AU2001268089C1 - Adenosine A2a receptor antagonists - Google Patents
Adenosine A2a receptor antagonists Download PDFInfo
- Publication number
- AU2001268089C1 AU2001268089C1 AU2001268089A AU2001268089A AU2001268089C1 AU 2001268089 C1 AU2001268089 C1 AU 2001268089C1 AU 2001268089 A AU2001268089 A AU 2001268089A AU 2001268089 A AU2001268089 A AU 2001268089A AU 2001268089 C1 AU2001268089 C1 AU 2001268089C1
- Authority
- AU
- Australia
- Prior art keywords
- alkyl
- alkoxy
- compound
- formula
- mmol
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired
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
- A61P25/08—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
Landscapes
- 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)
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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| AU2001268089A1 AU2001268089A1 (en) | 2002-02-28 |
| AU2001268089B2 AU2001268089B2 (en) | 2005-04-28 |
| AU2001268089C1 true AU2001268089C1 (en) | 2006-04-13 |
Family
ID=22769372
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2001268089A Expired AU2001268089C1 (en) | 2000-05-26 | 2001-05-24 | Adenosine A2a receptor antagonists |
| AU6808901A Pending AU6808901A (en) | 2000-05-26 | 2001-05-24 | Adenosine a2a receptor antagonists |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU6808901A Pending AU6808901A (en) | 2000-05-26 | 2001-05-24 | Adenosine a2a receptor antagonists |
Country Status (31)
| Country | Link |
|---|---|
| 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)
| 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 |
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| 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 |
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| EP3981395A1 (en) | 2011-02-08 | 2022-04-13 | Oryzon Genomics, S.A. | Lysine demethylase inhibitors for myeloproliferative disorders |
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| 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 |
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| 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 |
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| 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 |
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| 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 |
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| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995001356A1 (en) * | 1993-06-29 | 1995-01-12 | Schering-Plough S.P.A. | 1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE HETEROCYCLIC ANALOGUES HAVING ANTAGONISTIC ACTIVITY ON ADENOSINE A2 RECEPTOR |
| WO1998052568A1 (en) * | 1997-05-21 | 1998-11-26 | Schering-Plough S.P.A. | THE USE OF 1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE HETEROCYCLIC ANALOGUES FOR THE PREPARATION OF MEDICAMENTS USEFUL FOR THE TREATMENT OF CEREBROVASCULAR DISTURBANCES |
| US5935964A (en) * | 1995-07-28 | 1999-08-10 | Schering Corporation | 1,2,4-triazolo 1,5-c! pyrimidine heterocyclic analogues having antagonistic activity on adenosine A2a receptor |
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| 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 |
| CA2144330A1 (en) | 1993-07-27 | 1995-02-09 | Fumio Suzuki | A therapeutic agent for parkinson's disease |
| 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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| WO1995001356A1 (en) * | 1993-06-29 | 1995-01-12 | Schering-Plough S.P.A. | 1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE HETEROCYCLIC ANALOGUES HAVING ANTAGONISTIC ACTIVITY ON ADENOSINE A2 RECEPTOR |
| US5935964A (en) * | 1995-07-28 | 1999-08-10 | Schering Corporation | 1,2,4-triazolo 1,5-c! pyrimidine heterocyclic analogues having antagonistic activity on adenosine A2a receptor |
| WO1998052568A1 (en) * | 1997-05-21 | 1998-11-26 | Schering-Plough S.P.A. | THE USE OF 1,2,4-TRIAZOLO[1,5-c]PYRIMIDINE HETEROCYCLIC ANALOGUES FOR THE PREPARATION OF MEDICAMENTS USEFUL FOR THE TREATMENT OF CEREBROVASCULAR DISTURBANCES |
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