BR112017001726A2 - compostos de 6,7-di-hidropirazolo [1,5-a]pirazin-4(5h)-ona e seus usos como moduladores alostéricos negativos de receptores mglur2 - Google Patents
compostos de 6,7-di-hidropirazolo [1,5-a]pirazin-4(5h)-ona e seus usos como moduladores alostéricos negativos de receptores mglur2Info
- Publication number
- BR112017001726A2 BR112017001726A2 BR112017001726A BR112017001726A BR112017001726A2 BR 112017001726 A2 BR112017001726 A2 BR 112017001726A2 BR 112017001726 A BR112017001726 A BR 112017001726A BR 112017001726 A BR112017001726 A BR 112017001726A BR 112017001726 A2 BR112017001726 A2 BR 112017001726A2
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- dihydropyrazolo
- pyrazin
- allosteric modulators
- negative allosteric
- Prior art date
Links
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
- 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
-
- 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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
Abstract
a presente invenção se relaciona com novos derivados da 6,7-di-hidropirazolo[1,5-a]pirazin-4(5h)-ona como moduladores alostéricos negativos (nams) do receptor metabotrópico do glutamato do subtipo 2 ("mglur2"). a invenção está também dirigida a composições farmacêuticas compreendendo tais compostos, a processos para preparação de tais compostos e composições, e para o uso de tais com-postos e composições para a prevenção ou tratamento de distúrbios nos quais o subtipo mglur2 de receptores metabotrópicos está envolvido.
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 (1)
Publication Number | Publication Date |
---|---|
BR112017001726A2 true BR112017001726A2 (pt) | 2017-11-21 |
Family
ID=51257437
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017001726A BR112017001726A2 (pt) | 2014-08-01 | 2015-07-30 | compostos de 6,7-di-hidropirazolo [1,5-a]pirazin-4(5h)-ona e seus usos como moduladores alostéricos negativos de receptores mglur2 |
Country Status (33)
Country | Link |
---|---|
US (3) | US10005786B2 (pt) |
EP (1) | EP3177623B1 (pt) |
JP (1) | JP6662846B2 (pt) |
KR (1) | KR102531689B1 (pt) |
CN (1) | CN106573936B (pt) |
AR (1) | AR101392A1 (pt) |
AU (1) | AU2015295298B2 (pt) |
BR (1) | BR112017001726A2 (pt) |
CA (1) | CA2954093C (pt) |
CL (1) | CL2017000192A1 (pt) |
CY (1) | CY1121649T1 (pt) |
DK (1) | DK3177623T3 (pt) |
EA (1) | EA031087B1 (pt) |
ES (1) | ES2708215T3 (pt) |
HR (1) | HRP20181997T1 (pt) |
HU (1) | HUE042871T2 (pt) |
IL (1) | IL250298A0 (pt) |
JO (1) | JOP20150179B1 (pt) |
LT (1) | LT3177623T (pt) |
MA (1) | MA39582B1 (pt) |
ME (1) | ME03320B (pt) |
MX (1) | MX2017001452A (pt) |
NZ (1) | NZ728122A (pt) |
PH (1) | PH12017500161A1 (pt) |
PL (1) | PL3177623T3 (pt) |
PT (1) | PT3177623T (pt) |
RS (1) | RS58279B1 (pt) |
SG (1) | SG11201700638YA (pt) |
SI (1) | SI3177623T1 (pt) |
TR (1) | TR201901074T4 (pt) |
TW (1) | TWI696624B (pt) |
WO (1) | WO2016016380A1 (pt) |
ZA (1) | ZA201700759B (pt) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
KR20200126026A (ko) | 2014-01-21 | 2020-11-05 | 얀센 파마슈티카 엔.브이. | 대사 조절형 글루탐산 작동성 수용체 제2아형의 양성 알로스테릭 조절제 또는 오르토스테릭 작동제를 포함하는 조합 및 그 용도 |
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 |
US10072014B2 (en) | 2014-12-03 | 2018-09-11 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of MGLUR2 receptors |
US10967078B2 (en) | 2014-12-03 | 2021-04-06 | Janssen Pharmaceutica Nv | Radiolabelled mGluR2 PET ligands |
EA037941B1 (ru) | 2015-12-18 | 2021-06-09 | Янссен Фармацевтика Нв | ЛИГАНДЫ mGluR2/3 ДЛЯ PET, МЕЧЕННЫЕ РАДИОАКТИВНЫМИ ИЗОТОПАМИ |
PL3389727T3 (pl) | 2015-12-18 | 2021-02-08 | Janssen Pharmaceutica Nv | RADIOZNAKOWANE LIGANDY mGluR2/3 DO PET |
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 |
US11633395B2 (en) | 2017-11-24 | 2023-04-25 | Sumitomo Pharma Co., Ltd. | Substituted pyrazolo[1,5-a]pyrazines as negative allosteric modulators of group II metabotropic glutamate receptor |
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WO2016016383A1 (en) | 2014-08-01 | 2016-02-04 | Janssen Pharmaceutica Nv | 6,7-DIHYDROPYRAZOLO[1,5-α]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
WO2016016382A1 (en) | 2014-08-01 | 2016-02-04 | Janssen Pharmaceutica Nv | 6,7-dihydropyrazolo[1,5-a]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 |
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2015
- 2015-07-27 JO JOP/2015/0179A patent/JOP20150179B1/ar active
- 2015-07-30 AU AU2015295298A patent/AU2015295298B2/en active Active
- 2015-07-30 PL PL15750666T patent/PL3177623T3/pl unknown
- 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 US US15/500,600 patent/US10005786B2/en active Active
- 2015-07-30 EA EA201692540A patent/EA031087B1/ru unknown
- 2015-07-30 KR KR1020177005257A patent/KR102531689B1/ko active IP Right Grant
- 2015-07-30 ES ES15750666T patent/ES2708215T3/es active Active
- 2015-07-30 JP JP2017504775A patent/JP6662846B2/ja active Active
- 2015-07-30 NZ NZ728122A patent/NZ728122A/en not_active IP Right Cessation
- 2015-07-30 EP EP15750666.8A patent/EP3177623B1/en active Active
- 2015-07-30 HU HUE15750666A patent/HUE042871T2/hu unknown
- 2015-07-30 PT PT15750666T patent/PT3177623T/pt unknown
- 2015-07-30 CA CA2954093A patent/CA2954093C/en active Active
- 2015-07-30 DK DK15750666.8T patent/DK3177623T3/en active
- 2015-07-30 RS RS20190115A patent/RS58279B1/sr unknown
- 2015-07-30 TR TR2019/01074T patent/TR201901074T4/tr unknown
- 2015-07-30 CN CN201580041316.8A patent/CN106573936B/zh active Active
- 2015-07-30 BR BR112017001726A patent/BR112017001726A2/pt not_active Application Discontinuation
- 2015-07-30 MA MA39582A patent/MA39582B1/fr unknown
- 2015-07-30 LT LTEP15750666.8T patent/LT3177623T/lt unknown
- 2015-07-30 WO PCT/EP2015/067530 patent/WO2016016380A1/en active Application Filing
- 2015-07-30 MX MX2017001452A patent/MX2017001452A/es active IP Right Grant
- 2015-07-30 SI SI201530513T patent/SI3177623T1/sl unknown
- 2015-07-30 SG SG11201700638YA patent/SG11201700638YA/en 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 PH PH12017500161A patent/PH12017500161A1/en 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
- 2018-11-27 HR HRP20181997TT patent/HRP20181997T1/hr unknown
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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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