PE20240107A1 - Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterociclicos farmacologicamente activos - Google Patents
Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterociclicos farmacologicamente activosInfo
- Publication number
- PE20240107A1 PE20240107A1 PE2023000205A PE2023000205A PE20240107A1 PE 20240107 A1 PE20240107 A1 PE 20240107A1 PE 2023000205 A PE2023000205 A PE 2023000205A PE 2023000205 A PE2023000205 A PE 2023000205A PE 20240107 A1 PE20240107 A1 PE 20240107A1
- Authority
- PE
- Peru
- Prior art keywords
- derivatives
- pyrazolo
- group
- disorders
- c6alkyl
- Prior art date
Links
Classifications
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- 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
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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
- A61K31/495—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/14—Antitussive agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
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- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal 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)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (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
Refiere a nuevos derivados de pirazolo[1,5-a]pirimidina de formula (I) o sales farmaceuticamente aceptables, metabolitos biologicamente activos, profarmacos, racematos, enantiomeros, diastereomeros, solvatos e hidratos de estos que sirven como moduladores alostericos positivos del receptor GABAB. Dichos derivados se caracterizan porque R1, R2, R3, R4, R5, R6, R7, R8, R9 y R10 se seleccionan de C1-C6alquilo o halo-C1-C6alquilo; R9 y R10 pueden formar juntos el grupo oxo; X representa al grupo -CRxRy, -O- o -S(O)n-; Z al grupo -NR-, -O- o -S(O)2; y R4 mas CRx forman un anillo cicloalquilo. Asimismo, los derivados se seleccionan del grupo de -[(3R)-3-{6-etil-5-metil-2-[trans-4-(trifluorometil)ciclohexil]pirazolo[1,5-a]pirimidin-7-il}-3-metilpiperidin-1-il]etan-1-ona. Tambien, refiere a composiciones farmaceuticas que comprenden uno de los derivados de formula (I) como principio activo en combinacion con dos o mas agentes terapeuticos diferentes; al uso de estos nuevos derivados en el tratamiento y/o prevencion de trastornos psiquiatricos (depresion, esquizofrenia), trastornos del neurodesarrollo (sindrome del cromosoma X fragil) y trastornos cognitivos; y al metodo para la fabricacion de medicamentos utiles en el tratamiento y/o prevencion 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 |
|---|---|
| PE20240107A1 true PE20240107A1 (es) | 2024-01-22 |
Family
ID=89662993
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023000205A PE20240107A1 (es) | 2020-08-05 | 2021-08-05 | Derivados de pirazolo[1,5-a]pirimidina sustituidos con heterociclicos farmacologicamente activos |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US12473293B2 (es) |
| EP (1) | EP4192833B1 (es) |
| JP (1) | JP2023536197A (es) |
| KR (1) | KR20230049677A (es) |
| CN (2) | CN120590392A (es) |
| AR (1) | AR123154A1 (es) |
| AU (1) | AU2021319420B2 (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) |
| WO (1) | WO2022029666A1 (es) |
| ZA (1) | ZA202301873B (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20230017828A (ko) * | 2020-05-27 | 2023-02-06 | 에스테베 파마슈티칼스 에스에이 | 통증에 대한 다중모드 활성을 갖는 피라졸로[1,5-a]피리미딘 유도체 |
| IL300208A (en) | 2020-08-05 | 2023-03-01 | Richter Gedeon Nyrt | Pharmacologically active heterocyclic substituted pyrazolo[5,1-a]pyrimidine derivatives |
