专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009019508A1 CALCIUM ION CHANNEL MODULATORS & USES THEREOF 审中-公开
标题翻译：钙离子通道调制器及其用途
公开(公告)号：WO2009019508A1
公开(公告)日：2009-02-12
申请号：PCT/GB2008/050652
申请日：2008-08-01
申请人： LECTUS THERAPEUTICS LIMITED , BOFFEY, Raymond, John , BURCKHARDT, Svenja , CANSFIELD, Julie, Elaine , KHAN, Nawaz, Mohammed , LAWTON, Geoff , TICKLE, David , VO, Ngoc-Tri , KANUMILLI, Srinivasan , BUSTON, Jonathan, E., H. , SMITH, Andy , WYBROW, Robert, A., J. , KOZLOWSKI, Roland Zbigniew , HOGG, Dayle Spencer
发明人： BOFFEY, Raymond, John , BURCKHARDT, Svenja , CANSFIELD, Julie, Elaine , KHAN, Nawaz, Mohammed , LAWTON, Geoff , TICKLE, David , VO, Ngoc-Tri , KANUMILLI, Srinivasan , BUSTON, Jonathan, E., H. , SMITH, Andy , WYBROW, Robert, A., J. , KOZLOWSKI, Roland Zbigniew , HOGG, Dayle Spencer
IPC分类号： C07D209/18 , C07D333/60 , A61K31/404 , A61K31/381
CPC分类号： C07D209/18 , C07D333/60 , C07D401/12 , C07D409/12
摘要： The present invention relates to ion channel modulators, and more particularly to compounds which inhibit the interaction between the pore-forming (α) subunits of Cav voltage-gated calcium channels and accessory (Cavβ subunit) proteins. Coumpounds are of use in the treatment and prevention of a number of diseases and conditions including pain and lower urinary tract disorders, and have the following Formula (I).
摘要翻译：本发明涉及离子通道调节剂，更具体地涉及抑制Cav电压门控钙通道的成孔（a）亚基与辅助（Cavβ亚基）蛋白质之间相互作用的化合物。辅助治疗剂用于治疗和预防多种疾病和病症，包括疼痛和下尿路疾病，并具有下式（I）。

2. 发明申请

WO2010035032A1 CALCIUM ION CHANNEL MODULATORS & USES THEREOF 审中-公开
标题翻译：钙离子通道调制器及其用途
公开(公告)号：WO2010035032A1
公开(公告)日：2010-04-01
申请号：PCT/GB2009/051242
申请日：2009-09-23
申请人： LECTUS THERAPEUTICS LIMITED , KHAN, Nawaz Mohammed , BURCKHARDT, Svenja , CRANSFIELD, Julie Elaine , VO, Ngoc-Tri , ARMER, Richard Edward , BOFFEY, Raymond John
发明人： KHAN, Nawaz Mohammed , BURCKHARDT, Svenja , CRANSFIELD, Julie Elaine , VO, Ngoc-Tri , ARMER, Richard Edward , BOFFEY, Raymond John
IPC分类号： C07D209/12 , A61K31/404 , A61P13/00
CPC分类号： C07D209/12
摘要： Compounds of formula (I), wherein R1 is hydrogen, hydroxyl or aralkyl; R2 is an optionally substituted alkyl, aryl or heteroaryl (said substituents are selected from hydroxyl, alkoxyl, haloalkoxyl, aryl, heteroaryl, cycloalkyl, amino, monoalkylamino, dialkylamino, alkylsulphonyl, alkylsulphinyl, alkylsulphonylamino, acylamino, saturated or partially unsaturated heterocyclic groups and groups of formula COY); W is selected from oxygen, sulphur, groups of formula NR7, wherein R7 is hydrogen, alkyl, aryl or heteroaryl and groups of formula CR8R9, wherein R8 and R9 are hydrogen, alkyl, aryl or heteroaryl; and X is selected from nitrogen and groups of formula CR10, wherein R10 is hydrogen, alkyl, aryl, heteroaryl, halogen or haloalkyl, inhibit the interaction between Cavx channels and Cavβ proteins and are of use in the treatment and prevention of a number of diseases and conditions including pain and lower urinary tract disorders.
摘要翻译：式（I）的化合物，其中R 1是氢，羟基或芳烷基; R 2是任选取代的烷基，芳基或杂芳基（所述取代基选自羟基，烷氧基，卤代烷氧基，芳基，杂芳基，环烷基，氨基，单烷基氨基，二烷基氨基，烷基磺酰基，烷基亚磺酰基，烷基磺酰基氨基，酰基氨基，饱和或部分不饱和的杂环基和基团式COY）; W选自氧，硫，式NR7基团，其中R7是氢，烷基，芳基或杂芳基，式CR8R9基团，其中R8和R9是氢，烷基，芳基或杂芳基; 并且X选自氮和式CR10基团，其中R10是氢，烷基，芳基，杂芳基，卤素或卤代烷基，抑制Cavx通道和Cavβ蛋白之间的相互作用，并且可用于治疗和预防多种疾病和包括疼痛和下尿路疾病的病症。

