PE20240816A1 - DERIVADOS DE AMINA BICICLICOS COMO MODULADORES DE RECEPTOR GABAA (alfa)5 - Google Patents
DERIVADOS DE AMINA BICICLICOS COMO MODULADORES DE RECEPTOR GABAA (alfa)5Info
- Publication number
- PE20240816A1 PE20240816A1 PE2024000597A PE2024000597A PE20240816A1 PE 20240816 A1 PE20240816 A1 PE 20240816A1 PE 2024000597 A PE2024000597 A PE 2024000597A PE 2024000597 A PE2024000597 A PE 2024000597A PE 20240816 A1 PE20240816 A1 PE 20240816A1
- Authority
- PE
- Peru
- Prior art keywords
- receptor
- compounds
- gabaa
- alpha5
- alpha
- Prior art date
Links
- 150000001412 amines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 239000004480 active ingredient Substances 0.000 abstract 2
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 abstract 2
- -1 stereoisomers Chemical class 0.000 abstract 2
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 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
- 230000003281 allosteric effect Effects 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 229960003692 gamma aminobutyric acid Drugs 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 125000002950 monocyclic group Chemical group 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient 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
- 229920006395 saturated elastomer Polymers 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
-
- 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
- A61K31/435—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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invencion proporciona compuestos de la formula (I), y/o sales, estereoisomeros, enantiomeros, racematos, diastereomeros, metabolitos biologicamente activos, profarmacos, solvatos, hidratos o polimorfos de estos, que tienen afinidad y selectividad por el receptor A subunidad alfa5 del acido gamma-aminobutirico y actuan como moduladores alostericos positivos del receptor GABAA alfa5. En dichos compuestos, A esta representado por dos grupos descritos en la presente, R1 es un grupo alquilo C1-6, alcoxi C1-6 o haloalquilo C1-6; R2 es C3-7cicloalquilo o un sistema de anillos monovalente, saturado, parcialmente insaturado, monociclico, biciclico, fusionado, con puente o espiro, con 3 a 10 atomos y 1-4 heteroatomos seleccionados independientemente de N, O y S. Dichos compuestos se seleccionan de 6-{[5-metil-3-(6-metilpiridin-3-il)-1,2-oxazol-4-il]metoxi}-1,2,3,4-tetrahidro-2,7naftiridina, entre otros. Asimismo, se proporciona su uso en el tratamiento o prevencion de enfermedades relacionadas con el receptor GABAA alfa5, y refiere a una composicion farmaceutica que comprende uno de los compuestos como principio activo, un excipiente fisiologica o farmaceuticamente aceptable, y opcionalmente mas principios activos diferentes.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU2100338A HUP2100338A1 (hu) | 2021-09-29 | 2021-09-29 | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
| PCT/IB2022/059214 WO2023053015A1 (en) | 2021-09-29 | 2022-09-28 | BICYCLIC AMINE DERIVATIVES AS GABAA α5 RECEPTOR MODULATORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20240816A1 true PE20240816A1 (es) | 2024-04-18 |
Family
ID=89993434
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2024000597A PE20240816A1 (es) | 2021-09-29 | 2022-09-28 | DERIVADOS DE AMINA BICICLICOS COMO MODULADORES DE RECEPTOR GABAA (alfa)5 |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP4408842A1 (es) |
| JP (1) | JP2024536039A (es) |
| KR (1) | KR20240089056A (es) |
| CN (1) | CN118284606A (es) |
| AR (1) | AR127182A1 (es) |
| AU (1) | AU2022357572A1 (es) |
| CA (1) | CA3231776A1 (es) |
| CO (1) | CO2024005424A2 (es) |
| EC (1) | ECSP24032316A (es) |
| HU (1) | HUP2100338A1 (es) |
| IL (1) | IL311640A (es) |
| MX (1) | MX2024003812A (es) |
