EA202090521A1 - Новые модуляторы рецептора гамма-аминомасляной кислоты типа a против расстройств настроения - Google Patents

Новые модуляторы рецептора гамма-аминомасляной кислоты типа a против расстройств настроения

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Publication number
EA202090521A1
EA202090521A1 EA202090521A EA202090521A EA202090521A1 EA 202090521 A1 EA202090521 A1 EA 202090521A1 EA 202090521 A EA202090521 A EA 202090521A EA 202090521 A EA202090521 A EA 202090521A EA 202090521 A1 EA202090521 A1 EA 202090521A1
Authority
EA
Eurasian Patent Office
Prior art keywords
modulers
aminobacyric
type
mood disorders
acid receptor
Prior art date
Application number
EA202090521A
Other languages
English (en)
Inventor
Скотт ТОМПСОН
Адам Ван Дайк
Крейг Томас
Патрик Моррис
Original Assignee
Юниверсити Оф Мэриленд, Балтимор
Зе Юнайтид Стейтс Оф Америка, Эз Репризентид Бай Зе Секретари, Дипартмент Оф Хелс Энд Хьюман Сервисис
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.)
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Publication date
Application filed by Юниверсити Оф Мэриленд, Балтимор, Зе Юнайтид Стейтс Оф Америка, Эз Репризентид Бай Зе Секретари, Дипартмент Оф Хелс Энд Хьюман Сервисис filed Critical Юниверсити Оф Мэриленд, Балтимор
Publication of EA202090521A1 publication Critical patent/EA202090521A1/ru

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • 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
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • A61K31/42—Oxazoles
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Настоящее изобретение относится к новым селективным отрицательным аллостерическим модуляторам рецепторов GABA, содержащих субъединицу альфа5, которые подвергают дейтерированию для улучшения их медицинских свойств посредством увеличения периода их полувыведения, что делает их пригодными в качестве быстродействующих фармацевтических средств лечения расстройств, связанных с депрессией.
EA202090521A 2017-08-28 2018-08-28 Новые модуляторы рецептора гамма-аминомасляной кислоты типа a против расстройств настроения EA202090521A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762550826P 2017-08-28 2017-08-28
PCT/US2018/048339 WO2019046300A1 (en) 2017-08-28 2018-08-28 NOVEL MODULATORS OF GAMMA-AMINOBUTYRIC ACID RECEPTOR TYPE A FOR MOOD DISORDERS

Publications (1)

Publication Number Publication Date
EA202090521A1 true EA202090521A1 (ru) 2020-06-10

Family

ID=65525999

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202090521A EA202090521A1 (ru) 2017-08-28 2018-08-28 Новые модуляторы рецептора гамма-аминомасляной кислоты типа a против расстройств настроения

Country Status (11)

Country Link
US (2) US11459320B2 (ru)
EP (1) EP3675845B1 (ru)
JP (2) JP7403050B2 (ru)
KR (1) KR20200044906A (ru)
CN (1) CN111201016A (ru)
AU (1) AU2018323443B2 (ru)
BR (1) BR112020004116A2 (ru)
CA (1) CA3074110A1 (ru)
EA (1) EA202090521A1 (ru)
MX (1) MX2020002196A (ru)
WO (1) WO2019046300A1 (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112020004116A2 (pt) 2017-08-28 2020-09-01 University Of Maryland, Baltimore novos moduladores do receptor de ácido gama aminobutírico tipo a para distúrbios de humor
CA3216863A1 (en) 2021-05-05 2022-11-10 University College Cardiff Consultants Limited Heteroaryl compounds useful in the treatment of cognitive disorders

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2767536B1 (en) 2007-12-04 2015-09-02 F. Hoffmann-La Roche AG Isoxazolo-pyridine derivatives
US8222246B2 (en) * 2009-04-02 2012-07-17 Hoffmann-La Roche Inc. Substituted isoxazoles
US8604062B2 (en) * 2011-10-20 2013-12-10 Hoffman-La Roche Inc. Process for the preparation of isoxazolyl-methoxy nicotinic acids
US8785435B2 (en) 2011-10-20 2014-07-22 Hoffmann-La Roche Inc. Solid forms
WO2015153658A2 (en) 2014-03-31 2015-10-08 University Of Maryland, Baltimore Use of negative modulators of gaba receptors containing alpha5 subunits as fast acting antidepressants
KR20180014778A (ko) * 2015-06-03 2018-02-09 트리아스텍 인코포레이티드 제형 및 이의 용도
CA2968836A1 (en) * 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
BR112020004116A2 (pt) 2017-08-28 2020-09-01 University Of Maryland, Baltimore novos moduladores do receptor de ácido gama aminobutírico tipo a para distúrbios de humor

Also Published As

Publication number Publication date
EP3675845A4 (en) 2021-05-05
JP2021500309A (ja) 2021-01-07
WO2019046300A1 (en) 2019-03-07
EP3675845A1 (en) 2020-07-08
EP3675845B1 (en) 2024-07-17
CN111201016A (zh) 2020-05-26
JP2023133571A (ja) 2023-09-22
AU2018323443B2 (en) 2024-09-05
US11459320B2 (en) 2022-10-04
JP7403050B2 (ja) 2023-12-22
AU2018323443A1 (en) 2020-03-12
WO2019046300A9 (en) 2020-10-15
MX2020002196A (es) 2020-09-28
US20200199119A1 (en) 2020-06-25
US20220396572A1 (en) 2022-12-15
US11897875B2 (en) 2024-02-13
CA3074110A1 (en) 2019-03-07
BR112020004116A2 (pt) 2020-09-01
KR20200044906A (ko) 2020-04-29

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