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1. 发明申请

WO2010010380A1 POTASSIUM ION CHANNEL MODULATORS & USES THEREOF 审中-公开
标题翻译：钾离子通道调制器及其用途
公开(公告)号：WO2010010380A1
公开(公告)日：2010-01-28
申请号：PCT/GB2009/050887
申请日：2009-07-20
申请人： LECTUS THERAPEUTICS LIMITED , EDWARDS, Simon David , KIMBERLY, Meriel Ruth , ARMER, Richard Edward , KHAN, Nawaz Mohammed
发明人： EDWARDS, Simon David , KIMBERLY, Meriel Ruth , ARMER, Richard Edward , KHAN, Nawaz Mohammed
IPC分类号： C07C237/40 , C07D213/40 , A61K31/16
CPC分类号： A61K31/165 , A61K31/198 , A61K31/40 , A61K31/4402 , A61K31/445 , A61K31/5375 , A61K45/06 , C07C237/20 , C07D213/40
摘要： Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar 1 and Ar 2 are aryl or heteroaryl; a is 0 to 5; R 1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R 1 may be the same or different; b is 0 to 5; R 2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R 2 may be the same or different; V is selected from the group consisting of (CR 3a R 3b ) p CON(R 3b )X and (CR 3a R 3b ) p N(R 3b )CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR 4a , O, S, S=O, SO 2 and C(R 4a R 4b ) 2 ; X is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, cycloalkyl, aryl, heteroaryl, polyalkylene glycol, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkyl that is substituted with a groups of formula of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group, carboxyalkyl, alkoxycarbonylalkyl, haloalkoxycarbonylalkyl or aralkyloxycarbonylalkyl; Y and Z are the same or different and each is a substituent selected from the group consisting of (CR 5a R 5b ) n1 , C=O, SO 2 , C(=O)NR 5a ; C(=O)NR 5a SO 2 and C=O(R 5a R 5b ) n2 ; R 3a , R 3b , R 4a , R 4b , R 5a and R 5b are the same or different and each is selected from the hydrogen, alkyl, cycloalkyl, aryl and heteroaryl; n1 and n2 are the same or different and each is 0 to 2; and p is 0 to 2; are potassium ion channel modulators, making them particularly useful in treating and preventing conditions such as pain, lower urinary tract disorders and the like.
摘要翻译：式（I）化合物及其药理学上可接受的盐及其前药，其中：Ar1和Ar2为芳基或杂芳基; a是0到5; R1是烷基，卤素，卤代烷基，烷氧基，卤代烷氧基，烷氧基羰基，羧基，羟基，氨基，一烷基氨基，二烷基氨基，硝基，酰氨基，烷氧基羰基氨基，烷基磺酰基，烷基磺酰基氨基或氰基，其中a大于1，每个取代基R1可以是相同或不同; b为0〜5; R2是烷基，卤素，卤代烷基，卤代烷氧基，烷氧基，烷氧基羰基，羧基，羟基，氨基，单烷基氨基，二烷基氨基，硝基，酰氨基，烷氧基羰基氨基，烷基磺酰基，烷基磺酰基氨基或氰基，其中b大于1，每个取代基R2可以相同或不同; V选自（CR 3 a R 3 b）p CON（R 3 b）X和（CR 3 a R 3 b）p N（R 3 b）CO（X）），其中所述基团相对于取代基Z; W选自NR4a，O，S，S = O，SO2和C（R4aR4b）2; X是氢，烷基，羟基烷基，烷氧基烷基，卤代烷氧基烷基，芳氧基烷基，环烷基，芳基，杂芳基，聚亚烷基二醇，氨基烷基，单烷基氨基烷基，二烷基氨基烷基，被式NR8R9基团取代的烷基，其中R8和R9与氮原子一起它们连接在其上形成饱和或部分不饱和的杂环基，羧基烷基，烷氧基羰基烷基，卤代烷氧基羰基烷基或芳烷氧基羰基烷基; Y和Z相同或不同，分别为选自（CR5aR5b）n1，C = O，SO2，C（= O）NR5a的取代基; C（= O）NR5aSO2和C = O（R5aR5b）n2; R3a，R3b，R4a，R4b，R5a和R5b相同或不同，各自选自氢，烷基，环烷基，芳基和杂芳基; n1和n2相同或不同，各自为0〜2; p为0〜2; 是钾离子通道调节剂，使其在治疗和预防诸如疼痛，下尿路障碍等疾病中特别有用。

