EA202190857A1 - Бициклические производные как модуляторы 5 рецепторов gabaa - Google Patents

Бициклические производные как модуляторы 5 рецепторов gabaa

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Publication number
EA202190857A1
EA202190857A1 EA202190857A EA202190857A EA202190857A1 EA 202190857 A1 EA202190857 A1 EA 202190857A1 EA 202190857 A EA202190857 A EA 202190857A EA 202190857 A EA202190857 A EA 202190857A EA 202190857 A1 EA202190857 A1 EA 202190857A1
Authority
EA
Eurasian Patent Office
Prior art keywords
modulators
gabaa
compounds
gabaa receptors
relates
Prior art date
Application number
EA202190857A
Other languages
English (en)
Inventor
Дьёрдь Сабо
Дьёрдь Иштван Турош
Оливер Элиаш
Бенедек Имре Каройи
Петер Эрдейи
Габор Ласло Капуш
Original Assignee
Рихтер Гедеон Нирт.
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 Рихтер Гедеон Нирт. filed Critical Рихтер Гедеон Нирт.
Publication of EA202190857A1 publication Critical patent/EA202190857A1/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
    • A61K31/435—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/422—Oxazoles not condensed and 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
    • A61K31/4353—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
    • A61K31/33—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Настоящее изобретение относится к соединениям, имеющим формулу (I), и/или к их солям, и/или их геометрическим изомерам, и/или их стереоизомерам, и/или их энантиомерам, и/или их рацематам, и/или их диастереомерам, и/или их биологически активным метаболитам, и/или их пролекарствам, и/или их сольватам, и/или их гидратам, и/или их полиморфным формам, которые имеют сродство и селективность к субъединице альфа 5 рецептора A гамма-аминомасляной кислоты и действуют как отрицательные аллостерические модуляторы 5 GABAA и, таким образом, подходят для лечения или профилактики заболеваний, связанных с 5 GABAA-рецептора; изобретение также относится к способу получения указанных соединений, к фармацевтическим композициям, включающим их как таковые или в комбинации с одним или более другими активными ингредиентами, а также к их применению в качестве медикаментов.
EA202190857A 2018-09-28 2019-09-27 Бициклические производные как модуляторы 5 рецепторов gabaa EA202190857A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
HU1800333A HU231223B1 (hu) 2018-09-28 2018-09-28 GABAA A5 receptor modulátor hatású biciklusos vegyületek
PCT/IB2019/058208 WO2020065597A1 (en) 2018-09-28 2019-09-27 Bicyclic derivatives as gabaa α5 receptor modulators

Publications (1)

Publication Number Publication Date
EA202190857A1 true EA202190857A1 (ru) 2021-06-23

Family

ID=89992765

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202190857A EA202190857A1 (ru) 2018-09-28 2019-09-27 Бициклические производные как модуляторы 5 рецепторов gabaa

Country Status (15)

Country Link
US (1) US12370182B2 (ru)
EP (1) EP3856342B1 (ru)
JP (1) JP7480128B2 (ru)
KR (1) KR20210086631A (ru)
CN (1) CN112805063B (ru)
AR (1) AR116549A1 (ru)
AU (1) AU2019346147B2 (ru)
BR (1) BR112021005837A2 (ru)
CA (1) CA3113072A1 (ru)
EA (1) EA202190857A1 (ru)
HU (1) HU231223B1 (ru)
MX (1) MX2021003670A (ru)
TW (1) TWI868079B (ru)
UA (1) UA130217C2 (ru)
WO (1) WO2020065597A1 (ru)

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* Cited by examiner, † Cited by third party
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EP4126858B1 (en) * 2020-03-26 2026-03-18 Richter Gedeon Nyrt. Dihydro-2-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators
TWI901650B (zh) * 2020-03-26 2025-10-21 匈牙利商羅特格登公司 啶及吡啶并〔３，４－ｃ〕嗒衍生物
HU231691B1 (hu) * 2021-09-29 2025-10-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok

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Also Published As

Publication number Publication date
AR116549A1 (es) 2021-05-19
EP3856342A1 (en) 2021-08-04
US12370182B2 (en) 2025-07-29
MX2021003670A (es) 2021-08-19
CN112805063A (zh) 2021-05-14
BR112021005837A2 (pt) 2021-07-27
TW202035403A (zh) 2020-10-01
JP7480128B2 (ja) 2024-05-09
WO2020065597A1 (en) 2020-04-02
AU2019346147A1 (en) 2021-05-20
UA130217C2 (uk) 2025-12-24
HUP1800333A2 (hu) 2020-04-28
KR20210086631A (ko) 2021-07-08
CA3113072A1 (en) 2020-04-02
TWI868079B (zh) 2025-01-01
AU2019346147B2 (en) 2025-01-09
JP2022502366A (ja) 2022-01-11
EP3856342B1 (en) 2025-12-10
EP3856342C0 (en) 2025-12-10
HU231223B1 (hu) 2022-01-28
US20210386718A1 (en) 2021-12-16
CN112805063B (zh) 2024-02-23

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