CA2954218C - 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors - Google Patents

6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors Download PDF

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Publication number
CA2954218C
CA2954218C CA2954218A CA2954218A CA2954218C CA 2954218 C CA2954218 C CA 2954218C CA 2954218 A CA2954218 A CA 2954218A CA 2954218 A CA2954218 A CA 2954218A CA 2954218 C CA2954218 C CA 2954218C
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disorder
compound
disorders
4alkyl
formula
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CA2954218A
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English (en)
French (fr)
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CA2954218A1 (en
Inventor
Jose Ignacio Andres-Gil
Michiel Luc Maria Van Gool
Andres Avelino Trabanco-Suarez
Ana Isabel De Lucas Olivares
Sergio-Alvar Alonso-De Diego
Oscar Delgado-Gonzalez
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Janssen Pharmaceutica NV
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Janssen Pharmaceutica NV
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    • 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

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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2954218A 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 Active CA2954218C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14179599 2014-08-01
EP14179599.7 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 (2)

Publication Number Publication Date
CA2954218A1 CA2954218A1 (en) 2016-02-04
CA2954218C true CA2954218C (en) 2022-11-29

Family

ID=51257438

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2954218A Active CA2954218C (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

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)

* 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
RU2711382C2 (ru) * 2014-12-03 2020-01-16 Янссен Фармацевтика Нв 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4(5H)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2
EP3226915B1 (en) 2014-12-03 2019-02-20 Janssen Pharmaceutica NV Radiolabelled mglur2 pet ligands
JP6929285B2 (ja) 2015-12-18 2021-09-01 ヤンセン ファーマシューティカ エヌ.ベー. 放射性標識mGluR2/3PETリガンド
RS60981B1 (sr) 2015-12-18 2020-11-30 Janssen Pharmaceutica Nv Radiooznačeni mglur2/3 pet ligandi
WO2019103070A1 (ja) 2017-11-24 2019-05-31 大日本住友製薬株式会社 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
WO2006099972A1 (en) * 2005-03-23 2006-09-28 F. Hoffmann-La Roche Ag Acetylenyl-pyrazolo-pvrimidine derivatives as mglur2 antagonists
CN102439008B (zh) 2009-05-12 2015-04-29 杨森制药有限公司 1,2,4-三唑并[4,3-a]吡啶衍生物及其用于治疗或预防神经和精神病症的用途
JP2013545822A (ja) * 2010-12-17 2013-12-26 ヴァンダービルト ユニバーシティー mGluR5受容体のアロステリック調節剤としての、二環式トリアゾールラクタムおよびピラゾールラクタム
WO2012172093A1 (en) * 2011-06-17 2012-12-20 Merz Pharma Gmbh & Co. Kgaa Dihydroindolizine derivate as metabotropic glutamate receptor modulators
IN2014CN03234A (enExample) 2011-11-03 2015-07-03 Merck Sharp & Dohme
EP2666775A1 (en) 2012-05-21 2013-11-27 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
US20130345205A1 (en) * 2012-06-20 2013-12-26 Vanderbilt University Substituted bicyclic aralkyl pyrazole lactam analogs as allosteric modulators of mglur5 receptors
US20130345204A1 (en) * 2012-06-20 2013-12-26 Vanderbilt University Substituted bicyclic cycloalkyl pyrazole lactam analogs 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
CN104736140A (zh) 2012-10-23 2015-06-24 霍夫曼-拉罗奇有限公司 用于治疗自闭症的mGlu2/3拮抗剂
CA2954091C (en) * 2014-08-01 2022-08-02 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors

Also Published As

Publication number Publication date
CN106573935B (zh) 2020-01-17
JP6615864B2 (ja) 2019-12-04
CA2954218A1 (en) 2016-02-04
US20180222908A1 (en) 2018-08-09
ES2702192T3 (es) 2019-02-27
JO3601B1 (ar) 2020-07-05
US10112949B2 (en) 2018-10-30
KR102531693B1 (ko) 2023-05-10
WO2016016381A1 (en) 2016-02-04
EA201692496A1 (ru) 2017-06-30
CN106573935A (zh) 2017-04-19
MX2017001453A (es) 2017-05-11
AR101393A1 (es) 2016-12-14
EP3174880B1 (en) 2018-09-26
EA031038B1 (ru) 2018-11-30
BR112017001998A2 (pt) 2017-12-12
AU2015295299A1 (en) 2017-01-19
EP3174880A1 (en) 2017-06-07
TW201609742A (zh) 2016-03-16
JP2017523201A (ja) 2017-08-17
KR20170032464A (ko) 2017-03-22
AU2015295299B2 (en) 2019-05-02
TWI696625B (zh) 2020-06-21

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