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
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 5
- 102000017934 GABA-B receptor Human genes 0.000 abstract 2
- 108060003377 GABA-B receptor Proteins 0.000 abstract 2
- 230000003281 allosteric effect Effects 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 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
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000002723 alicyclic group Chemical group 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 239000002207 metabolite Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- XJLSEXAGTJCILF-UHFFFAOYSA-N nipecotic acid Chemical compound OC(=O)C1CCCNC1 XJLSEXAGTJCILF-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003217 pyrazoles Chemical class 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
-
- 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)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (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 (6)
| 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 |
| PL3595665T3 (pl) | 2017-03-13 | 2025-01-13 | Lundbeck La Jolla Research Center, Inc. | Podwójne inhibitory magl i faah |
| TWI901650B (zh) | 2020-03-26 | 2025-10-21 | 匈牙利商羅特格登公司 | 啶及吡啶并〔３，４－ｃ〕嗒衍生物 |
| IL300208A (en) | 2020-08-05 | 2023-03-01 | Richter Gedeon Nyrt | Pharmacologically active heterocyclic substituted pyrazolo[5,1-a]pyrimidine derivatives |
| 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 |
|---|---|---|---|---|
| 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 |
| 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 CA CA3056185A patent/CA3056185A1/en active Pending
- 2018-03-12 DK DK18713016.6T patent/DK3596080T3/da active
- 2018-03-12 MX MX2019011000A patent/MX2019011000A/es unknown
- 2018-03-12 PT PT18713016T patent/PT3596080T/pt unknown
- 2018-03-12 EP EP18713016.6A patent/EP3596080B1/en active Active
- 2018-03-12 US US16/493,453 patent/US11026946B2/en active Active
- 2018-03-12 HU HUE18713016A patent/HUE056562T2/hu unknown
- 2018-03-12 HR HRP20211850TT patent/HRP20211850T1/hr unknown
- 2018-03-12 CN CN201880017859.XA patent/CN110431142A/zh active Pending
- 2018-03-12 AU AU2018235266A patent/AU2018235266B2/en not_active Ceased
- 2018-03-12 KR KR1020197028833A patent/KR20190127779A/ko not_active Ceased
- 2018-03-12 ES ES18713016T patent/ES2893824T3/es active Active
- 2018-03-12 BR BR112019018843A patent/BR112019018843A2/pt not_active Application Discontinuation
- 2018-03-12 PE PE2019001773A patent/PE20191646A1/es unknown
- 2018-03-12 SG SG11201907864YA patent/SG11201907864YA/en unknown
- 2018-03-12 SI SI201830495T patent/SI3596080T1/sl unknown
- 2018-03-12 UA UAA201910328A patent/UA124783C2/uk unknown
- 2018-03-12 EA EA201992127A patent/EA038756B1/ru unknown
- 2018-03-12 RS RS20211334A patent/RS62533B1/sr unknown
- 2018-03-12 LT LTEPPCT/IB2018/051599T patent/LT3596080T/lt unknown
- 2018-03-12 PL PL18713016T patent/PL3596080T3/pl unknown
- 2018-03-12 WO PCT/IB2018/051599 patent/WO2018167630A1/en not_active Ceased
- 2018-03-12 MY MYPI2019004947A patent/MY195262A/en unknown
- 2018-03-12 JP JP2019549366A patent/JP7153662B2/ja active Active
- 2018-03-12 GE GEAP201815192A patent/GEP20217256B/en unknown
- 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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