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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chemical entity
formula
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mixture
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English (en)
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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Addiction (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (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 (OSRAM)
EP (1) EP3194403B1 (OSRAM)
JP (1) JP6612331B2 (OSRAM)
KR (1) KR102569031B1 (OSRAM)
CN (1) CN106715435B (OSRAM)
AU (1) AU2015317886A1 (OSRAM)
CA (1) CA2957898C (OSRAM)
DK (1) DK3194403T3 (OSRAM)
ES (1) ES2723436T3 (OSRAM)
IL (1) IL251027A0 (OSRAM)
MX (1) MX2017002775A (OSRAM)
RU (1) RU2017107558A (OSRAM)
SG (1) SG11201701853YA (OSRAM)
WO (1) WO2016044323A1 (OSRAM)
ZA (1) ZA201701069B (OSRAM)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2017516836A (ja) 2014-06-04 2017-06-22 リューゲン ホールディングス (ケイマン) リミテッド Nr2bnmda受容体アンタゴニストとしてのジフルオロエチルピリジン誘導体
SG11201701853YA (en) 2014-09-15 2017-04-27 Rugen Holdings Cayman Ltd Pyrrolopyrimidine derivatives 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
KR102613179B1 (ko) 2015-06-01 2023-12-14 뤼겐 홀딩스 (케이맨) 리미티드 Nr2b nmda 수용체 길항제로서의 3,3-디플루오로피페리딘 카바메이트 헤테로사이클릭 화합물
US10487055B2 (en) 2016-06-01 2019-11-26 Rhode Island Board Of Education Diindole compounds useful in treatment of nervous system disorders
EP3544610A1 (en) 2016-11-22 2019-10-02 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
ES2897050T3 (es) * 2017-12-08 2022-02-28 Boehringer Ingelheim Int Derivados de imidazopiridina y el uso de los mismos como medicamento
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
HUP0303258A3 (en) 2001-02-23 2004-06-28 Merck & Co Inc N-substituted nonaryl-heterocyclic nmda/nr2b antagonists and pharmaceutical compositions containing them
BRPI0410837A (pt) 2003-06-04 2006-06-27 Merck & Co Inc composto, composição farmacêutica, e, método para tratar ou prevenir uma doença ou condição
US7592360B2 (en) 2003-06-04 2009-09-22 Merck & Co., Inc. 3-fluoro-piperidines as NMDA/NR2B antagonists
JP2007502772A (ja) 2003-08-15 2007-02-15 メルク エンド カムパニー インコーポレーテッド 4−シクロアルキルアミノピラゾロピリミジンnmda/nr2b拮抗薬
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
US20070293515A1 (en) 2004-08-03 2007-12-20 Layton Mark E 1,3-Disubstituted Heteroaryl Nmda/Nr2b Antagonists
WO2006069287A1 (en) 2004-12-22 2006-06-29 Merck & Co., Inc. Process for making substituted piperidines
JP2008536927A (ja) * 2005-04-19 2008-09-11 メルク エンド カムパニー インコーポレーテッド N−アルキル−アザシクロアルキルnmda/nr2b拮抗物質
MX2008001334A (es) 2005-07-29 2008-03-24 Pfizer Prod Inc Derivados de pirrolo [2,3-d]pirimidina, sus intermedios y sintesis.
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
EP1988077A4 (en) 2006-02-23 2009-09-02 Shionogi & Co NUCLEIC HETEROCYCLIC DERIVATIVES SUBSTITUTED BY CYCLIC GROUPS
RU2009128693A (ru) 2006-12-27 2011-02-10 Санофи-Авентис (Fr) Замещенные производные изохинолина и изохинолинона
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JP2017516836A (ja) 2014-06-04 2017-06-22 リューゲン ホールディングス (ケイマン) リミテッド Nr2bnmda受容体アンタゴニストとしてのジフルオロエチルピリジン誘導体
SG11201701853YA (en) 2014-09-15 2017-04-27 Rugen Holdings Cayman Ltd Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
WO2016049048A1 (en) 2014-09-22 2016-03-31 Rugen Holdings (Cayman) Limited 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
KR102613179B1 (ko) 2015-06-01 2023-12-14 뤼겐 홀딩스 (케이맨) 리미티드 Nr2b nmda 수용체 길항제로서의 3,3-디플루오로피페리딘 카바메이트 헤테로사이클릭 화합물
EP3544610A1 (en) 2016-11-22 2019-10-02 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders

Also Published As

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

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