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1. 发明授权

US08114877B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US08114877B2
公开(公告)日：2012-02-14
申请号：US11722835
申请日：2006-01-12
申请人： Robin A Fairhurst , Roger J Taylor
发明人： Robin A Fairhurst , Roger J Taylor
IPC分类号： C07D473/16 , C07D473/40 , C07D473/34 , A61K31/52 , A61P11/06
CPC分类号： C07D473/00
摘要： Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A 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：游离或盐形式的式I化合物，其中R 1，R 2和R 3具有说明书中指出的含义，可用于治疗由腺苷A2A受体的活化，特别是炎性或阻塞性气道疾病介导的病症。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。

2. 发明授权

US07109202B2 Aminothaizoles and their use as adenosine receptor antagonists 失效
标题翻译：氨基噻唑及其作为腺苷受体拮抗剂的用途
公开(公告)号：US07109202B2
公开(公告)日：2006-09-19
申请号：US10432302
申请日：2001-11-19
申请人： Neil J Press , Roger J Taylor
发明人： Neil J Press , Roger J Taylor
IPC分类号： A61K31/427 , A61K31/497 , A61K31/4436 , C07D417/14 , C07D277/42
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of formula (I) in free or salt form, where A is a C6-C15 monovalent aromatic group. R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1–C8-alkyl, C1–C8-haloalkyl, C1–C8-alkoxy, C1–C8-alkoxy-C1–C8-alkyl or acyloxy, or a 5- or 6-membered monovalent heterocyclic group, R2 is hydrogen, C1-C8-alkyl, acyl or CON(R3)R4, provided that R2 is C1–C8-alkyl, acyl or CON(R3)R4 when R1 is hydrogen, R3 and R4 are each independently hydrogen, or C1–C8-alkyl, together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, and Zl, Z2, Z3 and Z4 are each independently N or CR5, at least one of them being CR5, and R5 is hydrogen, C1–C8-alkyl or C1–C8-alkoxy. The compounds are useful as adenosine receptor antagonists, particularly in the treatment of inflammatory or obstrucive airways diseases
摘要翻译：游离或盐形式的式（I）化合物，其中A是C 6 -C 15单价芳族基团。 R 1是氢，任选地被一个或多个选自卤素，氰基，羟基，C 1 -C 8 - 烷基的取代基取代的苯基， C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基，C 1 -C 8 - C 1 -C 8 - 烷氧基-C 1 -C 8 - 烷基或酰氧基，或5或6元一价杂环基团R 2是氢，C 1 -C 8 - 烷基，酰基或CON（R 3） R 4，其中R 2为C 1 -C 8 - 烷基，酰基或CON（R' 当R 1为氢时，R 3为3以及R 4为SO 4，则R 4为S 4 每个独立地是氢或C 1 -C 8 - 烷基与它们所连接的氮原子一起表示5-或6-元杂环基，Z Z 2，Z 3，Z 4和Z 4各自独立地为N或CR 5， SUP>，其中至少一个为CR 5，R 5为氢， C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基。这些化合物可用作腺苷受体拮抗剂，特别是用于治疗炎性或阻塞性气道疾病

3. 发明授权

US07273875B2 Naphthyridine derivatives, their preparation and their use as phosphodiesterase isoenzyme 4 (PDE4) inhibitors 有权
标题翻译：萘啶衍生物，其制备及其作为磷酸二酯酶同工酶4（PDE4）抑制剂的用途
公开(公告)号：US07273875B2
公开(公告)日：2007-09-25
申请号：US10494223
申请日：2002-11-04
申请人： Alastair Denholm , Thomas H Keller , Clive McCarthy , Neil J Press , Roger J Taylor
发明人： Alastair Denholm , Thomas H Keller , Clive McCarthy , Neil J Press , Roger J Taylor
IPC分类号： A61K31/4375 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to compounds of formula I in free or salt form, where R1 is a monovalent aromatic group having up to 10 carbon atoms, and R2 is a cycloaliphatic group having up to 8 ring carbon atoms. Compositions containing them, methods for their preparation and their use as pharmaceuticals are also described.
摘要翻译：本发明涉及游离或盐形式的式I化合物，其中R 1是具有至多10个碳原子的一价芳族基团，R 2是脂环族基团具有多达8个环碳原子。还描述了含有它们的组合物，其制备方法及其作为药物的用途。

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