JP4574112B2 - アデノシンa2aレセプターアンタゴニスト - Google Patents

アデノシンa2aレセプターアンタゴニスト Download PDF

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Publication number
JP4574112B2
JP4574112B2 JP2002500877A JP2002500877A JP4574112B2 JP 4574112 B2 JP4574112 B2 JP 4574112B2 JP 2002500877 A JP2002500877 A JP 2002500877A JP 2002500877 A JP2002500877 A JP 2002500877A JP 4574112 B2 JP4574112 B2 JP 4574112B2
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Japan
Prior art keywords
alkyl
alkoxy
compound
mmol
phenyl
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Expired - Lifetime
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JP2002500877A
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Japanese (ja)
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JP2003535094A (ja
JP2003535094A5 (OSRAM
Inventor
ベルナルド アール. ニュースタット,
ネイル エイ. リンド,
ウイリアム ジェイ. グリーンリー,
ディーン タルシアン,
リサ エス. シルバーマン,
ヤン シャ,
クレイグ ディー. ボイル,
サミュエル チャカラマニル,
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Merck Sharp and Dohme LLC
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Schering Corp
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Publication of JP2003535094A5 publication Critical patent/JP2003535094A5/ja
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2002500877A 2000-05-26 2001-05-24 アデノシンa2aレセプターアンタゴニスト Expired - Lifetime JP4574112B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20714300P 2000-05-26 2000-05-26
US60/207,143 2000-05-26
PCT/US2001/016954 WO2001092264A1 (en) 2000-05-26 2001-05-24 Adenosine a2a receptor antagonists

Related Child Applications (2)

Application Number Title Priority Date Filing Date
JP2006128415A Division JP4938348B2 (ja) 2000-05-26 2006-05-02 アデノシンa2aレセプターアンタゴニスト
JP2007069618A Division JP2007145875A (ja) 2000-05-26 2007-03-16 アデノシンa2aレセプターアンタゴニスト

Publications (3)

Publication Number Publication Date
JP2003535094A JP2003535094A (ja) 2003-11-25
JP2003535094A5 JP2003535094A5 (OSRAM) 2006-06-22
JP4574112B2 true JP4574112B2 (ja) 2010-11-04

Family

ID=22769372

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2002500877A Expired - Lifetime JP4574112B2 (ja) 2000-05-26 2001-05-24 アデノシンa2aレセプターアンタゴニスト
JP2006128415A Expired - Lifetime JP4938348B2 (ja) 2000-05-26 2006-05-02 アデノシンa2aレセプターアンタゴニスト
JP2007069618A Withdrawn JP2007145875A (ja) 2000-05-26 2007-03-16 アデノシンa2aレセプターアンタゴニスト

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2006128415A Expired - Lifetime JP4938348B2 (ja) 2000-05-26 2006-05-02 アデノシンa2aレセプターアンタゴニスト
JP2007069618A Withdrawn JP2007145875A (ja) 2000-05-26 2007-03-16 アデノシンa2aレセプターアンタゴニスト

Country Status (31)

Country Link
US (4) US6630475B2 (OSRAM)
EP (1) EP1283839B1 (OSRAM)
JP (3) JP4574112B2 (OSRAM)
KR (1) KR100520907B1 (OSRAM)
CN (2) CN100384847C (OSRAM)
AR (1) AR028621A1 (OSRAM)
AT (1) ATE293627T1 (OSRAM)
AU (2) AU2001268089C1 (OSRAM)
BR (1) BRPI0111015B8 (OSRAM)
CA (1) CA2410237C (OSRAM)
CZ (1) CZ303790B6 (OSRAM)
DE (1) DE60110219T2 (OSRAM)
DK (1) DK1283839T3 (OSRAM)
EC (1) ECSP024364A (OSRAM)
ES (1) ES2237576T3 (OSRAM)
HK (1) HK1049007B (OSRAM)
HU (1) HU230420B1 (OSRAM)
IL (3) IL152726A0 (OSRAM)
MX (1) MXPA02011625A (OSRAM)
MY (1) MY132006A (OSRAM)
NO (1) NO325008B1 (OSRAM)
NZ (1) NZ522326A (OSRAM)
PE (1) PE20020062A1 (OSRAM)
PL (1) PL218764B1 (OSRAM)
PT (1) PT1283839E (OSRAM)
RU (1) RU2315053C2 (OSRAM)
SI (1) SI1283839T1 (OSRAM)
SK (1) SK287748B6 (OSRAM)
TW (1) TWI288137B (OSRAM)
WO (1) WO2001092264A1 (OSRAM)
ZA (1) ZA200208898B (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007145875A (ja) * 2000-05-26 2007-06-14 Schering Plough Corp アデノシンa2aレセプターアンタゴニスト

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003022283A1 (en) * 2001-09-13 2003-03-20 Schering Corporation Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic
AR037243A1 (es) 2001-10-15 2004-11-03 Schering Corp Antagonistas del receptor de adenosina a2a,a5-amino-imidazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]pirimidina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de un medicamento
FR2832405B1 (fr) * 2001-11-19 2004-12-10 Sanofi Synthelabo Tetrahydropyridyl-alkyl-heterocycles azotes, procede pour leur preparation et compositions pharmaceutiques les contenant
PE20030739A1 (es) 2001-11-30 2003-08-28 Schering Corp Antagonistas del receptor de adenosina a2a
HUP0402324A3 (en) 2001-11-30 2008-09-29 Schering Corp [1,2,4]triazolo[1,5-a]pyridine and [1,2,4]triazolo[1,5-c]pyrimidine derivatives as adenosine a2a receptor antagonists and pharmaceutical compositions containing them
HUP0402018A3 (en) * 2001-11-30 2008-06-30 Schering Corp 5-amino-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives, their use and pharmaceutical compositions containing them
HUE039348T2 (hu) 2002-01-28 2018-12-28 Kyowa Hakko Kogyo Kk A2A receptor antagonisták mozgási rendellenességek kezelésében történõ alkalmazásra
HK1082662A1 (zh) 2002-05-30 2006-06-16 King Pharmaceuticals Research And Development Inc. 具有三环吡唑并三唑并嘧啶环结构的制药活性化合物及其使用方法
US20060106040A1 (en) * 2002-12-19 2006-05-18 Michael Grzelak Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
EP2295047A3 (en) * 2002-12-19 2011-05-18 Schering Corporation Use of adenosine A2a receptor antagonists for the treatment of restless leg syndrome and other movement disorders
EP1618109A2 (en) 2003-04-09 2006-01-25 Biogen Idec MA Inc. Triazolo[1,5-c]pyrimidines and pyrazolo[1,5-c]pyrimidines useful as a2a adenosine receptor antagonists
PT1622912E (pt) * 2003-04-23 2009-08-17 Schering Corp Antagonistas 2-alcinil- e 2-alcenilpirazolo-[4,3-b]-1,2,4- triazolo-[1,5-c]-pirimidina do receptor a2a da adenosina
WO2004108137A1 (en) * 2003-06-10 2004-12-16 Kyowa Hakko Kogyo Co., Ltd. A method of treating an anxiety disorder
EP1636187A1 (en) * 2003-06-12 2006-03-22 Novo Nordisk A/S Substituted piperazine carbamates for use as inhibitors of hormone sensitive lipase
EP1678168B1 (en) * 2003-10-24 2012-07-11 Exelixis, Inc. P70s6 kinase modulators and method of use
DK1678182T3 (da) 2003-10-28 2007-06-04 Schering Corp Fremgangsmåde til fremstilling af substituerede 5-amino-pyrazolo[4,3-E]-1,2,4-triazolo-[1,5-C]pyrimidiner
ATE377599T1 (de) * 2003-12-01 2007-11-15 Schering Corp Verfahren zur herstellung von substituierten 5- aminopyrazolo(4,3-e)-1,2,4-triazolo(1,5- c)pyrimidinen
JP2007514758A (ja) * 2003-12-19 2007-06-07 シェーリング コーポレイション 医薬組成物
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
ATE556712T1 (de) * 2005-06-07 2012-05-15 Kyowa Hakko Kirin Co Ltd A2a antagonisten zur behandlung von motorischen störungen
WO2007035542A1 (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
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.
US20090298878A1 (en) * 2006-07-14 2009-12-03 Akira Matsumura Oxime compounds and the use thereof
TW200840566A (en) * 2006-12-22 2008-10-16 Esteve Labor Dr Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments
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
WO2009114533A2 (en) 2008-03-10 2009-09-17 Cornell University Modulation of blood brain barrier permeability
WO2009110955A2 (en) * 2008-02-29 2009-09-11 Albert Einstein College Of Medicine Of Yeshiva University Ketoconazole-derivative antagonists of human pregnane x receptor and uses thereof
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
TWI473614B (zh) * 2008-05-29 2015-02-21 Kyowa Hakko Kirin Co Ltd Anti-analgesic inhibitors
EP2322223A4 (en) 2008-07-23 2012-08-22 Kyowa Hakko Kirin Co Ltd THERAPEUTIC AGENT AGAINST MIGRAINE