| PE (1) | PE20240816A1 (es) |
| TW (1) | TW202330518A (es) |
| WO (1) | WO2023053015A1 (es) |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU230518B1 (hu) | 2005-12-20 | 2016-10-28 | Richter Gedeon Nyrt. | Bradykinin B1 receptor szelektív antagonista hatással rendelkező új fenatridin származékok, eljárás előállításukra, és az ezeket tartalmazó gyógyszerkészítmények |
| HUP0600810A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New sulfonamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them |
| HUP0600809A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them |
| HUP0600808A3 (en) | 2006-10-27 | 2008-09-29 | Richter Gedeon Nyrt | New benzamide derivatives as bradykinin antagonists, process for their preparation and pharmaceutical compositions containing them |
| US7943619B2 (en) | 2007-12-04 | 2011-05-17 | Hoffmann-La Roche Inc. | Isoxazolo-pyridazine derivatives |
| US8742097B2 (en) | 2010-11-09 | 2014-06-03 | Hoffmann-La Roche Inc. | Triazole compounds I |
| IN2014DN11027A (es) | 2012-06-26 | 2015-09-25 | Aniona Aps | |
| WO2014001278A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| WO2014001279A1 (en) | 2012-06-26 | 2014-01-03 | Aniona Aps | A phenyl triazole derivative and its use for modulating the gabaa receptor complex |
| HUP1300139A2 (en) | 2013-03-06 | 2014-09-29 | Richter Gedeon Nyrt | Phenoxypiperidine h3 antagonists |
| EP3083569B1 (en) | 2013-12-20 | 2022-01-26 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| PT3439665T (pt) | 2016-03-18 | 2022-09-27 | Uwm Res Foundation Inc | Tratamento de sintomas cognitivos e de humor em distúrbios neurodegenerativos e neuropsiquiátricos com gaba contendo agonistas de recetores de gabaa contendo alfa5 |
| AR110498A1 (es) | 2016-12-08 | 2019-04-03 | Hoffmann La Roche | DERIVADOS DE ISOXAZOLIL ÉTER COMO MODULADORES ALOSTÉRICOS POSITIVOS (PAM) DE RECEPTORES DE GABAA a5 |
| HU231058B1 (hu) | 2017-03-13 | 2020-04-28 | Richter Gedeon Nyrt. | Gyógyászatilag hatékony aliciklusos-szubsztituált pirazolo[1,5-a]pirimidin származékok |
| HU231057B1 (hu) | 2017-03-13 | 2020-04-28 | Richter Gedeon Nyrt | Gyógyászatilag hatékony aril-szubsztituált pirazolo[1,5-a]pirimidin származékok |
| TW201938171A (zh) | 2017-12-15 | 2019-10-01 | 匈牙利商羅特格登公司 | 作為血管升壓素Ｖ１ａ受體拮抗劑之三環化合物 |
| HU231206B1 (hu) | 2017-12-15 | 2021-10-28 | Richter Gedeon Nyrt. | Triazolobenzazepinek |
| CR20200610A (es) | 2018-06-13 | 2021-02-05 | Hoffmann La Roche | Nuevos derivados de isoxazolit éter como pan de gaba a alfa 5 |
| HU231414B1 (hu) | 2018-07-13 | 2023-08-28 | Richter Gedeon Nyrt. | Tiadiazin származékok |
| HU231333B1 (hu) | 2018-07-13 | 2023-01-28 | Richter Gedeon Nyrt | Spirokromán származékok |
| HU231478B1 (hu) | 2018-07-13 | 2024-02-28 | Richter Gedeon Nyrt. | Szubsztituált (aza)indol származékok |
| BR102019014802A2 (pt) | 2018-07-20 | 2020-02-04 | Boehringer Ingelheim Int | difluorometil-fenil triazóis |
| HU231223B1 (hu) * | 2018-09-28 | 2022-01-28 | Richter Gedeon Nyrt. | GABAA A5 receptor modulátor hatású biciklusos vegyületek |
| 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 |
-
2021
- 2021-09-29 HU HU2100338A patent/HUP2100338A1/hu unknown
-
2022
- 2022-09-13 TW TW111134580A patent/TW202330518A/zh unknown
- 2022-09-28 CN CN202280074314.9A patent/CN118284606A/zh active Pending
- 2022-09-28 WO PCT/IB2022/059214 patent/WO2023053015A1/en active Application Filing
- 2022-09-28 JP JP2024518133A patent/JP2024536039A/ja active Pending
- 2022-09-28 MX MX2024003812A patent/MX2024003812A/es unknown
- 2022-09-28 AU AU2022357572A patent/AU2022357572A1/en active Pending
- 2022-09-28 IL IL311640A patent/IL311640A/en unknown
- 2022-09-28 EP EP22783047.8A patent/EP4408842A1/en active Pending
- 2022-09-28 CA CA3231776A patent/CA3231776A1/en active Pending
- 2022-09-28 PE PE2024000597A patent/PE20240816A1/es unknown