3. 发明申请

WO2010001179A2 CALCIUM ION CHANNEL MODULATORS & USES THEREOF 审中-公开
标题翻译：钙离子通道调制器及其用途
公开(公告)号：WO2010001179A2
公开(公告)日：2010-01-07
申请号：PCT/GB2009/050787
申请日：2009-07-03
申请人： LECTUS THERAPEUTICS LIMITED , KHAN, Nawaz Mohammed , BURCKHARDT, Svenja , CANSFIELD, Julie Elaine , VO, Ngoc-Tri , ARMER, Richard Edward , BOFFEY, Raymond John
发明人： KHAN, Nawaz Mohammed , BURCKHARDT, Svenja , CANSFIELD, Julie Elaine , VO, Ngoc-Tri , ARMER, Richard Edward , BOFFEY, Raymond John
IPC分类号： C07D209/12 , C07D209/18 , A61K31/404 , A61P13/00 , A61P29/00
CPC分类号： C07D491/056 , A61K31/404 , C07D209/18 , C07D209/24 , C07D401/06
摘要： Compounds of formula (1 ), salts and pro-drugs wherein: R1, R2, R3 and R4 are hydrogen, alkyl, hydroxyalkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, nitro, amino, monalkylamino, dialkylamino, acylamino, alkoxycarbonylamino, alkylsulphonyl, arylsulphonyl, alkylsulphonylamino, arylsulphonylamino, aminosulphonyl or cyano, or any two of R1 to R4 that are adjacent on the ring may together represent the moiety -O-(CH 2 ) n -O- wherein n is 1 to 3; R5 is hydrogen or alkyl; R6 is hydrogen or alkyl; and X is selected from the group consisting of: (a) groups of formula OR7 wherein R7 is hydrogen or alkyl which is optionally substituted with a substituent selected from alkylsulfonylalkyl, saturated or partially unsaturated heterocyclic, alkoxy, carboxyl, nitro, amino, monalkylamino, dialkylamino, halogen, and alkoxycarbonyl, provided that when R7 is hydrogen or ethyl, then R1, R2, R3 and R4 cannot be selected from hydrogen, halogen and alkyl; and (b) groups 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 which optionally contains at least one more heteroatom selected from nitrogen, oxygen and sulphur atoms, said saturated or partially unsaturated heterocyclic group optionally further being substituted by one or more substituents selected from alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, nitro, amino, monalkylamino, dialkylamino and hydroxyl, provided that: (i) when R8 + R9 +N = piperazine, and ≥ 1 of R1 to R4 are hydrogen, hydroxyl, nitro, amino, alkylamino, dialkylamino, alkoxycarbonylamino, halogen, alkoxy or alkyl, the nitrogen atom at the 4-position of the piperazine is not alkyl substituted, (ii) when each of R1, R2, R3, R4, R5 and R6 is hydrogen, X is not unsubstituted piperazinyl or unsubstituted morpholino, (iii) when each of R1, R2, R4, R5 and R6 is hydrogen and R3 hydrogen, bromine or hydroxyl, X is not methoxy, (iv) when each of R2 and R3 is methoxy or they together represent -0-CH 2 -O- and each of R1, R4, R5 and R6 is hydrogen, X is not unsubstituted piperidine, are Cavx channel blockers and are of use in the treatment of various conditions including pain.
摘要翻译：式（1）的化合物，其盐和前药，其中：R1，R2，R3和R4是氢，烷基，羟基烷基，卤素，卤代烷基，烷氧基，卤代烷氧基，烷氧基羰基，羧基，羟基，硝基，氨基，单烷基氨基，二烷基氨基，酰基氨基，烷氧基羰基氨基，烷基磺酰基，芳基磺酰基，烷基磺酰基氨基，芳基磺酰基氨基，氨基磺酰基或氰基，或在环上相邻的R 1至R 4中的任意两个可以一起代表-O-（CH 2）n O-部分，其中n为1至3; R5是氢或烷基; R6是氢或烷基; 并且X选自：（a）式OR7基团，其中R 7是氢或任选被选自烷基磺酰基烷基，饱和或部分不饱和杂环，烷氧基，羧基，硝基，氨基，单烷基氨基，二烷基氨基，卤素和烷氧基羰基，条件是当R 7为氢或乙基时，则R 1，R 2，R 3和R 4不能选自氢，卤素和烷基; 和（b）式NR8R9基团，其中R8和R9与它们所连接的氮原子一起形成饱和或部分不饱和的杂环基团，其任选地含有至少一个选自氮，氧和硫原子的杂原子，所述饱和或任选地进一步被一个或多个选自烷基，卤素，卤代烷基，烷氧基，烷氧基羰基，羧基，硝基，氨基，一烷基氨基，二烷基氨基和羟基的取代基取代的部分不饱和杂环基，条件是：（ⅰ）当R8 + R9 + 哌嗪，R1至R4中的= 1是氢，羟基，硝基，氨基，烷基氨基，二烷基氨基，烷氧基羰基氨基，卤素，烷氧基或烷基，哌嗪4-位上的氮原子不是烷基取代的，（ii） R 1，R 2，R 3，R 4，R 5和R 6中的每一个是氢，X不是未取代的哌嗪基或未被取代的吗啉代，（iii）当R 1，R 2，R 4，R 5和R 6各自为氢和R 3氢，溴或羟基，X不为甲氧基，（iv）当R 2和R 3各自为甲氧基或它们一起表示-O-CH 2 -O-并且R 1，R 4，R 5和R 6各自为氢时，X为未取代的哌啶，为Cavx通道可用于治疗包括疼痛在内的各种病症。

