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

Бициклические производные как модуляторы 5 рецепторов gabaa

Info

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

Links

Classifications

    • 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 (14)

Country Link
US (1) US20210386718A1 (ru)
EP (1) EP3856342A1 (ru)
JP (1) JP7480128B2 (ru)
KR (1) KR20210086631A (ru)
CN (1) CN112805063B (ru)
AR (1) AR116549A1 (ru)
AU (1) AU2019346147A1 (ru)
BR (1) BR112021005837A2 (ru)
CA (1) CA3113072A1 (ru)
EA (1) EA202190857A1 (ru)
HU (1) HU231223B1 (ru)
MX (1) MX2021003670A (ru)
TW (1) TW202035403A (ru)
WO (1) WO2020065597A1 (ru)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202202495A (zh) * 2020-03-26 2022-01-16 匈牙利商羅特格登公司 作為ｇａｍｍａ－胺基丁酸Ａ受體次單元ａｌｐｈａ ５受體調節劑之㖠啶及吡啶并〔３，４－ｃ〕嗒𠯤衍生物
US20240043418A1 (en) * 2020-03-26 2024-02-08 Richter Gedeon Nyrt. 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa a5 receptor modulators
HUP2100338A1 (hu) * 2021-09-29 2023-04-28 Richter Gedeon Nyrt GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU732455C (en) 1997-05-08 2002-09-05 Merck Sharp & Dohme Limited Substituted 1,2,4-triazolo{3,4-a}phthalazine derivatives as gaba alpha 5 ligands
GB9813576D0 (en) 1998-06-24 1998-08-19 Merck Sharp & Dohme Therapeutic agents
GB0017518D0 (en) 2000-07-17 2000-08-30 Merck Sharp & Dohme Therapeutic agents
JP4148672B2 (ja) 2000-11-17 2008-09-10 武田薬品工業株式会社 イソオキサゾール誘導体
JP2003261545A (ja) 2001-12-28 2003-09-19 Takeda Chem Ind Ltd 神経栄養因子産生・分泌促進剤
EP1888594A2 (en) 2005-05-16 2008-02-20 Wisys Technology Foundation, Inc. Gabaergic agents to treat memory deficits
US7790745B2 (en) 2005-10-21 2010-09-07 Bristol-Myers Squibb Company Tetrahydroisoquinoline LXR Modulators
ATE460403T1 (de) 2006-05-24 2010-03-15 Lilly Co Eli Verbindungen und verfahren zur modulierung von fx-rezeptoren
US20100249179A1 (en) 2007-06-13 2010-09-30 Smithkline Beecham Corporation Farnesoid X Receptor Agonists
BRPI0820112B8 (pt) 2007-12-04 2021-05-25 Hoffmann La Roche derivados de isoxazol-piridina, seu uso e processos de preparação e medicamento
US7943619B2 (en) 2007-12-04 2011-05-17 Hoffmann-La Roche Inc. Isoxazolo-pyridazine derivatives
EP2229383B1 (en) 2007-12-04 2017-01-18 F. Hoffmann-La Roche AG Isoxazolo-pyrazine derivatives
US8389550B2 (en) 2009-02-25 2013-03-05 Hoffmann-La Roche Inc. Isoxazoles / O-pyridines with ethyl and ethenyl linker
US8222246B2 (en) 2009-04-02 2012-07-17 Hoffmann-La Roche Inc. Substituted isoxazoles
CA2760746C (en) 2009-05-05 2017-07-11 F. Hoffmann-La Roche Ag Isoxazole-pyrazole derivatives
BRPI1013766A2 (pt) 2009-05-07 2016-04-05 Hoffmann La Roche "derivados de isoxazol-piridina como moduladores de gaba"
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
GB201016088D0 (en) 2010-09-24 2010-11-10 Phase Focus Ltd Improvements in imaging
KR20150123967A (ko) 2010-11-05 2015-11-04 에프. 호프만-라 로슈 아게 중추 신경계 질환의 치료를 위한 활성 약학 화합물의 용도
CN103189370B (zh) 2010-11-09 2015-07-08 霍夫曼-拉罗奇有限公司 作为gaba受体用配体的三唑衍生物
US8742097B2 (en) * 2010-11-09 2014-06-03 Hoffmann-La Roche Inc. Triazole compounds I
MX2013005454A (es) 2010-11-15 2013-06-24 Abbvie Inc Inhibidores de nampt y rock.
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
US8604062B2 (en) 2011-10-20 2013-12-10 Hoffman-La Roche Inc. Process for the preparation of isoxazolyl-methoxy nicotinic acids
CN104411699B (zh) 2012-06-26 2017-06-13 萨尼奥纳有限责任公司 苯基三唑衍生物及其用于调节gabaa 受体复合体的用途
WO2014001278A1 (en) * 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
WO2017133521A1 (zh) 2016-02-01 2017-08-10 山东轩竹医药科技有限公司 Fxr受体激动剂
UA125524C2 (uk) 2016-12-08 2022-04-13 Ф. Хоффманн-Ля Рош Аг Ефірні похідні ізоксазолу як позитивні алостеричні модулятори рецептора гамк а альфа-5

Also Published As

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

Similar Documents

Publication Publication Date Title
ECSP21080740A (es) Inhibidores del inflamasoma nlrp3
CR20210045A (es) Inhibidores de inflamasoma nlrp3
EA202190857A1 (ru) Бициклические производные как модуляторы 5 рецепторов gabaa
AR050914A1 (es) Agonista receptor de vasopresina peptidico
CR20200584A (es) Compuestos tetrahidro-1h-pirazino [2,1-a] isoindolilquinolina para el tratamiento de enfermedades autoinmunes
MX2020011405A (es) Derivados de bencimidazol como moduladores del receptor gamma huerfano (rory) relacionado con retinoide y usos farmaceuticos de los mismos.
PH12020500548A1 (en) Triazolobenzazepines as vasopressin v1a receptor antagonists
BR112022010754A2 (pt) Análogos de rapamicina e usos dos mesmos
MX2021008426A (es) Nuevos derivados de sulfonilurea sustituida.
CY1124708T1 (el) Φαρμακολογικως δραστικα αλικυκλικα υποκατεστημενα παραγωγα πυραζολο[1,5-a] πυριμιδινης
EA202192530A1 (ru) Соединения, композиции и способы
CL2019003467A1 (es) Compuestos bicíclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias.
EA202190064A1 (ru) Цианотриазоловые соединения и варианты их применения
MA39750A (fr) Dérivés d'acide aza-indol-acétique et leur utilisation comme modulateurs des récepteurs de la prostaglandine d2
BR112021019779A2 (pt) Novo composto e composição para prevenção ou tratamento de doenças respiratórias compreendendo os mesmos como ingrediente ativo
EA202190339A1 (ru) Пиридопиримидины в качестве ингибиторов н4-гистаминовых рецепторов
CO2022014877A2 (es) Derivados de naftiridina y pirido[3,4-c]piridazina como moduladores del receptor gabaa α5
BR112023001060A2 (pt) Composto, composição farmacêutica, combinação, processo para fabricar uma composição farmacêutica, e, método de tratamento e/ou prevenção de um transtorno
CO2024005424A2 (es) Derivados de amina bicíclicos como moduladores de receptor gabaa α5
EA202090532A1 (ru) Соли соединения и их кристаллические формы
EA202192121A1 (ru) Соединения, составы и способы
CR20220231A (es) Compuestos de 1,8-naftiridin-2-ona para el tratamiento de una enfermedad autoinmunitaria
EA202190329A1 (ru) Ингибиторы инфламмасомы nlrp3
EA202090644A1 (ru) ПРОИЗВОДНЫЕ ИМИДАЗО[1,5-a]ПИРАЗИНА КАК ИНГИБИТОРЫ PI3K
EA202190968A1 (ru) Индолиноновые соединения для применения в качестве ингибиторов map4k1