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1. 发明专利

JP2015010090A 治療剤としてのスピロオキシインドール化合物およびそれらの使用有权
标题翻译： SPIRO-OXINDOLE化合物及其作为治疗剂的用途
公开(公告)号：JP2015010090A
公开(公告)日：2015-01-19
申请号：JP2014084287
申请日：2014-04-16
申请人：ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. , Xenon Pharmaceuticals Inc , ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc.
发明人： CHAFEEV MIKHAIL , SULTAN CHOWDHURY , LAUREN FRASER , FU JIANMING , JONATHAN LANGILLE , SHIFENG LIU , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ALLA ZENOVA , QI JIA , JEAN-JACQUES CADIEUX , SIMON J GAUTHIER , AMY FRANCES DOUGLAS , HSIEH TOM , CHAKKA NAGASREE , ZORAN CIKOJEVIC
IPC分类号： C07D491/107 , A61K31/407 , A61K31/41 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/429 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/499 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383 , A61P9/00 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/24 , A61P43/00 , C07D491/20 , C07D491/22 , C07D495/20 , C07D498/20 , C07D513/20 , C07D513/22 , C07D519/00
CPC分类号： C07D513/22 , C07D491/10 , C07D491/107 , C07D491/20 , C07D491/22 , C07D495/20 , C07D498/20 , C07D513/20 , C07D519/00
摘要：【課題】ナトリウムチャネルによって媒介される疾患又は状態、例えば疼痛などの治療及び/または予防の為の、化合物の提供。【解決手段】一般式で表されるスピロオキシインドール化合物その立体異性体、鏡像異性体、互変異性体もしくはこれらの混合物又は薬学的に許容されるその塩、溶媒和物若しくはプロドラッグ。【選択図】なし
摘要翻译：要解决的问题：提供用于治疗和/或预防钠通道介导的疾病或病症例如疼痛的化合物。解决方案：本发明涉及由通式表示的螺 - 羟吲哚化合物，立体异构体，对映异构体或互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药。

2. 发明专利

JP2012246313A Spiro-oxindole compound and its use as therapeutic agent 有权
标题翻译： SPIRO-OXINDOLE化合物及其作为治疗剂使用
公开(公告)号：JP2012246313A
公开(公告)日：2012-12-13
申请号：JP2012201716
申请日：2012-09-13
申请人： Xenon Pharmaceuticals Inc , ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc.
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER ROBERT , FU JIANMIN , KAMBOJ RAJENDER , HOU DUANJIE , LIU SHIFENG , BAGHERZADEH MEHRAN SEID , SVIRIDOV SERGUEI , SUN SHAOYI , SUN JIANYU , CHAKKA NAGASREE , HSIEH TOM , RAINA VANDNA
IPC分类号： C07D491/107 , A61K31/407 , A61K31/4184 , A61K31/4192 , A61K31/422 , A61K31/4245 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P5/14 , A61P9/06 , A61P9/10 , A61P19/02 , A61P21/00 , A61P21/02 , A61P21/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D491/113 , C07D491/20 , C07D513/20
CPC分类号： C07D491/10
摘要： PROBLEM TO BE SOLVED: To provide compounds which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions.SOLUTION: The invention relates to spiro-oxindole compounds represented by formula (I) (wherein, k, j, Q, R, R, R, R, R, R, R, R, and Rare as defined in the specification) as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.
摘要翻译：待解决的问题：提供可用于治疗和/或预防钠通道介导的疾病或病症的化合物。解决方案：本发明涉及由式（I）表示的螺 - 羟吲哚化合物（其中，k，j，Q，R 1 ，R 2a ，R 2b ，R 2c ，R 2d < 3b> ，R 3a ，R 3b 作为其立体异构体，对映异构体，互变异构体或其混合物，在本说明书中定义的“SP POS =”POST“> 3d 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。还公开了包含化合物的药物组合物以及制备和使用化合物的方法。版权所有（C）2013，JPO＆INPIT