2. 发明申请

WO2009071947A3 POTASSIUM ION CHANNEL MODULATORS AND USES THEREOF 审中-公开
标题翻译：钾离子通道调节剂及其用途
公开(公告)号：WO2009071947A3
公开(公告)日：2010-03-11
申请号：PCT/GB2008051158
申请日：2008-12-05
申请人： LECTUS THERAPEUTICS LTD , EDWARDS SIMON DAVID , KIMBERLY MERIEL RUTH , SUTHAHARAN KANESALINGAM , KHAN NAWAZ MOHAMMED , LAWTON GEOFF
发明人： EDWARDS SIMON DAVID , KIMBERLY MERIEL RUTH , SUTHAHARAN KANESALINGAM , KHAN NAWAZ MOHAMMED , LAWTON GEOFF
IPC分类号： C07C311/17 , A61K31/18 , A61P13/00 , A61P25/00 , A61P27/00
CPC分类号： C07C311/35 , C07C311/40
摘要： Compounds of formula (I) and pharmacologically acceptable salts wherein: Ar1 and Ar2 = aryl or heteroaryl; are excellent selective modulators of potassium ion flux.through KCNQ2, KCNQ3 and/or KCNQ2/3 channels, making them of use in treating and preventing a number of conditions including pain and lower urinary tract disorders.
摘要翻译：式（I）化合物及其药理学上可接受的盐，其中：Ar1和Ar2 =芳基或杂芳基; 是通过KCNQ2，KCNQ3和/或KCNQ2 / 3通道的优异的钾离子通道选择性调节剂，使其用于治疗和预防许多病症，包括疼痛和下尿路疾病。

3. 发明申请

WO2009071947A2 POTASSIUM ION CHANNEL MODULATORS & USES THEREOF 审中-公开
标题翻译：钾离子通道调制器及其用途
公开(公告)号：WO2009071947A2
公开(公告)日：2009-06-11
申请号：PCT/GB2008/051158
申请日：2008-12-05
申请人： LECTUS THERAPEUTICS LIMITED , EDWARDS, Simon, David , KIMBERLY, Meriel, Ruth , SUTHAHARAN, Kanesalingam , KHAN, Nawaz, Mohammed , LAWTON, Geoff
发明人： EDWARDS, Simon, David , KIMBERLY, Meriel, Ruth , SUTHAHARAN, Kanesalingam , KHAN, Nawaz, Mohammed , LAWTON, Geoff
IPC分类号： C07C311/17 , A61K31/18 , A61P13/00 , A61P25/00 , A61P27/00
CPC分类号： C07C311/35 , C07C311/40
摘要： Compounds of formula (I) and pharmacologically acceptable salts and pro- drugs wherein: Ar 1 and Ar 2 =aryl orheteroaryl; a = 0 to 5; R 1 =alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and, where a is >1, each R 1 is thesame or different; b =0 to 5; R 2 =alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano andwhere b is >1, each R 2 is the same or different; V =(CR 3a R 3b )p SO 2 N(R 3b )X and (CR 3a R 3b ) pN(R 3b )SO 2 (X); W =NR 4a , O, S, S=O, SO 2 and C(R 4a R 4b ) 2 ; X =hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, polyalkylene glycol residues, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl and alkyl groups substituted with >1 NR8R9 groups wherein R8 and R9 +nitrogen atom form a saturated or partially unsaturated heterocyclic group which isoptionally further substituted by >1 substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monoalkylamino, dialkylamino and hydroxyl; Y and Z each =(CR 5a R 5b ) n1 , C=O, SO 2 , C(=O)NR 5a , C(=O)NR 5a SO 2 or C=O(R 5a R 5b ) n2 ; R 3a , R 3b , R 4a , R 4b , R 5a and R 5b each =hydrogen, alkyl, cycloalkyl, aryl or heteroaryl; n1 and n2 each =0 to 2; and p =0 to 2; are excellent selective modulators of potassium ion flux through KCNQ2, KCNQ3 and/or KCNQ2/3 channels, making them of use in treating and preventing a number of conditions including pain and lower urinary tract disorders.
摘要翻译：式（I）化合物和药理学上可接受的盐和前药，其中：Ar1和Ar2 =芳基杂芳基; a = 0〜5; R 1 =烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，羟基，氨基，一烷基氨基，二烷基氨基，硝基，酰氨基，烷氧基羰基氨基，烷基磺酰基，烷基磺酰基氨基和氰基，其中a≥1，每个R 1是不同的; b = 0〜5; R 2 =烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，羟基，氨基，单烷基氨基，二烷基氨基，硝基，酰氨基，烷氧基羰基氨基，烷基磺酰基，烷基磺酰基氨基和氰基，其中b为> 1，每个R 2相同或不同; V =（CR3a R3b）p SO2N（R3b）X和（CR3a R3b）pN（R3b）SO2（X）; W = NR4a，O，S，S = O，SO2和C（R4aR 4b）2; X =羟基烷基，烷氧基烷基，卤代烷氧基烷基，芳氧基烷基，聚亚烷基二醇残基，氨基烷基，单烷基氨基烷基，二烷基氨基烷基和被> 1 NR8R9基团取代的烷基，其中R8和R9 +氮原子形成饱和或部分不饱和的杂环基，选自烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，硝基，氨基，单烷基氨基，二烷基氨基和羟基的取代基; Y和Z各自=（CR 5a R 5b）n1，C = O，SO2，C（= O）NR 5a，C（= O）NR5a SO2或C = O（R5aR 5b）n2; R3a，R3b，R4a，R4b，R5a和R5b各自为氢，烷基，环烷基，芳基或杂芳基; n1和n2各自= 0至2; 和p = 0至2; 是通过KCNQ2，KCNQ3和/或KCNQ2 / 3通道的钾离子通量的优异选择性调节剂，可用于治疗和预防许多病症，包括疼痛和下尿路疾病。

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