CN1247588C - 腺苷A2a受体拮抗剂 - Google Patents

腺苷A2a受体拮抗剂 Download PDF

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Publication number
CN1247588C
CN1247588C CNB018134491A CN01813449A CN1247588C CN 1247588 C CN1247588 C CN 1247588C CN B018134491 A CNB018134491 A CN B018134491A CN 01813449 A CN01813449 A CN 01813449A CN 1247588 C CN1247588 C CN 1247588C
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China
Prior art keywords
alkyl
alkoxy
mmol
compound
phenyl
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Expired - Lifetime
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CNB018134491A
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English (en)
Chinese (zh)
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CN1451007A (zh
Inventor
B·R·纽斯塔德特
N·A·林多
W·J·格林李
D·图尔施安
L·S·西尔弗曼
夏岩
C·D·博伊尔
S·查卡拉曼尼尔
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Merck Sharp and Dohme LLC
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Schering Corp
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    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/24—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
    • A61P25/28—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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CNB018134491A 2000-05-26 2001-05-24 腺苷A2a受体拮抗剂 Expired - Lifetime CN1247588C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20714300P 2000-05-26 2000-05-26
US60/207,143 2000-05-26

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CNB2006100049297A Division CN100384847C (zh) 2000-05-26 2001-05-24 腺苷A2a受体拮抗剂

Publications (2)

Publication Number Publication Date
CN1451007A CN1451007A (zh) 2003-10-22
CN1247588C true CN1247588C (zh) 2006-03-29

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CNB018134491A Expired - Lifetime CN1247588C (zh) 2000-05-26 2001-05-24 腺苷A2a受体拮抗剂
CNB2006100049297A Expired - Lifetime CN100384847C (zh) 2000-05-26 2001-05-24 腺苷A2a受体拮抗剂

