CN107018661B - 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途 - Google Patents

6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途 Download PDF

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CN107018661B
CN107018661B CN201580041302.6A CN201580041302A CN107018661B CN 107018661 B CN107018661 B CN 107018661B CN 201580041302 A CN201580041302 A CN 201580041302A CN 107018661 B CN107018661 B CN 107018661B
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CN107018661A (zh
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S.康德-赛德
M.L.M.范戈尔
M.L.马丁-马丁
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Janssen Pharmaceutica NV
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    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN201580041302.6A 2014-08-01 2015-07-30 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途 Expired - Fee Related CN107018661B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP14179601.1 2014-08-01
EP14179601 2014-08-01
PCT/EP2015/067534 WO2016016382A1 (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
CN107018661A CN107018661A (zh) 2017-08-04
CN107018661B true CN107018661B (zh) 2020-01-03

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CN201580041302.6A Expired - Fee Related CN107018661B (zh) 2014-08-01 2015-07-30 6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其作为MGLUR2受体的负向别构调节剂的用途

Country Status (9)

Country Link
US (3) US10220032B2 (2)
EP (1) EP3174882B1 (2)
JP (1) JP6517340B2 (2)
CN (1) CN107018661B (2)
AU (1) AU2015295300B2 (2)
CA (1) CA2954091C (2)
ES (1) ES2707525T3 (2)
RU (1) RU2708391C2 (2)
WO (1) WO2016016382A1 (2)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2015295301B2 (en) * 2014-08-01 2019-05-09 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo[1,5-alpha]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
JO3601B1 (ar) * 2014-08-01 2020-07-05 Janssen Pharmaceutica Nv مركبات 6 ، 7 ثاني هيدرو بيرازولو [ 1، 5 الفا ] بيرازين – 4 (5 يد) – اون واستخدامها كمنظمات الوسترية سلبية لمستقبلات ملجور 2
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
JP7266010B2 (ja) 2019-05-30 2023-04-27 住友ファーマ株式会社 6,7-ジヒドロピラゾロ[1,5-a]ピラジノン誘導体又はその塩を含有する医薬

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
EP2666775A1 (en) * 2012-05-21 2013-11-27 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
WO2013192350A1 (en) * 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic aralkyl 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

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US7329662B2 (en) * 2003-10-03 2008-02-12 Hoffmann-La Roche Inc. Pyrazolo-pyridine
JP5048675B2 (ja) * 2005-09-27 2012-10-17 エフ.ホフマン−ラ ロシュ アーゲー mGluR2アンタゴニストとしてのオキサジアゾリルピラゾロ−ピリミジン類
GB0625827D0 (en) * 2006-12-22 2007-02-07 Astex Therapeutics Ltd New compounds
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
MX2013000103A (es) * 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
IN2014CN03234A (2) 2011-11-03 2015-07-03 Merck Sharp & Dohme
US20130345204A1 (en) 2012-06-20 2013-12-26 Vanderbilt University Substituted bicyclic cycloalkyl pyrazole lactam 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

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
EP2666775A1 (en) * 2012-05-21 2013-11-27 Domain Therapeutics Substituted pyrazoloquinazolinones and pyrroloquinazolinones as allosteric modulators of group II metabotropic glutamate receptors
WO2013192350A1 (en) * 2012-06-20 2013-12-27 Vanderbilt University Substituted bicyclic aralkyl 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

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Publication number Publication date
US20190160061A1 (en) 2019-05-30
EP3174882A1 (en) 2017-06-07
US10668065B2 (en) 2020-06-02
CN107018661A (zh) 2017-08-04
RU2708391C2 (ru) 2019-12-06
RU2017106489A3 (2) 2019-01-28
AU2015295300B2 (en) 2019-05-02
JP2017528515A (ja) 2017-09-28
AU2015295300A1 (en) 2017-01-12
ES2707525T3 (es) 2019-04-03
US10220032B2 (en) 2019-03-05
JP6517340B2 (ja) 2019-05-22
EP3174882B1 (en) 2018-11-07
US20170273976A1 (en) 2017-09-28
RU2017106489A (ru) 2018-09-04
WO2016016382A1 (en) 2016-02-04
US20200261450A1 (en) 2020-08-20
CA2954091C (en) 2022-08-02
CA2954091A1 (en) 2016-02-04

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