ES2723436T3 - Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B - Google Patents

Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B Download PDF

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Publication number
ES2723436T3
ES2723436T3 ES15779059T ES15779059T ES2723436T3 ES 2723436 T3 ES2723436 T3 ES 2723436T3 ES 15779059 T ES15779059 T ES 15779059T ES 15779059 T ES15779059 T ES 15779059T ES 2723436 T3 ES2723436 T3 ES 2723436T3
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Prior art keywords
fluoro
optionally substituted
receptor antagonists
alkyl
nr2b receptor
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ES15779059T
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English (en)
Spanish (es)
Inventor
Gideon Shapiro
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Rugen Holdings Cayman Ltd
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Rugen Holdings Cayman Ltd
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    • 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

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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)
  • Biomedical Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (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)
ES15779059T 2014-09-15 2015-09-15 Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B Active ES2723436T3 (es)

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
ES2723436T3 true ES2723436T3 (es) 2019-08-27

Family

ID=54293326

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15779059T Active ES2723436T3 (es) 2014-09-15 2015-09-15 Derivados de pirrolopirimidina como antagonistas del receptor NMDA NR2B

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
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CN106795163B (zh) 2014-06-04 2019-07-30 卢郡控股(开曼)有限公司 作为nr2b nmda受体拮抗剂的二氟乙基吡啶衍生物
KR102569031B1 (ko) 2014-09-15 2023-08-22 뤼겐 홀딩스 (케이맨) 리미티드 Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체
EP3253761A4 (en) 2015-02-04 2018-06-20 Rugen Holdings (Cayman) Limited 3,3-difluoro-piperidine derivatives as nr2b nmda receptor antagonists
WO2016196513A1 (en) 2015-06-01 2016-12-08 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
WO2018098128A1 (en) 2016-11-22 2018-05-31 Rugen Holdings (Cayman) Limited Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders
HRP20211726T1 (hr) * 2017-12-08 2022-02-18 Boehringer Ingelheim International Gmbh Derivati imidazopiridina i njihova uporaba kao lijeka
WO2020087031A1 (en) 2018-10-26 2020-04-30 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
UA75392C2 (en) 2001-02-23 2006-04-17 Merck & Co Inc N-substituted non-aryl heterocyclic antagonists nmda/nr2b
MXPA05013151A (es) 2003-06-04 2006-03-17 Merck & Co Inc 3-fluoro-piperidinas como antagonistas de n-metil-d-aspartato/nr2b.
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
JP2008509139A (ja) * 2004-08-03 2008-03-27 メルク エンド カムパニー インコーポレーテッド 1,3−二置換ヘテロアリールnmda/nr2b拮抗薬
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EP1874318A2 (en) * 2005-04-19 2008-01-09 Merck & Co., Inc. N-alkyl-azacycloalkyl nmda/nr2b antagonists
PL1913000T3 (pl) 2005-07-29 2012-05-31 Pfizer Prod Inc Pochodne pirolo[2,3-d]pirymidyny, ich związki pośrednie i synteza
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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KR102569031B1 (ko) 2014-09-15 2023-08-22 뤼겐 홀딩스 (케이맨) 리미티드 Nr2b nmda 수용체 길항제로서의 피롤로피리미딘 유도체
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WO2016196513A1 (en) 2015-06-01 2016-12-08 Rugen Holdings (Cayman) Limited 3,3-difluoropiperidine carbamate heterocyclic compounds as nr2b nmda receptor antagonists
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
US20170209449A1 (en) 2017-07-27
WO2016044323A1 (en) 2016-03-24
CA2957898C (en) 2023-02-21
KR102569031B1 (ko) 2023-08-22
ZA201701069B (en) 2019-07-31
IL251027A0 (en) 2017-04-30
KR20170049602A (ko) 2017-05-10
CN106715435A (zh) 2017-05-24
US20160075713A1 (en) 2016-03-17
AU2015317886A1 (en) 2017-03-09
US20180303834A1 (en) 2018-10-25
SG11201701853YA (en) 2017-04-27
DK3194403T3 (en) 2019-04-15
BR112017004868A2 (pt) 2017-12-12
MX2017002775A (es) 2017-08-10
EP3194403B1 (en) 2019-02-06
JP6612331B2 (ja) 2019-11-27
JP2017526724A (ja) 2017-09-14
CA2957898A1 (en) 2016-03-24
US9968610B2 (en) 2018-05-15
RU2017107558A (ru) 2018-10-18
EP3194403A1 (en) 2017-07-26
RU2017107558A3 (enExample) 2019-03-18
US10420768B2 (en) 2019-09-24
CN106715435B (zh) 2019-10-01

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