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1. 发明授权

US07468370B2 [1,7]naphthyridines as PDE4 inhibitors 失效
标题翻译： [1,7]萘啶类作为PDE4抑制剂
公开(公告)号：US07468370B2
公开(公告)日：2008-12-23
申请号：US10538355
申请日：2003-12-15
申请人： Alastair Denholm , Thomas Hugo Keller , Clive McCarthy , Neil John Press , Roger John Taylor
发明人： Alastair Denholm , Thomas Hugo Keller , Clive McCarthy , Neil John Press , Roger John Taylor
IPC分类号： C07D471/02 , C07D401/00 , A61K31/497 , A61K31/44 , A01N43/42
CPC分类号： C07D471/04
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 of phosphodiesterase type 4 or the down-regulation or inhibition of TNF-α release, particularly obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：具有游离或盐形式的式I化合物，其中R1，R2和R3具有说明书中所示的含义，可用于治疗由磷酸二酯酶4介导的病症或TNF-α释放的下调或抑制，特别是阻塞性或炎症性气道疾病。还描述了含有化合物的药物组合物和用于制备化合物的方法。

2. 发明授权

US07745462B2 Quinoline-2-one derivatives for the treatment of airways diseases 有权
标题翻译：喹啉-2-酮衍生物用于治疗气道疾病
公开(公告)号：US07745462B2
公开(公告)日：2010-06-29
申请号：US10552023
申请日：2004-04-02
申请人： Robin Alec Fairhurst , David Andrew Sandham , David Beattie , Ian Bruce , Bernard Cuenoud , Reamonn Madden , Neil John Press , Roger John Taylor , Katharine Louise Turner , Simon James Watson
发明人： Robin Alec Fairhurst , David Andrew Sandham , David Beattie , Ian Bruce , Bernard Cuenoud , Reamonn Madden , Neil John Press , Roger John Taylor , Katharine Louise Turner , Simon James Watson
IPC分类号： A61K31/02 , C07D215/38
CPC分类号： C07D215/227 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D417/14
摘要： Compounds of formula I in free or salt form, wherein —C—Y—, R1 and R2 are G have the meanings as indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the β2-adrenoreceptor. 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-C-Y-，R 1和R 2为G具有本说明书中指出的含义，可用于治疗通过活化2-肾上腺素受体而预防或缓解的病症。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。

3. 发明申请

US20090233938A1 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：US20090233938A1
公开(公告)日：2009-09-17
申请号：US10585614
申请日：2005-01-20
申请人： Neil John Press , Roger John Taylor
发明人： Neil John Press , Roger John Taylor
IPC分类号： A61K31/501 , C07D417/14 , A61K31/506 , C07D417/12
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 C1-C8-haloalkyl, or naphthyl, 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, carboxy, C1-C8-alkoxycarbonyl and acyloxy, or R1 is a 5- or 6-membered monovalent heterocyclic group, R2 is hydrogen, C1-C8-alkyl, acyl or —CON(R3)R4, R3 and R4 are each independently hydrogen or C1-C8-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 C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkylthio, C1-C8-alkyl amino, di(C1-C8-alkyl) amino or acylamino group. The compounds are useful as pharmaceuticals.
摘要翻译：游离或盐形式的式（I）化合物，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，任选被一个或多个取代基取代的苯基卤素，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， 5-或6-元一价杂环基，R 2为氢，C 1 -C 8 - 烷基，酰基或-CON（R 3）R 4，R 3和R 4各自独立地为氢或C 1 -C 8烷基，或与氮原子它们所连接的表示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 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。

4. 发明授权

US08633211B2 Bicyclic organic compounds suitable for the treatment of inflammatory or allergic conditions 失效
标题翻译：适用于治疗炎症或过敏症状的双环有机化合物
公开(公告)号：US08633211B2
公开(公告)日：2014-01-21
申请号：US12449537
申请日：2008-03-04
申请人： Roger John Taylor
发明人： Roger John Taylor
IPC分类号： A61K31/517 , C07D239/80 , A61P29/00
CPC分类号： C07D495/14 , C07D215/36 , C07D239/54 , C07D239/80 , C07D239/96 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07D495/04
摘要： A compound of formula (I): in free or salt form, wherein A, R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
摘要翻译：式（I）化合物：游离或盐形式，其中A，R1，R3，Qa，Qb和Q如本文所定义，用于治疗由S1P2或S1P3受体介导的疾病，例如炎性或阻塞性气道疾病

