NO332182B1 - 2-alkynyl- og 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidin-adenosin A2a-reseptorantagonist, anvendelse derav for fremstilling av et medikament, og farmasoytisk preparat omfattende forbindelsen - Google Patents

2-alkynyl- og 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidin-adenosin A2a-reseptorantagonist, anvendelse derav for fremstilling av et medikament, og farmasoytisk preparat omfattende forbindelsen Download PDF

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Publication number
NO332182B1
NO332182B1 NO20055510A NO20055510A NO332182B1 NO 332182 B1 NO332182 B1 NO 332182B1 NO 20055510 A NO20055510 A NO 20055510A NO 20055510 A NO20055510 A NO 20055510A NO 332182 B1 NO332182 B1 NO 332182B1
Authority
NO
Norway
Prior art keywords
alkyl
mmol
preparation
mixture
product
Prior art date
Application number
NO20055510A
Other languages
English (en)
Norwegian (no)
Other versions
NO20055510D0 (no
NO20055510L (no
Inventor
Bernard R Neustadt
Samuel Chackalamannil
Andrew W Stamford
Craig D Boyle
Jinsong Hao
Hong Liu
Unmesh G Shah
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of NO20055510D0 publication Critical patent/NO20055510D0/no
Publication of NO20055510L publication Critical patent/NO20055510L/no
Publication of NO332182B1 publication Critical patent/NO332182B1/no

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Classifications

    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
NO20055510A 2003-04-23 2005-11-22 2-alkynyl- og 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidin-adenosin A2a-reseptorantagonist, anvendelse derav for fremstilling av et medikament, og farmasoytisk preparat omfattende forbindelsen NO332182B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46484003P 2003-04-23 2003-04-23
PCT/US2004/012471 WO2004094431A2 (en) 2003-04-23 2004-04-21 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine a2a receptor antagonists

Publications (3)

Publication Number Publication Date
NO20055510D0 NO20055510D0 (no) 2005-11-22
NO20055510L NO20055510L (no) 2006-01-20
NO332182B1 true NO332182B1 (no) 2012-07-23

Family

ID=33310963

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20055510A NO332182B1 (no) 2003-04-23 2005-11-22 2-alkynyl- og 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidin-adenosin A2a-reseptorantagonist, anvendelse derav for fremstilling av et medikament, og farmasoytisk preparat omfattende forbindelsen

Country Status (31)

Country Link
US (2) US6897217B2 (de)
EP (1) EP1622912B1 (de)
JP (2) JP4527712B2 (de)
KR (1) KR100831107B1 (de)
CN (1) CN100503609C (de)
AR (1) AR044041A1 (de)
AT (1) ATE432282T1 (de)
AU (1) AU2004233334B2 (de)
BR (1) BRPI0409787B8 (de)
CA (1) CA2522813C (de)
CL (1) CL2004000847A1 (de)
CO (1) CO5700766A2 (de)
CY (1) CY1109263T1 (de)
DE (1) DE602004021250D1 (de)
DK (1) DK1622912T3 (de)
EC (1) ECSP056115A (de)
ES (1) ES2326270T3 (de)
HR (1) HRP20090394T1 (de)
IL (1) IL171567A (de)
MX (1) MXPA05011366A (de)
MY (1) MY139344A (de)
NO (1) NO332182B1 (de)
NZ (1) NZ542823A (de)
PE (1) PE20050141A1 (de)
PL (2) PL378867A1 (de)
PT (1) PT1622912E (de)
RU (1) RU2373210C2 (de)
SI (1) SI1622912T1 (de)
TW (2) TWI375677B (de)
WO (1) WO2004094431A2 (de)
ZA (1) ZA200508489B (de)