US20100093702A1 (en) * 2008-10-13 2010-04-15 Barbay J Kent METHYLENE AMINES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS
CA2748174A1 (en) 2008-12-30 2010-07-08 Arqule, Inc. Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds
US20120053182A1 (en) 2009-01-20 2012-03-01 Schering Corporation Methods of alleviating or treating signs and/or symptoms associated with moderate to severe parkinson's disease
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
WO2010103547A2 (en) 2009-03-13 2010-09-16 Advinus Therapeutics Private Limited Substituted fused pyrimidine compounds
US8343961B2 (en) 2009-03-31 2013-01-01 Arqule, Inc. Substituted heterocyclic compounds
WO2010147941A1 (en) 2009-06-15 2010-12-23 Marvell World Trade Ltd. System and methods for gamut bounded saturation adaptive color enhancement
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
BR112012006572A2 (pt) 2009-09-25 2016-04-26 Oryzon Genomics Sa inibidores de demetilase-1 de lisina específicos e seu uso
EP2486002B1 (en) 2009-10-09 2019-03-27 Oryzon Genomics, S.A. Substituted heteroaryl- and aryl- cyclopropylamine acetamides and their use
WO2011101861A1 (en) 2010-01-29 2011-08-25 Msn Laboratories Limited Process for preparation of dpp-iv inhibitors
US9616058B2 (en) 2010-02-24 2017-04-11 Oryzon Genomics, S.A. Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use
WO2011106106A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
JP5868948B2 (ja) 2010-04-19 2016-02-24 オリゾン・ジェノミックス・ソシエダッド・アノニマOryzon Genomics S.A. リジン特異的脱メチル化酵素1阻害薬およびその使用
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
ES2674747T3 (es) 2010-07-29 2018-07-03 Oryzon Genomics, S.A. Inhibidores de demetilasa LSD1 basados en arilciclopropilamina y sus usos médicos
CN103261202B (zh) * 2010-09-24 2016-01-20 阿迪维纳斯疗法有限公司 作为腺苷受体拮抗剂的稠合三环化合物
WO2012045883A1 (en) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Cyclopropylamine inhibitors of oxidases
WO2012072713A2 (en) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with flaviviridae
EP3981395A1 (en) 2011-02-08 2022-04-13 Oryzon Genomics, S.A. Lysine demethylase inhibitors for myeloproliferative disorders
WO2012129381A1 (en) * 2011-03-22 2012-09-27 Concert Pharmaceuticals Inc. Deuterated preladenant
WO2012127472A1 (en) * 2011-03-22 2012-09-27 Mapi Pharma Ltd. Process and intermediates for the preparation of preladenant and related compounds
WO2013024474A1 (en) * 2011-08-18 2013-02-21 Mapi Phrarma Ltd. Polymorphs of preladenant
RU2668952C2 (ru) 2011-10-20 2018-10-05 Оризон Дженомикс, С.А. (гетеро)арилциклопропиламины в качестве ингибиторов lsd1
EP2768805B1 (en) 2011-10-20 2020-03-25 Oryzon Genomics, S.A. (hetero)aryl cyclopropylamine compounds as lsd1 inhibitors
WO2014071512A1 (en) * 2012-11-06 2014-05-15 Universite Laval Combination therapy and methods for the treatment of respiratory diseases
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
MX381180B (es) 2014-11-18 2025-03-12 Merck Sharp & Dohme Compuestos aminopirazina con propiedades antagonistas a2a.
WO2016126570A1 (en) 2015-02-06 2016-08-11 Merck Sharp & Dohme Corp. Aminoquinazoline compounds as a2a antagonist
WO2016200717A1 (en) 2015-06-11 2016-12-15 Merck Sharp & Dohme Corp. Aminopyrazine compounds with a2a antagonist properties
WO2017008205A1 (en) 2015-07-10 2017-01-19 Merck Sharp & Dohme Corp. Substituted aminoquinazoline compounds as a2a antagonist
US9675585B1 (en) 2016-03-24 2017-06-13 Ezra Pharma Extended release pharmaceutical formulations
US9687475B1 (en) 2016-03-24 2017-06-27 Ezra Pharma Llc Extended release pharmaceutical formulations with controlled impurity levels
WO2018178338A1 (en) * 2017-03-30 2018-10-04 Iteos Therapeutics 2-oxo-thiazole derivatives as a2a inhibitors and compounds for use in the treatment of cancers
CN110678472B (zh) * 2017-03-30 2023-01-24 伊忒欧斯比利时股份公司 作为a2a抑制剂的2-氧代噻唑衍生物和用于治疗癌症的化合物
