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1. 发明授权

US08685977B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US08685977B2
公开(公告)日：2014-04-01
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： A01N43/58 , A61K31/50 , A01N43/40 , A61K31/435 , A01N43/56 , A61K31/415 , A01N43/36 , A61K31/40
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。

2. 发明授权

US08541588B2 Sulfonamide derivatives 有权
标题翻译：磺酰胺衍生物
公开(公告)号：US08541588B2
公开(公告)日：2013-09-24
申请号：US13400356
申请日：2012-02-20
申请人： Serge Beaudoin , Michael Christopher Laufersweiler , Christopher John Markworth , Brian Edward Marron , David Simon Millan , David James Rawson , Steven Michael Reister , Kosuke Sasaki , Robert Ian Storer , Paul Anthony Stupple , Nigel Alan Swain , Christopher William West , Shulan Zhou
发明人： Serge Beaudoin , Michael Christopher Laufersweiler , Christopher John Markworth , Brian Edward Marron , David Simon Millan , David James Rawson , Steven Michael Reister , Kosuke Sasaki , Robert Ian Storer , Paul Anthony Stupple , Nigel Alan Swain , Christopher William West , Shulan Zhou
IPC分类号： C07D277/00 , C07D211/72 , A61K31/44
CPC分类号： C07D417/12 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D263/50 , C07D275/03 , C07D277/18 , C07D285/08 , C07D401/12 , C07D413/12 , C07D417/14 , C07F9/6539
摘要： The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
摘要翻译：本发明涉及下式的化合物及其药学上可接受的盐，溶剂合物或互变异构体，其制备方法，用于制备的中间体和含有这些化合物的组合物，以及这些化合物的用途，特别是用于治疗疼痛。

3. 发明申请

US20130109708A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20130109708A1
公开(公告)日：2013-05-02
申请号：US13808653
申请日：2011-07-04
申请人： Alan Daniel Brown , David James Rawson , Robert Ian Storer , Nigel Alan Swain
发明人： Alan Daniel Brown , David James Rawson , Robert Ian Storer , Nigel Alan Swain
IPC分类号： C07D213/69 , C07D213/30 , C07D213/65 , C07D471/04 , A61K45/06 , A61K31/472 , C07D217/02 , A61K31/505 , C07D239/34 , A61K31/44 , A61K31/437
CPC分类号： C07D213/69 , A61K31/437 , A61K31/44 , A61K31/472 , A61K31/505 , A61K45/06 , C07D213/30 , C07D213/64 , C07D213/65 , C07D217/02 , C07D217/24 , C07D239/34 , C07D471/04
摘要： The invention relates to sulfonamide derivatives, to their use in medicine, to 5 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):10 X NH O S O O R1 R2 R5 R4 R3 Het1 (I) or a pharmaceutically acceptable salt thereof, wherein X, Het1, R1, R2, R3, R4 and R5 are as defined in the description. 15 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，其在医药中的用途，含有它们的5种组合物，其制备方法和用于此类方法的中间体。更具体地，本发明涉及式（I）的新的磺酰胺Nav1.7抑制剂：10X NH OSOO R1 R2 R5 R4 R3 Het1（I）或其药学上可接受的盐，其中X，Het1，R1，R2，R3， R4和R5如说明书中所定义。 15 Nav 1.7抑制剂可用于治疗各种各样的疾病，特别是疼痛。

4. 发明申请

US20130109696A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20130109696A1
公开(公告)日：2013-05-02
申请号：US13808633
申请日：2011-07-01
申请人： Benjamin Scott Greener , Brian Edward Marron , David Simon Millan , David James Rawson , Robert Ian Storer , Nigel Alan Swain
发明人： Benjamin Scott Greener , Brian Edward Marron , David Simon Millan , David James Rawson , Robert Ian Storer , Nigel Alan Swain
IPC分类号： C07D285/135 , C07D285/08 , A61K45/06 , C07D417/12 , A61K31/4439 , C07D401/12 , A61K31/433 , A61K31/501
CPC分类号： C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/501 , A61K45/06 , C07D285/08 , C07D401/12 , C07D417/12
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 new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 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）的新型磺酰胺Nav1.7抑制剂或其药学上可接受的盐，其中X，Y1，Y2，Z，R1，R2和R3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。

5. 发明授权

US06586439B2 Pharmaceutically active compounds 失效
公开(公告)号：US06586439B2
公开(公告)日：2003-07-01
申请号：US10189680
申请日：2002-07-03
申请人： Graham Nigel Maw , David James Rawson
发明人： Graham Nigel Maw , David James Rawson
IPC分类号： A61K31495
CPC分类号： C07D473/30
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