- 2022-09-28 KR KR1020247013656A patent/KR20240089056A/ko unknown
- 2022-09-29 AR ARP220102623A patent/AR127182A1/es unknown
-
2024
- 2024-04-26 EC ECSENADI202432316A patent/ECSP24032316A/es unknown
- 2024-04-26 CO CONC2024/0005424A patent/CO2024005424A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN118284606A (zh) | 2024-07-02 |
| WO2023053015A1 (en) | 2023-04-06 |
| HUP2100338A1 (hu) | 2023-04-28 |
| CO2024005424A2 (es) | 2024-05-10 |
| JP2024536039A (ja) | 2024-10-04 |
| AR127182A1 (es) | 2023-12-27 |
| AU2022357572A1 (en) | 2024-05-02 |
| TW202330518A (zh) | 2023-08-01 |
| ECSP24032316A (es) | 2024-05-31 |
| MX2024003812A (es) | 2024-04-25 |
| KR20240089056A (ko) | 2024-06-20 |
| EP4408842A1 (en) | 2024-08-07 |
| IL311640A (en) | 2024-05-01 |
| CA3231776A1 (en) | 2023-04-06 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR054560A1 (es) | Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer | |
| ES2710190T3 (es) | Derivados de 4-azaindol | |
| AR059328A1 (es) | Derivados de antranilamida-2-amino-heteroareno-carboxamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y el uso de estos compuestos para la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por cetp | |
| ES2623777T3 (es) | Inhibidores de la replicación del virus de la inmunodeficiencia humana | |
| AR069510A1 (es) | Arilo y heteroarilo imidazo[1,5-a]pirazinas fusionadas como inhibidores de la fosfodiesterasa 10 | |
| AR080878A1 (es) | Derivados heterociclicos de ariletinilo, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos en el tratamiento de la esquizofrenia y trastornos cognitivos. | |
| AR047098A1 (es) | Derivados de arilanilina como agonistas del receptor adrenergico beta2 | |
| AR079205A1 (es) | Morfolinotiazoles como moduladores alostericos positivos alfa 7 | |
| AR075517A1 (es) | Derivados de isoxazol-isoxazol y de isoxazol-isotiazol | |
| AR068635A1 (es) | Derivados de 1, 1, 1 - trifluor - 2 - hidroxi - 3 - fenilpropano, un metodo para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades asociadas con la modulacion del receptor de glucocorticoides. | |
| AR087915A1 (es) | N-(3-(2-amino-6,6-difluor-4,4a,5,6,7,7a-hexahidro-ciclopenta-[e][1,3]oxazin-4-il)-fenil)-amidas como inhibidores de la bace1 | |
| AR076401A1 (es) | Bisaril alquinilamidas como moduladores alostericos negativos del receptor metabotropico de glutamato 5 (mglur5) | |
| AR079467A1 (es) | Derivados heterociclicos nitrogenados de etinilo, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para tratar y/o prevenir enfermedades cognitivas o esquizofrenia. | |
| PE20190964A1 (es) | Inhibidores de dopamina-b-hidroxilasa penetrantes de la barrera hematoencefalica | |
| HRP20090565T1 (hr) | Novi triciklički derivati, postupak njihove priprave i farmaceutski pripravci koji ih sadrže | |
| AR125367A1 (es) | Moduladores alostéricos positivos del receptor muscarínico m1 de acetilcolina | |
| PE20220704A1 (es) | Derivados de 3,6-diamino-piridazin-3-ilo, composiciones farmaceuticas que los contienen y sus usos como agentes proapoptoticos | |
| CL2020001564A1 (es) | Triazolobenzazepinas como antagonistas del receptor v1a de la vasopresina. | |
| DE60214401D1 (de) | Hetero-bicyclische crf antagonisten | |
| EA202190857A1 (ru) | Бициклические производные как модуляторы 5 рецепторов gabaa | |
| AR069286A1 (es) | Derivados heterociclicos | |
| AR111176A1 (es) | Derivados pirazol[1,5-a]pirimidina sustituidos con alicíclicos farmacológicamente activos | |
| CL2019003467A1 (es) | Compuestos bicíclicos 5,6-fusionados y composiciones para el tratamiento de enfermedades parasitarias. | |
| PE20232044A1 (es) | Compuestos heterociclicos de heteroarilo y usos de los mismos | |
| PE20240816A1 (es) | DERIVADOS DE AMINA BICICLICOS COMO MODULADORES DE RECEPTOR GABAA (alfa)5 |