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
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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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- 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)
Abstract
La présente invention concerne de nouveaux dérivés de 6,7-dihydropyrazolo [1,5-a]pyrazin-4(5h)-one utilisés comme modulateurs allostériques négatifs (nams) du récepteur métabotropique du glutamate sous-type 2 ("mglur2"). L'invention concerne aussi des compositions pharmaceutiques comprenant de tels composés, des procédés de préparation de tels composés et de telles compositions, et l'utilisation de tels composés et de telles compositions pour la prévention ou le traitement de troubles dans lesquels mglur2 est impliqué.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP14179598 | 2014-08-01 | ||
PCT/EP2015/067530 WO2016016380A1 (fr) | 2014-08-01 | 2015-07-30 | Composés de 6,7-dihydropyrazolo [1,5-α]pyrazin -4 (5h)-one et leur utilisation en tant que modulateurs négatifs allostériques des récepteurs métabotropiques du glutamate |
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)
Country | Link |
---|---|
US (3) | US10005786B2 (fr) |
EP (1) | EP3177623B1 (fr) |
JP (1) | JP6662846B2 (fr) |
KR (1) | KR102531689B1 (fr) |
CN (1) | CN106573936B (fr) |
AR (1) | AR101392A1 (fr) |
AU (1) | AU2015295298B2 (fr) |
BR (1) | BR112017001726A2 (fr) |
CA (1) | CA2954093C (fr) |
CL (1) | CL2017000192A1 (fr) |
CY (1) | CY1121649T1 (fr) |
DK (1) | DK3177623T3 (fr) |
EA (1) | EA031087B1 (fr) |
ES (1) | ES2708215T3 (fr) |
HR (1) | HRP20181997T1 (fr) |
HU (1) | HUE042871T2 (fr) |
IL (1) | IL250298A0 (fr) |
JO (1) | JOP20150179B1 (fr) |
LT (1) | LT3177623T (fr) |
MA (1) | MA39582B1 (fr) |
ME (1) | ME03320B (fr) |
MX (1) | MX376289B (fr) |
NZ (1) | NZ728122A (fr) |
PH (1) | PH12017500161B1 (fr) |
PL (1) | PL3177623T3 (fr) |
PT (1) | PT3177623T (fr) |
RS (1) | RS58279B1 (fr) |
SG (1) | SG11201700638YA (fr) |
SI (1) | SI3177623T1 (fr) |
SM (1) | SMT201900038T1 (fr) |
TR (1) | TR201901074T4 (fr) |
TW (1) | TWI696624B (fr) |
WO (1) | WO2016016380A1 (fr) |
ZA (1) | ZA201700759B (fr) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SMT202100103T1 (it) | 2014-01-21 | 2021-03-15 | Janssen Pharmaceutica Nv | Combinazione comprendente modulatori allosterici postivi del recettore glutammatergico metabotropico sottotipo 2 e loro utilizzo |
HUE045610T2 (hu) | 2014-01-21 | 2020-01-28 | Janssen Pharmaceutica Nv | 2-es altípusú metabotróp glutamáterg receptor pozitív allosztérikus modulátorait vagy ortosztérikus agonistáit tartalmazó kombinációk és alkalmazásuk |
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 |
WO2016087487A1 (fr) | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | Composés de 6,7-dihydropyrazolo[1,5-α]pyrazin-4(5h)-one et leur utilisation comme modulateurs allostériques négatifs des récepteurs mglur2 |
CA2967542C (fr) | 2014-12-03 | 2022-11-29 | Janssen Pharmaceutica Nv | Ligands radiomarques des recepteurs mglur2 utilises en tep |
ES2828976T3 (es) | 2015-12-18 | 2021-05-28 | Janssen Pharmaceutica Nv | Ligandos de mGluR2/3 radiomarcados para TEP |
WO2017103179A1 (fr) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Ligands radiomarqués des récepteurs mglur2/3 utilisés en tep |
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 |