EP3723754A4 (en) 2017-12-13 2021-05-19 Merck Sharp & Dohme Corp. IMIDAZO [1,2-C] QUINAZOLINE-5-AMINE COMPOUNDS WITH PROPERTIES OF A2A ANTAGONIST
WO2019135259A1 (en) * 2018-01-04 2019-07-11 Impetis Biosciences Ltd. Tricyclic compounds, compositions and medicinal applications thereof
CR20230030A (es) 2018-02-27 2023-03-10 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b (divisional 2020-0441)
CN108276345A (zh) * 2018-03-22 2018-07-13 重庆奥舍生物化工有限公司 一种药物中间体嘧啶-5-甲醛的制备方法
JP2021520392A (ja) * 2018-04-08 2021-08-19 ベイジーン リミテッド A2a受容体アンタゴニストとしてのピラゾロトリアゾロピリミジン誘導体
MX2020012376A (es) 2018-05-18 2021-03-09 Incyte Corp Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b.
CN108864114B (zh) * 2018-06-04 2020-11-06 应世生物科技(南京)有限公司 选择性a2a受体拮抗剂
MX2021000116A (es) 2018-07-05 2021-03-29 Incyte Corp Derivados de pirazina fusionados como inhibidores de a2a/a2b.
CN110742893B (zh) * 2018-07-23 2024-04-05 百济神州(北京)生物科技有限公司 A2a受体拮抗剂治疗癌症的方法
PE20211768A1 (es) 2018-11-30 2021-09-07 Merck Sharp & Dohme Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmaceuticas y su uso
BR112021011948A2 (pt) 2018-12-20 2021-09-08 Incyte Corporation Compostos de imidazopiridazina e imidazopiridina e usos dos mesmos
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
WO2020227156A1 (en) * 2019-05-03 2020-11-12 Nektar Therapeutics Adenosine 2 receptor antagonists
DE102019116986A1 (de) 2019-06-24 2020-12-24 Helmholtz-Zentrum Dresden-Rossendorf E. V. Deuterierte 7-(3-(4-(2-([18F]Fluor)ethoxy)phenyl)propyl)-2-(furan-2-yl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amin-Derivate
JP2022540583A (ja) * 2019-07-17 2022-09-16 テオン セラピューティクス,インク. アデノシンa2a受容体アンタゴニスト及びその使用
CN112608330B (zh) 2019-07-30 2021-09-28 杭州阿诺生物医药科技有限公司 A2a和/或a2b受体抑制剂
CN112574214B (zh) 2019-07-30 2021-09-28 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂的制备方法
CN111072675A (zh) * 2019-12-12 2020-04-28 广东东阳光药业有限公司 含氮稠合三环衍生物及其用途
CN113773327B (zh) * 2021-09-13 2022-07-15 八叶草健康产业研究院(厦门)有限公司 一种吡唑并嘧啶并三唑环类化合物的制备方法
CN118812544A (zh) * 2024-06-19 2024-10-22 厦门大学 一种腺苷a2ar靶向小分子化合物、核素标记探针及其制备方法、应用和药物组合物
CN118812539B (zh) * 2024-06-19 2025-11-28 苏州大学 一种5-氨基三唑并嘧啶衍生物及其制备方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3677445D1 (de) 1985-09-30 1991-03-14 Ciba Geigy Ag 2-substituierte-e-kondensierte(1,5-c)-pyrimidine, pharmazeutische zubereitungen und ihre verwendung.
SU1739850A3 (ru) * 1987-08-31 1992-06-07 Такеда Кемикал Индастриз, Лтд (Фирма) Способ получени конденсированных производных пиразоло[3,4- @ ]пиримидина
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
WO1995003806A1 (en) 1993-07-27 1995-02-09 Kyowa Hakko Kogyo Co., Ltd. Remedy for parkinson's disease
IT1277392B1 (it) 1995-07-28 1997-11-10 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina
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
IL152726A0 (en) * 2000-05-26 2003-06-24 Schering Corp Adenosine a2a receptor antagonists
HUP0402018A3 (en) * 2001-11-30 2008-06-30 Schering Corp 5-amino-7h-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine derivatives, their use and pharmaceutical compositions containing them
EP2295047A3 (en) * 2002-12-19 2011-05-18 Schering Corporation Use of adenosine A2a receptor antagonists for the treatment of restless leg syndrome and other movement disorders
DK1678182T3 (da) * 2003-10-28 2007-06-04 Schering Corp Fremgangsmåde til fremstilling af substituerede 5-amino-pyrazolo[4,3-E]-1,2,4-triazolo-[1,5-C]pyrimidiner
ATE377599T1 (de) * 2003-12-01 2007-11-15 Schering Corp Verfahren zur herstellung von substituierten 5- aminopyrazolo(4,3-e)-1,2,4-triazolo(1,5- c)pyrimidinen
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
WO2007035542A1 (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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007145875A (ja) * 2000-05-26 2007-06-14 Schering Plough Corp アデノシンa2aレセプターアンタゴニスト

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