AU2015295301B2 - 6,7-dihydropyrazolo[1,5-alpha]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors - Google Patents

6,7-dihydropyrazolo[1,5-alpha]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors Download PDF

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Publication number
AU2015295301B2
AU2015295301B2 AU2015295301A AU2015295301A AU2015295301B2 AU 2015295301 B2 AU2015295301 B2 AU 2015295301B2 AU 2015295301 A AU2015295301 A AU 2015295301A AU 2015295301 A AU2015295301 A AU 2015295301A AU 2015295301 B2 AU2015295301 B2 AU 2015295301B2
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4alkyl
disorders
disorder
group
compound
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AU2015295301A1 (en
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Susana Conde-Ceide
Maria Luz Martin-Martin
Michiel Luc Maria Van Gool
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2015295301A 2014-08-01 2015-07-30 6,7-dihydropyrazolo[1,5-alpha]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors Ceased AU2015295301B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14179602 2014-08-01
EP14179602.9 2014-08-01
PCT/EP2015/067538 WO2016016383A1 (en) 2014-08-01 2015-07-30 6,7-DIHYDROPYRAZOLO[1,5-α]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS

Publications (2)

Publication Number Publication Date
AU2015295301A1 AU2015295301A1 (en) 2017-01-19
AU2015295301B2 true AU2015295301B2 (en) 2019-05-09

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Family Applications (1)

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AU2015295301A Ceased AU2015295301B2 (en) 2014-08-01 2015-07-30 6,7-dihydropyrazolo[1,5-alpha]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors

Country Status (9)

Country Link
US (1) US10017514B2 (enExample)
EP (1) EP3174884B1 (enExample)
JP (1) JP6661605B2 (enExample)
CN (1) CN107001373B (enExample)
AU (1) AU2015295301B2 (enExample)
CA (1) CA2954222C (enExample)
ES (1) ES2702194T3 (enExample)
RU (1) RU2696135C2 (enExample)
WO (1) WO2016016383A1 (enExample)

Families Citing this family (9)

* 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
RS60981B1 (sr) 2015-12-18 2020-11-30 Janssen Pharmaceutica Nv Radiooznačeni mglur2/3 pet ligandi
EA037941B1 (ru) 2015-12-18 2021-06-09 Янссен Фармацевтика Нв ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ
US9849817B2 (en) 2016-03-16 2017-12-26 Ford Global Technologies, Llc Composite seat structure
JP6904425B2 (ja) 2017-09-13 2021-07-14 日本電気株式会社 リチウムイオン二次電池
MY201041A (en) * 2017-11-24 2024-01-31 Sumitomo Pharma Co Ltd Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group ii metabotropic glutamate receptor

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012083224A1 (en) * 2010-12-17 2012-06-21 Vanderbilt University Bicyclic triazole and pyrazole lactams as allosteric modulators of mglur5 receptors
WO2013192343A1 (en) * 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors
WO2013192347A1 (en) * 2012-06-20 2013-12-27 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

Family Cites Families (6)

* 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
HRP20131122T1 (hr) * 2009-05-12 2013-12-20 Janssen Pharmaceuticals, Inc. Derivati 1,2,4-triazolo[4,3-a] piridina i njihova uporaba u lijeäśenju ili prevenciji neuroloških i psihijatrijskih poremeä†aja
US9278960B2 (en) 2011-11-03 2016-03-08 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
HK1206615A1 (en) 2012-10-23 2016-01-15 霍夫曼-拉罗奇有限公司 Mglu2/3 antagonists for the treatment of autistic disorders
RU2708391C2 (ru) * 2014-08-01 2019-12-06 Янссен Фармацевтика Нв 6,7-дигидропиразоло[1,5-а]пиразин-4(5h)-оновые соединения и их применение в качестве отрицательных аллостерических модуляторов рецепторов mglur2

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012083224A1 (en) * 2010-12-17 2012-06-21 Vanderbilt University Bicyclic triazole and pyrazole lactams as allosteric modulators of mglur5 receptors
WO2013192343A1 (en) * 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors
WO2013192347A1 (en) * 2012-06-20 2013-12-27 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

Also Published As

Publication number Publication date
WO2016016383A1 (en) 2016-02-04
EP3174884B1 (en) 2018-09-26
RU2017106100A3 (enExample) 2019-02-21
EP3174884A1 (en) 2017-06-07
ES2702194T3 (es) 2019-02-27
AU2015295301A1 (en) 2017-01-19
CN107001373B (zh) 2020-01-07
RU2696135C2 (ru) 2019-07-31
CA2954222C (en) 2022-11-29
CA2954222A1 (en) 2016-02-04
US20170267682A1 (en) 2017-09-21
CN107001373A (zh) 2017-08-01
RU2017106100A (ru) 2018-09-03
US10017514B2 (en) 2018-07-10
JP2017523202A (ja) 2017-08-17
JP6661605B2 (ja) 2020-03-11

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