4. 发明申请

WO2009133387A1 INDOLE- 3 -GLYOXYLAMIDE DERIVATIVES FOR USE AS CALCIUM ION CHANNEL MODULATORS 审中-公开
标题翻译：用作钙离子通道调节剂的吲哚-3-甲氧基酰胺衍生物
公开(公告)号：WO2009133387A1
公开(公告)日：2009-11-05
申请号：PCT/GB2009/050422
申请日：2009-04-24
申请人： LECTUS THERAPEUTICS LIMITED , KHAN, Nawaz, Mohammed , BURCKHARDT, Svenja , CANSFIELD, Julie, Elaine , BOFFEY, Raymond, John , ARMER, Richard, Edward , VO, Ngoc-Tri
发明人： KHAN, Nawaz, Mohammed , BURCKHARDT, Svenja , CANSFIELD, Julie, Elaine , BOFFEY, Raymond, John , ARMER, Richard, Edward , VO, Ngoc-Tri
IPC分类号： C07D209/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , A61K31/404 , A61P13/00
CPC分类号： C07D209/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I) are of use in treating a range of conditions, including pain.
摘要翻译：式（I）化合物可用于治疗一系列病症，包括疼痛。

5. 发明申请

WO2010001179A3 CALCIUM ION CHANNEL MODULATORS & USES THEREOF 审中-公开
标题翻译：钙离子通道调制器及其用途
公开(公告)号：WO2010001179A3
公开(公告)日：2010-11-11
申请号：PCT/GB2009050787
申请日：2009-07-03
申请人： LECTUS THERAPEUTICS LTD , KHAN NAWAZ MOHAMMED , BURCKHARDT SVENJA , CANSFIELD JULIE ELAINE , VO NGOC-TRI , ARMER RICHARD EDWARD , BOFFEY RAYMOND JOHN
发明人： KHAN NAWAZ MOHAMMED , BURCKHARDT SVENJA , CANSFIELD JULIE ELAINE , VO NGOC-TRI , ARMER RICHARD EDWARD , BOFFEY RAYMOND JOHN
IPC分类号： C07D209/12 , A61K31/404 , A61P13/00 , A61P29/00 , C07D209/18
CPC分类号： C07D491/056 , A61K31/404 , C07D209/18 , C07D209/24 , C07D401/06
摘要： Compounds of formula (I) and salts according to following formula: which are Cavx channel blockers and are of use in the treatment of various conditions including pain.
摘要翻译：式（I）的化合物和根据下式的盐：它们是Cavx通道阻滞剂并且可用于治疗包括疼痛在内的各种病症。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式