| 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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL143409A0 (en) | 1998-12-18 | 2002-04-21 | Schering Corp | Farnesyl protein transferase inhibitors |
| WO2005094828A1 (en) | 2004-03-02 | 2005-10-13 | F. Hoffmann-La Roche Ag | 4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as gaba receptor ligands for the treatment of anxiety, depression and epilepsy |
| GB0512844D0 (en) | 2005-06-23 | 2005-08-03 | Novartis Ag | Organic compounds |
| CA2661220A1 (en) | 2006-08-21 | 2008-02-28 | James R. Hauske | Multimediator transporter inhibitors for use in treatment of central nervous system disorders |
| KR20120049940A (ko) | 2009-09-04 | 2012-05-17 | 노파르티스 아게 | 키나제 억제제로서의 헤테로아릴 화합물 |
| 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 |
| CN106459062A (zh) | 2014-04-23 | 2017-02-22 | 达特神经科学(开曼)有限公司 | 作为PDE2抑制剂的取代的[1,2,4]三唑并[1,5‑a]嘧啶‑7‑基化合物 |
| AU2015265478B2 (en) | 2014-05-28 | 2017-09-14 | Novartis Ag | Novel pyrazolo pyrimidine derivatives and their use as MALT1 inhibitors |
| 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 |
| 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 |
| HU231150B1 (hu) | 2017-03-13 | 2021-03-29 | Richter Gedeon Nyrt | Eljárás racém 3-alkilpiperidin-3-karbonsav-etil-észterek optikai izomerjeinek elválasztására |
| IL300208A (en) | 2020-08-05 | 2023-03-01 | Richter Gedeon Nyrt | Pharmacologically active heterocyclic substituted pyrazolo[5,1-a]pyrimidine derivatives |
-
2021
- 2021-08-05 IL IL300208A patent/IL300208A/en unknown
- 2021-08-05 AR ARP210102183A patent/AR123154A1/es unknown
- 2021-08-05 BR BR112023001060A patent/BR112023001060A2/pt unknown
- 2021-08-05 KR KR1020237007966A patent/KR20230049677A/ko active Pending
- 2021-08-05 MX MX2023001444A patent/MX2023001444A/es unknown
- 2021-08-05 US US18/040,456 patent/US12473293B2/en active Active
- 2021-08-05 JP JP2023507435A patent/JP2023536197A/ja active Pending
- 2021-08-05 CN CN202510616684.6A patent/CN120590392A/zh active Pending
- 2021-08-05 PE PE2023000205A patent/PE20240107A1/es unknown
- 2021-08-05 AU AU2021319420A patent/AU2021319420B2/en active Active
- 2021-08-05 EP EP21755582.0A patent/EP4192833B1/en active Active
- 2021-08-05 WO PCT/IB2021/057180 patent/WO2022029666A1/en not_active Ceased
- 2021-08-05 CN CN202180058179.4A patent/CN116075514A/zh active Pending
- 2021-08-05 CA CA3185566A patent/CA3185566A1/en active Pending
-
2023
- 2023-02-03 CL CL2023000352A patent/CL2023000352A1/es unknown
- 2023-02-08 CO CONC2023/0001367A patent/CO2023001367A2/es unknown
- 2023-02-15 ZA ZA2023/01873A patent/ZA202301873B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20230286988A1 (en) | 2023-09-14 |
| EP4192833B1 (en) | 2026-01-21 |
| CO2023001367A2 (es) | 2023-02-16 |
| CL2023000352A1 (es) | 2023-09-01 |
| CN116075514A (zh) | 2023-05-05 |
| CN120590392A (zh) | 2025-09-05 |
| MX2023001444A (es) | 2023-03-08 |
| AR123154A1 (es) | 2022-11-02 |
| ZA202301873B (en) | 2024-09-25 |
| CA3185566A1 (en) | 2022-02-10 |
| WO2022029666A1 (en) | 2022-02-10 |
| AU2021319420B2 (en) | 2026-01-29 |
| IL300208A (en) | 2023-03-01 |
| US12473293B2 (en) | 2025-11-18 |
| BR112023001060A2 (pt) | 2023-03-07 |
| JP2023536197A (ja) | 2023-08-23 |
| TW202220992A (zh) | 2022-06-01 |
| AU2021319420A1 (en) | 2023-03-16 |
| KR20230049677A (ko) | 2023-04-13 |
| EP4192833A1 (en) | 2023-06-14 |
| AU2021319420A8 (en) | 2023-03-30 |
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