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US (4) US6630475B2 (enExample)
EP (1) EP1283839B1 (enExample)
JP (3) JP4574112B2 (enExample)
KR (1) KR100520907B1 (enExample)
CN (2) CN1247588C (enExample)
AR (1) AR028621A1 (enExample)
AT (1) ATE293627T1 (enExample)
AU (2) AU2001268089C1 (enExample)
BR (1) BRPI0111015B8 (enExample)
CA (1) CA2410237C (enExample)
CZ (1) CZ303790B6 (enExample)
DE (1) DE60110219T2 (enExample)
DK (1) DK1283839T3 (enExample)
EC (1) ECSP024364A (enExample)
ES (1) ES2237576T3 (enExample)
HK (1) HK1049007B (enExample)
HU (1) HU230420B1 (enExample)
IL (3) IL152726A0 (enExample)
MX (1) MXPA02011625A (enExample)
MY (1) MY132006A (enExample)
NO (1) NO325008B1 (enExample)
NZ (1) NZ522326A (enExample)
PE (1) PE20020062A1 (enExample)
PL (1) PL218764B1 (enExample)
PT (1) PT1283839E (enExample)
RU (1) RU2315053C2 (enExample)
SI (1) SI1283839T1 (enExample)
SK (1) SK287748B6 (enExample)
TW (1) TWI288137B (enExample)
WO (1) WO2001092264A1 (enExample)
ZA (1) ZA200208898B (enExample)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1283839B1 (en) * 2000-05-26 2005-04-20 Schering Corporation Adenosine a2a receptor antagonists
EP1425017A1 (en) * 2001-09-13 2004-06-09 Schering Corporation Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic
MY124864A (en) 2001-10-15 2006-07-31 Schering Corp Adenosine a2a receptor antagonists
FR2832405B1 (fr) * 2001-11-19 2004-12-10 Sanofi Synthelabo Tetrahydropyridyl-alkyl-heterocycles azotes, procede pour leur preparation et compositions pharmaceutiques les contenant
US6916811B2 (en) * 2001-11-30 2005-07-12 Schering Corporation Adenosine A2a receptor antagonists
AR038366A1 (es) 2001-11-30 2005-01-12 Schering Corp Compuestos de 1,2,4-triazolo [1,5-c] pirimidinas sustituidas, antagonistas del receptor de adenosina a2a, composiciones farmaceuticas, el uso de dichos compuestos para la manufactura de un medicamento para el tratamiento de enfermedades del sistema nervioso central y un kit que comprende combinacion
US6875772B2 (en) 2001-11-30 2005-04-05 Schering Corporation [1,2,4]-Triazole bicyclic adeonsine A2a receptor antagonists
US20040198753A1 (en) 2002-01-28 2004-10-07 Hiroshi Kase Methods of treating patients suffering from movement disorders
BR0304963A (pt) * 2002-05-30 2004-09-28 King Pharmaceuticals Res & Dev Compostos, composição farmacêutica, e, métodos para modular a atividade de adenosina em um mamìfero, e para tratar um mamìfero sofrendo de ou suscetìvel às doenças
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
BR0317436A (pt) * 2002-12-19 2005-11-16 Schering Corp Usos de antagonistas do receptor a2a de adenosina
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
MY139344A (en) * 2003-04-23 2009-09-30 Schering Corp 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine a2a receptor antagonists
KR20060037252A (ko) * 2003-06-10 2006-05-03 교와 핫꼬 고교 가부시끼가이샤 불안 장애의 치료 방법
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
HRP20070063T3 (hr) * 2003-10-28 2007-04-30 Schering Corporation POSTUPAK DOBIVANJA SUPSTITUIRANIH 5-AMINOPIRAZOLO[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA
ES2293380T3 (es) 2003-12-01 2008-03-16 Schering Corporation Procedimiento para preparar 5-amino-pirazolo-(4,3-e)-1,2,4-triazolo(1,5-c)pirimidinas sustituidos.
US20060009504A1 (en) * 2003-12-19 2006-01-12 Schering Corporation Pharmaceutical compositions
ES2342082T3 (es) * 2004-04-21 2010-07-01 Schering Corporation Antagonistas de receptores a2a de adenosina de pirazolo(4,3-e)-1,2,4-triazolo(1,5-c)pirimidina.
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
CN101312978A (zh) * 2005-09-19 2008-11-26 先灵公司 作为腺苷A2a受体拮抗剂的2－杂芳基－吡唑并－[4,3－e]－1,2,4－三唑并－[1,5－c]－嘧啶
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.
EP2040698A4 (en) * 2006-07-14 2011-08-10 Shionogi & Co OXIM CONNECTIONS AND ITS USE
TW200840566A (en) * 2006-12-22 2008-10-16 Esteve Labor Dr Heterocyclyl-substituted-ethylamino-phenyl derivatives, their preparation and use as medicaments
US7723343B2 (en) 2007-03-30 2010-05-25 King Pharmaceuticals Research And Development, Inc. Adenosine A2A receptor antagonists
US8669260B2 (en) * 2008-02-29 2014-03-11 Albert Einstein College Of Medicine Of Yeshiva University Ketoconazole-derivative antagonist of human pregnane X receptor and uses thereof
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
US20110064671A1 (en) 2008-03-10 2011-03-17 Cornell University Modulation of blood brain barrier permeability
TWI473614B (zh) 2008-05-29 2015-02-21 Kyowa Hakko Kirin Co Ltd Anti-analgesic inhibitors
WO2010010908A1 (ja) 2008-07-23 2010-01-28 協和発酵キリン株式会社 片頭痛治療剤
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
TW201036614A (en) 2008-12-30 2010-10-16 Arqule Inc Substituted 1H-pyrazolo[3,4-d]pyrimidine-6-amine compounds
MX2011007678A (es) 2009-01-20 2011-08-08 Schering Corp Metodos para aliviar o tratar señales y/o sintomas asociados con enfermedad de parkinson de moderada a severa.
EP2389362B1 (en) 2009-01-21 2019-12-11 Oryzon Genomics, S.A. Phenylcyclopropylamine derivatives and their medical use
BRPI1009398A2 (pt) 2009-03-13 2016-03-08 Advinus Therapeutics Private Ltd compostos de pirimidina fundida substituída
EP2414361A1 (en) 2009-03-31 2012-02-08 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
