ECSP19072975A - Derivados pirazol[1,5-a]pirimidina sustituidos con alicíclicos farmacológicamente activos - Google Patents
Derivados pirazol[1,5-a]pirimidina sustituidos con alicíclicos farmacológicamente activosInfo
- Publication number
- ECSP19072975A ECSP19072975A ECSENADI201972975A ECDI201972975A ECSP19072975A EC SP19072975 A ECSP19072975 A EC SP19072975A EC SENADI201972975 A ECSENADI201972975 A EC SENADI201972975A EC DI201972975 A ECDI201972975 A EC DI201972975A EC SP19072975 A ECSP19072975 A EC SP19072975A
- Authority
- EC
- Ecuador
- Prior art keywords
- compounds
- pyrimidine derivatives
- pyrazole
- allicyclics
- pharmacologically active
- Prior art date
Links
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title abstract 2
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 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
- 229940079593 drug Drugs 0.000 abstract 1
- 150000004677 hydrates Chemical class 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
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/14—Ortho-condensed systems
- C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Nuevos derivados de pirazol[1,5-a]pirimidina de la fórmula (I) o sales farmacéuticamente aceptables, metabolitos biológicamente activos, profármacos, racematos, enantiómeros, diastereómeros, solvatos e hidratos de los mismos que sirven como moduladores alostéricos positivos del receptor del GABAB. La invención también se relaciona con el proceso para producir dichos compuestos. La invención se relaciona además con composiciones farmacéuticas que comprenden dichos compuestos, opcionalmente en combinación con dos o más agentes terapéuticos diferentes, y con el empleo de dichos compuestos en métodos de tratamiento de enfermedades y condiciones mediadas y moduladas por el mecanismo alostérico positivo del receptor del GABAB. La invención también provee un método para elaborar medicamentos que son de utilidad en el tratamiento de dichos trastornos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU1700108A HU231058B1 (hu) | 2017-03-13 | 2017-03-13 | Gyógyászatilag hatékony aliciklusos-szubsztituált pirazolo[1,5-a]pirimidin származékok |
| PCT/IB2018/051599 WO2018167630A1 (en) | 2017-03-13 | 2018-03-12 | PHARMACOLOGICALLY ACTIVE ALICYCLIC-SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP19072975A true ECSP19072975A (es) | 2019-11-30 |
Family
ID=89992389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI201972975A ECSP19072975A (es) | 2017-03-13 | 2019-10-10 | Derivados pirazol[1,5-a]pirimidina sustituidos con alicíclicos farmacológicamente activos |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US11026946B2 (es) |
| EP (1) | EP3596080B1 (es) |
| JP (1) | JP7153662B2 (es) |
| KR (1) | KR20190127779A (es) |
| CN (1) | CN110431142A (es) |
| AR (1) | AR111176A1 (es) |
| AU (1) | AU2018235266B2 (es) |
| BR (1) | BR112019018843A2 (es) |
| CA (1) | CA3056185A1 (es) |
| CL (1) | CL2019002601A1 (es) |
| CO (1) | CO2019010120A2 (es) |
| CY (1) | CY1124708T1 (es) |
| DK (1) | DK3596080T3 (es) |
| EA (1) | EA038756B1 (es) |
| EC (1) | ECSP19072975A (es) |
| ES (1) | ES2893824T3 (es) |
| GE (1) | GEP20217256B (es) |
| HR (1) | HRP20211850T1 (es) |
| HU (2) | HU231058B1 (es) |
| IL (1) | IL268923A (es) |
| LT (1) | LT3596080T (es) |
| MX (1) | MX2019011000A (es) |
| MY (1) | MY195262A (es) |
| PE (1) | PE20191646A1 (es) |
| PH (1) | PH12019501968A1 (es) |
| PL (1) | PL3596080T3 (es) |
| PT (1) | PT3596080T (es) |
| RS (1) | RS62533B1 (es) |
| SG (1) | SG11201907864YA (es) |
| SI (1) | SI3596080T1 (es) |
| UA (1) | UA124783C2 (es) |