5. 发明申请

US20080242683A1 Organic Compounds 审中-公开
标题翻译：有机化合物
公开(公告)号：US20080242683A1
公开(公告)日：2008-10-02
申请号：US11908620
申请日：2006-03-13
申请人： Robin Alec Fairhurst , Roger John Taylor
发明人： Robin Alec Fairhurst , Roger John Taylor
IPC分类号： A61K31/52 , C07D473/16
CPC分类号： C07D473/00 , C07D473/16 , C07H19/167
摘要： Compounds of (I) or stereoisomers or pharmaceutically acceptable salts thereof, where W, R1, R2, R3 and R4 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：（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 2， 4具有如说明书中所示的含义，可用于治疗腺苷A 2A受体活化介导的病症，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。

6. 发明授权

US09056867B2 N-substituted heterocyclyl carboxamides 有权
标题翻译： N-取代的杂环基甲酰胺
公开(公告)号：US09056867B2
公开(公告)日：2015-06-16
申请号：US14345022
申请日：2012-09-14
申请人： Kamlesh Jagdis Bala , Emma Budd , Lee Edwards , Catherine Howsham , Darren Mark LeGrand , Roger John Taylor
发明人： Kamlesh Jagdis Bala , Emma Budd , Lee Edwards , Catherine Howsham , Darren Mark LeGrand , Roger John Taylor
IPC分类号： A61K31/4427 , C07D487/04 , A61K31/415 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K31/4985 , A61K31/5377 , A61K31/444 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/4985 , A61K31/5377 , A61K45/06 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14
摘要： A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
摘要翻译：式I化合物及其药学上可接受的盐和溶剂合物，其中R1，R2，R3，Ra，A，B，D和E全部如本文所定义。该化合物调节CFTR的活性，并且可用于治疗炎性或阻塞性气道疾病或粘膜水合，包括例如囊性纤维化。还描述了含有化合物的药物组合物和用于制备化合物的方法。

7. 发明授权

US08318750B2 Organic compounds 失效
标题翻译：有机化合物
公开(公告)号：US08318750B2
公开(公告)日：2012-11-27
申请号：US13218865
申请日：2011-08-26
申请人： Robin Alec Fairhurst , Roger John Taylor , Brian Cox
发明人： Robin Alec Fairhurst , Roger John Taylor , Brian Cox
IPC分类号： C07D473/16 , A61K31/52 , C07D401/14 , C07D233/64 , C07D473/40 , C07D413/12 , A61P11/06 , A61P11/08 , A61P11/00 , A61P27/02
CPC分类号： C07D473/16 , C07D473/34
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 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的制备和用途，其中R 1，R 2和R 3如本文所定义。

8. 发明授权

US08258141B2 Organic compounds 失效
公开(公告)号：US08258141B2
公开(公告)日：2012-09-04
申请号：US12297291
申请日：2007-04-19
申请人： Robin Alec Fairhurst , Roger John Taylor , Brian Cox
发明人： Robin Alec Fairhurst , Roger John Taylor , Brian Cox
IPC分类号： C07D473/16 , A61K31/52 , C07D401/14 , C07D233/64 , C07D473/40 , C07D413/12 , A61P11/06 , A61P11/08 , A61P11/00 , A61P27/02
CPC分类号： C07D473/16 , C07D473/34
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.

9. 发明申请

US20100286126A1 Organic Compounds 失效
标题翻译：有机化合物
公开(公告)号：US20100286126A1
公开(公告)日：2010-11-11
申请号：US12297291
申请日：2007-04-19
申请人： Robin Alec Fairhurst , Roger John Taylor , Brian Cox
发明人： Robin Alec Fairhurst , Roger John Taylor , Brian Cox
IPC分类号： A61K31/52 , C07D473/16 , C07D473/34 , A61K31/5377 , A61K31/551 , A61P29/00 , A61P11/00 , A61P11/08 , A61P11/14
CPC分类号： C07D473/16 , C07D473/34
摘要： A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 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的制备和用途，其中R 1，R 2和R 3如本文所定义。

10. 发明申请

US20100240680A1 Purine derivatives as a2a agonists 失效
标题翻译：嘌呤衍生物作为a2a激动剂
公开(公告)号：US20100240680A1
公开(公告)日：2010-09-23
申请号：US12308637
申请日：2007-07-11
申请人： Robin Alec Fairhurst , Roger John Taylor
发明人： Robin Alec Fairhurst , Roger John Taylor
IPC分类号： A61K31/52 , C07D473/16 , A61P11/06 , A61P11/08 , A61P11/14 , A61P29/00 , A61P37/08
CPC分类号： C07D473/16
摘要： Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, 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：式（I）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和R 3具有说明书中所示的含义，可用于治疗腺苷A2A受体活化介导的病症，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。

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