BR112017001998A2 - compostos 6,7-di-hidropirazolo[1,5-a]pirazin-4(5h)-ona e seu uso como moduladores alostéricos negativos de receptores mglur2 - Google Patents
compostos 6,7-di-hidropirazolo[1,5-a]pirazin-4(5h)-ona e seu uso como moduladores alostéricos negativos de receptores mglur2Info
- Publication number
- BR112017001998A2 BR112017001998A2 BR112017001998A BR112017001998A BR112017001998A2 BR 112017001998 A2 BR112017001998 A2 BR 112017001998A2 BR 112017001998 A BR112017001998 A BR 112017001998A BR 112017001998 A BR112017001998 A BR 112017001998A BR 112017001998 A2 BR112017001998 A2 BR 112017001998A2
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- dihydropyrazolo
- pyrazin
- allosteric modulators
- negative allosteric
- Prior art date
Links
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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Neurosurgery (AREA)
- Neurology (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
a presente invenção refere-se a novos derivados da 6,7-di-hidropirazolo[1,5-a]pirazin-4(5h)-ona como moduladores alostéricos negativos (nams) do receptor metabotrópico do glutamato do subtipo 2 ("mglur2"). a invenção está também dirigida a composições farmacêuticas compreendendo tais compostos, a processos para preparação de tais compostos e composições, e ao uso de tais compostos e composições para a prevenção ou o tratamento de distúrbios nos quais o subtipo mglur2 de receptores metabotrópicos está envolvido.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP14179599 | 2014-08-01 | ||
PCT/EP2015/067533 WO2016016381A1 (en) | 2014-08-01 | 2015-07-30 | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112017001998A2 true BR112017001998A2 (pt) | 2017-12-12 |
Family
ID=51257438
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017001998A BR112017001998A2 (pt) | 2014-08-01 | 2015-07-30 | compostos 6,7-di-hidropirazolo[1,5-a]pirazin-4(5h)-ona e seu uso como moduladores alostéricos negativos de receptores mglur2 |
Country Status (15)
Country | Link |
---|---|
US (1) | US10112949B2 (pt) |
EP (1) | EP3174880B1 (pt) |
JP (1) | JP6615864B2 (pt) |
KR (1) | KR102531693B1 (pt) |
CN (1) | CN106573935B (pt) |
AR (1) | AR101393A1 (pt) |
AU (1) | AU2015295299B2 (pt) |
BR (1) | BR112017001998A2 (pt) |
CA (1) | CA2954218C (pt) |
EA (1) | EA031038B1 (pt) |
ES (1) | ES2702192T3 (pt) |
JO (1) | JO3601B1 (pt) |
MX (1) | MX2017001453A (pt) |
TW (1) | TWI696625B (pt) |
WO (1) | WO2016016381A1 (pt) |
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 |
AU2015357169B2 (en) | 2014-12-03 | 2021-03-04 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
EP3227295B1 (en) * | 2014-12-03 | 2019-02-20 | Janssen Pharmaceutica NV | 6,7-dihydropyrazolo[1,5- ]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors |
EP3389727B1 (en) * | 2015-12-18 | 2020-08-12 | Janssen Pharmaceutica NV | Radiolabelled mglur2/3 pet ligands |
CA3003962A1 (en) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Radiolabelled mglur2/3 pet ligands |
JP7242548B2 (ja) | 2017-11-24 | 2023-03-20 | 住友ファーマ株式会社 | 6,7-ジヒドロピラゾロ[1,5-a]ピラジノン誘導体及びその医薬用途 |
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 |
RU2412943C2 (ru) * | 2005-03-23 | 2011-02-27 | Ф. Хоффманн-Ля Рош Аг | ПРОИЗВОДНЫЕ АЦЕТИЛЕНИЛ-ПИРАЗОЛО-ПИРИМИДИНА В КАЧЕСТВЕ АНТАГОНИСТОВ mGluR2 |
RS53075B (en) | 2009-05-12 | 2014-04-30 | Janssen Pharmaceuticals Inc. | 1,2,4-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THEIR USE IN 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 |
CN104010504B (zh) | 2011-11-03 | 2016-04-06 | 默沙东公司 | 作为mGluR2负变构调节剂的喹啉甲酰胺和喹啉甲腈的衍生物、组合物、及其用途 |
EP2666775A1 (en) | 2012-05-21 | 2013-11-27 | Domain Therapeutics | Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors |
CN104736156A (zh) * | 2012-06-20 | 2015-06-24 | 范德比尔特大学 | 作为mglur5受体变构调节剂的取代的双环烷氧基吡唑类似物 |
US20130345204A1 (en) * | 2012-06-20 | 2013-12-26 | Vanderbilt University | Substituted bicyclic cycloalkyl pyrazole lactam 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 |
WO2016016382A1 (en) * | 2014-08-01 | 2016-02-04 | 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 CN CN201580041306.4A patent/CN106573935B/zh active Active
- 2015-07-30 CA CA2954218A patent/CA2954218C/en active Active
- 2015-07-30 TW TW104124697A patent/TWI696625B/zh not_active IP Right Cessation
- 2015-07-30 MX MX2017001453A patent/MX2017001453A/es active IP Right Grant
- 2015-07-30 EA EA201692496A patent/EA031038B1/ru not_active IP Right Cessation
- 2015-07-30 EP EP15742317.9A patent/EP3174880B1/en active Active
- 2015-07-30 AU AU2015295299A patent/AU2015295299B2/en active Active
- 2015-07-30 BR BR112017001998A patent/BR112017001998A2/pt not_active Application Discontinuation
- 2015-07-30 US US15/500,553 patent/US10112949B2/en active Active
- 2015-07-30 ES ES15742317T patent/ES2702192T3/es active Active
- 2015-07-30 KR KR1020177005638A patent/KR102531693B1/ko active IP Right Grant
- 2015-07-30 JP JP2017505456A patent/JP6615864B2/ja active Active
- 2015-07-30 WO PCT/EP2015/067533 patent/WO2016016381A1/en active Application Filing
- 2015-07-31 AR ARP150102462A patent/AR101393A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
TW201609742A (zh) | 2016-03-16 |
CN106573935A (zh) | 2017-04-19 |
JP6615864B2 (ja) | 2019-12-04 |
AU2015295299B2 (en) | 2019-05-02 |
AR101393A1 (es) | 2016-12-14 |
MX2017001453A (es) | 2017-05-11 |
EP3174880B1 (en) | 2018-09-26 |
US10112949B2 (en) | 2018-10-30 |
KR102531693B1 (ko) | 2023-05-10 |
US20180222908A1 (en) | 2018-08-09 |
EA201692496A1 (ru) | 2017-06-30 |
CA2954218A1 (en) | 2016-02-04 |
ES2702192T3 (es) | 2019-02-27 |
EP3174880A1 (en) | 2017-06-07 |
CA2954218C (en) | 2022-11-29 |
JO3601B1 (ar) | 2020-07-05 |
WO2016016381A1 (en) | 2016-02-04 |
EA031038B1 (ru) | 2018-11-30 |
CN106573935B (zh) | 2020-01-17 |
JP2017523201A (ja) | 2017-08-17 |
TWI696625B (zh) | 2020-06-21 |
KR20170032464A (ko) | 2017-03-22 |
AU2015295299A1 (en) | 2017-01-19 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
B11B | Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements |