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)
  • Neurology (AREA)
  • Neurosurgery (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)
  • Biomedical Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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) TWI355381B (pt)
WO (1) WO2004094431A2 (pt)
ZA (1) ZA200508489B (pt)

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US6916811B2 (en) * 2001-11-30 2005-07-12 Schering Corporation Adenosine A2a receptor antagonists
AU2003304527B2 (en) 2002-12-19 2010-09-09 Merck Sharp & Dohme Corp. Uses of 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
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
KR20060135901A (ko) * 2004-04-21 2006-12-29 쉐링 코포레이션 피라졸로-[4,3-ｅ]-1,2,4-트리아졸로-[1,5-ｃ]피리미딘아데노신 Ａ2ａ 수용체 길항제
EP1902716A4 (en) * 2005-06-07 2009-05-13 Kyowa Hakko Kirin Co Ltd PROPHYLACTIC AND / OR THERAPEUTIC AGENT FOR MOTOR TROUBLESHOOTING
CA2622741A1 (en) 2005-09-19 2007-03-29 Schering Corporation 2-heteroaryl-pyrazolo-[4, 3-e]-1, 2, 4-triazolo-[1,5-c]-pyrimidine as adenosine a2a receptor antagonists
PE20070521A1 (es) * 2005-09-23 2007-07-13 Schering Corp 7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA COMO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2a
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
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AU2009222047A1 (en) * 2008-03-04 2009-09-11 Schering Corporation 1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo [4,3-e] -1,2,4-triazolo [4,3-c] pyrimidin-3-one compounds for use as adenosine A2a receptor antagonists
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)
WO2010104194A1 (en) 2009-03-10 2010-09-16 Takeda Pharmaceutical Company Limited Benzofuran derivatives
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
KR101795562B1 (ko) * 2011-12-27 2017-11-08 (주)바이오팜솔루션즈 뇌졸중의 치료 또는 예방에 사용되는 페닐카바메이트 화합물
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
HUE051195T2 (hu) * 2013-03-14 2021-03-01 Galapagos Nv Új vegyületek és gyógyászati készítményeik gyulladásos rendellenességek kezelésére
US11498923B2 (en) 2017-12-13 2022-11-15 Merck Sharp & Dohme Llc Substituted imidazo[1,2-c]quinazolines as A2A antagonists
CN114667287A (zh) * 2019-07-17 2022-06-24 泰昂治疗公司 腺苷a2a受体拮抗剂及其用途
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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Also Published As

Publication number Publication date
US6897217B2 (en) 2005-05-24
KR20060005379A (ko) 2006-01-17
TWI375677B (en) 2012-11-01
NO20055510D0 (no) 2005-11-22
IL171567A (en) 2013-01-31
US20050222164A1 (en) 2005-10-06
CN1777609A (zh) 2006-05-24
CA2522813C (en) 2009-09-08
WO2004094431A2 (en) 2004-11-04
NO20055510L (no) 2006-01-20
DK1622912T3 (da) 2009-09-07
JP4527712B2 (ja) 2010-08-18
CA2522813A1 (en) 2004-11-04
WO2004094431A3 (en) 2004-12-02
JP2006523619A (ja) 2006-10-19
PE20050141A1 (es) 2005-04-01
AU2004233334A1 (en) 2004-11-04
ATE432282T1 (de) 2009-06-15
HK1085466A1 (en) 2006-08-25
DE602004021250D1 (de) 2009-07-09
BRPI0409787B1 (pt) 2018-08-21
PL378867A1 (pl) 2006-05-29
US20040220194A1 (en) 2004-11-04
KR100831107B1 (ko) 2008-05-20
PL1622912T3 (pl) 2009-11-30
CL2004000847A1 (es) 2005-03-11
AR044041A1 (es) 2005-08-24
MXPA05011366A (es) 2005-11-28
EP1622912B1 (en) 2009-05-27
AU2004233334B2 (en) 2010-08-12
ES2326270T3 (es) 2009-10-06
BRPI0409787B8 (pt) 2021-05-25
TW200427689A (en) 2004-12-16
HRP20090394T1 (hr) 2009-08-31
CO5700766A2 (es) 2006-11-30
RU2373210C2 (ru) 2009-11-20
CY1109263T1 (el) 2014-07-02
US7368449B2 (en) 2008-05-06
TW201144317A (en) 2011-12-16
RU2005136166A (ru) 2006-06-10
ECSP056115A (es) 2006-03-01
MY139344A (en) 2009-09-30
TWI355381B (en) 2012-01-01
CN100503609C (zh) 2009-06-24
ZA200508489B (en) 2007-04-25
EP1622912A2 (en) 2006-02-08
NZ542823A (en) 2009-03-31
NO332182B1 (no) 2012-07-23
JP2010059178A (ja) 2010-03-18
PT1622912E (pt) 2009-08-17
SI1622912T1 (sl) 2009-10-31

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Owner name: MERCK SHARP AND DOHME CORP. (US)

B25G Requested change of headquarter approved

Owner name: MERCK SHARP AND DOHME CORP. (US)

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Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]
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