ECSP056115A - ANTAGONISTAS DEL RECEPTOR A2a DE 2-ALQUINIL- Y 2-ALQUENIL-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA ADENOSINA - Google Patents

ANTAGONISTAS DEL RECEPTOR A2a DE 2-ALQUINIL- Y 2-ALQUENIL-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA ADENOSINA

Info

Publication number
ECSP056115A
ECSP056115A EC2005006115A ECSP056115A ECSP056115A EC SP056115 A ECSP056115 A EC SP056115A EC 2005006115 A EC2005006115 A EC 2005006115A EC SP056115 A ECSP056115 A EC SP056115A EC SP056115 A ECSP056115 A EC SP056115A
Authority
EC
Ecuador
Prior art keywords
alkyl
alquinil
alquenil
pirazolo
pirimidine
Prior art date
Application number
EC2005006115A
Other languages
English (en)
Inventor
Bernard R Neustadt
Jinsong Hao
Hong Liu
Craig D Boyle
Samuel Chackalamannil
Andrew Stamford
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 ECSP056115A publication Critical patent/ECSP056115A/es

Links

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

Landscapes

  • 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)

Abstract

Se describen compuestos que tienen la fórmula estructural I o su sal farmacéuticamente aceptable, en donde R es R1, R2, R3, R4 y R5 son H, alquilo o alcoxialquilo;R6 es H, alquilo, hidroxialquilo o -CH2F;R7, R8 y R9 son H, alquilo, alcoxi, alquiltio, alcoxialquilo, halo o -CF3; y Z es opcionalmente arilo sustituido, heteroarilo o heteroaril-alquilo. También se describe el uso de los compuestos de fórmula I en el tratamiento de enfermedades del sistema nervioso central, en particular la enfermedad de Parkinson, solos o en combinación con otros agentes para el tratamiento de la Enfermedad de Parkinson, y composiciones farmacéuticas que los comprenden.
EC2005006115A 2003-04-23 2005-10-21 ANTAGONISTAS DEL RECEPTOR A2a DE 2-ALQUINIL- Y 2-ALQUENIL-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA ADENOSINA ECSP056115A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US46484003P 2003-04-23 2003-04-23

Publications (1)

Publication Number Publication Date
ECSP056115A true ECSP056115A (es) 2006-03-01

Family

ID=33310963

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2005006115A ECSP056115A (es) 2003-04-23 2005-10-21 ANTAGONISTAS DEL RECEPTOR A2a DE 2-ALQUINIL- Y 2-ALQUENIL-PIRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PIRIMIDINA ADENOSINA

Country Status (31)

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

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MXPA05006790A (es) 2002-12-19 2005-09-08 Schering Corp Usos de antagonistas del receptor adenosina a2a.
EP1622912B1 (en) * 2003-04-23 2009-05-27 Schering Corporation 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists
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.
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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 (en) 2009-08-07 2017-09-20 Merck Sharp & Dohme Corp. PROCESS FOR PREPARING A 2-ALKYNYL SUBSTITUTED 5-AMINO-PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE
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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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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Also Published As

Publication number Publication date
EP1622912B1 (en) 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
NO332182B1 (no) 2012-07-23
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 (en) 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
KR100831107B1 (ko) 2008-05-20
TW200427689A (en) 2004-12-16
PL378867A1 (pl) 2006-05-29
ES2326270T3 (es) 2009-10-06

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