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1. 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。

2. 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）。

3. 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。

4. 发明申请

WO2007036727A1 CONDENSED PYRAZOLE DERIVATIVES AS PPAR AGONISTS II 审中-公开
标题翻译：浓缩的吡唑衍生物作为PPAR激动剂II
公开(公告)号：WO2007036727A1
公开(公告)日：2007-04-05
申请号：PCT/GB2006/003608
申请日：2006-09-28
申请人： INPHARMATICA LIMITED , AYSCOUGH, Andrew , THOMPSON, Stephen , TAYLOR, Susanne , KHAN, Nawaz, Mohammed
发明人： AYSCOUGH, Andrew , THOMPSON, Stephen , TAYLOR, Susanne , KHAN, Nawaz, Mohammed
IPC分类号： C07D231/56 , C07D471/04 , A61K31/416 , A61K31/437 , A61P3/00
CPC分类号： C07D471/04 , C07D231/56
摘要： The invention discloses compounds of formula (I) wherein: R is a carboxylic acid or a derivative thereof; R 1 and R 2 are independently H or alkyl, or together R 1 and R 2 form an alkylene group; L 1 is a single bond, NH, NCH 3 , O, S, CH 2 or CH, wherein when L 1 is CH the dashed line indicates a double bond and R 2 is absent, otherwise the dashed line is a single bond; R 8 and R 9 are independently H, halo, alkyl or alkoxy; L 2 is O or S; L 3 is CH 2 or CH 2 CH 2 ; R 10 and R 11 are independently H, halo, CF 3 , OCF 3 , alkyl or alkoxy; Y 1 is CH or N; Y 2 is CH or N; and R 12 and R 13 are independently H, halo, CF 3 , OCF 3 , alkyl or alkoxy; or a pharmaceutically acceptable derivative thereof, useful for treating disorders mediated by peroxisome-proliferator-activated receptor (PPAR) subtype δ (PPARδ). The compounds of the invention are therefore useful in the treatment of metabolic syndrome, obesity, type-II diabetes, dyslipidemia, wound healing, inflammation, neurodegenerative disorders and multiple sclerosis.
摘要翻译：本发明公开了式（I）的化合物，其中：R是羧酸或其衍生物; R 1和R 2独立地是H或烷基，或者一起R 1和R 2形成亚烷基 ; L 1是单键，NH，NCH 3，O，S，CH 2或CH，其中当L 1， / SUP>是CH，虚线表示双键并且R 2不存在，否则虚线是单键; R 8和R 9独立地是H，卤素，烷基或烷氧基; L 2是O或S; CH 3是CH 2或CH 2 CH 2; R 10和R 11独立地为H，卤素，CF 3，OCF 3，烷基或烷氧基; Y 1是CH或N; Y 2是CH或N; R 12和R 12独立地为H，卤素，CF 3，OCF 3，烷基或烷氧基; 或其药学上可接受的衍生物，其可用于治疗由过氧化物酶体增殖物激活受体（PPAR）亚型d（PPARd）介导的病症。因此，本发明的化合物可用于治疗代谢综合征，肥胖症，II型糖尿病，血脂异常，伤口愈合，炎症，神经变性疾病和多发性硬化。

5. 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。

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明申请

WO2005072733A1 DYARYLUREA COMPOUNDS AS CHK-1 INHIBITORS 审中-公开
标题翻译： DYARYLUREA化合物作为CHK-1抑制剂
公开(公告)号：WO2005072733A1
公开(公告)日：2005-08-11
申请号：PCT/US2005/000635
申请日：2005-01-07
申请人： MILLENNIUM PHARMACEUTICALS, INC. , BOYLE, Robert, G. , IMOGAL, Hassan, Julien , CHERRY, Michael , KHAN, Nawaz, Mohammed
发明人： BOYLE, Robert, G. , IMOGAL, Hassan, Julien , CHERRY, Michael , KHAN, Nawaz, Mohammed
IPC分类号： A61K31/44
CPC分类号： C07D213/75 , C07D213/82 , C07D213/85 , C07D241/20 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： This invention provides compounds and methods for treating cancer. More particularly, the invention provides compounds that inhibit Chk-1. These compounds potentiate the action of DNA-damaging agents such as chemotherapy and radiation therapy. The ChK-1 inhibitors of the present invention have the formula: (I); or a pharmaceutically acceptable salt thereof, wherein: X 1 -X 3 are independently CH or N, provided that X 1 -X 3 are not all N; X 4 is CH or N; Z is O, S, N-R, or N-CN; R 1 is-T-W-or -V-T-W; W is -C(O)N(R 9 ) 2 , -N(R 6 )-C(O)-R 10 , -N(R 6 )-C(O)-N(R 9 ) 2 , -N(R 6 )-C(O)-OR 11 ,-O-C(O)-N(R 9 ) 2 , -NH-C(=NH)-R 10 , or -NH-(=NH)-NH-R 9 .
摘要翻译：本发明提供了治疗癌症的化合物和方法。更具体地，本发明提供抑制Chk-1的化合物。这些化合物增强DNA损伤剂如化学疗法和放射治疗的作用。本发明的ChK-1抑制剂具有下式：（I）; 或其药学上可接受的盐，其中：X1-X3独立地为CH或N，条件是X1-X3不全为N; X4是CH或N; Z是O，S，N-R或N-CN; R 1是-T-W-或-V-T-W; W是-C（O）N（R 9）2，-N（R 6）-C（O）-R 10，-N（R 6）-C（O）-N （R 9）2，-N（R 6）-C（O）-OR 11， - OC（O）-N（R 9）2，-NH-C（= NH） -R 10，或-NH - （= NH）-NH-R 9。

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