DK3194403T3 - PYRROLOPYRIMIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS - Google Patents

PYRROLOPYRIMIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS Download PDF

Info

Publication number
DK3194403T3
DK3194403T3 DK15779059.3T DK15779059T DK3194403T3 DK 3194403 T3 DK3194403 T3 DK 3194403T3 DK 15779059 T DK15779059 T DK 15779059T DK 3194403 T3 DK3194403 T3 DK 3194403T3
Authority
DK
Denmark
Prior art keywords
mmol
formula
chemical entity
difluoro
ethyl
Prior art date
Application number
DK15779059.3T
Other languages
Danish (da)
English (en)
Inventor
Gideon Shapiro
Original Assignee
Rugen Holdings Cayman Ltd
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 Rugen Holdings Cayman Ltd filed Critical Rugen Holdings Cayman Ltd
Application granted granted Critical
Publication of DK3194403T3 publication Critical patent/DK3194403T3/en

Links

Classifications

    • 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
    • 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

Landscapes

  • 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)
DK15779059.3T 2014-09-15 2015-09-15 PYRROLOPYRIMIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS DK3194403T3 (en)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
DK3194403T3 true DK3194403T3 (en) 2019-04-15

Family

ID=54293326

Family Applications (1)

Application Number Title Priority Date Filing Date
DK15779059.3T DK3194403T3 (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
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

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP2519241A2 (en) 2009-12-28 2012-11-07 Afraxis, Inc. Methods for treating autism
CA2794808C (en) 2010-04-16 2019-08-20 Ac Immune S.A. Compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
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
EP2582374A4 (en) 2010-06-16 2014-03-19 Afraxis Holdings Inc METHOD FOR TREATING NERVOUS ELEMENTS
US9737531B2 (en) 2012-07-12 2017-08-22 Glytech, Llc Composition and method for treatment of depression and psychosis in humans
US20140005188A1 (en) 2011-03-11 2014-01-02 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
DK2713722T3 (en) 2011-05-31 2017-07-03 Celgene Int Ii Sarl Newly known GLP-1 receptor stabilizers and modulators
AU2013251079B2 (en) 2012-04-20 2017-03-23 Ucb Pharma S.A. Methods for treating Parkinson's disease
PE20151436A1 (es) 2013-01-29 2015-10-10 Naurex Inc Moduladores de receptores nmda de espiro-lactama y sus usos
MX2016014581A (es) 2014-05-06 2018-02-16 Univ Northwestern Composiciones de compuestos que modulan nmdar.
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
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
CA2957898C (en) 2023-02-21
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

Similar Documents

Publication Publication Date Title
DK3194403T3 (en) PYRROLOPYRIMIDINE DERIVATIVES AS NR2B NMDA RECEPTOR ANTAGONISTS
EP3152213B1 (en) Difluoroethylpyridine derivatives as nr2b nmda receptor antagonists
AU2016270677B2 (en) 3,3-difluoropiperidine carbamate heterocyclic compounds as NR2B NMDA receptor antagonists
WO2016100349A2 (en) Bicyclic azaheterocyclic compounds as nr2b nmda receptor antagonists
WO2016126869A1 (en) 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
BR112017004868B1 (pt) Derivados de pirrolopirimidina como antagonistas do receptor nmda nr2b e composição farmacêutica que os compreende
HK1241366A1 (en) Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
HK1241366B (en) Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
HK1253023B (en) 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists