ES2707525T3 - Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona y su uso como moduladores alostéricos negativos de receptores de mGlu2 - Google Patents
Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona y su uso como moduladores alostéricos negativos de receptores de mGlu2 Download PDFInfo
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- ES2707525T3 ES2707525T3 ES15744568T ES15744568T ES2707525T3 ES 2707525 T3 ES2707525 T3 ES 2707525T3 ES 15744568 T ES15744568 T ES 15744568T ES 15744568 T ES15744568 T ES 15744568T ES 2707525 T3 ES2707525 T3 ES 2707525T3
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- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 238000004611 spectroscopical analysis Methods 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008223 sterile water Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 235000000346 sugar Nutrition 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000002636 symptomatic treatment Methods 0.000 description 1
- 210000000225 synapse Anatomy 0.000 description 1
- 230000003956 synaptic plasticity Effects 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 238000001308 synthesis method Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 238000007910 systemic administration Methods 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 239000008399 tap water Substances 0.000 description 1
- 235000020679 tap water Nutrition 0.000 description 1
- LFKDJXLFVYVEFG-UHFFFAOYSA-N tert-butyl carbamate Chemical group CC(C)(C)OC(N)=O LFKDJXLFVYVEFG-UHFFFAOYSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- QKSQWQOAUQFORH-UHFFFAOYSA-N tert-butyl n-[(2-methylpropan-2-yl)oxycarbonylimino]carbamate Chemical compound CC(C)(C)OC(=O)N=NC(=O)OC(C)(C)C QKSQWQOAUQFORH-UHFFFAOYSA-N 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
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- 231100000027 toxicology Toxicity 0.000 description 1
- 230000009529 traumatic brain injury Effects 0.000 description 1
- 208000018726 traumatic encephalopathy Diseases 0.000 description 1
- PQDJYEQOELDLCP-UHFFFAOYSA-N trimethylsilane Chemical group C[SiH](C)C PQDJYEQOELDLCP-UHFFFAOYSA-N 0.000 description 1
- YFTHZRPMJXBUME-UHFFFAOYSA-N tripropylamine Chemical class CCCN(CCC)CCC YFTHZRPMJXBUME-UHFFFAOYSA-N 0.000 description 1
- 238000001851 vibrational circular dichroism spectroscopy Methods 0.000 description 1
- 235000012431 wafers Nutrition 0.000 description 1
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Classifications
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P25/24—Antidepressants
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic 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
- C07D261/08—Heterocyclic 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2707525T3 true ES2707525T3 (es) | 2019-04-03 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES15744568T Active ES2707525T3 (es) | 2014-08-01 | 2015-07-30 | Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5H)-ona y su uso como moduladores alostéricos negativos de receptores de mGlu2 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US10220032B2 (https=) |
| EP (1) | EP3174882B1 (https=) |
| JP (1) | JP6517340B2 (https=) |
| CN (1) | CN107018661B (https=) |
| AU (1) | AU2015295300B2 (https=) |
| CA (1) | CA2954091C (https=) |
| ES (1) | ES2707525T3 (https=) |
| RU (1) | RU2708391C2 (https=) |
| WO (1) | WO2016016382A1 (https=) |
Families Citing this family (10)
| 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 |
| 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 |
| CN107001373B (zh) * | 2014-08-01 | 2020-01-07 | 詹森药业有限公司 | 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 |
| 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 |
| AU2015357167B2 (en) * | 2014-12-03 | 2020-06-25 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo(1,5-alpha)pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors |
| JP6861154B2 (ja) | 2014-12-03 | 2021-04-21 | ヤンセン ファーマシューティカ エヌ．ベー． | 放射標識されたｍＧｌｕＲ２ ＰＥＴリガンド |
| EA037941B1 (ru) | 2015-12-18 | 2021-06-09 | Янссен Фармацевтика Нв | ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ |
| LT3389727T (lt) | 2015-12-18 | 2020-10-12 | Janssen Pharmaceutica Nv | Radioaktyviai pažymėti mglur2/3 pet ligandai |
| KR102688238B1 (ko) | 2017-11-24 | 2024-07-25 | 스미토모 파마 가부시키가이샤 | 6, 7-디히드로 피라졸로[1, 5-a]피라지논 유도체 및 그 의약 용도 |
| 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 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US7329662B2 (en) * | 2003-10-03 | 2008-02-12 | Hoffmann-La Roche Inc. | Pyrazolo-pyridine |
| AU2006298829B2 (en) * | 2005-09-27 | 2011-03-03 | F. Hoffmann-La Roche Ag | Oxadiazolyl pyrazolo-pyrimidines as mGluR2 antagonists |
| 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 |
| CA2803802A1 (en) * | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| WO2012083224A1 (en) * | 2010-12-17 | 2012-06-21 | Vanderbilt University | Bicyclic triazole and pyrazole lactams as allosteric modulators of mglur5 receptors |
| CN104010504B (zh) | 2011-11-03 | 2016-04-06 | 默沙东公司 | 作为mGluR2负变构调节剂的喹啉甲酰胺和喹啉甲腈的衍生物、组合物、及其用途 |
| 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 |
| 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 |
| EP2925292A1 (en) | 2012-10-23 | 2015-10-07 | F. Hoffmann-La Roche AG | Mglu2/3 antagonists for the treatment of autistic disorders |
-
2015
- 2015-07-30 WO PCT/EP2015/067534 patent/WO2016016382A1/en not_active Ceased
- 2015-07-30 CA CA2954091A patent/CA2954091C/en active Active
- 2015-07-30 AU AU2015295300A patent/AU2015295300B2/en not_active Ceased
- 2015-07-30 EP EP15744568.5A patent/EP3174882B1/en active Active
- 2015-07-30 US US15/500,234 patent/US10220032B2/en active Active
- 2015-07-30 JP JP2017526014A patent/JP6517340B2/ja not_active Expired - Fee Related
- 2015-07-30 RU RU2017106489A patent/RU2708391C2/ru active
- 2015-07-30 CN CN201580041302.6A patent/CN107018661B/zh not_active Expired - Fee Related
- 2015-07-30 ES ES15744568T patent/ES2707525T3/es active Active
-
2019
- 2019-01-31 US US16/263,731 patent/US10668065B2/en not_active Expired - Fee Related
-
2020
- 2020-05-04 US US16/865,685 patent/US20200261450A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2015295300B2 (en) | 2019-05-02 |
| AU2015295300A1 (en) | 2017-01-12 |
| CN107018661A (zh) | 2017-08-04 |
| CA2954091A1 (en) | 2016-02-04 |
| US10668065B2 (en) | 2020-06-02 |
| US20200261450A1 (en) | 2020-08-20 |
| CN107018661B (zh) | 2020-01-03 |
| RU2017106489A (ru) | 2018-09-04 |
| WO2016016382A1 (en) | 2016-02-04 |
| EP3174882B1 (en) | 2018-11-07 |
| RU2017106489A3 (https=) | 2019-01-28 |
| US20170273976A1 (en) | 2017-09-28 |
| US20190160061A1 (en) | 2019-05-30 |
| US10220032B2 (en) | 2019-03-05 |
| JP2017528515A (ja) | 2017-09-28 |
| RU2708391C2 (ru) | 2019-12-06 |
| CA2954091C (en) | 2022-08-02 |
| JP6517340B2 (ja) | 2019-05-22 |
| EP3174882A1 (en) | 2017-06-07 |
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