MA39582B1 - Composés de 6,7-dihydropyrazolo [1,5-?]pyrazin -4 (5h)-one et leur utilisation en tant que modulateurs négatifs allostériques des récepteurs métabotropiques du glutamate - Google Patents
Composés de 6,7-dihydropyrazolo [1,5-?]pyrazin -4 (5h)-one et leur utilisation en tant que modulateurs négatifs allostériques des récepteurs métabotropiques du glutamateInfo
- Publication number
- MA39582B1 MA39582B1 MA39582A MA39582A MA39582B1 MA 39582 B1 MA39582 B1 MA 39582B1 MA 39582 A MA39582 A MA 39582A MA 39582 A MA39582 A MA 39582A MA 39582 B1 MA39582 B1 MA 39582B1
- Authority
- MA
- Morocco
- Prior art keywords
- compounds
- dihydropyrazolo
- pyrazin
- metabotropic glutamate
- allosteric
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 102000016193 Metabotropic glutamate receptors Human genes 0.000 title abstract 2
- 108010010914 Metabotropic glutamate receptors Proteins 0.000 title abstract 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 title 1
- 230000003281 allosteric effect Effects 0.000 title 1
- 239000000203 mixture Substances 0.000 abstract 2
- 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 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 229940126662 negative allosteric modulator Drugs 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 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
- A61K31/495—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
-
- 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
- A61K31/41—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
- A61K31/505—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (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 (2)
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MA39582A1 MA39582A1 (fr) | 2018-06-29 |
| MA39582B1 true MA39582B1 (fr) | 2019-10-31 |
Family
ID=51257437
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MA39582A MA39582B1 (fr) | 2014-08-01 | 2015-07-30 | Composés de 6,7-dihydropyrazolo [1,5-?]pyrazin -4 (5h)-one et leur utilisation en tant que modulateurs négatifs allostériques des récepteurs métabotropiques du glutamate |
Country Status (34)
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL279202B2 (en) | 2014-01-21 | 2023-09-01 | Janssen Pharmaceutica Nv | Combinations containing positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic subtype 2 receptor and their use |
| CN109999025A (zh) | 2014-01-21 | 2019-07-12 | 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 |
| 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 |
| 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 |
| PL3389727T3 (pl) | 2015-12-18 | 2021-02-08 | Janssen Pharmaceutica Nv | RADIOZNAKOWANE LIGANDY mGluR2/3 DO PET |
| CA3003962A1 (en) | 2015-12-18 | 2017-06-22 | 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 |
| ES2991283T3 (es) | 2017-11-24 | 2024-12-03 | Sumitomo Pharma Co Ltd | Derivado de 6,7-dihidropirazolo[1,5-a]pirazinona y aplicación médica del mismo |
| WO2019145214A1 (en) * | 2018-01-26 | 2019-08-01 | 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 |
| US6831074B2 (en) | 2001-03-16 | 2004-12-14 | Pfizer Inc | Pharmaceutically active compounds |
| US20030114448A1 (en) | 2001-05-31 | 2003-06-19 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
| TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| WO2005061507A1 (en) | 2003-12-16 | 2005-07-07 | Pfizer Products Inc. | Bicyclic pyrazol-4-one cannabinoid receptor ligands and uses thereof |
| WO2005123738A1 (en) | 2004-06-21 | 2005-12-29 | F.Hoffmann-La Roche Ag | Pyrrazolo-pyrimidine derivatives |
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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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| CA2815120A1 (en) | 2010-11-08 | 2012-05-18 | Jose Ignacio Andres-Gil | Radiolabelled mglur2 pet ligands |
| EP2651222A4 (en) | 2010-12-17 | 2014-04-30 | Univ Vanderbilt | BICYCLIC TRIAZOL AND PYRAZOLLACTAME AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS |
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| CN104736156A (zh) * | 2012-06-20 | 2015-06-24 | 范德比尔特大学 | 作为mglur5受体变构调节剂的取代的双环烷氧基吡唑类似物 |
| KR20150070187A (ko) | 2012-10-23 | 2015-06-24 | 에프. 호프만-라 로슈 아게 | 자폐 장애의 치료를 위한 ｍｇｌｕ２／３ 길항제 |
| 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 |
| 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 |
| 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 |
| 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 |
| RU2708391C2 (ru) | 2014-08-01 | 2019-12-06 | Янссен Фармацевтика Нв | 6,7-дигидропиразоло[1,5-а]пиразин-4(5h)-оновые соединения и их применение в качестве отрицательных аллостерических модуляторов рецепторов mglur2 |
| 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 |
| 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 |
| 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 |
