WO2012125732A8 - Substituted imadazapyrinidin-5(6h)-ones as allosteric modulators of mglur5 receptors - Google Patents

Substituted imadazapyrinidin-5(6h)-ones as allosteric modulators of mglur5 receptors Download PDF

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Publication number
WO2012125732A8
WO2012125732A8 PCT/US2012/029085 US2012029085W WO2012125732A8 WO 2012125732 A8 WO2012125732 A8 WO 2012125732A8 US 2012029085 W US2012029085 W US 2012029085W WO 2012125732 A8 WO2012125732 A8 WO 2012125732A8
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WIPO (PCT)
Prior art keywords
compounds
allosteric modulators
imadazapyrinidin
ones
substituted
Prior art date
Application number
PCT/US2012/029085
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French (fr)
Other versions
WO2012125732A1 (en
Inventor
P. Jeffrey Conn
Craig W. LINSLEY
Shaun R. Stauffer
Jose Manuel Bartolome-Nebreda
Gregor James Macdonald
Susana Conde-Ceide
Carrie K. Jones
Maria Luz Martin-Martin
Han Min Tong
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Vanderbilt University
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Priority to EP12757940.7A priority Critical patent/EP2685825A4/en
Priority to CA2830220A priority patent/CA2830220A1/en
Priority to JP2013558139A priority patent/JP2014508172A/en
Priority to AU2012229983A priority patent/AU2012229983A1/en
Publication of WO2012125732A1 publication Critical patent/WO2012125732A1/en
Publication of WO2012125732A8 publication Critical patent/WO2012125732A8/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
    • 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
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
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    • AHUMAN NECESSITIES
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    • 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
    • A61P25/22Anxiolytics
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • A61P35/02Antineoplastic agents specific for leukemia
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    • 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)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

In one aspect, the invention relates to imidazopyrimidin-5(6H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
PCT/US2012/029085 2011-03-15 2012-03-14 Substituted imadazapyrinidin-5(6h)-ones as allosteric modulators of mglur5 receptors WO2012125732A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP12757940.7A EP2685825A4 (en) 2011-03-15 2012-03-14 Substituted imadazopyrimidin-5(6h)-ones as allosteric modulators of mglur5 receptors
CA2830220A CA2830220A1 (en) 2011-03-15 2012-03-14 Substituted imidazopyrimidin-5(6h)-ones as allosteric modulators of mglur5 receptors
JP2013558139A JP2014508172A (en) 2011-03-15 2012-03-14 Substituted imidazopyrimidin-5 (6H) -ones as allosteric modulators of the MGLUR5 receptor
AU2012229983A AU2012229983A1 (en) 2011-03-15 2012-03-14 Substituted imadazapyrinidin-5(6H)-ones as allosteric modulators of mGluR5 receptors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161452921P 2011-03-15 2011-03-15
US61/452,921 2011-03-15

Publications (2)

Publication Number Publication Date
WO2012125732A1 WO2012125732A1 (en) 2012-09-20
WO2012125732A8 true WO2012125732A8 (en) 2013-10-17

Family

ID=46831091

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2012/029085 WO2012125732A1 (en) 2011-03-15 2012-03-14 Substituted imadazapyrinidin-5(6h)-ones as allosteric modulators of mglur5 receptors

Country Status (5)

Country Link
EP (1) EP2685825A4 (en)
JP (1) JP2014508172A (en)
AU (1) AU2012229983A1 (en)
CA (1) CA2830220A1 (en)
WO (1) WO2012125732A1 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013544891A (en) 2010-12-08 2013-12-19 ヴァンダービルト ユニバーシティー Bicyclic pyrazole compounds as allosteric modulators of the mGLUR5 receptor
US8865725B2 (en) * 2011-03-15 2014-10-21 Vanderbilt University Substituted imidazopyrimidin-5(6H)-ones as allosteric modulators of MGLUR5 receptors
EP2864331B1 (en) * 2012-06-21 2017-08-09 Bristol-Myers Squibb Company Positive allosteric modulators of mglur2
TWI713497B (en) * 2015-02-26 2020-12-21 南韓商愛思開生物製藥股份有限公司 Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
AU2020370958A1 (en) * 2019-10-21 2022-06-09 Sk Biopharmaceuticals Co., Ltd. Use of imidazopyrimidine or imidazotriazine compounds for prevention, alleviation, or treatment of cognitive disorders, or for improving cognitive function
WO2023064223A1 (en) 2021-10-11 2023-04-20 Gossamer Bio Services, Inc. Tri-substituted pyridines

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8334210D0 (en) * 1983-12-22 1984-02-01 Roussel Lab Ltd Imidazo(1 2-c)pyrimidines
JPH01203366A (en) * 1988-02-10 1989-08-16 Mitsui Petrochem Ind Ltd N-substituted imidazole derivative
WO2007034282A2 (en) * 2005-09-19 2007-03-29 Pfizer Products Inc. Diaryl-imidazole compounds condensed with a heterocycle as c3a receptor antagonists
PL2054416T3 (en) * 2006-08-04 2011-05-31 Merz Pharma Gmbh & Co Kgaa Substituted pyrazolopyrimidines, a process for their preparation and their use as medicine
US20080146523A1 (en) * 2006-12-18 2008-06-19 Guido Galley Imidazole derivatives
GB0704230D0 (en) * 2007-03-05 2007-04-11 Novartis Ag Organic compounds
US8034806B2 (en) * 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
WO2012083224A1 (en) * 2010-12-17 2012-06-21 Vanderbilt University Bicyclic triazole and pyrazole lactams as allosteric modulators of mglur5 receptors

Also Published As

Publication number Publication date
EP2685825A1 (en) 2014-01-22
EP2685825A4 (en) 2014-09-10
JP2014508172A (en) 2014-04-03
CA2830220A1 (en) 2012-09-20
WO2012125732A1 (en) 2012-09-20
AU2012229983A1 (en) 2013-10-03

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