JP6615864B2 - ６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用 - Google Patents
６，７−ジヒドロピラゾロ［１，５−ａ］ピラジン−４（５Ｈ）−オン化合物およびＭＧＬＵＲ２受容体の負のアロステリック調節因子としてのそれらの使用 Download PDFInfo
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- JP6615864B2 JP6615864B2 JP2017505456A JP2017505456A JP6615864B2 JP 6615864 B2 JP6615864 B2 JP 6615864B2 JP 2017505456 A JP2017505456 A JP 2017505456A JP 2017505456 A JP2017505456 A JP 2017505456A JP 6615864 B2 JP6615864 B2 JP 6615864B2
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- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 229940107700 pyruvic acid Drugs 0.000 description 1
- WDXARTMCIRVMAE-UHFFFAOYSA-N quinoline-2-carbonitrile Chemical class C1=CC=CC2=NC(C#N)=CC=C21 WDXARTMCIRVMAE-UHFFFAOYSA-N 0.000 description 1
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- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- PFUVRDFDKPNGAV-UHFFFAOYSA-N sodium peroxide Chemical compound [Na+].[Na+].[O-][O-] PFUVRDFDKPNGAV-UHFFFAOYSA-N 0.000 description 1
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 1
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Classifications
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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
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)
- 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)
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| 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 |
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| JP2017523201A JP2017523201A (ja) | 2017-08-17 |
| JP2017523201A5 JP2017523201A5 (enExample) | 2018-09-06 |
| JP6615864B2 true JP6615864B2 (ja) | 2019-12-04 |
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| 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)
| 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 |
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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 |
| 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 |
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2015
- 2015-07-27 JO JOP/2015/0178A patent/JO3601B1/ar active
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- 2015-07-30 JP JP2017505456A patent/JP6615864B2/ja not_active Expired - Fee Related
- 2015-07-30 MX MX2017001453A patent/MX2017001453A/es active IP Right Grant
- 2015-07-30 CA CA2954218A patent/CA2954218C/en active Active
- 2015-07-30 BR BR112017001998A patent/BR112017001998A2/pt not_active Application Discontinuation
- 2015-07-30 US US15/500,553 patent/US10112949B2/en active Active
- 2015-07-30 EP EP15742317.9A patent/EP3174880B1/en active Active
- 2015-07-30 EA EA201692496A patent/EA031038B1/ru not_active IP Right Cessation
- 2015-07-30 WO PCT/EP2015/067533 patent/WO2016016381A1/en not_active Ceased
- 2015-07-30 TW TW104124697A patent/TWI696625B/zh not_active IP Right Cessation
- 2015-07-30 CN CN201580041306.4A patent/CN106573935B/zh not_active Expired - Fee Related
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- 2015-07-30 ES ES15742317T patent/ES2702192T3/es active Active
- 2015-07-31 AR ARP150102462A patent/AR101393A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2954218C (en) | 2022-11-29 |
| CN106573935B (zh) | 2020-01-17 |
| 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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