3. 发明专利

JP2014129422A Spiro-oxindole compound and its use as therapeutic agent 审中-公开
标题翻译： SPIRO-OXINDOLE化合物及其作为治疗剂使用
公开(公告)号：JP2014129422A
公开(公告)日：2014-07-10
申请号：JP2014078569
申请日：2014-04-07
申请人： Xenon Pharmaceuticals Inc , ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc.
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER ROBERT , FU JIANMIN , KAMBOJ RAJENDER , HOU DUANJIE , LIU SHIFENG , BAGHERZADEH MEHRAN SEID , SVIRIDOV SERGUEI , SUN SHAOYI , SUN JIANYU , CHAKKA NAGASREE , HSIEH TOM , RAINA VANDNA
IPC分类号： C07D491/20 , A61K31/407 , A61K31/4184 , A61K31/429 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61P1/04 , A61P3/12 , A61P5/14 , A61P5/24 , A61P9/06 , A61P9/10 , A61P11/00 , A61P13/10 , A61P17/02 , A61P19/02 , A61P21/00 , A61P21/02 , A61P21/04 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P29/00 , A61P35/00 , A61P43/00 , C07D491/107 , C07D513/20
CPC分类号： C07D491/10
摘要： PROBLEM TO BE SOLVED: To provide a compound useful for treatment and/or prevention of sodium channel-mediated diseases or conditions.SOLUTION: The invention relates to a spiro-oxindole compound represented by the formula (I), where k, j, Q, R, R, R, R, R, R, R, Rand Rare as defined in the specification as a stereoisomer, an enantiomer, a tautomer or a mixture thereof, or a pharmaceutically acceptable salt, a solvate or a prodrug thereof, and these are useful for treatment and/or prevention of sodium channel-mediated diseases or conditions such as pain. A pharmaceutical composition containing the compound, a method of manufacturing and using the compound are also disclosed.
摘要翻译：要解决的问题：提供一种可用于治疗和/或预防钠通道介导的疾病或病症的化合物。解决方案：本发明涉及由式（I）表示的螺 - 羟基吲哚化合物，其中k，j，Q R，R，R，R，R，R，R，R，R 3如本说明书中定义为立体异构体，对映异构体，互变异构体或其混合物，或其药学上可接受的盐，溶剂合物或前药，这些可用于治疗和/或预防钠通道介导的疾病或诸如疼痛的病症。还公开了含有该化合物的药物组合物，制备和使用该化合物的方法。

4. 发明专利

JP2013256539A Use of spiro-oxindole compound as therapeutic agent 审中-公开
标题翻译：作为治疗剂的螺旋氧化物的使用
公开(公告)号：JP2013256539A
公开(公告)日：2013-12-26
申请号：JP2013204440
申请日：2013-09-30
申请人： Xenon Pharmaceuticals Inc , ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc.
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER ROBERT , FU JIANMIN , KAMBOJ RAJENDER , HOU DUANJIE , LIU SHIFENG , SEID BAGHERZADEH MEHRAN , SVIRIDOV SERGUEI , SUN SHAOYI , SUN JIANYU , CHAKKA NAGASREE , HSIEH TOM , RAINA VANDNA
IPC分类号： A61K31/404 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61P3/06 , A61P13/08 , A61P17/04 , A61P35/00 , C07D491/107 , C07D491/20
CPC分类号： A61K31/407 , A61K31/437
摘要： PROBLEM TO BE SOLVED: To provide spiro-oxindole compounds as therapeutic agents.SOLUTION: This invention is directed to methods of using spiro-oxindolecompounds of formula (I): wherein k, j, Q, R, R, R, R, R, R, R, Rand Rare as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.
摘要翻译：本发明涉及使用式（I）的螺 - 羟基吲哚化合物的方法：其中k，j，Q，R，R，R，R，R，R 如本文所定义的R，R，Rare Rare，其立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。

5. 发明专利

SG10201703082XA SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS 未知
公开(公告)号：SG10201703082XA
公开(公告)日：2017-06-29
申请号：SG10201703082X
申请日：2009-10-13
申请人： XENON PHARMACEUTICALS INC
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER LAUREN , FU JIANMIN , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ZENOVA ALLA , JIA QI , CADIEUX JEAN-JACQUES , GAUTHIER SIMON J , DOUGLAS AMY FRANCES , HSIEH TOM , CHAKKA NAGASREE , CIKOJEVIC ZORAN
摘要： This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

