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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CA2957898A
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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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    • 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Medicinal 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Addiction (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (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 (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)

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TW201609741A (zh) 2014-06-04 2016-03-16 盧郡控股（開曼）有限公司 作為ｎｒ２ｂ ｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物
WO2016044323A1 (en) 2014-09-15 2016-03-24 Rugen Holdings (Cayman) Limited 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
MX380424B (es) 2015-06-01 2025-03-12 Rugen Holdings Cayman Ltd Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b.
US10487055B2 (en) 2016-06-01 2019-11-26 Rhode Island Board Of Education Diindole compounds useful in treatment of nervous system disorders
WO2018098128A1 (en) 2016-11-22 2018-05-31 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
EP3870292A4 (en) 2018-10-26 2022-11-09 The Research Foundation for The State University of New York COMBINATION OF SEROTONIN-SPECIFIC RESUPPUT INHIBITOR AND SEROTONIN 1A RECEPTOR PARTIAL AGONIST TO REDUCE 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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CZ296236B6 (cs) 1995-08-11 2006-02-15 Pfizer Inc. Trihydrát methansulfonátu (1S,2S)-1-(4-hydroxyfenyl)-2-(4-hydroxy-4-fenylpiperidin-1-yl)-1-propanolu, farmaceutický prostredek a farmaceutická kombinace s jeho obsahem
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
EA005974B1 (ru) * 2001-02-23 2005-08-25 Мерк Энд Ко., Инк. N-замещенные неарильные гетероциклические антагонисты nmda/nr2b
CA2527093C (en) 2003-06-04 2009-10-20 Merck & Co., Inc. 3-fluoro-piperidines as nmda/nr2b antagonists
US7592360B2 (en) 2003-06-04 2009-09-22 Merck & Co., Inc. 3-fluoro-piperidines as NMDA/NR2B antagonists
US7452893B2 (en) * 2003-08-15 2008-11-18 Merck & Co., Inc. 4-cycloakylaminopyrazolo 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
CN1993363A (zh) 2004-08-03 2007-07-04 默克公司 1,3－二取代的杂芳基nmda/nr2b拮抗剂
JP2008525486A (ja) 2004-12-22 2008-07-17 メルク エンド カムパニー インコーポレーテッド 置換ピペリジンの製造方法
WO2006113471A2 (en) 2005-04-19 2006-10-26 Merck & Co., Inc. N-alkyl-azacycloalkyl nmda/nr2b antagonists
CA2614907C (en) * 2005-07-29 2012-02-28 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
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
EP2520567A3 (en) 2006-02-23 2012-12-12 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
RU2009128693A (ru) 2006-12-27 2011-02-10 Санофи-Авентис (Fr) Замещенные производные изохинолина и изохинолинона
WO2010015637A1 (en) 2008-08-06 2010-02-11 Novartis Ag New antiviral modified nucleosides
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TW201609741A (zh) 2014-06-04 2016-03-16 盧郡控股（開曼）有限公司 作為ｎｒ２ｂ ｎｍｄａ受體拮抗劑之二氟乙基吡啶衍生物
WO2016044323A1 (en) 2014-09-15 2016-03-24 Rugen Holdings (Cayman) Limited 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
MX380424B (es) 2015-06-01 2025-03-12 Rugen Holdings Cayman Ltd Compuestos heterociclicos de 3,3-difluorpiperidina carbamato como antagonistas del receptor de n-metil-d-aspartato (nmda) nr2b.
WO2018098128A1 (en) 2016-11-22 2018-05-31 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders

Also Published As

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

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