AR101393A1 - COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2 - Google Patents
COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2Info
- Publication number
- AR101393A1 AR101393A1 ARP150102462A ARP150102462A AR101393A1 AR 101393 A1 AR101393 A1 AR 101393A1 AR P150102462 A ARP150102462 A AR P150102462A AR P150102462 A ARP150102462 A AR P150102462A AR 101393 A1 AR101393 A1 AR 101393A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- monohalo
- polyhalo
- compounds
- 4oxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 title 1
- 108010038421 metabotropic glutamate receptor 2 Proteins 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 17
- 125000000217 alkyl group Chemical group 0.000 abstract 9
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 abstract 3
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 229940126662 negative allosteric modulator Drugs 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- -1 2-pyridinyl Chemical group 0.000 abstract 1
- GLQXAHBYDJPCHG-UHFFFAOYSA-N 6,7-dihydro-5h-pyrazolo[1,5-a]pyrazin-4-one Chemical class O=C1NCCN2N=CC=C12 GLQXAHBYDJPCHG-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 102000006239 metabotropic receptors Human genes 0.000 abstract 1
- 108020004083 metabotropic receptors Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Psychiatry (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)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14179599 | 2014-08-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR101393A1 true AR101393A1 (es) | 2016-12-14 |
Family
ID=51257438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP150102462A AR101393A1 (es) | 2014-08-01 | 2015-07-31 | COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10112949B2 (enExample) |
| EP (1) | EP3174880B1 (enExample) |
| JP (1) | JP6615864B2 (enExample) |
| KR (1) | KR102531693B1 (enExample) |
| CN (1) | CN106573935B (enExample) |
| AR (1) | AR101393A1 (enExample) |
| AU (1) | AU2015295299B2 (enExample) |
| BR (1) | BR112017001998A2 (enExample) |
| CA (1) | CA2954218C (enExample) |
| EA (1) | EA031038B1 (enExample) |
| ES (1) | ES2702192T3 (enExample) |
| JO (1) | JO3601B1 (enExample) |
| MX (1) | MX2017001453A (enExample) |
| TW (1) | TWI696625B (enExample) |
| WO (1) | WO2016016381A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20150177B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| JOP20150179B1 (ar) | 2014-08-01 | 2021-08-17 | Janssen Pharmaceutica Nv | مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2 |
| JP6861154B2 (ja) | 2014-12-03 | 2021-04-21 | ヤンセン ファーマシューティカ エヌ．ベー． | 放射標識されたｍＧｌｕＲ２ ＰＥＴリガンド |
| CA2967153A1 (en) * | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-.alpha.]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
| ES2820823T3 (es) | 2015-12-18 | 2021-04-22 | Janssen Pharmaceutica Nv | Ligandos PET mGluR2/3 radiomarcados |
| EP3389727B1 (en) * | 2015-12-18 | 2020-08-12 | Janssen Pharmaceutica NV | Radiolabelled mglur2/3 pet ligands |
| SG11202004484UA (en) | 2017-11-24 | 2020-06-29 | Sumitomo Dainippon Pharma Co Ltd | 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZINONE DERIVATIVE AND MEDICAL USE THEREOF |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102004054665A1 (de) * | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte bi- und tricyclische Pyrazol-Derivate Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
| JP4801724B2 (ja) * | 2005-03-23 | 2011-10-26 | エフ．ホフマン−ラ ロシュ アーゲー | ｍＧｌｕＲ２アンタゴニストとしてのアセチレニル−ピラゾロ−ピリミジン誘導体 |