6. 发明专利

SG10201703086VA SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS 未知
公开(公告)号：SG10201703086VA
公开(公告)日：2017-05-30
申请号：SG10201703086V
申请日：2009-10-13
申请人： XENON PHARMACEUTICALS INC
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER LAUREN , FU JIANMIN , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ZENOVA ALLA , JIA QI , CADIEUX JEAN-JACQUES , GAUTHIER SIMON J , DOUGLAS AMY FRANCES , HSIEH TOM , CHAKKA NAGASREE , CIKOJEVIC ZORAN
摘要： This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

7. 发明专利

ES2546302T3 Compuestos de espiro-oxoindol y su uso como agentes terapéuticos 未知
公开(公告)号：ES2546302T3
公开(公告)日：2015-09-22
申请号：ES09740589
申请日：2009-10-13
申请人： XENON PHARMACEUTICALS INC
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER LAUREN , FU JIANMIN , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ZENOVA ALLA , JIA QI , CADIEUX JEAN-JACQUES , GAUTHIER SIMON J , DOUGLAS AMY FRANCES , HSIEH TOM , CHAKKA NAGASREE , CIKOJEVIC ZORAN
IPC分类号： C07D491/20 , A61K31/407 , A61P25/00 , C07D491/10 , C07D495/20 , C07D498/20 , C07D513/20
摘要： Un compuesto de fórmula (I):**Fórmula** en el cual: n es 1 ó 2; uno de J y K es -CH2- y el otro es -O-; o ambos J y K son cada uno -CH2-; R1 es hidrógeno, metilo, ciclopropilo, carboximetilo, (3-carboxi)bencilo, (3-metilsulfonilamino)bencilo, [(3- metilsulfonilamino)piridin-2-il]metilo, [(3-carboxi)piridin-2-il]metilo, [(etoxi)carbonil]metilo, 2-ciclopropiletilo, 1,3-tiazol- 5-ilmetilo, 3-metoxipropilo, (6-metilpiridin-2-il)metilo, piridin-3-ilmetilo, [3-(ciano)piridina-2-il]metilo, [3- (difluorometil)piridin-2-il]metilo, 3-(5-metil-1,2,4-oxadiazol-3-il)bencilo, 4-(5-metil-1,2,4-oxadiazol-3-il)bencilo, [5- (trifluorometil)-1,2,4-oxadiazol-3-il]metilo, [5-(trifluorometil)-1,3,4-oxadiazol-2-il]metilo, [4-(trifluorometil)piridin-2- il]metilo, (4-metil-1,2,5-oxadiazol-3-il)metilo, pirazin-2-ilmetilo, pirimidin-2-ilmetilo, (1-metil-1H-benzotriazol-5-il)metilo, [2-(terc-butoxicarbonilamino)piridin-5-il]metilo, [6-(dimetilamino)piridin-3-il]metilo, [6-(dimetilamino)piridin-2-il]metilo, {6-[(difenilmetilidano)amino]piridin-2-il}metilo, (5-morfolin-4-ilpiridin-2-il)metilo, [5-(dimetilamino)piridin-2-il]metilo, (6- aminopiridin-2-il)metilo, (6-oxo-1,6-dihidropiridin-3-il)metilo, (2-hidroxipirimidin-5-il)metilo, (1-metil-6-oxo-1,6- dihidropiridin-3-il)metilo, (6-aminopiridin-3-il)metilo, [1,2,4]triazolo[1,5-a]piridin-6-ilmetilo, (5-hidroxipiridin-2-il)metilo, (5-bromopiridin-2-il)metilo, hidrazinocarbonilmetilo, [6-deoxi-D-galactopiranosa]-6-ilo, (6-morfolin-4-ilpiridin-3-il)metilo, [3-(metilsulfonil)piridin-2-il]metilo, (4S)-2,2-dimetil-1,3-dioxolan-4-il]metilo, (3-bromopiridin-2-il)metilo, [(2- imidoformamido)piridina-5-il]metilo, (6-cianopiridin-2-il)metilo, (6-aminocarbonilpiridin-2-il)metilo, difenilmetilo, 4- metoxibencilo, 