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公开(公告)号：US06509476B1
公开(公告)日：2003-01-21
申请号：US09637434
申请日：2000-08-11
申请人： Nicholas James Bach , Stephen Richard Baker , Jeremy Gilmore , Russell Andrew Lewthwaite , Alexander McKillop , Jason Scott Sawyer , George Richard Stephenson , Michael William John Urquhart
发明人： Nicholas James Bach , Stephen Richard Baker , Jeremy Gilmore , Russell Andrew Lewthwaite , Alexander McKillop , Jason Scott Sawyer , George Richard Stephenson , Michael William John Urquhart
IPC分类号： A61K3140
CPC分类号： C07D401/14 , A61K31/4725 , C07D209/08
摘要： This invention relates to a method of making N-benzyl indoles, and to intermediates for use in the method, and to certain substantially optically pure N-benzyl indoles obtained by the method.
摘要翻译： 本发明涉及制备N-苄基吲哚的方法和用于本方法的中间体，以及通过该方法获得的某些基本上光学上纯的N-苄基吲哚。
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公开(公告)号：US6160120A
公开(公告)日：2000-12-12
申请号：US103858
申请日：1998-06-24
申请人： Nicholas James Bach , Stephen Richard Baker , Jeremy Gilmore , Russell Andrew Lewthwaite , Alexander McKillop , Jason Scott Sawyer , George Richard Stephenson , Michael William John Urquhart
发明人： Nicholas James Bach , Stephen Richard Baker , Jeremy Gilmore , Russell Andrew Lewthwaite , Alexander McKillop , Jason Scott Sawyer , George Richard Stephenson , Michael William John Urquhart
IPC分类号： A61K31/4725 , C07D209/08 , C07D401/14 , A61K31/47 , C07D215/12
CPC分类号： C07D401/14 , A61K31/4725 , C07D209/08
摘要： This invention relates to a method of making N-benzyl indoles, and to intermediates for use in the method, and to certain substantially optically pure N-benzyl indoles obtained by the method.
摘要翻译： 本发明涉及制备N-苄基吲哚的方法和用于本方法的中间体，以及通过该方法获得的某些基本上光学上纯的N-苄基吲哚。
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公开(公告)号：US5807866A
公开(公告)日：1998-09-15
申请号：US753024
申请日：1996-11-19
申请人： Nicholas James Bach , Stephen Richard Baker , Jeremy Gilmore , Russell Andrew Lewthwaite , Alexander McKillop , Jason Scott Sawyer , George Richard Stephenson , Michael William John Urquhart
发明人： Nicholas James Bach , Stephen Richard Baker , Jeremy Gilmore , Russell Andrew Lewthwaite , Alexander McKillop , Jason Scott Sawyer , George Richard Stephenson , Michael William John Urquhart
IPC分类号： C07D401/10 , C07D209/08 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D417/10 , C07D417/12 , C07D241/00 , A61K31/47
CPC分类号： C07D401/14 , C07D209/08
摘要： A process for producing a compound of the formu5la ##STR1## comprising the step of reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## to form a compound of the formula ##STR4## wherein R.sup.2a is selected from the groups recited above for R.sup.2, or R.sup.2a --X-- is a protected hydroxyl group, and Z is a group of formula --Y--R.sub.5 recited above, or a group that can be converted into a group of said formula --Y--R.sup.5. Intermediates of formula IV and composition containing substantially optically pure enantiomers of Formula (I) are included within the scope of the invention.
