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
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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
-
- 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)
Abstract
La presente solicitud se refiere a derivados de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona como moduladores alostéricos negativos (NAM) del receptor de glutamato metabotrópico subtipo 2 (mGluR2). También está dirigida a composiciones farmacéuticas que comprenden dichos compuestos, a procesos para preparar dichos compuestos y composiciones y al uso de dichos compuestos y composiciones para prevenir o tratar trastornos en los que está implicado el subtipo mGluR2 de receptores metabotrópicos. Reivindicación 1: Un compuesto de fórmula (1) o una forma estereoisomérica del mismo, en donde R¹ es fenilo o 2-piridinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -alquil C₁₋₄-OH, -CN, -alquil C₁₋₄-O-alquilo C₁₋₄, cicloalquilo C₃₋₇, -O-alquilo C₁₋₄, monohalo-alquil C₁₋₄oxi, polihalo-alquil C₁₋₄oxi, SF₅, alquil C₁₋₄tio, monohalo-alquil C₁₋₄tio y polihalo-alquil C₁₋₄tio; R² es fenilo o piridinilo, cada uno de los cuales está opcionalmente sustituido con uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -OH, -O-alquilo C₁₋₄, -alquil C₁₋₄-O-alquilo C₁₋₄, monohalo-alquil C₁₋₄oxi, polihalo-alquil C₁₋₄oxi, -alquil C₁₋₄-OH y NR⁵ᵃR⁵ᵇ; en donde R⁵ᵃ y R⁵ᵇ son cada uno independientemente hidrógeno o alquilo C₁₋₄; R³ es hidrógeno o alquilo C₁₋₄; R⁴ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -alquil C₁₋₄-O-alquilo C₁₋₄ y -alquil C₁₋₄-OH; o un N-óxido, o una sal farmacéuticamente aceptable o un solvato del mismo.
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 (es) |
| EP (1) | EP3174880B1 (es) |
| JP (1) | JP6615864B2 (es) |
| KR (1) | KR102531693B1 (es) |
| CN (1) | CN106573935B (es) |
| AR (1) | AR101393A1 (es) |
| AU (1) | AU2015295299B2 (es) |
| BR (1) | BR112017001998A2 (es) |
| CA (1) | CA2954218C (es) |
| EA (1) | EA031038B1 (es) |
| ES (1) | ES2702192T3 (es) |
| JO (1) | JO3601B1 (es) |
| MX (1) | MX2017001453A (es) |
| TW (1) | TWI696625B (es) |
| WO (1) | WO2016016381A1 (es) |
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 |
| WO2016087487A1 (en) | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | 6,7-DIHYDROPYRAZOLO[1,5-α]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| WO2016087489A1 (en) | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | Radiolabelled mglur2 pet ligands |
| AU2016374571B2 (en) | 2015-12-18 | 2021-05-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| EA037941B1 (ru) | 2015-12-18 | 2021-06-09 | Янссен Фармацевтика Нв | ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ |
| US11633395B2 (en) | 2017-11-24 | 2023-04-25 | Sumitomo Pharma Co., Ltd. | Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group II metabotropic glutamate receptor |
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 |
| KR100968989B1 (ko) * | 2005-03-23 | 2010-07-09 | 에프. 호프만-라 로슈 아게 | ｍＧｌｕＲ2 길항제로서 아세틸렌일-피라졸로-피리미딘 유도체 |
| SG10201402250TA (en) | 2009-05-12 | 2014-07-30 | Janssen Pharmaceuticals Inc | 1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders |
| AU2011343477A1 (en) * | 2010-12-17 | 2013-07-04 | 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 |
| JP5857136B2 (ja) | 2011-11-03 | 2016-02-10 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | ｍＧｌｕＲ２−陰性アロステリック調節因子としてのキノリンカルボキサミドおよびキノリンカルボニトリル誘導体、組成物、およびその使用 |
| EP2666775A1 (en) | 2012-05-21 | 2013-11-27 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
| WO2013192347A1 (en) | 2012-06-20 | 2013-12-27 | Vanderbilt University | Substituted bicyclic cycloalkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors |
| EP2863922A4 (en) * | 2012-06-20 | 2015-11-04 | Univ Vanderbilt | SUBSTITUTED BICYCLIC ALKOXYPYRAZOL ANALOGUES AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS |
| US20130345205A1 (en) | 2012-06-20 | 2013-12-26 | Vanderbilt University | Substituted bicyclic aralkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors |
| EP2925292A1 (en) * | 2012-10-23 | 2015-10-07 | F. Hoffmann-La Roche AG | Mglu2/3 antagonists for the treatment of autistic disorders |
| AU2015295300B2 (en) * | 2014-08-01 | 2019-05-02 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mGluR2 receptors |
-
2015
- 2015-07-27 JO JOP/2015/0178A patent/JO3601B1/ar active
- 2015-07-30 BR BR112017001998A patent/BR112017001998A2/pt not_active Application Discontinuation
- 2015-07-30 MX MX2017001453A patent/MX2017001453A/es active IP Right Grant
- 2015-07-30 CA CA2954218A patent/CA2954218C/en active Active
- 2015-07-30 JP JP2017505456A patent/JP6615864B2/ja not_active Expired - Fee Related
- 2015-07-30 CN CN201580041306.4A patent/CN106573935B/zh active Active
- 2015-07-30 EP EP15742317.9A patent/EP3174880B1/en active Active
- 2015-07-30 AU AU2015295299A patent/AU2015295299B2/en active Active
- 2015-07-30 EA EA201692496A patent/EA031038B1/ru not_active IP Right Cessation
- 2015-07-30 ES ES15742317T patent/ES2702192T3/es active Active
- 2015-07-30 TW TW104124697A patent/TWI696625B/zh not_active IP Right Cessation
- 2015-07-30 US US15/500,553 patent/US10112949B2/en active Active
- 2015-07-30 WO PCT/EP2015/067533 patent/WO2016016381A1/en active Application Filing
- 2015-07-30 KR KR1020177005638A patent/KR102531693B1/ko active IP Right Grant
- 2015-07-31 AR ARP150102462A patent/AR101393A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR102531693B1 (ko) | 2023-05-10 |
| TW201609742A (zh) | 2016-03-16 |
| ES2702192T3 (es) | 2019-02-27 |
| BR112017001998A2 (pt) | 2017-12-12 |
| JP2017523201A (ja) | 2017-08-17 |
| US10112949B2 (en) | 2018-10-30 |
| EP3174880B1 (en) | 2018-09-26 |
| EA201692496A1 (ru) | 2017-06-30 |
| MX2017001453A (es) | 2017-05-11 |
| EP3174880A1 (en) | 2017-06-07 |
| WO2016016381A1 (en) | 2016-02-04 |
| CA2954218C (en) | 2022-11-29 |
| EA031038B1 (ru) | 2018-11-30 |
| CN106573935B (zh) | 2020-01-17 |
| JP6615864B2 (ja) | 2019-12-04 |
| TWI696625B (zh) | 2020-06-21 |
| US20180222908A1 (en) | 2018-08-09 |
| CA2954218A1 (en) | 2016-02-04 |
| CN106573935A (zh) | 2017-04-19 |
| JO3601B1 (ar) | 2020-07-05 |
| AU2015295299B2 (en) | 2019-05-02 |
| AU2015295299A1 (en) | 2017-01-19 |
| KR20170032464A (ko) | 2017-03-22 |
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