PH12017500170B1 - 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors - Google Patents
6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptorsInfo
- Publication number
- PH12017500170B1 PH12017500170B1 PH12017500170A PH12017500170A PH12017500170B1 PH 12017500170 B1 PH12017500170 B1 PH 12017500170B1 PH 12017500170 A PH12017500170 A PH 12017500170A PH 12017500170 A PH12017500170 A PH 12017500170A PH 12017500170 B1 PH12017500170 B1 PH 12017500170B1
- Authority
- PH
- Philippines
- Prior art keywords
- compounds
- dihydropyrazolo
- pyrazin
- allosteric modulators
- negative allosteric
- Prior art date
Links
- 229940126662 negative allosteric modulator Drugs 0.000 title abstract 3
- GLQXAHBYDJPCHG-UHFFFAOYSA-N 6,7-dihydro-5h-pyrazolo[1,5-a]pyrazin-4-one Chemical class O=C1NCCN2N=CC=C12 GLQXAHBYDJPCHG-UHFFFAOYSA-N 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102100036837 Metabotropic glutamate receptor 2 Human genes 0.000 abstract 2
- 108010038421 metabotropic glutamate receptor 2 Proteins 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 abstract 1
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 102000006239 metabotropic receptors Human genes 0.000 abstract 1
- 108020004083 metabotropic receptors Proteins 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
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
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Dispersion Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Addiction (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14179600 | 2014-08-01 | ||
| EP14196083 | 2014-12-03 | ||
| PCT/EP2015/067572 WO2016016395A1 (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 |
|---|---|
| PH12017500170A1 PH12017500170A1 (en) | 2017-07-10 |
| PH12017500170B1 true PH12017500170B1 (en) | 2017-07-10 |
Family
ID=53765202
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12017500170A PH12017500170B1 (en) | 2014-08-01 | 2017-01-27 | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors |
Country Status (31)
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 |
| 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 |
| AU2016374568B2 (en) * | 2015-12-18 | 2020-08-27 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| AU2016374571B2 (en) | 2015-12-18 | 2021-05-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| JP2020011902A (ja) * | 2016-10-26 | 2020-01-23 | 大日本住友製薬株式会社 | 縮環ピロール誘導体およびその医薬用途 |
| CN111601811B (zh) | 2017-11-24 | 2023-05-05 | 住友制药株式会社 | 6,7-二氢吡唑并[1,5-a]吡嗪酮衍生物和其医药用途 |
| WO2024008909A1 (en) | 2022-07-08 | 2024-01-11 | Janssen Pharmaceutica Nv | Inhibitors of coronavirus |
| WO2025146502A1 (en) | 2024-01-05 | 2025-07-10 | Janssen Pharmaceutica Nv | Coronavirus inhibiting compounds |
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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 |
| RU2015101532A (ru) | 2012-06-20 | 2016-08-20 | Вандербилт Юниверсити | Замещенные бициклические алкокси-пиразольные аналоги в качестве аллостерических модуляторов рецепторов mglur5 |
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| 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 |
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| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| AU2015357169B2 (en) | 2014-12-03 | 2021-03-04 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| AU2016374571B2 (en) | 2015-12-18 | 2021-05-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
| AU2016374568B2 (en) | 2015-12-18 | 2020-08-27 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
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2015
- 2015-07-27 JO JOP/2015/0177A patent/JOP20150177B1/ar active
- 2015-07-30 WO PCT/EP2015/067572 patent/WO2016016395A1/en not_active Ceased
- 2015-07-30 EA EA201692544A patent/EA033052B1/ru unknown
- 2015-07-30 ME MEP-2019-9A patent/ME03341B/me unknown
- 2015-07-30 JP JP2017505447A patent/JP6609306B2/ja not_active Expired - Fee Related
- 2015-07-30 ES ES15744915T patent/ES2705425T3/es active Active
- 2015-07-30 EP EP15744915.8A patent/EP3174883B1/en active Active
- 2015-07-30 PL PL15744915T patent/PL3174883T3/pl unknown
- 2015-07-30 MX MX2017001454A patent/MX370182B/es active IP Right Grant
- 2015-07-30 SG SG11201700637WA patent/SG11201700637WA/en unknown
- 2015-07-30 TW TW104124698A patent/TWI688566B/zh not_active IP Right Cessation
- 2015-07-30 NZ NZ728025A patent/NZ728025A/en not_active IP Right Cessation
- 2015-07-30 KR KR1020177004410A patent/KR102531680B1/ko active Active
- 2015-07-30 HU HUE15744915A patent/HUE041777T2/hu unknown
- 2015-07-30 AU AU2015295313A patent/AU2015295313B2/en not_active Ceased
- 2015-07-30 SI SI201530532T patent/SI3174883T1/sl unknown
- 2015-07-30 BR BR112017001861A patent/BR112017001861A2/pt not_active Application Discontinuation
- 2015-07-30 CA CA2954094A patent/CA2954094C/en active Active
- 2015-07-30 SM SM20190013T patent/SMT201900013T1/it unknown
- 2015-07-30 CN CN201580041305.XA patent/CN107018662B/zh active Active
- 2015-07-30 DK DK15744915.8T patent/DK3174883T3/en active
- 2015-07-30 HR HRP20182114TT patent/HRP20182114T1/hr unknown
- 2015-07-30 LT LTEP15744915.8T patent/LT3174883T/lt unknown
- 2015-07-30 US US15/500,319 patent/US10005785B2/en active Active
- 2015-07-30 RS RS20190054A patent/RS58215B1/sr unknown
- 2015-07-30 PT PT15744915T patent/PT3174883T/pt unknown
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2017
- 2017-01-26 IL IL250303A patent/IL250303A0/en active IP Right Grant
- 2017-01-27 PH PH12017500170A patent/PH12017500170B1/en unknown
- 2017-01-31 ZA ZA2017/00758A patent/ZA201700758B/en unknown
- 2017-01-31 CL CL2017000249A patent/CL2017000249A1/es unknown
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2018
- 2018-05-10 US US15/976,223 patent/US10519162B2/en active Active
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2019
- 2019-01-15 CY CY191100040T patent/CY1121123T1/el unknown
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