2-(fluorometil)bencilo, 2-etoxietilo, 4-fluorofenilo, (2-fluorofenilaminocarbonil)metilo, 2-(2- metoxietoxi)etilo, 4-isoxazol-5-ilbencilo, 3-(benciloxi)propilo, (2S)-2,3-dihidroxipropilo, 4-metoxibutilo, pentilo, isopentilo, hexilo, 3-nitrobencilo, [3-(trifluorometil)piridin-2-il]metilo, [5-(trifluorometil)piridin-2-il]metilo, [(tercbutoxicarbonilamino) piridin-2-il]metilo, (3-(trifluorometil)piridin-2-il)metilo, (5-(trifluorometil)furan-2-il)metilo, tetrahidrofurano-2-ilmetilo, 3-metilbutilo, cianometilo, 4-hidroxibencilo, 3-cianobencilo, 4-fluoro-3-metoxibencilo, 4- cianobencilo, [6-(trifluorometil)piridin-3-il]metilo, [4-(trifluorometil)-1,3-tiazol-2-il]metilo, (3-fluoropiridin-2-il)metilo, (4- fluoropiridin-2-il)metilo, (5-fluoropiridin-3-il)metilo, (5-fluoropiridin-2-il)metilo, (3-cloropiridin-2-il)metilo, (3,5- difluoropiridin-2-il)metilo, (3-piridin-3-ilisoxazol-5-il)metilo, (2,2-difluorociclopropil)metilo, 2-oxobutilo, 2,1,3- benzotiadiazol-5-ilmetilo, 2,1,3-benzoxadiazol-5-ilmetilo, 1,3-benzotiazol-2-ilmetilo, (1-metil-1H-bencimidazol-2- il)metilo, [2-(1-metiletil)-1,3-tiazol-4-il]metilo, terc-butoxicarbonilo, [1-(terc-butoxicarbonil)piperidin-4-il]metilo, (2- metoxipirimidin-5-il)metilo, (6-metoxipiridin-3-il)metilo, (1-oxidopiridin-2-il)metilo, (3-aminopiridin-2-il)metilo, piperidin- 4-ilmetilo, [1-(1-metiletil)piperidin-4-il]metilo, (1-metilpiperidin-4-il)metilo, morfolin-2-ilmetilo, [4-(1-metiletil)morfolin-2- il]metilo, (4-metilmorfolin-2-il)metilo, (2S)-morfolin-2-ilmetilo, [(2S)-4-metilmorfolin-2-il]metilo, [5-(difluorometil)furan-2- il]metilo, tetrahidro-2H-piran-4-ilmetilo, tetrahidro-2H-piran-2-ilmetilo, (5-cloro-1-metil-1H-imidazol-2-il)metilo, (6- cloropiridin-2-il)metilo, (4,6-dimetoxipirimidin-2-il)metilo, [(3-metilaminocarbonil)piridin-2-il]metilo, 1-[2- (aminoetil)aminocarbonilpiridin-3-il]metilo, piridin-2-ilmetilo, (2R)-1,4-dioxan-2-ilmetilo, 1,4-dioxan-2-ilmetilo, 3,4- dimetoxibencilo, 3,5-dimetoxibencilo, 3-hidroxipropilo, 3-fthalimidopropilo, 3-aminobencilo, (3-aminocarbonil)bencilo, (4-aminocarbonil)bencilo, (3-N,N-dimetilaminocarbonil)bencilo, 4-(benciloxi)benzy, 4-fluorobencilo, 2,3- difluorobencilo, 3,5-difluorobencilo, 2-cloro-4-fluorobencilo, [3-(2-fluorofenil)aminocarbonil]bencilo, 3- (metoxicarbonil)bencilo, 4-(metoxicarbonil)bencilo, 4-(etoxicarbonil)bencilo, 3-(dimetilamino-sulfonil)bencilo, 3-(3- metil-1,2,4-oxadiazol-5-il)bencilo, 4-(3-amino-1H-pirazol-5-il)bencilo, 4-(3-metil-1,2,4-oxadiazol-5-il)bencilo, 3- (morfolin-4-ilsulfonil)bencilo, 2-(difluorometil)bencilo, (3-trifluorometoxi)bencilo, (2-fluoro-6-trifluorometil)bencilo, (2- fluoro-5-trifluorometil)bencilo, (2-trifluorometoxi)bencilo, 3-(amino(hidroxiimino)metil)bencilo, 2-amino-2- (hidroxiimino)etilo, (6-(N'-hidroxiformimidamido)piridin-3-il)metilo, 