BRPI0409787A - antagonistas receptores da 2-alquinil- e 2-alquenil-pirazol-[4,3-e]-1,2,4-triazol-[1,5-c]-pirimidina adenosina a2a - Google Patents

antagonistas receptores da 2-alquinil- e 2-alquenil-pirazol-[4,3-e]-1,2,4-triazol-[1,5-c]-pirimidina adenosina a2a

Info

Publication number
BRPI0409787A
BRPI0409787A BRPI0409787-4A BRPI0409787A BRPI0409787A BR PI0409787 A BRPI0409787 A BR PI0409787A BR PI0409787 A BRPI0409787 A BR PI0409787A BR PI0409787 A BRPI0409787 A BR PI0409787A
Authority
BR
Brazil
Prior art keywords
alkenyl
receptor antagonists
alkyl
pyrazolo
triazole
Prior art date
Application number
BRPI0409787-4A
Other languages
English (en)
Inventor
Bernard R Neustadt
Jinsong Hao
Hong Liu
Craig D Boyle
Samuel Chackalamannil
Unmesh G Shah
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 BRPI0409787A publication Critical patent/BRPI0409787A/pt
Publication of BRPI0409787B1 publication Critical patent/BRPI0409787B1/pt
Publication of BRPI0409787B8 publication Critical patent/BRPI0409787B8/pt

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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

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

"ANTAGONISTAS RECEPTORES DA 2-ALQUINIL E 2-ALQUENIL-PIRAZOL-¢4,3-e!-1,2,4-TRIAZOL-¢1,5-c!-PIRIMIDINA ADENOSINA A~ 2a~". A presente invenção refere-se a compostos tendo a fórmula estrutural (l) ou um sal farmaceuticamente aceitável dos mesmos, em que R é R¬ 1¬,R¬ 2¬, R¬ 3¬, R¬ 4¬ e R¬ 5¬ são H, alquila ou alcoxialquila; R¬ 6¬ é H, alquila, hidroxialquila ou -CH~ 2~F; R¬ 7¬, R¬ 8¬ e R¬ 9¬ são H, alquila, alcóxi, alquiltio, alcoxialquila, halo ou -CF~ 3~; e Z é arila, heteroarila ou heteroaril-alquila opcionalmente substituída. Também apresentado é o uso de compostos de fórmula 1 no tratamento de doenças do sistema nervoso central, em particular, a doença de Parkinson, isoladamente ou em combinação com outros agentes para o tratamento da doença de Parkinson, e composições farmacêuticas compreendendo-os.
BRPI0409787-4 2003-04-23 2004-04-21 antagonistas receptores da 2-alquinil- e 2-alquenil-pirazol-[4,3-e]-1,2,4-triazol-[1,5-c]-pirimidina adenosina a2a BRPI0409787B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US46484003P 2003-04-23 2003-04-23
US60/464,840 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
BRPI0409787A true BRPI0409787A (pt) 2006-05-30
BRPI0409787B1 BRPI0409787B1 (pt) 2018-08-21
BRPI0409787B8 BRPI0409787B8 (pt) 2021-05-25

Family

ID=33310963

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0409787-4 BRPI0409787B8 (pt) 2003-04-23 2004-04-21 antagonistas receptores da 2-alquinil- e 2-alquenil-pirazol-[4,3-e]-1,2,4-triazol-[1,5-c]-pirimidina adenosina a2a

Country Status (31)

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

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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 (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.
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 (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
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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
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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B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

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B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2719 DE 14-02-2023 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.