016-08-23 2025-08-29 Sage Therapeutics Inc A crystalline 19-nor C3, 3-disubstituted C21-N-pyrazolyl steroid
WO2019113494A1 (en) 2017-12-08 2019-06-13 Sage Therapeutics, Inc. Deuterated 21 -[4-cyano-pyrazol-1 -yl]-19-nor-pregan-3. alpha-ol-20-one derivatives for treating cns disorders
AR114044A1 (es) 2017-12-22 2020-07-15 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos en el sistema nervioso central
EP3737687B1 (en) 2018-01-12 2025-10-22 Sage Therapeutics, Inc. Aza-, oxa and thia-pregnan-20-one-3.alpha.-ol compounds for use in treating cns disorders
ES3018614T3 (es) * 2018-02-11 2025-05-16 Jiangsu Hansoh Pharmaceutical Group Co Ltd Reguladores derivados de esteroides, método para prepararlos y usos de los mismos
US11634453B2 (en) 2018-10-12 2023-04-25 Sage Therapeutics, Inc. Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders
TWI874337B (zh) 2018-12-05 2025-03-01 美商賽吉醫療公司 神經活性類固醇及其使用方法
EP3909967A4 (en) * 2019-01-08 2022-11-09 Chengdu Kanghong Pharmaceutical Co., Ltd. STEROID COMPOUND AND USE THEREOF AND METHOD OF MANUFACTURE THEREOF
CR20240234A (es) 2019-05-31 2024-07-09 Sage Therapeutics Inc ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629)
CA3143545A1 (en) 2019-06-27 2020-12-30 Sage Therapeutics, Inc. Compounds for treating cns disorders
TWI896547B (zh) * 2019-06-27 2025-09-11 美商賽吉醫療公司 用於治療cns病症之組合物及方法
KR20220038681A (ko) * 2019-06-27 2022-03-29 세이지 테라퓨틱스, 인크. Cns 장애를 치료하기 위한 조성물 및 방법
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
CN119306783A (zh) * 2023-07-14 2025-01-14 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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AR114044A1 (es) 2017-12-22 2020-07-15 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos en el sistema nervioso central
EP3909967A4 (en) * 2019-01-08 2022-11-09 Chengdu Kanghong Pharmaceutical Co., Ltd. STEROID COMPOUND AND USE THEREOF AND METHOD OF MANUFACTURE THEREOF
KR20220038681A (ko) 2019-06-27 2022-03-29 세이지 테라퓨틱스, 인크. Cns 장애를 치료하기 위한 조성물 및 방법

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MX2020006608A (es) 2020-11-06
RU2020123930A (ru) 2022-01-26
BR112020012761A2 (pt) 2021-02-17
CN111741965A (zh) 2020-10-02
JP2025078783A (ja) 2025-05-20
JP2021506904A (ja) 2021-02-22
CN111741965B (zh) 2024-06-25
TW201938172A (zh) 2019-10-01
KR20200104349A (ko) 2020-09-03
AU2018392093B2 (en) 2024-02-01
AR114044A1 (es) 2020-07-15
AU2023285947A1 (en) 2024-01-25
IL275506A (en) 2020-08-31
JP7689160B2 (ja) 2025-06-05
EP3728285A1 (en) 2020-10-28
MX2023002004A (es) 2023-02-27
CN118085004A (zh) 2024-05-28
MX2023002006A (es) 2023-02-27
US20250171492A1 (en) 2025-05-29
JP2023119042A (ja) 2023-08-25
AU2018392093A1 (en) 2020-07-09
WO2019126761A1 (en) 2019-06-27
CN118772223A (zh) 2024-10-15
US20220315621A1 (en) 2022-10-06
MA51316A (fr) 2020-10-28
RU2020123930A3 (enExample) 2022-02-04

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