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1. 发明申请

WO2007121920A3 PURINE DERIVATIVES FOR USE AS ADENOSIN A2A RECEPTOR AGONISTS 审中-公开
标题翻译：用作腺苷A2A受体激动剂的嘌呤衍生物
公开(公告)号：WO2007121920A3
公开(公告)日：2008-01-10
申请号：PCT/EP2007003435
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN , COX BRIAN
发明人： FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN , COX BRIAN
IPC分类号： C07D473/16 , A61K31/52 , A61K31/7076 , A61P29/00 , C07D473/18 , C07D473/34 , C07H19/167
CPC分类号： C07D473/16 , C07D473/34
摘要： Purine derivatives of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 are as defined herein. The compounds are useful for the treatment of a condition mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions comprising a purine derivative as active ingredient and a process for the preparation of these compounds.
摘要翻译：式（I）的嘌呤衍生物或其立体异构体或其药学上可接受的盐，其中R 1，R 2和R 3如本文所定义。该化合物可用于治疗由腺苷A2A受体的活化介导的病症，特别是炎性或阻塞性气道疾病。包含嘌呤衍生物作为活性成分的药物组合物和这些化合物的制备方法。

2. 发明申请

WO2007147659A1 ADENOSINE A3 RECEPTOR AGONISTS 审中-公开
标题翻译：腺苷A3受体激动剂
公开(公告)号：WO2007147659A1
公开(公告)日：2007-12-27
申请号：PCT/EP2007/053847
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： C07D403/08 , C07D473/00 , A61K31/52
CPC分类号： C07D473/34 , C07D473/40
摘要： A compound of formula (I) and their preparation and use as pharmaceuticals wherein R 1 , R 2 and R 3 are as defined herein.
摘要翻译：式（I）化合物及其制备和用途，其中R 1，R 2，

3. 发明申请

WO2006097260A1 ADENOSINE DERIVATIVES HAVING A2A RECEPTOR ACTIVITY 审中-公开
标题翻译：具有A2A受体活性的腺苷衍生物
公开(公告)号：WO2006097260A1
公开(公告)日：2006-09-21
申请号：PCT/EP2006/002281
申请日：2006-03-13
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： C07H19/167 , C07D473/16 , C07D473/00 , A61K31/7076 , A61P9/00
CPC分类号： C07D473/00 , C07D473/16 , C07H19/167
摘要： Compounds of (I), or stereoisomers or pharmaceutically acceptable salts thereof, where W, R 1 , R 2 , R 3 and R 4 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A 2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：（I）的化合物或其立体异构体或其药学上可接受的盐，其中W，R 1，R 2，R 3和R SUP > 4 具有说明书中所示的含义，可用于治疗由腺苷A 2A受体的活化介导的病症，特别是炎性或阻塞性气道疾病。还描述了含有化合物的药物组合物和制备该化合物的方法。

4. 发明申请

WO2006045552A1 PURINE DERIVATIVES FOR USE AS ADENOSIN A-2A RECEPTOR AGONISTS 审中-公开
标题翻译：用作腺苷A-2A受体激动剂的嘌呤衍生物
公开(公告)号：WO2006045552A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/011344
申请日：2005-10-21
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John , SINGH, Paul
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John , SINGH, Paul
IPC分类号： C07D473/16 , C07D473/32 , C07D473/40 , A61K31/52 , A61P29/00
CPC分类号： C07D473/32 , C07D473/16 , C07D473/40
摘要： Compounds of formula (I) in free or salt form, wherein R 1 , R 2 and R 3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A 2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：游离或盐形式的其中R 1，R 2和R 3的式（I）化合物具有如说明书中所示的含义可用于治疗腺苷A 2A受体激活介导的病症，特别是炎性或阻塞性气道疾病。还描述了含有化合物的药物组合物和制备该化合物的方法。

5. 发明申请

WO2005070926A1 THIAZOLE DERIVATIVES AS A2B ANTAGONISTS 审中-公开
标题翻译：噻唑衍生物作为A2B拮抗剂
公开(公告)号：WO2005070926A1
公开(公告)日：2005-08-04
申请号：PCT/EP2005/000542
申请日：2005-01-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , PRESS, Neil, John , TAYLOR, Roger, John
发明人： PRESS, Neil, John , TAYLOR, Roger, John
IPC分类号： C07D417/04
CPC分类号： C07D417/04 , C07D417/14
摘要： Compounds of formula (I) in free or salt form, where Ar is phenyl substituted by one or more substituents selected from halogen, cyano and C 1- C 8 -haloalkyl, or naphthyl, R 1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkoxy-C l -C 8 alkyl, carboxy, C 1 -C 8 -alkoxycarbonyl and acyloxy, or R 1 is a 5- or 6- membered monovalent heterocyclic group, R 2 is hydrogen, C l -C 8 -alkyl, acyl or -CON(R 3 )R 4 , R 3 and R 4 are each independently hydrogen or C 1 -C s -alkyl, or together with the nitrogen atom to which they are attached denote a 5- or 6- membered heterocyclic group, and Y is a pyrimidinyl or pyridazinyl group, optionally substituted by at least one C 1 -C s -alkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -alkylthio, C 1 -C 8 -alkyl amino, di(C l -C 8 -alkyl) amino or acylamino group. The compounds are useful as pharmaceuticals.
摘要翻译：式（I）化合物为游离或盐形式，其中Ar为被一个或多个选自卤素，氰基和C 1 -C 8 - 卤代烷基或萘基的取代基取代的苯基，R 1为氢，任选被一个或多个更多选自卤素，氰基，羟基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷氧基-C 1 -C 8烷基，羧基，C 1 -C 8 - 烷氧基羰基和酰氧基的取代基或 R 1是5-或6-元一价杂环基，R 2是氢，C 1 -C 8 - 烷基，酰基或-CON（R 3）R 4，R 3和R 4独立地为氢或C 1 -C 8 - 烷基，或与它们所连接的氮原子一起表示5-或6-元杂环基，Y为嘧啶基或哒嗪基，任选被至少一个C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - 烷硫基，C 1 -C 8烷基氨基，二（C 1 -C 8 - 烷基）氨基或酰氨基。这些化合物可用作药物。

