PE20191646A1 - Derivados pirazol [1,5-a] pirimidina sustituidos con aliciclicos farmacologicamente activos - Google Patents
Derivados pirazol [1,5-a] pirimidina sustituidos con aliciclicos farmacologicamente activosInfo
- Publication number
- PE20191646A1 PE20191646A1 PE2019001773A PE2019001773A PE20191646A1 PE 20191646 A1 PE20191646 A1 PE 20191646A1 PE 2019001773 A PE2019001773 A PE 2019001773A PE 2019001773 A PE2019001773 A PE 2019001773A PE 20191646 A1 PE20191646 A1 PE 20191646A1
- Authority
- PE
- Peru
- Prior art keywords
- 6alkyl
- compounds
- alicyclics
- derivatives
- pharmacologically active
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine 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
- A61K31/495—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
- 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
-
- 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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (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
Referido a un compuesto de formula I, en donde R1 y R2 se seleccionan independientemente entre H, halogeno, C1-6alquilo, entre otros; R3 es H, halogeno, C1-6alquilo, ciano; R4 es C1-6alquilo; y R5 es C1-6alquilo opcionalmente sustituido; R6 es H, hidroxilo, C1-6alquilo, entre otros; sales farmaceuticamente aceptables, metabolitos biologicamente activos, profarmacos, racematos, enantiomeros, diastereomeros, solvatos e hidratos de los mismos. Un compuesto preferido es acido (3S)-1-[5-metil-6-(propan-2-il)-2-[trans-4-(trifluorometil)ciclohexil]pirazol[1,5-a]pirimidin-7-il]piperidin-3-carboxilico. Estos compuestos son derivados de pirazol[1,5-a]pirimidina sustituidos con aliciclicos farmacologicamente activos y son moduladores alosterico positivo del receptor del GABA B. Tambien se refiere a un proceso para producir dichos compuestos, una composicion farmaceutica que comprende dichos compuestos, una combinacion que los comprenden con dos o mas agentes terapeuticos diferentes, un proceso para elaborar dicha composicion, y su uso en el tratamiento o prevencion de trastornos asociados a la actividad moduladora alosterico positivo del receptor del GABA B, tales como ansiedad, esquizofrenia, epilepsia, entre otros.
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 |
|---|---|
| PE20191646A1 true PE20191646A1 (es) | 2019-11-07 |
Family
ID=89992389
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019001773A PE20191646A1 (es) | 2017-03-13 | 2018-03-12 | Derivados pirazol [1,5-a] pirimidina sustituidos con aliciclicos farmacologicamente 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 (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU231057B1 (hu) | 2017-03-13 | 2020-04-28 | Richter Gedeon Nyrt | Gyógyászatilag hatékony aril-szubsztituált pirazolo[1,5-a]pirimidin származékok |
| 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 |
| TW202220992A (zh) | 2020-08-05 | 2022-06-01 | 匈牙利商羅特格登公司 | 具藥理活性之經雜環取代的吡唑并〔１，５－ａ〕嘧啶衍生物 |
| HUP2100338A1 (hu) | 2021-09-29 | 2023-04-28 | 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 |
|---|---|---|---|---|
| KR100802863B1 (ko) | 2004-03-02 | 2008-02-12 | 에프. 호프만-라 로슈 아게 | 불안증, 우울증 및 간질의 치료를 위한 ｇａｂａ 수용체리간드로서 4-(설파닐-피리미딘-4-일메틸)-모폴린 유도체및 관련 화합물 |
| 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 |
| US8461163B2 (en) * | 2008-03-31 | 2013-06-11 | Takeda Pharmaceutical Company Limited | Substituted N-(pyrazolo[1,5-a]pyrimidin-5-yl)amides as inhibitors of apoptosis signal-regulating kinase 1 |
| 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 |
| 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 |
-
2017
- 2017-03-13 HU HU1700108A patent/HU231058B1/hu not_active IP Right Cessation
-
2018
- 2018-03-12 PL PL18713016T patent/PL3596080T3/pl unknown
- 2018-03-12 RS RS20211334A patent/RS62533B1/sr unknown
- 2018-03-12 CN CN201880017859.XA patent/CN110431142A/zh active Pending
- 2018-03-12 UA UAA201910328A patent/UA124783C2/uk unknown
- 2018-03-12 AU AU2018235266A patent/AU2018235266B2/en not_active Ceased
- 2018-03-12 PT PT18713016T patent/PT3596080T/pt unknown
- 2018-03-12 JP JP2019549366A patent/JP7153662B2/ja active Active
- 2018-03-12 MX MX2019011000A patent/MX2019011000A/es unknown
- 2018-03-12 ES ES18713016T patent/ES2893824T3/es active Active
- 2018-03-12 PE PE2019001773A patent/PE20191646A1/es unknown
- 2018-03-12 KR KR1020197028833A patent/KR20190127779A/ko not_active Ceased
- 2018-03-12 WO PCT/IB2018/051599 patent/WO2018167630A1/en active Application Filing
- 2018-03-12 US US16/493,453 patent/US11026946B2/en active Active
- 2018-03-12 LT LTEPPCT/IB2018/051599T patent/LT3596080T/lt unknown
- 2018-03-12 EA EA201992127A patent/EA038756B1/ru unknown
- 2018-03-12 SG SG11201907864YA patent/SG11201907864YA/en unknown
- 2018-03-12 MY MYPI2019004947A patent/MY195262A/en unknown
- 2018-03-12 SI SI201830495T patent/SI3596080T1/sl unknown
- 2018-03-12 DK DK18713016.6T patent/DK3596080T3/da active
- 2018-03-12 HU HUE18713016A patent/HUE056562T2/hu unknown
- 2018-03-12 HR HRP20211850TT patent/HRP20211850T1/hr unknown
- 2018-03-12 EP EP18713016.6A patent/EP3596080B1/en active Active
- 2018-03-12 BR BR112019018843A patent/BR112019018843A2/pt not_active Application Discontinuation
- 2018-03-12 GE GEAP201815192A patent/GEP20217256B/en 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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