JP7242548B2 (ja) | 2017-11-24 | 2023-03-20 | 住友ファーマ株式会社 | 6,7-ジヒドロピラゾロ[1,5-a]ピラジノン誘導体及びその医薬用途 |
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 |
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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 |
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 |
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 |
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 |
EP3174882B1 (fr) | 2014-08-01 | 2018-11-07 | Janssen Pharmaceutica NV | Composés 6,7-dihydropyrazolo [1,5-a] pyrazine-4 (5h)-one et leur utilisation en tant que modulateurs allostériques négatifs de récepteurs mglu2 |
CA2967542C (fr) | 2014-12-03 | 2022-11-29 | Janssen Pharmaceutica Nv | Ligands radiomarques des recepteurs mglur2 utilises en tep |
WO2016087487A1 (fr) | 2014-12-03 | 2016-06-09 | Janssen Pharmaceutica Nv | Composés de 6,7-dihydropyrazolo[1,5-α]pyrazin-4(5h)-one et leur utilisation comme modulateurs allostériques négatifs des récepteurs mglur2 |
WO2017103179A1 (fr) | 2015-12-18 | 2017-06-22 | Janssen Pharmaceutica Nv | Ligands radiomarqués des récepteurs mglur2/3 utilisés en tep |
ES2828976T3 (es) | 2015-12-18 | 2021-05-28 | Janssen Pharmaceutica Nv | Ligandos de mGluR2/3 radiomarcados para TEP |
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2015
- 2015-07-27 JO JOP/2015/0179A patent/JOP20150179B1/ar active
- 2015-07-30 BR BR112017001726A patent/BR112017001726A2/pt not_active Application Discontinuation
- 2015-07-30 JP JP2017504775A patent/JP6662846B2/ja active Active
- 2015-07-30 WO PCT/EP2015/067530 patent/WO2016016380A1/fr active Application Filing
- 2015-07-30 PL PL15750666T patent/PL3177623T3/pl unknown
- 2015-07-30 HU HUE15750666A patent/HUE042871T2/hu unknown
- 2015-07-30 RS RS20190115A patent/RS58279B1/sr unknown
- 2015-07-30 EA EA201692540A patent/EA031087B1/ru unknown
- 2015-07-30 MX MX2017001452A patent/MX376289B/es active IP Right Grant
- 2015-07-30 CA CA2954093A patent/CA2954093C/fr active Active
- 2015-07-30 NZ NZ728122A patent/NZ728122A/en not_active IP Right Cessation
- 2015-07-30 KR KR1020177005257A patent/KR102531689B1/ko active Active
- 2015-07-30 TW TW104124696A patent/TWI696624B/zh not_active IP Right Cessation
- 2015-07-30 SM SM20190038T patent/SMT201900038T1/it unknown
- 2015-07-30 US US15/500,600 patent/US10005786B2/en active Active
- 2015-07-30 PH PH1/2017/500161A patent/PH12017500161B1/en unknown
- 2015-07-30 ME MEP-2019-24A patent/ME03320B/fr unknown
- 2015-07-30 AU AU2015295298A patent/AU2015295298B2/en not_active Ceased
- 2015-07-30 SI SI201530513T patent/SI3177623T1/sl unknown
- 2015-07-30 TR TR2019/01074T patent/TR201901074T4/tr unknown
- 2015-07-30 ES ES15750666T patent/ES2708215T3/es active Active
- 2015-07-30 MA MA39582A patent/MA39582B1/fr unknown
- 2015-07-30 CN CN201580041316.8A patent/CN106573936B/zh active Active
- 2015-07-30 PT PT15750666T patent/PT3177623T/pt unknown
- 2015-07-30 SG SG11201700638YA patent/SG11201700638YA/en unknown
- 2015-07-30 DK DK15750666.8T patent/DK3177623T3/en active
- 2015-07-30 EP EP15750666.8A patent/EP3177623B1/fr active Active
- 2015-07-30 LT LTEP15750666.8T patent/LT3177623T/lt 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
-
2018
- 2018-05-10 US US15/976,037 patent/US10512646B2/en active Active
- 2018-11-27 HR HRP20181997TT patent/HRP20181997T1/hr unknown
-
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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