SMT201900038T1 - Composti di 6,7-diidropirazolo[1,5-a]pirazin-4(5h)-one e loro utilizzo come modulatori allosterici negativi di recettori mglu2 - Google Patents
Composti di 6,7-diidropirazolo[1,5-a]pirazin-4(5h)-one e loro utilizzo come modulatori allosterici negativi di recettori mglu2Info
- Publication number
- SMT201900038T1 SMT201900038T1 SM20190038T SMT201900038T SMT201900038T1 SM T201900038 T1 SMT201900038 T1 SM T201900038T1 SM 20190038 T SM20190038 T SM 20190038T SM T201900038 T SMT201900038 T SM T201900038T SM T201900038 T1 SMT201900038 T1 SM T201900038T1
- Authority
- SM
- San Marino
- Prior art keywords
- dihydropyrazolo
- pyrazin
- compounds
- allosteric modulators
- negative allosteric
- Prior art date
Links
- 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 1
- 229940126662 negative allosteric modulator Drugs 0.000 title 1
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
- A61K31/41—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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles 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
- A61K31/4985—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
- A61K31/505—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
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (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 |
|---|---|---|---|
| EP14179598 | 2014-08-01 | ||
| PCT/EP2015/067530 WO2016016380A1 (en) | 2014-08-01 | 2015-07-30 | 6,7-DIHYDROPYRAZOLO[1,5-α]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
| EP15750666.8A EP3177623B1 (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 mglu2 receptors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SMT201900038T1 true SMT201900038T1 (it) | 2019-02-28 |
Family
ID=51257437
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SM20190038T SMT201900038T1 (it) | 2014-08-01 | 2015-07-30 | Composti di 6,7-diidropirazolo[1,5-a]pirazin-4(5h)-one e loro utilizzo come modulatori allosterici negativi di recettori mglu2 |
Country Status (34)
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20191646T1 (hr) | 2014-01-21 | 2019-12-13 | Janssen Pharmaceutica Nv | Kombinacije koje sadržavaju pozitivne alosteričke modulatore ili ortosteričke agoniste metabotropnog glutamatergičnog receptora podtip 2 i njihova uporaba |
| CN109999033B (zh) | 2014-01-21 | 2022-12-23 | 詹森药业有限公司 | 包括代谢型谷氨酸能受体亚型2的正别构调节物或正位激动剂的组合及其用途 |
| 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 |
| 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 |
| 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 |
| US10967078B2 (en) | 2014-12-03 | 2021-04-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| HRP20201372T1 (hr) | 2015-12-18 | 2020-11-27 | Janssen Pharmaceutica Nv | Radioaktivno označeni pet mglur2/3 ligandi |
| AU2016374568B2 (en) | 2015-12-18 | 2020-08-27 | 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 |
| CN107298682B (zh) * | 2017-06-29 | 2019-03-01 | 天津药明康德新药开发有限公司 | 一种4,5,6,7-四氢吡唑并[1,5-a]吡嗪-2-甲酸乙酯的合成方法 |
| 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 |
| AU2019212093B2 (en) * | 2018-01-26 | 2024-05-30 | Recordati Industria Chimica E Farmaceutica S.P.A | Triazole, imidazole and pyrrole condensed piperazine derivatives and their use as modulators of mGlu5 receptors |
| GB201905721D0 (en) | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
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| US6482821B2 (en) | 1996-12-20 | 2002-11-19 | Hoechst Aktiengellschaft | Vitronectin receptor antagonists, their preparation and their use |
| US6754375B1 (en) | 1999-07-16 | 2004-06-22 | Packard Bioscience Company | Method and system for interactively developing at least one grid pattern and computer-readable storage medium having a program for executing the method |