| AU2010246609B2 (en) | 2009-05-12 | 2013-09-05 | Addex Pharma S.A. | 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders |
| US8592422B2 (en) * | 2010-12-17 | 2013-11-26 | Vanderbilt University | Bicyclic triazole and pyrazole lactams as allosteric modulators of mGluR5 receptors |
| WO2012172093A1 (en) * | 2011-06-17 | 2012-12-20 | Merz Pharma Gmbh & Co. Kgaa | Dihydroindolizine derivate as metabotropic glutamate receptor modulators |
| EP2775841B1 (en) | 2011-11-03 | 2017-09-13 | Merck Sharp & Dohme Corp. | QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| EP2666775A1 (en) | 2012-05-21 | 2013-11-27 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
| US20130345204A1 (en) | 2012-06-20 | 2013-12-26 | Vanderbilt University | Substituted bicyclic cycloalkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors |
| AU2013277152A1 (en) * | 2012-06-20 | 2015-01-22 | Vanderbilt University | Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mGluR5 receptors |
| WO2013192350A1 (en) * | 2012-06-20 | 2013-12-27 | Vanderbilt University | Substituted bicyclic aralkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors |
| JP2015534993A (ja) | 2012-10-23 | 2015-12-07 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａ | 自閉症性障害の処置のためのｍＧｌｕ２／３アンタゴニスト |
| EP3174882B1 (en) * | 2014-08-01 | 2018-11-07 | Janssen Pharmaceutica NV | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors |
-
2015
- 2015-07-27 JO JOP/2015/0178A patent/JO3601B1/ar active
- 2015-07-30 KR KR1020177005638A patent/KR102531693B1/ko active Active
- 2015-07-30 CN CN201580041306.4A patent/CN106573935B/zh not_active Expired - Fee Related
- 2015-07-30 ES ES15742317T patent/ES2702192T3/es active Active
- 2015-07-30 US US15/500,553 patent/US10112949B2/en active Active
- 2015-07-30 CA CA2954218A patent/CA2954218C/en active Active
- 2015-07-30 BR BR112017001998A patent/BR112017001998A2/pt not_active Application Discontinuation
- 2015-07-30 WO PCT/EP2015/067533 patent/WO2016016381A1/en not_active Ceased
- 2015-07-30 AU AU2015295299A patent/AU2015295299B2/en not_active Ceased
- 2015-07-30 EP EP15742317.9A patent/EP3174880B1/en active Active
- 2015-07-30 MX MX2017001453A patent/MX2017001453A/es active IP Right Grant
- 2015-07-30 JP JP2017505456A patent/JP6615864B2/ja not_active Expired - Fee Related
- 2015-07-30 TW TW104124697A patent/TWI696625B/zh not_active IP Right Cessation
- 2015-07-30 EA EA201692496A patent/EA031038B1/ru not_active IP Right Cessation
- 2015-07-31 AR ARP150102462A patent/AR101393A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU2015295299A1 (en) | 2017-01-19 |
| US20180222908A1 (en) | 2018-08-09 |
| CN106573935B (zh) | 2020-01-17 |
| CA2954218C (en) | 2022-11-29 |
| EA201692496A1 (ru) | 2017-06-30 |
| KR20170032464A (ko) | 2017-03-22 |
| WO2016016381A1 (en) | 2016-02-04 |
| JP6615864B2 (ja) | 2019-12-04 |
| US10112949B2 (en) | 2018-10-30 |
| AU2015295299B2 (en) | 2019-05-02 |
| EP3174880A1 (en) | 2017-06-07 |
| JP2017523201A (ja) | 2017-08-17 |
| EA031038B1 (ru) | 2018-11-30 |
| JO3601B1 (ar) | 2020-07-05 |
| ES2702192T3 (es) | 2019-02-27 |
| BR112017001998A2 (pt) | 2017-12-12 |
| TW201609742A (zh) | 2016-03-16 |
| EP3174880B1 (en) | 2018-09-26 |
| CA2954218A1 (en) | 2016-02-04 |
| MX2017001453A (es) | 2017-05-11 |
| KR102531693B1 (ko) | 2023-05-10 |
| TWI696625B (zh) | 2020-06-21 |
| CN106573935A (zh) | 2017-04-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |