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 mglur2

Info

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
Application number
BR112017001998A
Other languages
English (en)
Inventor
Isabel De Lucas Olivares Ana
Avelino Trabanco-Suarez Andrés
Ignacio Andrés-Gil José
Luc Maria Van Gool Michiel
Alonso De Diego Sergio-Alvar
Delgado-González Óscar
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR112017001998A2 publication Critical patent/BR112017001998A2/pt

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/26Psychostimulants, 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.
BR112017001998A 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 BR112017001998A2 (pt)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

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

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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.

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