6. 发明授权

US06440982B1 Pharmaceutically active compounds 失效
标题翻译：药物活性化合物
公开(公告)号：US06440982B1
公开(公告)日：2002-08-27
申请号：US09650848
申请日：2000-08-29
申请人： Graham Nigel Maw , David James Rawson
发明人： Graham Nigel Maw , David James Rawson
IPC分类号： A61K3152
CPC分类号： C07D473/30
摘要： There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
摘要翻译：提供式IA和式IB的化合物，其中R1，R2，R3，Het1和X具有描述中给出的含义，其可用于治疗和预防性治疗环状鸟苷3' ，需要5'-单磷酸磷酸二酯酶（例如cGMP PDE5）。

7. 发明授权

US06306852B1 Indole derivatives useful as endothelin receptor antagonists 失效
标题翻译：用作内皮素受体拮抗剂的吲哚衍生物
公开(公告)号：US06306852B1
公开(公告)日：2001-10-23
申请号：US09556651
申请日：2000-04-24
申请人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
发明人： David James Rawson , Kevin Neil Dack , Roger Peter Dickinson , Kim James
IPC分类号： A61P910
CPC分类号： C07D405/06 , C07D209/18 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or CONHSO2(C1-4 alkyl); Ar1-3 indenpendently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het1 and Het2 independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.
摘要翻译：式（I）化合物及其药学上可接受的衍生物，其中R 1和R 2是任选的取代基并且独立地表示任选被CO 2 H或CO 2（C 1-6烷基）取代的C 1-6烷基，C 2-6烯基，C 2-6炔基，（CH 2）m CO 2 R 8，O（CH 2）q CO 2 R 8，（CH 2）m COOR 8，（CH 2）mOR 8，O（CH 2）pOR 8，C 1 -C 3全氟烷基，（CH 2）mr 1，（CH 2）m Het1，（CH 2）m CONR 7 R 8，（CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1; R3表示H，C1-6烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）

8. 发明授权

US09096558B2 N-sulfonylbenzamide compounds 有权
标题翻译： N-磺酰基苯甲酰胺化合物
公开(公告)号：US09096558B2
公开(公告)日：2015-08-04
申请号：US13808633
申请日：2011-07-01
申请人： Benjamin Scott Greener , Brian Edward Marron , David Simon Millan , David James Rawson , Robert Ian Storer , Nigel Alan Swain
发明人： Benjamin Scott Greener , Brian Edward Marron , David Simon Millan , David James Rawson , Robert Ian Storer , Nigel Alan Swain
IPC分类号： C07D285/08 , C07D417/02 , C07D417/06 , C07D417/12 , A61K31/433 , A61K31/501 , A61K31/4439 , C07D285/135 , C07D401/12 , A61K45/06
CPC分类号： C07D285/135 , A61K31/433 , A61K31/4439 , A61K31/501 , A61K45/06 , C07D285/08 , C07D401/12 , C07D417/12
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 new sulfonamide Nav1.7 inhibitors of formula (I) or pharmaceutically acceptable salts thereof, wherein X, Y1, Y2, Z, R1, R2 and R3 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）的新型磺酰胺Nav1.7抑制剂或其药学上可接受的盐，其中X，Y1，Y2，Z，R1，R2和R3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。

9. 发明授权

US09096500B2 Acyl sulfonamide compounds 有权
标题翻译：酰基磺酰胺化合物
公开(公告)号：US09096500B2
公开(公告)日：2015-08-04
申请号：US13808639
申请日：2011-07-04
申请人： Alan Daniel Brown , David James Rawson , Robert Ian Storer , Nigel Alan Swain
发明人： Alan Daniel Brown , David James Rawson , Robert Ian Storer , Nigel Alan Swain
IPC分类号： C07C311/04 , A61K31/18 , C07C311/51 , C07D231/12 , A61K31/277 , A61K31/415 , A61K31/4245 , A61K31/451 , A61K31/495 , A61K31/50 , A61K45/06 , C07D211/22 , C07D237/08 , C07D241/04 , C07D271/06
CPC分类号： C07C311/04 , A61K31/18 , A61K31/277 , A61K31/415 , A61K31/4245 , A61K31/451 , A61K31/495 , A61K31/50 , A61K45/06 , C07C311/51 , C07D211/22 , C07D231/12 , C07D237/08 , C07D241/04 , C07D271/06
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 X, Ar1, 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X，Ar1，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。

10. 发明申请

US20130116285A1 Chemical Compounds 失效
标题翻译：化学化合物
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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