KR101736218B1 (ko) 2009-09-25 2017-05-16 오리존 지노믹스 에스.에이. 라이신 특이적 디메틸라아제-1 억제제 및 이의 용도
US8946296B2 (en) 2009-10-09 2015-02-03 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
WO2011106573A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Lysine demethylase inhibitors for diseases and disorders associated with hepadnaviridae
WO2011106574A2 (en) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibitors for antiviral use
BR122019020471B1 (pt) 2010-04-19 2021-06-22 Oryzon Genomics S.A. Inibidores da desmetilase específica para lisina 1, seus usos e método para sua identificação, e composições farmacêuticas
US9006449B2 (en) 2010-07-29 2015-04-14 Oryzon Genomics, S.A. Cyclopropylamine derivatives useful as LSD1 inhibitors
WO2012013728A1 (en) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Arylcyclopropylamine based demethylase inhibitors of lsd1 and their medical use
US9006177B2 (en) * 2010-09-24 2015-04-14 Advinus Therapeutics Limited Fused tricyclic compounds as adenosine receptor antagonist
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
WO2012127472A1 (en) * 2011-03-22 2012-09-27 Mapi Pharma Ltd. Process and intermediates for the preparation of preladenant and related compounds
WO2012129381A1 (en) * 2011-03-22 2012-09-27 Concert Pharmaceuticals Inc. Deuterated preladenant
WO2013024474A1 (en) * 2011-08-18 2013-02-21 Mapi Phrarma Ltd. Polymorphs of preladenant
UA116765C2 (uk) 2011-10-20 2018-05-10 Орізон Джіномікс, С.А. (гетеро)арилциклопропіламіни як інгібітори lsd1
CN104203914B (zh) 2011-10-20 2017-07-11 奥瑞泽恩基因组学股份有限公司 作为lsd1抑制剂的(杂)芳基环丙胺化合物
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
KR20170083136A (ko) 2014-11-18 2017-07-17 머크 샤프 앤드 돔 코포레이션 A2a 길항제 특성을 갖는 아미노피라진 화합물
EP3253390B1 (en) 2015-02-06 2022-04-13 Merck Sharp & Dohme Corp. Aminoquinazoline compounds as a2a antagonist
EP3307067B1 (en) 2015-06-11 2022-11-02 Merck Sharp & Dohme LLC Aminopyrazine compounds with a2a antagonist properties
WO2017008205A1 (en) 2015-07-10 2017-01-19 Merck Sharp & Dohme Corp. Substituted aminoquinazoline compounds as a2a antagonist
US9687475B1 (en) 2016-03-24 2017-06-27 Ezra Pharma Llc Extended release pharmaceutical formulations with controlled impurity levels
US9675585B1 (en) 2016-03-24 2017-06-13 Ezra Pharma Extended release pharmaceutical formulations
TWI801372B (zh) * 2017-03-30 2023-05-11 比利時商艾特歐斯比利時有限公司 作為a2a抑制劑的硫胺甲酸酯衍生物以及用於癌症治療的方法
LT3601296T (lt) * 2017-03-30 2022-09-26 iTeos Belgium SA 2-okso-tiazolo derivatai kaip a2a inhibitoriai ir junginiai, skirti naudoti gydant vėžį
US11498923B2 (en) 2017-12-13 2022-11-15 Merck Sharp & Dohme Llc Substituted imidazo[1,2-c]quinazolines as A2A antagonists
JP7361697B2 (ja) * 2018-01-04 2023-10-16 インペティス・バイオサイエンシーズ・リミテッド 三環性化合物、組成物及びその医薬品用途
MA52422A (fr) 2018-02-27 2021-01-06 Incyte Corp Imidazopyrimidines et triazolopyrimidines en tant qu'inhibiteurs a2a/a2b
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
MX2020010618A (es) * 2018-04-08 2020-11-12 Beigene Ltd Derivados de pirazolotriazolopiriminina como antagonista del receptor a2a.
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
MA53097A (fr) 2018-07-05 2021-05-12 Incyte Corp Dérivés de pyrazine fusionnés en tant qu'inhibiteurs d'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
CR20210271A (es) 2018-11-30 2021-07-14 Merck Sharp & Dohme Derivados de amino triazolo quinazolina 9-sustituidos como antagonistas del receptor de adenosina, composiciones farmacéuticas y su uso
MA54551A (fr) 2018-12-20 2021-10-27 Incyte Corp Composés d'imidazopyridazine et d'imidazopyridine utilisés en tant qu'inhibiteurs de la kinase 2 de type récepteur de l'activine
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
US12325708B2 (en) 2019-05-03 2025-06-10 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
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
CN111825698B (zh) 2019-07-30 2021-10-15 杭州阿诺生物医药科技有限公司 腺苷受体拮抗剂
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
EP0217748B1 (en) 1985-09-30 1991-02-06 Ciba-Geigy Ag 2-Substituted-e-fused-[1,2,4,]triazolo-[1,5-c]pyrimidines pharmaceutical compositions and uses thereof
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
CA2144330A1 (en) 1993-07-27 1995-02-09 Fumio Suzuki A therapeutic agent 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
EP1283839B1 (en) * 2000-05-26 2005-04-20 Schering Corporation Adenosine a2a receptor antagonists
US6916811B2 (en) * 2001-11-30 2005-07-12 Schering Corporation Adenosine A2a receptor antagonists
BR0317436A (pt) * 2002-12-19 2005-11-16 Schering Corp Usos de antagonistas do receptor a2a de adenosina
HRP20070063T3 (hr) * 2003-10-28 2007-04-30 Schering Corporation POSTUPAK DOBIVANJA SUPSTITUIRANIH 5-AMINOPIRAZOLO[4,3-e]-1,2,4-TRIAZOLO[1,5-c]PIRIMIDINA
ES2293380T3 (es) * 2003-12-01 2008-03-16 Schering Corporation Procedimiento para preparar 5-amino-pirazolo-(4,3-e)-1,2,4-triazolo(1,5-c)pirimidinas sustituidos.
ES2342082T3 (es) * 2004-04-21 2010-07-01 Schering Corporation Antagonistas de receptores a2a de adenosina de pirazolo(4,3-e)-1,2,4-triazolo(1,5-c)pirimidina.
CN101312978A (zh) * 2005-09-19 2008-11-26 先灵公司 作为腺苷A2a受体拮抗剂的2－杂芳基－吡唑并－[4,3－e]－1,2,4－三唑并－[1,5－c]－嘧啶

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