| CA3003962A1 (en) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Radiolabelled mglur2/3 pet ligands |
| PL3389727T3 (pl) | 2015-12-18 | 2021-02-08 | Janssen Pharmaceutica Nv | RADIOZNAKOWANE LIGANDY mGluR2/3 DO PET |
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2015
- 2015-07-27 JO JOP/2015/0179A patent/JOP20150179B1/ar active
- 2015-07-30 PH PH1/2017/500161A patent/PH12017500161B1/en unknown
- 2015-07-30 EA EA201692540A patent/EA031087B1/ru unknown
- 2015-07-30 PT PT15750666T patent/PT3177623T/pt unknown
- 2015-07-30 AU AU2015295298A patent/AU2015295298B2/en not_active Ceased
- 2015-07-30 PL PL15750666T patent/PL3177623T3/pl unknown
- 2015-07-30 US US15/500,600 patent/US10005786B2/en active Active
- 2015-07-30 TW TW104124696A patent/TWI696624B/zh not_active IP Right Cessation
- 2015-07-30 ME MEP-2019-24A patent/ME03320B/me unknown
- 2015-07-30 ES ES15750666T patent/ES2708215T3/es active Active
- 2015-07-30 CN CN201580041316.8A patent/CN106573936B/zh active Active
- 2015-07-30 SM SM20190038T patent/SMT201900038T1/it unknown
- 2015-07-30 TR TR2019/01074T patent/TR201901074T4/tr unknown
- 2015-07-30 HR HRP20181997TT patent/HRP20181997T1/hr unknown
- 2015-07-30 MA MA39582A patent/MA39582B1/fr unknown
- 2015-07-30 BR BR112017001726A patent/BR112017001726A2/pt not_active Application Discontinuation
- 2015-07-30 NZ NZ728122A patent/NZ728122A/en not_active IP Right Cessation
- 2015-07-30 HU HUE15750666A patent/HUE042871T2/hu unknown
- 2015-07-30 SG SG11201700638YA patent/SG11201700638YA/en unknown
- 2015-07-30 MX MX2017001452A patent/MX376289B/es active IP Right Grant
- 2015-07-30 JP JP2017504775A patent/JP6662846B2/ja not_active Expired - Fee Related
- 2015-07-30 DK DK15750666.8T patent/DK3177623T3/en active
- 2015-07-30 CA CA2954093A patent/CA2954093C/en active Active
- 2015-07-30 WO PCT/EP2015/067530 patent/WO2016016380A1/en not_active Ceased
- 2015-07-30 LT LTEP15750666.8T patent/LT3177623T/lt unknown
- 2015-07-30 KR KR1020177005257A patent/KR102531689B1/ko active Active
- 2015-07-30 RS RS20190115A patent/RS58279B1/sr unknown
- 2015-07-30 EP EP15750666.8A patent/EP3177623B1/en active Active
- 2015-07-30 SI SI201530513T patent/SI3177623T1/sl unknown
- 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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| MA40893B1 (fr) | Dérivés de phényltriazole à substitution hydroxyalkyle et utilisations associées | |
| MA41134A (fr) | Composés substitués de 5-amino-6h-thiazolo[4,5-d]pyrimidine-2,7-dione pour le traitement et la prophylaxie des infections virales | |
| MA40523A (fr) | 2-(morpholin-4-yl)-1,7-naphthyridines | |
| MX2017001454A (es) | Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5h)-ona y su uso como moduladores alostericos negativos de receptores de glutamato metabotropico subtipo 2 (mglu2r2). | |
| MA42397B1 (fr) | 4-azaindoles substituées et leur utilisation comme modulatoeurs de la récepteur glun2b | |
| MA42230B1 (fr) | Dérivés bicycliques, leur procédé de préparation, et compositions pharmaceutiques les contenant | |
| MA38146B1 (fr) | Nouveaux dérivés du benzimidazole comme antagonistes ep4 | |
| MA40875A (fr) | 2,4-diamino-quinoléine substituée servant de nouveaux agents anticancéreux | |
| MA33419B1 (fr) | Composés et compositions pour le traitement de maladies parasitaires | |
| MA41238B1 (fr) | Dérivés 5-[(pipérazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione en tant qu'inhibiteurs d'adamts pour le traitement de l'ostéoarthrit | |
| MX2017001453A (es) | Compuestos de 6,7-dihidropirazolo[1,5-a]pirazin-4(5h)-ona y su uso como moduladores alostericos negativos de receptores de glutamato metabotropico subtipo 2 (mglur2). | |
| MX392132B (es) | DERIVADOS DE CROMANO, ISOCROMANO Y DIHIDROISOBENZOFURANOS COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE mG1uR2, COMPOSICIONES Y SU USO. | |
| MA43913A (fr) | Modulateurs allostériques positifs du récepteur m1 muscarinique | |
| MA41174B1 (fr) | Dérivés d'imidazopyridazine utilisés en tant qu'inhibiteurs de pi3kbeta | |
| MA39750A (fr) | Dérivés d'acide aza-indol-acétique et leur utilisation comme modulateurs des récepteurs de la prostaglandine d2 | |
| MA43250B1 (fr) | Composés d'oxadiazaspiro pour le traitement de l'abus et la dépendance aux drogues | |
| MA53898B1 (fr) | Dérivés de 4-pyrazin-2-ylméthyl-morpholine et leur utilisation comme médicament | |
| MA39583A1 (fr) | Composés 6,7-dihydropyrazolo[1,5-a] pyrazin-4(5h)-one et leur utilisation comme modulateurs allostériques négatifs des récepteurs mglur2 | |
| MA38642A1 (fr) | Compositions pharmaceutiques de composes triazolopyridines substitues pour une utilsation en tant qu'agents anticancereux | |
| MA45867B1 (fr) | Modulateurs du récepteur des oestrogènes | |
| MA56098B1 (fr) | Immunomodulateurs hétérocycliques autant qu'inhibiteurs de pdl1 |