EA202190857A1 - Бициклические производные как модуляторы 5 рецепторов gabaa - Google Patents
Бициклические производные как модуляторы 5 рецепторов gabaaInfo
- 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
Links
- 102000027484 GABAA receptors Human genes 0.000 title abstract 2
- 108091008681 GABAA receptors Proteins 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 102000005915 GABA Receptors Human genes 0.000 abstract 1
- 108010005551 GABA Receptors Proteins 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 230000003281 allosteric effect Effects 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
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
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.
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)
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 |
WO2021191837A1 (en) * | 2020-03-26 | 2021-09-30 | Richter Gedeon Nyrt. | 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa α5 receptor modulators |
HUP2100338A1 (hu) * | 2021-09-29 | 2023-04-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
Family Cites Families (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0986562B1 (en) | 1997-05-08 | 2002-08-07 | MERCK SHARP & DOHME LTD. | 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 |
US7595395B2 (en) | 2005-05-16 | 2009-09-29 | Wisys Technology Foundation | Gabaergic agents to treat memory deficits |
US7790745B2 (en) | 2005-10-21 | 2010-09-07 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline LXR Modulators |
JP5225984B2 (ja) | 2006-05-24 | 2013-07-03 | イーライ リリー アンド カンパニー | Fxrを調節する化合物及び方法 |
WO2008157270A1 (en) | 2007-06-13 | 2008-12-24 | Smithkline Beecham Corporation | Farnesoid x receptor agonists |
US7943619B2 (en) | 2007-12-04 | 2011-05-17 | Hoffmann-La Roche Inc. | Isoxazolo-pyridazine derivatives |
AU2008333326B2 (en) | 2007-12-04 | 2013-05-30 | F. Hoffmann-La Roche Ag | Isoxazolo-pyridine derivatives |
AU2008333320B2 (en) | 2007-12-04 | 2012-12-20 | 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 |
KR101384829B1 (ko) | 2009-05-05 | 2014-04-15 | 에프. 호프만-라 로슈 아게 | 이속사졸-피라졸 유도체 |
WO2010127978A1 (en) | 2009-05-07 | 2010-11-11 | F. Hoffmann-La Roche Ag | Isoxazole-pyridine derivatives as gaba modulators |
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 |
EP2635277B1 (en) | 2010-11-05 | 2018-12-19 | F.Hoffmann-La Roche Ag | Use of active pharmaceutical compounds for the treatment of central nervous system conditions |
JP5919291B2 (ja) | 2010-11-09 | 2016-05-18 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Gaba受容体リガンドとしてのトリアゾール誘導体 |
US8742097B2 (en) | 2010-11-09 | 2014-06-03 | Hoffmann-La Roche Inc. | Triazole compounds I |
UY33726A (es) | 2010-11-15 | 2012-06-29 | Abbott Lab | 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 |
KR20150033678A (ko) | 2012-06-26 | 2015-04-01 | 사니오나 에이피에스 | 페닐 트리아졸 유도체 및 이의 gabaa 수용체 복합체 조절용 용도 |
WO2014001278A1 (en) * | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
CN108602811B (zh) | 2016-02-01 | 2021-11-16 | 轩竹生物科技有限公司 | 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 |
-
2018
- 2018-09-28 HU HU1800333A patent/HU231223B1/hu unknown
-
2019
- 2019-09-27 KR KR1020217012783A patent/KR20210086631A/ko unknown
- 2019-09-27 AR ARP190102762A patent/AR116549A1/es unknown
- 2019-09-27 CA CA3113072A patent/CA3113072A1/en active Pending
- 2019-09-27 TW TW108135172A patent/TW202035403A/zh unknown
- 2019-09-27 EA EA202190857A patent/EA202190857A1/ru unknown
- 2019-09-27 AU AU2019346147A patent/AU2019346147A1/en active Pending
- 2019-09-27 MX MX2021003670A patent/MX2021003670A/es unknown
- 2019-09-27 EP EP19779613.9A patent/EP3856342A1/en active Pending
- 2019-09-27 BR BR112021005837-0A patent/BR112021005837A2/pt unknown
- 2019-09-27 US US17/279,654 patent/US20210386718A1/en active Pending
- 2019-09-27 CN CN201980063431.3A patent/CN112805063B/zh active Active
- 2019-09-27 WO PCT/IB2019/058208 patent/WO2020065597A1/en unknown
- 2019-09-27 JP JP2021516369A patent/JP7480128B2/ja active Active
Also Published As
Publication number | Publication date |
---|---|
JP2022502366A (ja) | 2022-01-11 |
JP7480128B2 (ja) | 2024-05-09 |
EP3856342A1 (en) | 2021-08-04 |
HUP1800333A2 (hu) | 2020-04-28 |
KR20210086631A (ko) | 2021-07-08 |
CN112805063B (zh) | 2024-02-23 |
CN112805063A (zh) | 2021-05-14 |
TW202035403A (zh) | 2020-10-01 |
BR112021005837A2 (pt) | 2021-07-27 |
CA3113072A1 (en) | 2020-04-02 |
AR116549A1 (es) | 2021-05-19 |
WO2020065597A1 (en) | 2020-04-02 |
US20210386718A1 (en) | 2021-12-16 |
HU231223B1 (hu) | 2022-01-28 |
AU2019346147A1 (en) | 2021-05-20 |
MX2021003670A (es) | 2021-08-19 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
ECSP21080740A (es) | Inhibidores del inflamasoma nlrp3 | |
MX2021000925A (es) | Inhibidores de inflamasoma nlrp3. | |
EA202190857A1 (ru) | Бициклические производные как модуляторы 5 рецепторов gabaa | |
AR050914A1 (es) | Agonista receptor de vasopresina peptidico | |
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 | |
DOP2019000299A (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 | |
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 | |
EA202190339A1 (ru) | Пиридопиримидины в качестве ингибиторов н4-гистаминовых рецепторов | |
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 | |
EA202190968A1 (ru) | Индолиноновые соединения для применения в качестве ингибиторов map4k1 | |
EA201992577A1 (ru) | 5,6-конденсированные бициклические соединения и композиции для лечения паразитарных заболеваний | |
DOP2007000086A (es) | Nuevos derivados de quinolinas |