2-(2,2,5-trimetil-1,3-dioxan-2-il)etilo, (4- bencilmorfolin-2-il)metilo, [(2S)-4-bencilmorfolin-2-il]metilo, 2,3-dihidro-1,4-benzodioxin-6-ilmetilo, [5- (trifluorometil)furan-2-il]metilo, 3-(trifluorometil)bencilo, [3-(trifluorometil)pirazin-2-il]metilo, [4-(trifluorometil)piridin-3- il]metilo, (5-metoxicarbonilfuran-2-il)metilo, 5-carboxifuran-2-ilmetilo, 5-(dimetilaminocarbonil)furan-2ilmetilo, [2- (trifluorometil)piridin-3-il]metilo, metilcarbonilo, etoxicarbonilo, terc-butoxicarbonilo o [(3aR,5R,5aS,8aS,8bR)-2,2,7,7- tetrametiltetrahidro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]piran-5-il]metilo; cada R2 es independientemente hidrógeno, hidroxi, amino, (hexanilaminocarbonil)amino, 50 (ciclopentilaminocarbonil)amino, bencilamino, (ciclohexilaminocarbonil)amino, metilsulfonilamino, (metil)carbonilamino, N,N-dimetilaminocarbonilo, (etil)carbonilamino, (butil)carbonilamino, (terc-butil)carbonilamino, (pentanil)carbonilamino, (hexanil)carbonilamino, (metoximetil)carbonilamino, ciclobutilcarbonilamino, [2- metoxi(etoximetil)]carbonilamino, (metilsulfonil)amino, (2-trifluorometilfenil)carbonilamino, (ciclohexanil)carbonilamino, (ciclopentanil)carbonilamino, (ciclopropanil)carbonilamino, (fenil)carbonilamino, bromo, ciano, fluoro, metilo, metoxi, hidroxicarbonilo, metilcarbonilo, pirrolidinilcarbonilo, aminocarbonilo, metilaminocarbonilo, (2-metoxietil)aminocarbonilo, (ciclopropil)aminocarbonilo, pentilaminocarbonilo, (ciclobutil)aminocarbonilo, (ciclopentil)aminocarbonilo, hexanilaminocarbonilo, (ciclohexil)aminocarbonilo, (4- fluorofenil)aminocarbonilo, (4-fluorobencil)aminocarbonilo, (piridin-2-ilmetil)aminocarbonilo, 2-(2-metoxietoxi)etoxi, [3- (trifluorometil)piridin-2-il]oxilo, quinolinilo, fenoxicarbonilo, 2-oxocromenoilo, 2-oxopirrolidinilo, morfolinilo, 2- oxopiridinilo, benciloxilo, [3-(trifluorometil)piridin-2-il]metoxi, piridina-2-ilmetoxi, piridin-2-iloxi, 4-(trifluorometil)fenoxi, 2-metil-1,3-tiazol-4-ilo, 2-amino-1,3-tiazol-4-ilo, 6-(dimetilamino)piridin-3-ilo, furan-3-ilo, 1H-pirazol-3-ilo, 1H-pirazol-4- ilo, 1-metil-1H-pirazol-4-ilo, 5-hidroxi-1H-pirazol-3-ilo, 5-metil-1,2,4-oxadiazol-3-ilo, (6-metoxipiridin-3-il)oxi, 1,3- benzodioxol-5-iloxi, 4-fluorobenciloxi, 3,5-dimetilisoxazol-4-ilo, fenoxi, 3-metoxifenoxi, 4-metoxifenoxi, 3-morfolin-4- ilfenoxi, 4-fluorofenoxi, 4-metoxifenilo o 4-fenoxifenilo; o dos R2 adyacentes, junto con los carbonos adyacentes al que están unidos, de un anillo tiazolilo fusionado, un anillo piridilo fusionado o un anillo dioxinilo fusionado; como un estereoisómero, enantiómero, tautómero de estos o mezclas de estos; o una sal, un solvato o un profármaco farmacéuticamente aceptables de estos, donde el profármaco se selecciona de derivados de acetato, formato y benzoato de alcohol o derivados de amida de groupos funcionales amina en el compuesto.

