ECSP024364A - Antagonistas receptores de adenosina a2a - Google Patents
Antagonistas receptores de adenosina a2aInfo
- Publication number
- ECSP024364A ECSP024364A EC2002004364A ECSP024364A ECSP024364A EC SP024364 A ECSP024364 A EC SP024364A EC 2002004364 A EC2002004364 A EC 2002004364A EC SP024364 A ECSP024364 A EC SP024364A EC SP024364 A ECSP024364 A EC SP024364A
- Authority
- EC
- Ecuador
- Prior art keywords
- phenyl
- optionally substituted
- adenosine
- antagonists
- receiving
- Prior art date
Links
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 title 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 title 1
- 229960005305 adenosine Drugs 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical class 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000003884 phenylalkyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
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)
- 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)
Abstract
Compuestos que tienen la fórmula estructural I o una de los mismos farmacéuticamente aceptables, en la cual R es fenilo opcionalmente substituido, cicloalquenilo o heteroarilo X es alquileno o C(O) CH2 Y es N(R2) CH2 CH2 (R3)-, -OCH2 CH2 N (R2)-, -0-, -S-, -ch2s-, - (ch2 (2-NH-,o opcionalmente substituido, - (gráfico)- r myn son 2-3, y- Q es nitrógeno o carbono opcionalmente sustituido; Z es fenilo opcionalmente sustituido, fenilo, fenilalquilo o heteroarilo, difenilmetilo (gráfico) R6_ C(0=-, R6_SO2-, R6-0C(o)-, R7- N (R8)-C (0)-, R7- N (R8)-C(S)-, fenilo- CH (OH)-, o fenilo- C-(= NOR2)-; 0 cuando Q es CH, fenilamino 0 piridilamino; 0 Z y Y conjuntamente son piperidinilo substituido o fenilo substituido; y R2, R3, R6, R7, y R8 son tal como se han definido en la memoria, y su uso para el tratamiento de enfermedad de Parkinson, solo o en combinación con otros agentes para tratar la enfermedad de Parkinson, y las composiciones farmacéuticas que los comprenden; y se describe también un procedimiento para preparar intermedio útiles para preparar los compuestos de la fórmula I.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20714300P | 2000-05-26 | 2000-05-26 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP024364A true ECSP024364A (es) | 2003-03-31 |
Family
ID=22769372
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2002004364A ECSP024364A (es) | 2000-05-26 | 2002-11-25 | Antagonistas receptores de adenosina a2a |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US6630475B2 (es) |
| EP (1) | EP1283839B1 (es) |
| JP (3) | JP4574112B2 (es) |
| KR (1) | KR100520907B1 (es) |
| CN (2) | CN100384847C (es) |
| AR (1) | AR028621A1 (es) |
| AT (1) | ATE293627T1 (es) |
| AU (2) | AU2001268089C1 (es) |
| BR (1) | BRPI0111015B8 (es) |
| CA (1) | CA2410237C (es) |
| CZ (1) | CZ303790B6 (es) |
| DE (1) | DE60110219T2 (es) |
| DK (1) | DK1283839T3 (es) |
| EC (1) | ECSP024364A (es) |
| ES (1) | ES2237576T3 (es) |
| HK (1) | HK1049007B (es) |
| HU (1) | HU230420B1 (es) |
| IL (3) | IL152726A0 (es) |
| MX (1) | MXPA02011625A (es) |
| MY (1) | MY132006A (es) |
| NO (1) | NO325008B1 (es) |
| NZ (1) | NZ522326A (es) |
| PE (1) | PE20020062A1 (es) |
| PL (1) | PL218764B1 (es) |
| PT (1) | PT1283839E (es) |
| RU (1) | RU2315053C2 (es) |
| SI (1) | SI1283839T1 (es) |
| SK (1) | SK287748B6 (es) |
| TW (1) | TWI288137B (es) |
| WO (1) | WO2001092264A1 (es) |
| ZA (1) | ZA200208898B (es) |
Families Citing this family (88)
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| FR2832405B1 (fr) * | 2001-11-19 | 2004-12-10 | Sanofi Synthelabo | Tetrahydropyridyl-alkyl-heterocycles azotes, procede pour leur preparation et compositions pharmaceutiques les contenant |
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| 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 |
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| 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 |
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| ES2273599B1 (es) | 2005-10-14 | 2008-06-01 | Universidad De Barcelona | Compuestos para el tratamiento de la fibrilacion auricular. |
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| 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 |
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| 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 |
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