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 receptors

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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
Application number
PH12017500170A
Other languages
English (en)
Other versions
PH12017500170A1 (en
Inventor
Diego Sergio-Alvar Alonso-De
Gool Michiel Luc Maria Van
Mar¡A Luz Martin-Martin
Susana Conde-Ceide
Jos‚ Ignacio AndrS-Gil
Oscar Delgado-Gonzalez
Gary John Tresadern
Andr‚S Trabanco-Suarez
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PH12017500170A1 publication Critical patent/PH12017500170A1/en
Publication of PH12017500170B1 publication Critical patent/PH12017500170B1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • 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)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Dispersion Chemistry (AREA)
  • Dermatology (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
PH12017500170A 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 PH12017500170B1 (en)

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

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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)

Country Link
US (2) US10005785B2 (enExample)
EP (1) EP3174883B1 (enExample)
JP (1) JP6609306B2 (enExample)
KR (1) KR102531680B1 (enExample)
CN (1) CN107018662B (enExample)
AU (1) AU2015295313B2 (enExample)
BR (1) BR112017001861A2 (enExample)
CA (1) CA2954094C (enExample)
CL (1) CL2017000249A1 (enExample)
CY (1) CY1121123T1 (enExample)
DK (1) DK3174883T3 (enExample)
EA (1) EA033052B1 (enExample)
ES (1) ES2705425T3 (enExample)
HR (1) HRP20182114T1 (enExample)
HU (1) HUE041777T2 (enExample)
IL (1) IL250303A0 (enExample)
JO (1) JOP20150177B1 (enExample)
LT (1) LT3174883T (enExample)
ME (1) ME03341B (enExample)
MX (1) MX370182B (enExample)
NZ (1) NZ728025A (enExample)
PH (1) PH12017500170B1 (enExample)
PL (1) PL3174883T3 (enExample)
PT (1) PT3174883T (enExample)
RS (1) RS58215B1 (enExample)
SG (1) SG11201700637WA (enExample)
SI (1) SI3174883T1 (enExample)
SM (1) SMT201900013T1 (enExample)
TW (1) TWI688566B (enExample)
WO (1) WO2016016395A1 (enExample)
ZA (1) ZA201700758B (enExample)

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ES2727158T3 (es) 2014-12-03 2019-10-14 Janssen Pharmaceutica Nv Ligandos para PET de mGluR2 radiomarcados
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WO2025146502A1 (en) 2024-01-05 2025-07-10 Janssen Pharmaceutica Nv Coronavirus inhibiting compounds

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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
EP3174884B1 (en) 2014-08-01 2018-09-26 Janssen Pharmaceutica NV 6,7-dihydropyrazolo[1,5- ]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors
EP3174882B1 (en) 2014-08-01 2018-11-07 Janssen Pharmaceutica NV 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5h)-one compounds and their use as negative allosteric modulators of mglu2 receptors
ES2727158T3 (es) 2014-12-03 2019-10-14 Janssen Pharmaceutica Nv Ligandos para PET de mGluR2 radiomarcados
AU2015357167B2 (en) 2014-12-03 2020-06-25 Janssen Pharmaceutica Nv 6,7-dihydropyrazolo(1,5-alpha)pyrazin-4(5H)-one compounds and their use as negative allosteric modulators of mGluR2 receptors
US11045562B2 (en) 2015-12-18 2021-06-29 Janssen Pharmaceutica Nv Radiolabelled mGluR2/3 PET ligands
WO2017103182A1 (en) 2015-12-18 2017-06-22 Janssen Pharmaceutica Nv Radiolabelled mglur2/3 pet ligands

Also Published As

Publication number Publication date
EA201692544A1 (ru) 2017-08-31
IL250303A0 (en) 2017-03-30
MX370182B (es) 2019-12-04
KR20170033373A (ko) 2017-03-24
CY1121123T1 (el) 2019-12-11
CA2954094A1 (en) 2016-02-04
PH12017500170A1 (en) 2017-07-10
EP3174883B1 (en) 2018-10-24
HRP20182114T1 (hr) 2019-02-08
JOP20150177B1 (ar) 2021-08-17
SG11201700637WA (en) 2017-02-27
AU2015295313B2 (en) 2019-05-02
AU2015295313A1 (en) 2017-01-05
KR102531680B1 (ko) 2023-05-10
TWI688566B (zh) 2020-03-21
BR112017001861A2 (pt) 2017-11-21
NZ728025A (en) 2022-04-29
MX2017001454A (es) 2017-05-09
RS58215B1 (sr) 2019-03-29
DK3174883T3 (en) 2019-02-04
US10519162B2 (en) 2019-12-31
HUE041777T2 (hu) 2019-05-28
CN107018662A (zh) 2017-08-04
ME03341B (me) 2019-10-20
ES2705425T3 (es) 2019-03-25
CN107018662B (zh) 2020-01-07
US20180258096A1 (en) 2018-09-13
EP3174883A1 (en) 2017-06-07
PT3174883T (pt) 2019-01-21
US20170217971A1 (en) 2017-08-03
PL3174883T3 (pl) 2019-04-30
SMT201900013T1 (it) 2019-02-28
EA033052B1 (ru) 2019-08-30
LT3174883T (lt) 2019-01-10
US10005785B2 (en) 2018-06-26
ZA201700758B (en) 2020-01-29
JP6609306B2 (ja) 2019-11-20
WO2016016395A1 (en) 2016-02-04
CL2017000249A1 (es) 2017-08-18
CA2954094C (en) 2023-02-14
TW201625630A (zh) 2016-07-16
SI3174883T1 (sl) 2019-01-31
JP2017526659A (ja) 2017-09-14

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