6. 发明申请

WO2007121918A3 USE OF 2-(PURIN-9-YL)-TETRAHYDOFURAN-3,4-DIOL DERIVATIVES AS ADENOSINE A2A RECEPTOR AGONISTS 审中-公开
标题翻译：作为腺苷A2A受体激动剂使用2-（嘌呤-9-基）-TETRAHYDOFURA-3,4-二醇衍生物
公开(公告)号：WO2007121918A3
公开(公告)日：2008-04-10
申请号：PCT/EP2007003433
申请日：2007-04-19
申请人： NOVARTIS AG , FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN
发明人： FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN
IPC分类号： A61K31/52 , A61P29/00 , C07D473/16 , C07H19/167
CPC分类号： A61K31/52 , C07D473/16 , C07H19/16
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals (I) wherein R 1 R 2 R 3 , R 4 and W are as defined herein.
摘要翻译：式（I）化合物或其立体异构体或其药学上可接受的盐及其作为药物（I）的制备和用途，其中R 1，R 2，R 3， R 4，W 4如本文所定义。

7. 发明申请

WO2008031875A1 ADENOSINE DERIVATIVES AS A2A RECEPTOR AGONISTS 审中-公开
标题翻译：腺苷衍生物作为A2A受体激动剂
公开(公告)号：WO2008031875A1
公开(公告)日：2008-03-20
申请号：PCT/EP2007/059666
申请日：2007-09-13
申请人： NOVARTIS AG , FAIRHURST, Robin Alec , TAYLOR, Roger John
发明人： FAIRHURST, Robin Alec , TAYLOR, Roger John
IPC分类号： C07D473/00 , A61K31/495 , A61P11/00 , A61P29/00
CPC分类号： C07D473/00
摘要： A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, formula (1), or stereoisomers or pharmaceutically acceptable salts thereof, wherein A, U 1 , U 2 , R 1a , R 1b , R 2 and R 3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A 2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
摘要翻译：式（I）化合物或其立体异构体或其药学上可接受的盐，式（1）或其立体异构体或其药学上可接受的盐，其中A，U 1，U 2 >，R 1a，R 1b，R 2和R 3具有说明书中指出的含义，可用于治疗由腺苷A 2A受体激活介导的病症，特别是炎性或阻塞性气道疾病。还描述了含有化合物的药物组合物和制备该化合物的方法。

8. 发明申请

WO2007121919A1 PURINE DERIVATIVES WITH ACTIVITY TO THE ADENOSINE A2A RECEPTOR 审中-公开
标题翻译：具有对腺苷A2A受体活性的嘌呤衍生物
公开(公告)号：WO2007121919A1
公开(公告)日：2007-11-01
申请号：PCT/EP2007/003434
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： C07D473/16 , C07D473/34 , A61K31/522 , A61P29/00
CPC分类号： C07D473/34 , C07D473/16
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein U, R 1 , R 2 and R 3 are as defined herein.
摘要翻译：式（I）化合物或其立体异构体或其药学上可接受的盐及其制备和用途，其中U，R 1，R 2和R 3 如本文所定义。

9. 发明申请

WO2007121917A3 PURINE DERIVATIVES AS ADENOSINE RECEPTOR ACTIVATOR 审中-公开
公开(公告)号：WO2007121917A3
公开(公告)日：2007-11-01
申请号：PCT/EP2007/003432
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST, Robin, Alec , TAYLOR, Roger, John
发明人： FAIRHURST, Robin, Alec , TAYLOR, Roger, John
IPC分类号： C07D473/16 , C07D473/34 , A61K31/522 , A61P29/00
摘要： A compound of formula (I) and their preparation and use as pharmaceuticals wherein R 1 , R 2 and R 3 are as defined herein.

10. 发明申请

WO2007121917A2 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2007121917A2
公开(公告)日：2007-11-01
申请号：PCT/EP2007003432
申请日：2007-04-19
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN
发明人： FAIRHURST ROBIN ALEC , TAYLOR ROGER JOHN
IPC分类号： C07D473/16 , A61K31/522 , A61P29/00 , C07D473/34
CPC分类号： C07D473/16 , C07D473/34
摘要： A compound of formula (I) and their preparation and use as pharmaceuticals wherein R 1 , R 2 and R 3 are as defined herein.
摘要翻译：式（I）化合物及其作为其中R 1，R 2和R 3的药物的制备和用途如本文所定义。

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