AU2018392093B2 - Compositions and methods for treating CNS disorders - Google Patents

Compositions and methods for treating CNS disorders Download PDF

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Publication number
AU2018392093B2
AU2018392093B2 AU2018392093A AU2018392093A AU2018392093B2 AU 2018392093 B2 AU2018392093 B2 AU 2018392093B2 AU 2018392093 A AU2018392093 A AU 2018392093A AU 2018392093 A AU2018392093 A AU 2018392093A AU 2018392093 B2 AU2018392093 B2 AU 2018392093B2
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substituted
unsubstituted
alkyl
compound
pharmaceutically acceptable
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AU2018392093A1 (en
Inventor
Maria Jesus Blanco-Pillado
Boyd L. Harrison
Daniel La
Albert Jean Robichaud
Francesco G. Salituro
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Sage Therapeutics Inc
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Sage Therapeutics Inc
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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)
AU2018392093A 2017-12-22 2018-12-21 Compositions and methods for treating CNS disorders Active AU2018392093B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2023285947A AU2023285947A1 (en) 2017-12-22 2023-12-22 Compositions and methods for treating CNS disorders

Applications Claiming Priority (19)

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
US201762612070P 2017-12-29 2017-12-29
US201762612164P 2017-12-29 2017-12-29
US201762612067P 2017-12-29 2017-12-29
US62/612,164 2017-12-29
US62/612,067 2017-12-29
US62/611,977 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

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AU2018392093A1 AU2018392093A1 (en) 2020-07-09
AU2018392093B2 true AU2018392093B2 (en) 2024-02-01

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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 (2) IL275506A (enExample)
MA (1) MA51316A (enExample)
MX (3) MX2020006608A (enExample)
WO (1) WO2019126761A1 (enExample)

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CA2862076C (en) 2012-01-23 2020-04-21 Sage Therapeutics, Inc. Neuroactive steroid formulations and methods of treating cns disorders
PL2887944T3 (pl) 2012-08-21 2022-02-21 Sage Therapeutics, Inc. Allopregnanolon do leczenia lekoopornego stanu padaczkowego
MX362543B (es) 2013-04-17 2019-01-24 Sage Therapeutics Inc Esteroides c21-n-pirazolilo 19-nor c3,3- disustituidos y metodos de uso de los mismos.
WO2015195962A1 (en) 2014-06-18 2015-12-23 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
RS60343B1 (sr) 2014-11-27 2020-07-31 Sage Therapeutics Inc Kompozicije i postupci za lečenje poremećaja cns-a
JOP20190022B1 (ar) 2016-08-23 2023-03-28 Sage Therapeutics Inc ستيرويد 19- نور c3، 3- به استبدال ثنائي لـ c21-n بيرازوليل بلوري
US20200291059A1 (en) 2017-12-08 2020-09-17 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
AU2018392093B2 (en) 2017-12-22 2024-02-01 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
US11718642B2 (en) 2018-01-12 2023-08-08 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
CN114085260B (zh) * 2018-02-11 2023-10-20 江苏豪森药业集团有限公司 甾族类衍生物调节剂、其制备方法和应用
EP4321519A3 (en) 2018-10-12 2024-05-01 Sage Therapeutics, Inc. Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
TW202521129A (zh) 2018-12-05 2025-06-01 美商賽吉醫療公司 神經活性類固醇及其使用方法
KR102821994B1 (ko) * 2019-01-08 2025-06-19 쳉두 캉홍 파마슈티칼 코., 엘티디. 스테로이드 화합물, 및 이의 용도와 제조방법
AR119047A1 (es) 2019-05-31 2021-11-17 Sage Therapeutics Inc Esteroides neuroactivos como moduladores de gabaa y su uso en el tratamiento de trastornos del snc
US20230303616A9 (en) * 2019-06-27 2023-09-28 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CA3143545A1 (en) * 2019-06-27 2020-12-30 Sage Therapeutics, Inc. Compounds for treating cns disorders
CN114787174A (zh) * 2019-06-27 2022-07-22 萨奇治疗股份有限公司 用于治疗cns病症的组合物和方法
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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MX2023002004A (es) 2023-02-27
CN118772223A (zh) 2024-10-15
BR112020012761A2 (pt) 2021-02-17
EP3728285A1 (en) 2020-10-28
CA3086189A1 (en) 2019-06-27
US20220315621A1 (en) 2022-10-06
JP2025078783A (ja) 2025-05-20
JP2023119042A (ja) 2023-08-25
JP2021506904A (ja) 2021-02-22
WO2019126761A1 (en) 2019-06-27
JP7689160B2 (ja) 2025-06-05
CN118085004A (zh) 2024-05-28
RU2020123930A (ru) 2022-01-26
IL275506A (en) 2020-08-31
IL323780A (en) 2025-12-01
MA51316A (fr) 2020-10-28
TW201938172A (zh) 2019-10-01
MX2020006608A (es) 2020-11-06
AU2018392093A1 (en) 2020-07-09
CN111741965B (zh) 2024-06-25
US20250171492A1 (en) 2025-05-29
MX2023002006A (es) 2023-02-27
AU2023285947A1 (en) 2024-01-25
CN111741965A (zh) 2020-10-02
AR114044A1 (es) 2020-07-15
KR20200104349A (ko) 2020-09-03
RU2020123930A3 (enExample) 2022-02-04

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