CA2957898C - Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists - Google Patents

Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists Download PDF

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Publication number
CA2957898C
CA2957898C CA2957898A CA2957898A CA2957898C CA 2957898 C CA2957898 C CA 2957898C CA 2957898 A CA2957898 A CA 2957898A CA 2957898 A CA2957898 A CA 2957898A CA 2957898 C CA2957898 C CA 2957898C
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French (fr)
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CA2957898A1 (en
Inventor
Gideon Shapiro
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Rugen Holdings (cayman) Ltd
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Rugen Holdings (cayman) Ltd
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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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2957898A 2014-09-15 2015-09-15 Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists Active CA2957898C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462050692P 2014-09-15 2014-09-15
US62/050,692 2014-09-15
PCT/US2015/050267 WO2016044323A1 (en) 2014-09-15 2015-09-15 Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists

Publications (2)

Publication Number Publication Date
CA2957898A1 CA2957898A1 (en) 2016-03-24
CA2957898C true CA2957898C (en) 2023-02-21

Family

ID=54293326

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2957898A Active CA2957898C (en) 2014-09-15 2015-09-15 Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists

Country Status (15)

Country Link
US (3) US9567341B2 (enExample)
EP (1) EP3194403B1 (enExample)
JP (1) JP6612331B2 (enExample)
KR (1) KR102569031B1 (enExample)
CN (1) CN106715435B (enExample)
AU (1) AU2015317886A1 (enExample)
CA (1) CA2957898C (enExample)
DK (1) DK3194403T3 (enExample)
ES (1) ES2723436T3 (enExample)
IL (1) IL251027A0 (enExample)
MX (1) MX2017002775A (enExample)
RU (1) RU2017107558A (enExample)
SG (1) SG11201701853YA (enExample)
WO (1) WO2016044323A1 (enExample)
ZA (1) ZA201701069B (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2950285A1 (en) 2014-06-04 2015-12-10 Rugen Holdings (Cayman) Limited Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
ES2723436T3 (es) 2014-09-15 2019-08-27 Rugen Holdings Cayman Ltd Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B
EP3253761A4 (en) 2015-02-04 2018-06-20 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
EP3303323B1 (en) 2015-06-01 2020-01-08 Rugen Holdings (Cayman) Limited 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists
US10487055B2 (en) 2016-06-01 2019-11-26 Rhode Island Board Of Education Diindole compounds useful in treatment of nervous system disorders
US11000526B2 (en) 2016-11-22 2021-05-11 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
DK3720855T3 (da) * 2017-12-08 2021-11-08 Boehringer Ingelheim Int Imidazopyridinderivater og avendelsen deraf som medikament
US20210393621A1 (en) 2018-10-26 2021-12-23 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
EP4074317A1 (en) 2021-04-14 2022-10-19 Bayer AG Phosphorus derivatives as novel sos1 inhibitors
CN117185897A (zh) * 2023-08-31 2023-12-08 上海泰坦科技股份有限公司 一种二氟甲基卤苯的合成方法

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US6476041B1 (en) 1999-10-29 2002-11-05 Merck & Co., Inc. 1,4 substituted piperidinyl NMDA/NR2B antagonists
HU227197B1 (en) 2000-10-24 2010-10-28 Richter Gedeon Nyrt Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them
CZ20032258A3 (cs) * 2001-02-23 2004-01-14 Merck & Co., Inc. N-substituované nearylové heterocyklické sloučeniny
KR20060017839A (ko) 2003-06-04 2006-02-27 머크 앤드 캄파니 인코포레이티드 Nmda/nr2b 길항제로서 3-플루오로-피페리딘
US7592360B2 (en) 2003-06-04 2009-09-22 Merck & Co., Inc. 3-fluoro-piperidines as NMDA/NR2B antagonists
WO2005019221A1 (en) * 2003-08-15 2005-03-03 Merck & Co., Inc. 4-cycloalkylaminopyrazolo pyrimidine nmda/nr2b antagonists
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
CA2575430A1 (en) 2004-08-03 2006-02-16 Merck & Co., Inc. 1,3-disubstituted heteroaryl nmda/nr2b antagonists
WO2006069287A1 (en) 2004-12-22 2006-06-29 Merck & Co., Inc. Process for making substituted piperidines
AU2006236625A1 (en) * 2005-04-19 2006-10-26 Merck & Co., Inc. N-alkyl-azacycloalkyl NMDA/NR2B antagonists
DK1913000T3 (da) 2005-07-29 2012-03-12 Pfizer Prod Inc Pyrrolo[2,3-D]pyrimidinderivater; deres mellemprodukter og syntese
WO2007061868A2 (en) 2005-11-17 2007-05-31 Trustees Of Tufts College Treatment of stereotypic, self-injurious and compulsive behaviors using specific serotonin reuptake inhibitors and antagonists of nmda receptors
US7935706B2 (en) 2006-02-23 2011-05-03 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
MX2009006517A (es) 2006-12-27 2009-06-26 Sanofi Aventis Nuevos derivados de isoquinolina e isoquinolinona sustituidos.
WO2010015637A1 (en) 2008-08-06 2010-02-11 Novartis Ag New antiviral modified nucleosides
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EP2580213A4 (en) 2010-06-09 2013-12-25 Afraxis Holdings Inc 8- (HETEROARYLMETHYL) PYRIDO [2,3-D] PYRIMIDIN-7 (8H) -ONES FOR THE TREATMENT OF CNS DISORDERS
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CA2950285A1 (en) 2014-06-04 2015-12-10 Rugen Holdings (Cayman) Limited Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
ES2723436T3 (es) 2014-09-15 2019-08-27 Rugen Holdings Cayman Ltd Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B
US20180271869A1 (en) 2014-09-22 2018-09-27 Jie Liu Treatment of anxiety disorders and autism spectrum disorders
WO2016100349A2 (en) 2014-12-16 2016-06-23 Rugen Holdings (Cayman) Limited Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists
EP3253761A4 (en) 2015-02-04 2018-06-20 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
EP3303323B1 (en) 2015-06-01 2020-01-08 Rugen Holdings (Cayman) Limited 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists
US11000526B2 (en) 2016-11-22 2021-05-11 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders

Also Published As

Publication number Publication date
CA2957898A1 (en) 2016-03-24
DK3194403T3 (en) 2019-04-15
KR20170049602A (ko) 2017-05-10
US10420768B2 (en) 2019-09-24
JP6612331B2 (ja) 2019-11-27
US20170209449A1 (en) 2017-07-27
JP2017526724A (ja) 2017-09-14
CN106715435A (zh) 2017-05-24
SG11201701853YA (en) 2017-04-27
EP3194403A1 (en) 2017-07-26
IL251027A0 (en) 2017-04-30
WO2016044323A1 (en) 2016-03-24
ES2723436T3 (es) 2019-08-27
EP3194403B1 (en) 2019-02-06
ZA201701069B (en) 2019-07-31
BR112017004868A2 (pt) 2017-12-12
CN106715435B (zh) 2019-10-01
RU2017107558A (ru) 2018-10-18
US9968610B2 (en) 2018-05-15
US20160075713A1 (en) 2016-03-17
US9567341B2 (en) 2017-02-14
KR102569031B1 (ko) 2023-08-22
US20180303834A1 (en) 2018-10-25
RU2017107558A3 (enExample) 2019-03-18
AU2015317886A1 (en) 2017-03-09
MX2017002775A (es) 2017-08-10

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