| WO (1) | WO2018167630A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN117510468A (zh) | 2017-03-13 | 2024-02-06 | 灵北拉荷亚研究中心公司 | 双重magl和faah抑制剂 |
| HU231057B1 (hu) | 2017-03-13 | 2020-04-28 | Richter Gedeon Nyrt | Gyógyászatilag hatékony aril-szubsztituált pirazolo[1,5-a]pirimidin származékok |
| IL296716A (en) | 2020-03-26 | 2022-11-01 | Richter Gedeon Nyrt | History of naphthyridine and pyrido[4,3-c]pyridazine as gabaa alpha 5 receptor modulators |
| CN116075514A (zh) * | 2020-08-05 | 2023-05-05 | 吉瑞工厂 | 药理学活性的杂环取代的吡唑并[1,5-a]嘧啶衍生物 |
| HU231691B1 (hu) | 2021-09-29 | 2025-10-28 | Richter Gedeon Nyrt | GABAA ALFA5 receptor modulátor hatású biciklusos aminszármazékok |
| CN115872095A (zh) * | 2022-11-28 | 2023-03-31 | 南通三鑫车灯配件有限公司 | 一种汽车车灯反光罩的生产线流转装置 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE367163T1 (de) | 2004-03-02 | 2007-08-15 | Hoffmann La Roche | 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 |
| KR100753017B1 (ko) | 2006-05-25 | 2007-08-30 | 한국화학연구원 | 7-(3,4-디알콕시페닐)-피라졸로[1,5-ａ]피리미딘 화합물을포함하는 관절염, 아토피 피부염, 백혈병을 포함한 암 및알쯔하이머, 우울증 또는 기억력 감소 등의 뇌질환의 치료및 예방을 위한 약제학적 조성물 |
| WO2009123986A1 (en) * | 2008-03-31 | 2009-10-08 | Takeda Pharmaceutical Company Limited | Apoptosis signal-regulating kinase 1 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 |
| EP3286192A1 (en) | 2015-04-20 | 2018-02-28 | 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 |
-
2017
- 2017-03-13 HU HU1700108A patent/HU231058B1/hu not_active IP Right Cessation
-
2018
- 2018-03-12 MY MYPI2019004947A patent/MY195262A/en unknown
- 2018-03-12 LT LTEPPCT/IB2018/051599T patent/LT3596080T/lt unknown
- 2018-03-12 EP EP18713016.6A patent/EP3596080B1/en active Active
- 2018-03-12 HU HUE18713016A patent/HUE056562T2/hu unknown
- 2018-03-12 PL PL18713016T patent/PL3596080T3/pl unknown
- 2018-03-12 PT PT18713016T patent/PT3596080T/pt unknown
- 2018-03-12 SG SG11201907864YA patent/SG11201907864YA/en unknown
- 2018-03-12 BR BR112019018843A patent/BR112019018843A2/pt not_active Application Discontinuation
- 2018-03-12 AU AU2018235266A patent/AU2018235266B2/en not_active Ceased
- 2018-03-12 PE PE2019001773A patent/PE20191646A1/es unknown
- 2018-03-12 MX MX2019011000A patent/MX2019011000A/es unknown
- 2018-03-12 WO PCT/IB2018/051599 patent/WO2018167630A1/en not_active Ceased
- 2018-03-12 US US16/493,453 patent/US11026946B2/en active Active
- 2018-03-12 GE GEAP201815192A patent/GEP20217256B/en unknown
- 2018-03-12 HR HRP20211850TT patent/HRP20211850T1/hr unknown
- 2018-03-12 KR KR1020197028833A patent/KR20190127779A/ko not_active Ceased
- 2018-03-12 UA UAA201910328A patent/UA124783C2/uk unknown
- 2018-03-12 EA EA201992127A patent/EA038756B1/ru unknown
- 2018-03-12 ES ES18713016T patent/ES2893824T3/es active Active
- 2018-03-12 CN CN201880017859.XA patent/CN110431142A/zh active Pending
- 2018-03-12 RS RS20211334A patent/RS62533B1/sr unknown
- 2018-03-12 DK DK18713016.6T patent/DK3596080T3/da active
- 2018-03-12 JP JP2019549366A patent/JP7153662B2/ja active Active
- 2018-03-12 SI SI201830495T patent/SI3596080T1/sl unknown
- 2018-03-12 CA CA3056185A patent/CA3056185A1/en active Pending
- 2018-03-13 AR ARP180100580A patent/AR111176A1/es unknown
-
2019
- 2019-08-26 IL IL26892319A patent/IL268923A/en unknown
- 2019-08-27 PH PH12019501968A patent/PH12019501968A1/en unknown
- 2019-09-12 CL CL2019002601A patent/CL2019002601A1/es unknown
- 2019-09-18 CO CONC2019/0010120A patent/CO2019010120A2/es unknown
- 2019-10-10 EC ECSENADI201972975A patent/ECSP19072975A/es unknown
-
2021
- 2021-11-08 CY CY20211100964T patent/CY1124708T1/el unknown
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