CO2023001367A2 - Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterocíclicos farmacológicamente activos - Google Patents
Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterocíclicos farmacológicamente activosInfo
- Publication number
- CO2023001367A2 CO2023001367A2 CONC2023/0001367A CO2023001367A CO2023001367A2 CO 2023001367 A2 CO2023001367 A2 CO 2023001367A2 CO 2023001367 A CO2023001367 A CO 2023001367A CO 2023001367 A2 CO2023001367 A2 CO 2023001367A2
- Authority
- CO
- Colombia
- Prior art keywords
- pyrimidine derivatives
- compounds
- pharmacologically active
- relates
- heterocyclic substituted
- Prior art date
Links
- LDIJKUBTLZTFRG-UHFFFAOYSA-N pyrazolo[1,5-a]pyrimidine Chemical class N1=CC=CN2N=CC=C21 LDIJKUBTLZTFRG-UHFFFAOYSA-N 0.000 title abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 title 1
- 238000000034 method Methods 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- 230000003281 allosteric effect Effects 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 239000003814 drug Substances 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
- 201000010099 disease Diseases 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000002207 metabolite Substances 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
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61K31/495—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (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)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La invención se refiere a nuevos derivados de pirazolo[1,5-a]pirimidina de fórmula (I) o sales farmacéuticamente aceptables, metabolitos biológicamente activos, profármacos, racematos, enantiómeros, diastereómeros, solvatos e hidratos de estos que sirven como moduladores alostéricos positivos del receptor GABAB. La invención también se refiere al proceso para producir dichos compuestos y los intermedios clave utilizados en el proceso. La invención se refiere además a las composiciones farmacéuticas que comprenden dichos compuestos opcionalmente en combinación con dos o más agentes terapéuticos diferentes y al uso de dichos compuestos en métodos para tratar enfermedades y afecciones mediadas y moduladas por el mecanismo alostérico positivo del receptor GABAB. La invención también proporciona un método para la fabricación de medicamentos útiles en el tratamiento de dichos trastornos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HUP2000254 | 2020-08-05 | ||
| PCT/IB2021/057180 WO2022029666A1 (en) | 2020-08-05 | 2021-08-05 | PHARMACOLOGICALLY ACTIVE HETEROCYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO2023001367A2 true CO2023001367A2 (es) | 2023-02-16 |
Family
ID=89662993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CONC2023/0001367A CO2023001367A2 (es) | 2020-08-05 | 2023-02-08 | Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterocíclicos farmacológicamente activos |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20230286988A1 (es) |
| EP (1) | EP4192833A1 (es) |
| JP (1) | JP2023536197A (es) |
| KR (1) | KR20230049677A (es) |
| CN (1) | CN116075514A (es) |
| AR (1) | AR123154A1 (es) |
| AU (1) | AU2021319420A1 (es) |
| BR (1) | BR112023001060A2 (es) |
| CA (1) | CA3185566A1 (es) |
| CL (1) | CL2023000352A1 (es) |
| CO (1) | CO2023001367A2 (es) |
| IL (1) | IL300208A (es) |