摘要翻译： （II）的化合物与式（II）的化合物制备式（ⅩⅤ）化合物的化合物的方法，以形成下式的化合物（Ⅳ），其中R 2a选自 对于R2所述的基团，或R 2a-X-是受保护的羟基，Z是上述式-Y-R5的基团，或可以转化为所述式-Y-R5的基团的基团。 式IV的中间体和含有基本上光学纯的对映异构体（I）的组合物包括在本发明的范围内。
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公开(公告)号：US20120010183A1
公开(公告)日：2012-01-12
申请号：US13179587
申请日：2011-07-11
申请人： Andrew Simon Bell , Alan Daniel Brown , Marcel John De Groot , Russell Andrew Lewthwaite , Ian Roger Marsh , David Simon Millan , Manuel Perez Pacheco , David James Rawson , Nunzio Sciammetta , Robert Ian Storer , Nigel Alan Swain , Steven Matthieu Gaulier
发明人： Andrew Simon Bell , Alan Daniel Brown , Marcel John De Groot , Russell Andrew Lewthwaite , Ian Roger Marsh , David Simon Millan , Manuel Perez Pacheco , David James Rawson , Nunzio Sciammetta , Robert Ian Storer , Nigel Alan Swain , Steven Matthieu Gaulier
IPC分类号： A61K31/44 , C07D401/04 , C07D215/20 , C07D405/12 , C07D231/56 , A61P29/00 , A61K31/506 , A61K31/47 , A61K31/4427 , A61K31/416 , A61K31/4545 , A61K31/4439 , C07D213/69 , C07D401/12
CPC分类号： C07D213/69 , C07D213/63 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/85 , C07D215/20 , C07D231/56 , C07D239/47 , C07D401/04 , C07D405/12 , C07D487/04
摘要： The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Het1, X, R1, R2, R3, R4 and R5 are as defined in the description.Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
摘要翻译： 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中Het1，X，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。
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公开(公告)号：US07241810B2
公开(公告)日：2007-07-10
申请号：US11086035
申请日：2005-03-21
申请人： Alan Daniel Brown , Mark Edward Bunnage , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Paul Alan Glossop , Kim James , David Anthony Price
发明人： Alan Daniel Brown , Mark Edward Bunnage , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Paul Alan Glossop , Kim James , David Anthony Price
IPC分类号： A61K31/167 , C07C233/24
CPC分类号： C07C237/20 , C07C237/30 , C07C237/32 , C07C255/60 , C07C311/37 , C07C311/46 , C07C317/32 , C07C323/32 , C07C323/41 , C07C323/42 , C07C2601/14 , C07C2602/08 , C07C2603/74 , C07D209/48 , C07D211/32 , C07D213/38 , C07D213/40 , C07D217/06 , C07D217/16 , C07D221/22 , C07D221/24 , C07D295/192 , C07D335/02
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译： 本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。 根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。
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公开(公告)号：US07183294B2
公开(公告)日：2007-02-27
申请号：US10800253
申请日：2004-03-12
申请人： Alan Daniel Brown , Justin Stephen Bryans , Mark Edward Bunnage , Paul Alan Glossop , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Simon John Mantell
发明人： Alan Daniel Brown , Justin Stephen Bryans , Mark Edward Bunnage , Paul Alan Glossop , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Simon John Mantell
IPC分类号： A61K31/4439 , A61K31/427 , A61K31/4045 , C07D401/12 , C07D209/14
CPC分类号： C07D209/42 , C07D401/12 , C07D417/12
摘要： The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译： 本发明涉及吲哚衍生物和制备用于制备含有这些衍生物的组合物和用途的中间体的方法。 根据本发明的吲哚衍生物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。
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公开(公告)号：US20130116285A1
公开(公告)日：2013-05-09
申请号：US13808658
申请日：2011-07-06
申请人： Andrew Simon Bell , Alan Daniel Brown , Russell Andrew Lewthwaite , Manuel Perez-Pacheco , David James Rawson , Robert Ian Storer , Nigel Alan Swain
发明人： Andrew Simon Bell , Alan Daniel Brown , Russell Andrew Lewthwaite , Manuel Perez-Pacheco , David James Rawson , Robert Ian Storer , Nigel Alan Swain
