TWI696625B - 6,7-二氫吡唑並[1,5-α]吡-4(5H)-酮化合物及其作為MGLUR2受體的負性別構調節物之用途 - Google Patents

6,7-二氫吡唑並[1,5-α]吡-4(5H)-酮化合物及其作為MGLUR2受體的負性別構調節物之用途 Download PDF

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Publication number
TWI696625B
TWI696625B TW104124697A TW104124697A TWI696625B TW I696625 B TWI696625 B TW I696625B TW 104124697 A TW104124697 A TW 104124697A TW 104124697 A TW104124697 A TW 104124697A TW I696625 B TWI696625 B TW I696625B
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Taiwan
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disorders
alkyl
compound
pharmaceutically acceptable
acceptable salt
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TW104124697A
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English (en)
Chinese (zh)
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TW201609742A (zh
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荷西 安傑斯吉爾
米契爾 凡古
安傑斯 特拉班可蘇芮茲
安娜 得盧卡斯奧利維斯
薩吉歐艾維 艾隆索德迪哥
奧斯卡 德蓋多岡賽茲
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比利時商健生藥品公司
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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
    • 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

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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)
  • 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)
TW104124697A 2014-08-01 2015-07-30 6,7-二氫吡唑並[1,5-α]吡-4(5H)-酮化合物及其作為MGLUR2受體的負性別構調節物之用途 TWI696625B (zh)

Applications Claiming Priority (2)

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

Publications (2)

Publication Number Publication Date
TW201609742A TW201609742A (zh) 2016-03-16
TWI696625B true TWI696625B (zh) 2020-06-21

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TW104124697A TWI696625B (zh) 2014-08-01 2015-07-30 6,7-二氫吡唑並[1,5-α]吡-4(5H)-酮化合物及其作為MGLUR2受體的負性別構調節物之用途

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
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
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 (2)

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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

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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
PT1863818E (pt) * 2005-03-23 2010-04-09 Hoffmann La Roche Derivados de acetilenil-pirazolo-pirimidina como antagonistas de mglur2
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
EP2651222A4 (en) * 2010-12-17 2014-04-30 Univ Vanderbilt BICYCLIC TRIAZOL AND PYRAZOLLACTAME 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
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
BR112014031896A2 (pt) * 2012-06-20 2017-06-27 Univ Vanderbilt composto, composição farmacêutica, e, método para o tratamento de um distúrbio
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
MX2017001453A (es) 2017-05-11
CN106573935A (zh) 2017-04-19
EA031038B1 (ru) 2018-11-30
WO2016016381A1 (en) 2016-02-04
JP2017523201A (ja) 2017-08-17
ES2702192T3 (es) 2019-02-27
AU2015295299B2 (en) 2019-05-02
CA2954218A1 (en) 2016-02-04
US10112949B2 (en) 2018-10-30
EP3174880A1 (en) 2017-06-07
TW201609742A (zh) 2016-03-16
JO3601B1 (ar) 2020-07-05
EA201692496A1 (ru) 2017-06-30
AR101393A1 (es) 2016-12-14
JP6615864B2 (ja) 2019-12-04
KR102531693B1 (ko) 2023-05-10
EP3174880B1 (en) 2018-09-26
AU2015295299A1 (en) 2017-01-19
CA2954218C (en) 2022-11-29
KR20170032464A (ko) 2017-03-22
CN106573935B (zh) 2020-01-17
BR112017001998A2 (pt) 2017-12-12
US20180222908A1 (en) 2018-08-09

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