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AU2002346503A1 (en) * 2001-11-30 2003-06-17 Schering Corporation Adenosine A2a receptor antagonists
US20060128694A1 (en) * 2002-12-19 2006-06-15 Michael Grzelak Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
MXPA05006790A (es) 2002-12-19 2005-09-08 Schering Corp Usos de antagonistas del receptor adenosina a2a.
EP1622912B1 (de) * 2003-04-23 2009-05-27 Schering Corporation 2-alkinyl- und 2-alkenyl-pyrazolo-[4,3-e] -1,2,4-triazolo-[1,5-c] -pyrimidinadenosin a2a rezeptorantagonisten
ATE461932T1 (de) * 2004-04-21 2010-04-15 Schering Corp Pyrazoloä4,3-eü-1,2,4-triazoloä1,5-cüpyrimidine als antagonisten des adenosin-a2a-rezeptors
JPWO2006132275A1 (ja) 2005-06-07 2009-01-08 協和醗酵工業株式会社 運動障害の予防および／または治療剤
AR057817A1 (es) * 2005-09-19 2007-12-19 Schering Corp Antagonistas del receptor a2a de 2-heteroaril-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidin adenosina. composiciones farmaceuticas
AR056080A1 (es) * 2005-09-23 2007-09-19 Schering Corp 7-[2-[4-(6-fluoro-3-metil-1,2-benciosoxazol-5-il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c] -pirimidin-5-amine
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
US7691869B2 (en) 2007-03-30 2010-04-06 King Pharmaceuticals Research And Development, Inc. Pyrrolotriazolopyrimidine derivatives, pharmaceutical compositions containing them and methods of treating conditions and diseases mediated by the adenosine A2A receptor activity
JP2011513417A (ja) * 2008-03-04 2011-04-28 シェーリング コーポレイション アデノシンＡ２ａ受容体アンタゴニストとして使用するための１，２，４−トリアゾロ［４，３−ｃ］ピリミジン−３−オンおよびピラゾロ［４，３−ｅ］−１，２，４−トリアゾロ［４，３−ｃ］ピリミジン−３−オン化合物
US8501997B2 (en) 2008-08-25 2013-08-06 Air Products And Chemicals, Inc. Curing agent for low temperature cure applications
US8512594B2 (en) * 2008-08-25 2013-08-20 Air Products And Chemicals, Inc. Curing agent of N,N′-dimethyl-meta-xylylenediamine and multifunctional amin(s)
KR20110128913A (ko) 2009-03-10 2011-11-30 다케다 야쿠힌 고교 가부시키가이샤 벤조푸란 유도체
EP2462144B1 (de) 2009-08-07 2017-09-20 Merck Sharp & Dohme Corp. Verfahren zur herstellung eines 2-alkinyl substituierten 5-amino-pyrazolo-[4, 3-e]-1,2,4-triazolo [1,5-c] pyrimidins
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
RU2632659C2 (ru) * 2011-12-27 2017-10-09 Байо-Фарм Солюшнс Ко., Лтд. Фенилкарбаматные соединения для применения в предупреждении или лечении эпилепсии
WO2014101120A1 (en) 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
WO2014139882A1 (en) * 2013-03-14 2014-09-18 Galapagos Nv Compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
US11498923B2 (en) 2017-12-13 2022-11-15 Merck Sharp & Dohme Llc Substituted imidazo[1,2-c]quinazolines as A2A antagonists
WO2021011670A1 (en) * 2019-07-17 2021-01-21 Teon Therapeutics, Inc. Adenosine a2a receptor antagonists and uses thereof
CN115160120B (zh) * 2022-08-02 2024-08-27 乐威医药（江苏）股份有限公司 一种多烷氧基芳香酮的合成方法

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IT1264901B1 (it) 1993-06-29 1996-10-17 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina
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IT1291372B1 (it) 1997-05-21 1999-01-07 Schering Plough S P A Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie
DE19826843A1 (de) * 1998-06-16 1999-12-23 Boehringer Ingelheim Pharma Neue Imidazotriazolopyrimidine, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
PT1283839E (pt) * 2000-05-26 2005-08-31 Schering Corp Antagonistas do receptor a2a da adenosina
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JP4545437B2 (ja) 2001-10-15 2010-09-15 シェーリング コーポレイション アデノシンａ２ａ受容体アンタゴニストとしてのイミダゾ（４，３−ｅ）−１，２，４−トリアゾロ（１，５−ｃ）ピリミジン
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EP1622912B1 (de) * 2003-04-23 2009-05-27 Schering Corporation 2-alkinyl- und 2-alkenyl-pyrazolo-[4,3-e] -1,2,4-triazolo-[1,5-c] -pyrimidinadenosin a2a rezeptorantagonisten

Also Published As

Publication number Publication date
EP1622912B1 (de) 2009-05-27
KR20060005379A (ko) 2006-01-17
WO2004094431A2 (en) 2004-11-04
CA2522813C (en) 2009-09-08
PT1622912E (pt) 2009-08-17
TW201144317A (en) 2011-12-16
NO20055510D0 (no) 2005-11-22
PL1622912T3 (pl) 2009-11-30
DK1622912T3 (da) 2009-09-07
AU2004233334B2 (en) 2010-08-12
NZ542823A (en) 2009-03-31
CY1109263T1 (el) 2014-07-02
HK1085466A1 (en) 2006-08-25
AU2004233334A1 (en) 2004-11-04
US6897217B2 (en) 2005-05-24
ZA200508489B (en) 2007-04-25
IL171567A (en) 2013-01-31
TWI375677B (en) 2012-11-01
HRP20090394T1 (hr) 2009-08-31
CA2522813A1 (en) 2004-11-04
BRPI0409787B8 (pt) 2021-05-25
JP2006523619A (ja) 2006-10-19
MXPA05011366A (es) 2005-11-28
JP4527712B2 (ja) 2010-08-18
DE602004021250D1 (de) 2009-07-09
CN100503609C (zh) 2009-06-24
EP1622912A2 (de) 2006-02-08
WO2004094431A3 (en) 2004-12-02
MY139344A (en) 2009-09-30
BRPI0409787B1 (pt) 2018-08-21
CL2004000847A1 (es) 2005-03-11
US20040220194A1 (en) 2004-11-04
PE20050141A1 (es) 2005-04-01
ATE432282T1 (de) 2009-06-15
US20050222164A1 (en) 2005-10-06
TWI355381B (en) 2012-01-01
AR044041A1 (es) 2005-08-24
RU2005136166A (ru) 2006-06-10
RU2373210C2 (ru) 2009-11-20
NO20055510L (no) 2006-01-20
CN1777609A (zh) 2006-05-24
BRPI0409787A (pt) 2006-05-30
CO5700766A2 (es) 2006-11-30
SI1622912T1 (sl) 2009-10-31
JP2010059178A (ja) 2010-03-18
US7368449B2 (en) 2008-05-06
ECSP056115A (es) 2006-03-01
KR100831107B1 (ko) 2008-05-20
TW200427689A (en) 2004-12-16
PL378867A1 (pl) 2006-05-29
ES2326270T3 (es) 2009-10-06

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Owner name: MERCK SHARP AND DOHME CORP

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