8. 发明专利

BRPI0719857A2 未知
公开(公告)号：BRPI0719857A2
公开(公告)日：2014-06-03
申请号：BRPI0719857
申请日：2007-10-12
申请人： XENON PHARMACEUTICALS INC
发明人： CADIEUX JEAN-JACQUES , CHOWDHURY SULTAN , FU JIANMIN , KAMBOJ RAJENDER , HSIEH TOM , JIA QI , LIU SHIFENG , SUN JIANYU
IPC分类号： C07D471/20 , A61K31/4747 , A61P25/04
摘要： This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R1, R2a, R2b, R2c, R2d and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, N-oxide, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

9. 发明专利

AU2006235593B2 Spiro-oxindole compounds and their uses as therapeutic agents 未知
公开(公告)号：AU2006235593B2
公开(公告)日：2012-07-05
申请号：AU2006235593
申请日：2006-04-11
申请人： XENON PHARMACEUTICALS INC
发明人： CHAFEEV MIKHAIL , CHAKKA NAGASREE , KAMBOJ RAJENDER , BAGHERZADEH MEHRAN SEID , HSIEH TOM , CHOWDHURY SULTAN , SUN JIANYU , HOU DUANJIE , LIU SHIFENG , RAINA VANDNA , FRASER ROBERT , SUN SHAOYI , FU JIANMIN , SVIRIDOV SERGUEI
IPC分类号： C07D498/10 , A61K31/404 , A61P29/00
摘要： This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R, R, R, R, R, R, R, R, and R are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

10. 发明专利

PE05862011A1 COMPUESTOS ESPIRO-OXINDOLICOS CON ACTIVIDAD SOBRE LOS CANALES DE SODIO 未知
公开(公告)号：PE05862011A1
公开(公告)日：2011-09-03
申请号：PE0009102011
申请日：2009-10-13
申请人： XENON PHARMACEUTICALS INC
发明人： CHAFEEV MIKHAIL , CHOWDHURY SULTAN , FRASER LAUREN , FU JIANMIN , LANGILLE JONATHAN , LIU SHIFENG , SUN JIANYU , SUN SHAOYI , SVIRIDOV SERGUEI , WOOD MARK , ZENOVA ALLA , JIA QI , CADIEUX JEAN-JACQUES , GAUTHIER SIMON J , DOUGLAS AMY FRANCES , HSIEH TOM , CHAKKA NAGASREE , CIKOJEVIC ZORAN
IPC分类号： C07D491/10 , A61K31/407 , A61P25/00
CPC分类号： C07D513/22 , C07D491/10 , C07D491/107 , C07D491/20 , C07D491/22 , C07D495/20 , C07D498/20 , C07D513/20 , C07D519/00
摘要： REFERIDA A UN COMPUESTO ESPIRO-OXINDOLICO DE FORMULA (I), DONDE R1 ES H, METILO, CICLOPROPILO, ENTRE OTROS; R2 ES H, OH, AMINO, ENTRE OTROS; J Y K SON -CH2- U OXIGENO. SON COMPUESTOS PREFERIDOS: 1'-METIL-2'-OXO-N-PENTIL-1',2,2',3-TETRAHIDROESPIRO[FURO[2,3-g][1,4]BENZODIOXIN-8,3'-INDOL]-4'-CARBOXAMIDA, 1'-(DIFENILMETIL)-4',6'-DIMETOXI-2,3-DIHIDROESPIRO[FURO[2,3-g][1,4]BENZODIOXIN-8,3'-INDOL]-2'(1'H)-ONA, (8R)-1'-[(2R)-1,4-DIOXAN-2-ILMETIL]-2,3-DIHIDROESPIRO[FURO[2,3-g][1,4]BENZODIOXIN-8,3'-INDOL]-2'(1'H)-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD SOBRE LOS CANALES DE SODIO Y SON UTILES EN EL TRATAMIENTO DEL DOLOR, AFECCIONES CARDIOVASCULARES, GLAUCOMA, ENTRE OTROS

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