CN107001375B - 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 PDFInfo
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- CN107001375B CN107001375B CN201580065918.7A CN201580065918A CN107001375B CN 107001375 B CN107001375 B CN 107001375B CN 201580065918 A CN201580065918 A CN 201580065918A CN 107001375 B CN107001375 B CN 107001375B
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- 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
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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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- 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
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- 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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- 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
- A61P25/32—Alcohol-abuse
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- 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
- A61P25/34—Tobacco-abuse
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- 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
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Addiction (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychology (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14196082.3 | 2014-12-03 | ||
| EP14196082 | 2014-12-03 | ||
| PCT/EP2015/078285 WO2016087487A1 (en) | 2014-12-03 | 2015-12-02 | 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 |
|---|---|
| CN107001375A CN107001375A (zh) | 2017-08-01 |
| CN107001375B true CN107001375B (zh) | 2020-06-09 |
Family
ID=52002818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580065918.7A Expired - Fee Related CN107001375B (zh) | 2014-12-03 | 2015-12-02 | 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 (1) | US10072014B2 (enExample) |
| EP (1) | EP3227295B1 (enExample) |
| JP (1) | JP6689856B2 (enExample) |
| CN (1) | CN107001375B (enExample) |
| AU (1) | AU2015357167B2 (enExample) |
| CA (1) | CA2967153A1 (enExample) |
| ES (1) | ES2727379T3 (enExample) |
| RU (1) | RU2711382C2 (enExample) |
| WO (1) | WO2016087487A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| ES2727379T3 (es) | 2014-12-03 | 2019-10-15 | Janssen Pharmaceutica Nv | Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona y su uso como moduladores alostéricos negativos de receptores de mGlu2 |
| EP3226915B1 (en) | 2014-12-03 | 2019-02-20 | Janssen Pharmaceutica NV | Radiolabelled mglur2 pet ligands |
| ES2820823T3 (es) | 2015-12-18 | 2021-04-22 | Janssen Pharmaceutica Nv | Ligandos PET mGluR2/3 radiomarcados |
| HRP20201372T1 (hr) | 2015-12-18 | 2020-11-27 | Janssen Pharmaceutica Nv | Radioaktivno označeni pet mglur2/3 ligandi |
| US11129906B1 (en) | 2016-12-07 | 2021-09-28 | David Gordon Bermudes | Chimeric protein toxins for expression by therapeutic bacteria |
| UY37557A (es) | 2017-01-10 | 2018-07-31 | Bayer Ag | Derivados heterocíclicos como pesticidas |
| AU2018207776B2 (en) | 2017-01-10 | 2021-06-17 | Bayer Aktiengesellschaft | Heterocyclene derivatives as pest control agents |
| 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 |
| 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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2012083224A1 (en) * | 2010-12-17 | 2012-06-21 | Vanderbilt University | Bicyclic triazole and pyrazole lactams as allosteric modulators of mglur5 receptors |
| WO2013066736A1 (en) * | 2011-11-03 | 2013-05-10 | Merck Sharp & Dohme Corp. | QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| 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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| US6482821B2 (en) | 1996-12-20 | 2002-11-19 | Hoechst Aktiengellschaft | Vitronectin receptor antagonists, their preparation and their use |
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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 |
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| 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 |
| JO3368B1 (ar) | 2013-06-04 | 2019-03-13 | Janssen Pharmaceutica Nv | مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2 |
| FR3024461B1 (fr) | 2014-07-31 | 2017-12-29 | Total Marketing Services | Compositions lubrifiantes pour vehicule a moteur |
| JP6517340B2 (ja) * | 2014-08-01 | 2019-05-22 | ヤンセン ファーマシューティカ エヌ.ベー. | 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 |
| CA2954222C (en) | 2014-08-01 | 2022-11-29 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglur2 receptors |
| 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 |
| 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 |
| 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 |
| ES2727379T3 (es) | 2014-12-03 | 2019-10-15 | Janssen Pharmaceutica Nv | Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona y su uso como moduladores alostéricos negativos de receptores de mGlu2 |
| EP3226915B1 (en) | 2014-12-03 | 2019-02-20 | Janssen Pharmaceutica NV | Radiolabelled mglur2 pet ligands |
| ES2820823T3 (es) | 2015-12-18 | 2021-04-22 | Janssen Pharmaceutica Nv | Ligandos PET mGluR2/3 radiomarcados |
| HRP20201372T1 (hr) | 2015-12-18 | 2020-11-27 | Janssen Pharmaceutica Nv | Radioaktivno označeni pet mglur2/3 ligandi |
-
2015
- 2015-12-02 ES ES15802148T patent/ES2727379T3/es active Active
- 2015-12-02 RU RU2017123038A patent/RU2711382C2/ru active
- 2015-12-02 US US15/533,308 patent/US10072014B2/en active Active
- 2015-12-02 EP EP15802148.5A patent/EP3227295B1/en active Active
- 2015-12-02 CA CA2967153A patent/CA2967153A1/en active Pending
- 2015-12-02 CN CN201580065918.7A patent/CN107001375B/zh not_active Expired - Fee Related
- 2015-12-02 WO PCT/EP2015/078285 patent/WO2016087487A1/en not_active Ceased
- 2015-12-02 JP JP2017529629A patent/JP6689856B2/ja not_active Expired - Fee Related
- 2015-12-02 AU AU2015357167A patent/AU2015357167B2/en not_active Ceased
Patent Citations (3)
| 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 |
| WO2013066736A1 (en) * | 2011-11-03 | 2013-05-10 | Merck Sharp & Dohme Corp. | QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE |
| 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 |
|---|---|
| RU2711382C2 (ru) | 2020-01-16 |
| CA2967153A1 (en) | 2016-06-09 |
| RU2017123038A (ru) | 2019-01-09 |
| RU2017123038A3 (enExample) | 2019-07-17 |
| ES2727379T3 (es) | 2019-10-15 |
| WO2016087487A1 (en) | 2016-06-09 |
| CN107001375A (zh) | 2017-08-01 |
| EP3227295B1 (en) | 2019-02-20 |
| US20170369493A1 (en) | 2017-12-28 |
| JP6689856B2 (ja) | 2020-04-28 |
| US10072014B2 (en) | 2018-09-11 |
| AU2015357167A1 (en) | 2017-05-25 |
| JP2017536399A (ja) | 2017-12-07 |
| AU2015357167B2 (en) | 2020-06-25 |
| EP3227295A1 (en) | 2017-10-11 |
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