IPC分类号： A61K31/444 , A61K31/4418 , A61K45/06 , A61K31/4164 , C07C311/13 , A61K31/18 , C07D233/64 , C07D213/64 , C07D401/12
CPC分类号： A61K31/444 , A61K31/18 , A61K31/4164 , A61K31/4418 , A61K45/06 , C07C311/13 , C07C311/51 , C07D213/64 , C07D213/65 , C07D213/69 , C07D231/12 , C07D233/64 , C07D239/26 , C07D239/42 , C07D401/12
摘要： The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
摘要翻译： 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式10（I）：（I）的新型磺酰胺Nav1.7抑制剂或其药学上可接受的盐，其中Z，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。
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公开(公告)号：US20120010207A1
公开(公告)日：2012-01-12
申请号：US13179585
申请日：2011-07-11
申请人： Andrew Simon Bell , Alan Daniel Brown , Russell Andrew Lewthwaite , Ian Roger Marsh , David Simon Millan , Manuel Perez Pacheco , David James Rawson , Nunzio Sciammetta , Robert Ian Storer , Paul Anthony Stupple , Nigel Alan Swain , Marcel John De Groot
发明人： Andrew Simon Bell , Alan Daniel Brown , Russell Andrew Lewthwaite , Ian Roger Marsh , David Simon Millan , Manuel Perez Pacheco , David James Rawson , Nunzio Sciammetta , Robert Ian Storer , Paul Anthony Stupple , Nigel Alan Swain , Marcel John De Groot
IPC分类号： A61K31/18 , C07D231/12 , C07D233/64 , A61P29/00 , A61K31/415 , A61K31/4164 , A61K31/50 , A61K31/277 , C07C311/51 , C07D237/08
CPC分类号： C07C311/51 , C07C2601/02 , C07D231/12 , C07D233/60 , C07D237/08
摘要： The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes.More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I): or a pharmaceutically acceptable salt thereof, wherein Ar1, X, R1, R2, R3, R4 and R5 are as defined in the description.Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
摘要翻译： 本发明涉及磺酰胺衍生物，其在医学上的用途，含有它们的组合物，其制备方法以及在这些方法中使用的中间体。 更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：或其药学上可接受的盐，其中Ar1，X，R1，R2，R3，R4和R5如说明书中所定义。 Nav 1.7抑制剂可用于治疗各种疾病，特别是疼痛。
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9.发明授权公开(公告)号：US08076356B2
公开(公告)日：2011-12-13
申请号：US12371719
申请日：2009-02-16
IPC分类号： A61K31/437 , A61P11/06
CPC分类号： C07D471/04
摘要： A compound of formula (I), or a pharmaceutical acceptable salt and/or solvate (including hydrate) thereof; and the use of a compound of formula (I) in the treatment of a TNF-mediated disease, disorder, or condition, or a p38-mediated disease, disorder, or condition, in particular the allergic and non-allergic airways diseases, more particularly obstructive or inflammatory airways diseases, preferably chronic obstructive pulmonary disease.
摘要翻译： 式（I）化合物或其药学上可接受的盐和/或其溶剂合物（包括水合物）; 和式（I）化合物在治疗TNF介导的疾病，病症或病症或p38介导的疾病，病症或病症，特别是过敏性和非过敏性气道疾病中的用途更多 特别是阻塞性或炎症性气道疾病，优选慢性阻塞性肺疾病。
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公开(公告)号：US07547731B2
公开(公告)日：2009-06-16
申请号：US11773012
申请日：2007-07-03
申请人： Alan Daniel Brown , Mark Edward Bunnage , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Paul Alan Glossop , Kim James , David Anthony Price
发明人： Alan Daniel Brown , Mark Edward Bunnage , Charlotte Alice Louise Lane , Russell Andrew Lewthwaite , Paul Alan Glossop , Kim James , David Anthony Price
IPC分类号： A61K31/167 , C07C233/24
CPC分类号： C07C237/20 , C07C237/30 , C07C237/32 , C07C255/60 , C07C311/37 , C07C311/46 , C07C317/32 , C07C323/32 , C07C323/41 , C07C323/42 , C07C2601/14 , C07C2602/08 , C07C2603/74 , C07D209/48 , C07D211/32 , C07D213/38 , C07D213/40 , C07D217/06 , C07D217/16 , C07D221/22 , C07D221/24 , C07D295/192 , C07D335/02
摘要： The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
摘要翻译： 本发明涉及式（1）化合物以及制备用于制备含这些衍生物的组合物和用途的中间体的方法。 根据本发明的化合物可用于许多疾病，病症和病症，特别是炎症，过敏和呼吸道疾病，病症和病症。
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