| MX (1) | MX2023001444A (es) |
| PE (1) | PE20240107A1 (es) |
| TW (1) | TW202220992A (es) |
| WO (1) | WO2022029666A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN116077459B (zh) * | 2023-04-10 | 2023-07-07 | 上海赛默罗生物科技有限公司 | α5-GABAA受体调节剂的胶囊剂及其制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CO5160344A1 (es) | 1998-12-18 | 2002-05-30 | Schering Corp | Inhibidores de transferasa de proteina farnesilo |
| DE602005001696T2 (de) | 2004-03-02 | 2008-04-10 | F. Hoffmann-La Roche Ag | 4-(sulfanylpyrimidin-4-ylmethyl)morpholin-derivate und verwandte verbindungen als gaba-rezeptorliganden zur behandlung von angst, depression und epilepsie |
| GB0512844D0 (en) | 2005-06-23 | 2005-08-03 | Novartis Ag | Organic compounds |
| CN101573334A (zh) | 2006-08-21 | 2009-11-04 | 普雷萨药品公司 | 用于治疗中枢神经系统障碍的多介质转运体抑制剂 |
| EP2473502A1 (en) | 2009-09-04 | 2012-07-11 | Novartis AG | Heteroaryl compounds as kinase inhibitors |
| TWI648281B (zh) | 2013-10-17 | 2019-01-21 | 日商安斯泰來製藥股份有限公司 | 含硫二環式化合物 |
| PL3597649T3 (pl) | 2014-04-23 | 2022-04-04 | Dart Neuroscience Llc | Kompozycje zawierające podstawione związki [1,2,4]triazolo[1,5-a]pirymidyn-7-ylowe jako inhibitory pde2 |
| SI3149001T1 (sl) * | 2014-05-28 | 2019-08-30 | Novartis Ag | Novi derivati pirazolo pirimidina in njihova uporaba kot inhimitorji malt1 |
| US9828381B2 (en) | 2015-04-20 | 2017-11-28 | AbbVie Deutschland GmbH & Co. KG | Substituted pyrazolopyrimidines and method of use |
| JP2018199623A (ja) | 2015-10-22 | 2018-12-20 | 大正製薬株式会社 | 含窒素縮合複素環化合物 |
| HU231057B1 (hu) | 2017-03-13 | 2020-04-28 | Richter Gedeon Nyrt | Gyógyászatilag hatékony aril-szubsztituált pirazolo[1,5-a]pirimidin származékok |
| HU231150B1 (hu) | 2017-03-13 | 2021-03-29 | Richter Gedeon Nyrt | Eljárás racém 3-alkilpiperidin-3-karbonsav-etil-észterek optikai izomerjeinek elválasztására |
| HU231058B1 (hu) * | 2017-03-13 | 2020-04-28 | Richter Gedeon Nyrt. | Gyógyászatilag hatékony aliciklusos-szubsztituált pirazolo[1,5-a]pirimidin származékok |
-
2021
- 2021-08-02 TW TW110128314A patent/TW202220992A/zh unknown
- 2021-08-05 PE PE2023000205A patent/PE20240107A1/es unknown
- 2021-08-05 KR KR1020237007966A patent/KR20230049677A/ko unknown
- 2021-08-05 CA CA3185566A patent/CA3185566A1/en active Pending
- 2021-08-05 JP JP2023507435A patent/JP2023536197A/ja active Pending
- 2021-08-05 EP EP21755582.0A patent/EP4192833A1/en active Pending
- 2021-08-05 AR ARP210102183A patent/AR123154A1/es unknown
- 2021-08-05 WO PCT/IB2021/057180 patent/WO2022029666A1/en active Application Filing
- 2021-08-05 AU AU2021319420A patent/AU2021319420A1/en active Pending
- 2021-08-05 MX MX2023001444A patent/MX2023001444A/es unknown
- 2021-08-05 IL IL300208A patent/IL300208A/en unknown
- 2021-08-05 BR BR112023001060A patent/BR112023001060A2/pt unknown
- 2021-08-05 CN CN202180058179.4A patent/CN116075514A/zh active Pending
- 2021-08-05 US US18/040,456 patent/US20230286988A1/en active Pending
-
2023
- 2023-02-03 CL CL2023000352A patent/CL2023000352A1/es unknown
- 2023-02-08 CO CONC2023/0001367A patent/CO2023001367A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2023536197A (ja) | 2023-08-23 |
| EP4192833A1 (en) | 2023-06-14 |
| CN116075514A (zh) | 2023-05-05 |
| WO2022029666A1 (en) | 2022-02-10 |
| CL2023000352A1 (es) | 2023-09-01 |
| IL300208A (en) | 2023-03-01 |
| KR20230049677A (ko) | 2023-04-13 |