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| US20130345204A1 (en) | 2012-06-20 | 2013-12-26 | Vanderbilt University | Substituted bicyclic cycloalkyl 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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| EP2925292A1 (en) * | 2012-10-23 | 2015-10-07 | F. Hoffmann-La Roche AG | Mglu2/3 antagonists for the treatment of autistic disorders |
| CN103772686B (zh) | 2012-10-26 | 2015-01-07 | 苏州雷纳药物研发有限公司 | 一种两亲性嵌段共聚物及其制备方法、以及该共聚物与抗肿瘤药物形成的胶束载药系统 |
| 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 |
| 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 |
| US10017514B2 (en) | 2014-08-01 | 2018-07-10 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-α]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors |
| 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 |
| 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 |
| 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 |
| US10967078B2 (en) | 2014-12-03 | 2021-04-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
| HRP20201372T1 (hr) | 2015-12-18 | 2020-11-27 | Janssen Pharmaceutica Nv | Radioaktivno označeni pet mglur2/3 ligandi |
| AU2016374568B2 (en) | 2015-12-18 | 2020-08-27 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2/3 PET ligands |
-
2015
- 2015-07-27 JO JOP/2015/0179A patent/JOP20150179B1/ar active
- 2015-07-30 CA CA2954093A patent/CA2954093C/en active Active
- 2015-07-30 EP EP15750666.8A patent/EP3177623B1/en active Active
- 2015-07-30 TW TW104124696A patent/TWI696624B/zh not_active IP Right Cessation
- 2015-07-30 HR HRP20181997TT patent/HRP20181997T1/hr unknown
- 2015-07-30 LT LTEP15750666.8T patent/LT3177623T/lt unknown
- 2015-07-30 SM SM20190038T patent/SMT201900038T1/it unknown
- 2015-07-30 SG SG11201700638YA patent/SG11201700638YA/en unknown
- 2015-07-30 JP JP2017504775A patent/JP6662846B2/ja not_active Expired - Fee Related
- 2015-07-30 RS RS20190115A patent/RS58279B1/sr unknown
- 2015-07-30 HU HUE15750666A patent/HUE042871T2/hu unknown
- 2015-07-30 US US15/500,600 patent/US10005786B2/en active Active
- 2015-07-30 CN CN201580041316.8A patent/CN106573936B/zh active Active
- 2015-07-30 AU AU2015295298A patent/AU2015295298B2/en not_active Ceased
- 2015-07-30 ES ES15750666T patent/ES2708215T3/es active Active
- 2015-07-30 MA MA39582A patent/MA39582B1/fr unknown
- 2015-07-30 MX MX2017001452A patent/MX376289B/es active IP Right Grant
- 2015-07-30 ME MEP-2019-24A patent/ME03320B/me unknown
- 2015-07-30 SI SI201530513T patent/SI3177623T1/sl unknown
- 2015-07-30 DK DK15750666.8T patent/DK3177623T3/en active
- 2015-07-30 BR BR112017001726A patent/BR112017001726A2/pt not_active Application Discontinuation
- 2015-07-30 PH PH1/2017/500161A patent/PH12017500161B1/en unknown
- 2015-07-30 PT PT15750666T patent/PT3177623T/pt unknown
- 2015-07-30 WO PCT/EP2015/067530 patent/WO2016016380A1/en not_active Ceased
- 2015-07-30 EA EA201692540A patent/EA031087B1/ru unknown
- 2015-07-30 PL PL15750666T patent/PL3177623T3/pl unknown
- 2015-07-30 NZ NZ728122A patent/NZ728122A/en not_active IP Right Cessation
- 2015-07-30 TR TR2019/01074T patent/TR201901074T4/tr unknown
- 2015-07-30 KR KR1020177005257A patent/KR102531689B1/ko active Active
- 2015-07-31 AR ARP150102461A patent/AR101392A1/es unknown
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2017
- 2017-01-25 CL CL2017000192A patent/CL2017000192A1/es unknown
- 2017-01-26 IL IL250298A patent/IL250298A0/en active IP Right Grant
- 2017-01-31 ZA ZA2017/00759A patent/ZA201700759B/en unknown
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2018
- 2018-05-10 US US15/976,037 patent/US10512646B2/en active Active
-
2019
- 2019-01-24 CY CY20191100101T patent/CY1121649T1/el unknown
- 2019-11-07 US US16/677,034 patent/US20200121677A1/en not_active Abandoned
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