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

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

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 (32)

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)
HK (1) HK1085466A1 (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) PL1622912T3 (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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MXPA04005209A (es) * 2001-11-30 2004-08-19 Schering Corp Antagonistas del receptor de adenosina a2a.
EP2269596A3 (en) 2002-12-19 2011-09-14 Schering Corporation Use of adenosine A2a receptor antagonists for the treatment of extrapyramidal syndrome and other movement disorders
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
RU2373210C2 (ru) * 2003-04-23 2009-11-20 Шеринг Корпорейшн 2-АЛКИНИЛ- И 2-АЛКЕНИЛ-ПИРАЗОЛ-[4,3-e]-1, 2, 4-ТРИАЗОЛО-[1,5-c]-ПИРИМИДИНОВЫЕ АНТАГОНИСТЫ A2A РЕЦЕПТОРА АДЕНОЗИНА
DE602005020127D1 (de) * 2004-04-21 2010-05-06 Schering Corp Pyrazoloä4,3-eü-1,2,4-triazoloä1,5-cüpyrimidine als antagonisten des adenosin-a2a-rezeptors
EP2258372B8 (en) * 2005-06-07 2012-12-19 Kyowa Hakko Kirin Co., Ltd. A2A antagonists for use in the treatment of motor disorders
EP1934227B1 (en) * 2005-09-19 2011-12-21 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.
US7723343B2 (en) * 2007-03-30 2010-05-25 King Pharmaceuticals Research And Development, Inc. Adenosine A2A receptor antagonists
CA2717172A1 (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
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)
US8501997B2 (en) * 2008-08-25 2013-08-06 Air Products And Chemicals, Inc. Curing agent for low temperature cure applications
ES2487616T3 (es) 2009-03-10 2014-08-22 Takeda Pharmaceutical Company Limited Derivados de benzofurano
WO2011017299A2 (en) * 2009-08-07 2011-02-10 Schering Corporation 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
JP6298765B2 (ja) * 2011-12-27 2018-03-20 バイオ−ファーム ソリューションズ カンパニー リミテッド 脳卒中の治療または予防に使用されるするためのフェニルカルバメート化合物
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
PT2970255T (pt) * 2013-03-14 2017-09-05 Galapagos Nv Compostos e as suas composições farmacêuticas para o tratamento de doenças inflamatórias
EP3723754A4 (en) 2017-12-13 2021-05-19 Merck Sharp & Dohme Corp. IMIDAZO [1,2-C] QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
WO2021011670A1 (en) * 2019-07-17 2021-01-21 Teon Therapeutics, Inc. Adenosine a2a receptor antagonists and uses thereof
CN115160120A (zh) * 2022-08-02 2022-10-11 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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RU2373210C2 (ru) * 2003-04-23 2009-11-20 Шеринг Корпорейшн 2-АЛКИНИЛ- И 2-АЛКЕНИЛ-ПИРАЗОЛ-[4,3-e]-1, 2, 4-ТРИАЗОЛО-[1,5-c]-ПИРИМИДИНОВЫЕ АНТАГОНИСТЫ A2A РЕЦЕПТОРА АДЕНОЗИНА

Also Published As

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

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