| PE20240107A1 (es) | 2024-01-22 |
| CA3185566A1 (en) | 2022-02-10 |
| AR123154A1 (es) | 2022-11-02 |
| AU2021319420A8 (en) | 2023-03-30 |
| AU2021319420A1 (en) | 2023-03-16 |
| TW202220992A (zh) | 2022-06-01 |
| US20230286988A1 (en) | 2023-09-14 |
| MX2023001444A (es) | 2023-03-08 |
| BR112023001060A2 (pt) | 2023-03-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ECSP19072975A (es) | Derivados pirazol[1,5-a]pirimidina sustituidos con alicíclicos farmacológicamente activos | |
| PA8587101A1 (es) | Nuevos derivados de dihidropirimido [4,5-d] pirimidinona sustituida por amiino, fabricacion y uso de los mismos como agentes farmaceuticos | |
| PA8580301A1 (es) | Nuevos derivados de benzoimidazol utiles como agentes antiproliferativos | |
| UY28135A1 (es) | Derivados de pirimidina para el tratamiento de crecimiento celular anormal | |
| ATE440834T1 (de) | Substituierte arylaminderivate und verwendungsverfahren | |
| EA202091450A1 (ru) | Производные 2h-индазола в качестве ингибиторов cdk4 и cdk6 и их терапевтические применения | |
| EA200500018A1 (ru) | Бензконденсированные гетероариламидные производные тиенопиридинов, применяемые в качестве терапевтических агентов, фармацевтические композиции, включающие их, и способы их применения | |
| BRPI0614168A2 (pt) | Composto ou um sal, hidrato, solvato, isoforma, tautômero, isômero óptico farmaceuticamente aceitável ou uma combinação dos mesmos, composição farmacêutica, método para o tratamento ou prevenção de distúrbios neurológicos e psquiátricos, uso de um composto, e, processo para a preparação de um composto | |
| UY28578A1 (es) | Derivados de amida | |
| PA8550101A1 (es) | Derivados de benzamida tiazol y composiciones farmacéuticas para inhibir la proliferación de células, y métodos para su utilización | |
| PT665843E (pt) | Quinuclidinas substituidas como antagonistas da substancia p | |
| CO2023001367A2 (es) | Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterocíclicos farmacológicamente activos | |
| UY28695A1 (es) | Derivados de difenilazetidona | |
| GT200100201A (es) | Derivados de pirazol para el tratamiento der enfermedades viricas. | |
| ECSP055958A (es) | 4-aminopirimidina-5-ona | |
| CY1124346T1 (el) | ΠΑΡΑΓΩΓΑ ΧΡΩΜΑΝΙΟΥ, ΙΣΟΧΡΩΜΑΝΙΟΥ ΚΑΙ ΔΙΥΔΡΟΪΣΟΒΕΝΖΟΦΟΥΡΑΝΙΟΥ ΩΣ mGluR2-APNHTIKOI ΑΛΛΟΣΤΕΡΙΚΟΙ ΔΙΑΜΟΡΦΩΤΕΣ, ΣΥΝΘΕΣΕΙΣ, ΚΑΙ ΧΡΗΣΗ ΑΥΤΩΝ | |
| AR121296A1 (es) | Moduladores de monoacilglicerol lipasa | |
| CL2022002386A1 (es) | Compuestos de amino pirimidina fusionados | |
| CO2024003953A2 (es) | Derivados de benzodiazepina como moduladores alostéricos positivos del receptor de gaba a gamma1 | |
| EA202190857A1 (ru) | Бициклические производные как модуляторы 5 рецепторов gabaa | |
| MX2023009285A (es) | Compuestos novedosos. | |
| ES2052019T3 (es) | Espiro-isoquinolein-pirrolidin tetronas y analogos de las mismas, utiles como inhibidores de la aldosa-reductasa. | |
| UY28440A1 (es) | "n-(3-(3-sustituidas.pirazolo (1,5-a)pirimidin-7-il)-fenil)-sulfonamidas y composiciones y métodos relacionados" | |
| AR005472A1 (es) | Inhibidores de la formacion cd23 humana soluble, un procedimiento para su preparacion, el uso de los mismos para la manufactura de un medicamento,composicion farmaceutica y compuestos intermediarios | |
| ECSP23073082A (es) | Nuevos moduladores alostéricos negativos ciclopenta[c]pirrol de NR2B |