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31. 发明授权

US08163754B2 Purine derivatives for use as adenosine A-2A receptor agonists 失效
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：US08163754B2
公开(公告)日：2012-04-24
申请号：US11576607
申请日：2005-10-21
申请人： Robin Alec Fairhurst , Roger John Taylor , Harinder Pal Singh
发明人： Robin Alec Fairhurst , Roger John Taylor , Harinder Pal Singh
IPC分类号： C07D473/16 , C07D473/40 , C07D473/34 , A61K31/52 , A61P11/06
CPC分类号： C07D473/32 , C07D473/16 , C07D473/40
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。

32. 发明申请

US20120004212A1 ORGANIC COMPOUNDS 失效
公开(公告)号：US20120004212A1
公开(公告)日：2012-01-05
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： A61K31/52 , A61K31/5377 , A61P11/00 , A61P29/00 , A61P11/08 , A61P11/14 , C07D473/34 , A61K31/551
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.

33. 发明授权

US08071565B2 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：US08071565B2
公开(公告)日：2011-12-06
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： C07D473/16 , A61K31/52 , C07H19/16 , A61P29/00 , A61P11/06 , C07D473/40 , C07D231/12
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。

34. 发明申请

US20090281127A1 Organic Compounds 审中-公开
公开(公告)号：US20090281127A1
公开(公告)日：2009-11-12
申请号：US12297007
申请日：2007-04-19
申请人： Robin Alec Fairhurst , Roger John Taylor
发明人： Robin Alec Fairhurst , Roger John Taylor
IPC分类号： A61K31/52 , C07D473/34
CPC分类号： C07D473/16 , C07D473/34
摘要： A compound of formula (I) and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.

35. 发明授权

US5952478A Intermediates for dinucleotide and oligonucleotide analogues 失效
公开(公告)号：US5952478A
公开(公告)日：1999-09-14
申请号：US793725
申请日：1997-04-14
申请人： Anthony David Baxter , Roger John Taylor , Stephen Paul Collingwood
发明人： Anthony David Baxter , Roger John Taylor , Stephen Paul Collingwood
IPC分类号： A61K31/70 , A61K31/7024 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/7135 , A61P31/12 , A61P35/00 , A61P43/00 , C07D405/04 , C07F9/32 , C07F19/00 , C07H9/04 , C07H13/02 , C07H13/04 , C07H13/06 , C07H13/08 , C07H19/01 , C07H19/04 , C07H19/06 , C07H19/16 , C07H21/00 , C07H23/00 , C07H19/00 , A01N43/04 , C07H21/02 , C07H21/04
CPC分类号： C07H9/04 , C07H13/04 , C07H13/08 , C07H19/04 , C07H21/00 , Y02P20/55
摘要： A compound of formula (I) or salts thereof, where R.sup.0 is hydrogen or together with R.sup.7 O denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.1 is hydrogen, R.sup.1.sub.a or a group of formula (II), R.sup.1.sub.a is R.sup.1.sub.b or a protecting group Q, R.sup.1.sub.b is C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.3 -C.sub.10 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R.sup.2 is R.sup.2.sub.a or --OR.sup.15 or together with R.sup.5 denotes an oxy group --O--, provided that R.sup.2 is --OR.sup.15 when R.sup.1 is a group of formula (II), R.sup.2.sub.a is a C.sub.1 -C.sub.20 aliphatic group, a C.sub.3 -C.sub.10 cycloaliphatic group, a C.sub.6 -C.sub.15 aromatic group, a C.sub.7 -C.sub.16 araliphatic group, or a 5- or 6-membered heterocyclic group attached by a carbon atom in the heterocyclic group to the indicated phosphorus atom, R.sup.3 is R.sup.3.sub.a or Z, R.sup.3.sub.a is hydrogen, halogen, hydroxy, R.sup.16, --OR.sup.16, OCOR.sup.16, --OSO.sub.2 R.sup.16, or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyloxy, R.sup.4 is hydrogen, halogen or R.sup.17, R.sup.5 is R.sup.5.sub.a or Z or together with R.sup.2 denotes an oxy group --O--, R.sup.5.sub.a is hydrogen, halogen, hydroxy, R.sup.18, --OR.sup.18, --OCOR.sup.18, --OSO.sub.2 R.sup.18, or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyloxy, or together with R.sup.6 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.6 is halogen, hydroxy, --OR.sup.19, --OCOR.sup.19, --OSO.sub.2 R.sup.19 or B.sup.1, or together with R.sup.5 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, provided that R.sup.6 is not B.sup.1 when R.sup.1 is a group of formula (II) in which R.sup.14 is B.sup.2, R.sup.7 is hydrogen or R.sup.7.sub.a, R.sup.7.sub.a is R.sup.20, --COR.sup.20, --SO.sub.2 R.sup.20 or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyl, or together with the attached oxygen atom and R.sup.0 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.8 is hydrogen, halogen, hydroxy, R.sup.21, --OR.sup.21, --OCOR.sup.21, --OSO.sub.2 R.sup.21 or together with R.sup.10 denotes a valence bond, R.sup.9 is hydrogen, halogen or R.sup.22, R.sup.10 is hydrogen, halogen, hydroxy, R.sup.23, --OR.sup.23, --OCOR.sup.23 or --OSO.sub.2 R.sup.23, or together with R.sup.8 denotes a valence bond, R.sup.11 is hydrogen, halogen or R.sup.24, R.sup.12 is hydrogen or R.sup.12.sub.a, or R.sup.12 O-- together with R.sup.13 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.12.sub.a is R.sup.25, --COR.sup.25, --SO.sub.2 R.sup.25 or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyl, R.sup.13 is R.sup.13.sub.a or Z, R.sup.13.sub.a is hydrogen, halogen, hydroxy, R.sup.26, --OR.sup.26, --OCOR.sup.26, --OSO.sub.2 R.sup.26 or tri(C.sub.1 -C.sub.15 hydrocarbyl)silyloxy, or together with R.sup.14 denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, or together with R.sup.12 O-- denotes a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, R.sup.14 is halogen, hydroxy, --OR.sup.27, --OCOR.sup.27, --OSO.sub.2 R.sup.27, or B.sup.2 or together with R.sup.13 denoted a C.sub.1 -C.sub.15 hydrocarbylidenedioxy group, provided that R.sup.14 is not B.sup.2 when R.sup.6 is B.sup.1, R.sup.15 is hydrogen or R.sup.15.sub.a, R.sup.15.sub.a is a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.8 cycloaliphatic group, a C.sub.6 to C.sub.15 aromatic group or a C.sub.7 to C.sub.16 araliphatic group, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.20, R.sup.21, R.sup.22, R.sup.23, R.sup.24, R.sup.25, R.sup.26 and R.sup.27 are independently a C.sub.1 to C.sub.10 aliphatic group, a C.sub.3 to C.sub.10 cycloaliphatic group, a C.sub.6 to C.sub.15 aromatic group or a C.sub.7 to C.sub.30 araliphatic group, B.sup.1 and B.sup.2 are independently each a monovalent nucleoside base radical, and Z is substituted or unsubstituted C.sub.6 to C.sub.10 aryloxythiocarbonyloxy. ##STR1##

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