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1. 发明申请

WO2008125833A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008125833A1
公开(公告)日：2008-10-23
申请号：PCT/GB2008/001292
申请日：2008-04-14
申请人： PIRAMED LIMITED , THE INSTITUTE OF CANCER RESEARCH , BAKER, Stewart, James , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , KRINTEL, Sussie, Lerche , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
发明人： BAKER, Stewart, James , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , KRINTEL, Sussie, Lerche , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D487/04 , A61K31/5377 , A61P35/00
CPC分类号： C07D487/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14
摘要： The invention provides a compound which is a pyrimidine of formula (I): The compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了一种化合物，其是式（I）的嘧啶：该化合物是PI3K的抑制剂，因此可用于治疗与PI3激酶例如癌症，免疫疾病相关的异常细胞生长，功能或行为引起的疾病和病症，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍。

2. 发明申请

WO2008125839A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008125839A2
公开(公告)日：2008-10-23
申请号：PCT/GB2008001301
申请日：2008-04-14
申请人： PIRAMED LTD , CANCER RES INST , GOLDSMITH PAUL JOHN , HANCOX TIMOTHY COLIN , PEGG NEIL ANTHONY , SHUTTLEWORTH STEPHEN JOSEPH , DECHAUX ELSA AMANDINE , PRICE STEPHEN , LARGE JONATHAN MARTIN , MCDONALD EDWARD
发明人： GOLDSMITH PAUL JOHN , HANCOX TIMOTHY COLIN , PEGG NEIL ANTHONY , SHUTTLEWORTH STEPHEN JOSEPH , DECHAUX ELSA AMANDINE , PRICE STEPHEN , LARGE JONATHAN MARTIN , MCDONALD EDWARD
IPC分类号： C07D403/04 , A61K31/506 , A61P35/00 , C07D401/14 , C07D417/14
CPC分类号： C07D403/04 , C07D401/14 , C07D417/14
摘要： The invention provides compounds which are pyrimidines of formula (I): wherein R 2 is bonded at ring position 2 and -YR 1 is bonded at ring position 5 or 6, or YR 1 is bonded at ring position 2 and R 2 is bonded at ring position 6; R is an indol-4-yl group which is substituted at the 5- or 6-position; either: (a) Y is selected from -O-(CH 2 ) n -, -NH-(CH 2 ) n -,. -NHC(O)-(CH 2 )n and -C(O)NH-(CH2) n - wherein n is 0 or an integer of 1 to 3, and R 1 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted and a group -NR 3 R 4 wherein R 3 and R 4 , which are the same or different, are each independently selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted, C 3 - C 10 cycloalkyl which is unsubstituted or substituted, -C(O)R, -C(O)N(R) 2 and -S(O) m R, or R 3 and R4 together form, with the nitrogen atom to which they are attached, a saturated 5-, 6- or 7- membered N-containing heterocyclic group which is unsubstituted or substituted; (b) Y is a direct bond and R 1 is selected from an unsaturated 5- to 12-membered carbocyclic or heterocyclic group which is unsubstituted or substituted, and a group -NR3R4 wherein R 3 and R 4 , which are the same or different, are each independently selected from H, C 1 -C 6 alkyl which is unsubstituted or substituted, C 3 -C 10 cycloalkyl which is unsubstituted or substituted, -C(O)R, -C(O)N(R) 2 and -S(O) m R; R is selected from H, C 1 -C 6 alkyl, C 3 -C 10 cycloalkyl and a 5- to 12-membered aryl or heteroaryl group, which group is unsubstituted or substituted; and m is 1 or 2; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of PO K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PB kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：本发明提供了式（I）的嘧啶的化合物：其中R 2在环位置2键合，-YR 1在环5或6上键合，或 YR 1连接在环位置2，R 2结合在环位置6; R是在5或6位被取代的吲哚基-4-基; 或者：（a）Y选自-O-（CH 2）n - ， - NH-（CH 2 CH 2） ñ - ,. -NHC（O） - （CH 2）n和-C（O）NH-（CH 2）n - ，其中n为0或1〜3的整数， R 1和R 2选自未取代或取代的不饱和5至12元碳环或杂环基，且-NR 3 R 4，其中R 3和R 4相同或不同，各自独立地选自H，C 1 -C 3 未取代或取代的C 1 -C 6烷基，未取代或取代的C 1 -C 10环烷基，-C（O）R 1 -C（O ）N（R）2和-S（O）m R R或R 3和R 4一起与氮原子一起形成它们是未取代或取代的饱和的5-，6-或7-元的含N杂环基团; （b）Y是直接键，R 1选自未取代或取代的不饱和5-12元碳环或杂环基，和-NR 3 R 4基团，其中R 3 R 4和R 4相同或不同，各自独立地选自H，C 1 -C 6烷基，其中未取代或取代的C 3 -C 10烷基，未取代或取代的-C（O）R 1 -C（O）N（R） 2和-S（O）m R; R选自H，C 1 -C 6烷基，C 3 -C 10环烷基和5 至12元芳基或杂芳基，该基团是未取代的或取代的; m为1或2; 或其药学上可接受的盐。这些化合物是POK的抑制剂，因此可用于治疗与PB激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍相关的异常细胞生长，功能或行为引起的疾病和障碍和神经障碍。

3. 发明申请

WO2007115410A1 COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS 审中-公开
标题翻译：用于调制离子通道的组合物和方法
公开(公告)号：WO2007115410A1
公开(公告)日：2007-10-18
申请号：PCT/CA2007/000596
申请日：2007-04-10
申请人： PAINCEPTOR PHARMA CORPORATION , VOHRA, Rahul , GAN, Zhonghong , WEI, Chang-Qing , PRICE, Stephen , DYKE, Hazel, Joan , DECHAUX, Elsa, Amandine
发明人： VOHRA, Rahul , GAN, Zhonghong , WEI, Chang-Qing , PRICE, Stephen , DYKE, Hazel, Joan , DECHAUX, Elsa, Amandine
IPC分类号： C07D217/04 , A61K31/472 , A61K31/4725 , A61K31/497 , A61K31/501 , C07D401/04 , C07D401/14 , C07D413/04
CPC分类号： C07D471/04 , C07D209/40
摘要： The present invention relates to compounds of the Formula (I),(II), (III), (IV) or (V) useful to modulate the activity of gated ion channels. The invention further relates to methods wherein said compounds are used to modulate gated ion channels comprised of at least one subunit which is a member of the DEG/ENaC, P2X or TRPV gene superfamilies. The activity of the gated ion channels which are modulated by compounds I-V are associated with pain, inflammatory disorders or neurological disorders.
摘要翻译：本发明涉及可用于调节门控离子通道活性的式（I），（II），（III），（IV）或（V）化合物。本发明还涉及其中所述化合物用于调节由至少一个亚基组成的门控离子通道的方法，该亚基是DEG / ENaC，P2X或TRPV基因超家族的成员。由化合物I-V调节的门控离子通道的活性与疼痛，炎症性疾病或神经障碍有关。

4. 发明申请

WO2008152390A1 THIAZOLIOPYRIMIDINES AND THEIR USE AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3 KINASE 审中-公开
标题翻译：噻唑吡啶类和它们作为磷脂酰肌醇3激酶的抑制剂
公开(公告)号：WO2008152390A1
公开(公告)日：2008-12-18
申请号：PCT/GB2008/002014
申请日：2008-06-12
申请人： F.HOFFMANN-LA ROCHE AG , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , BESWICK, Mandy, Christine , BLENCH, Toby, Jonathan , DECHAUX, Elsa, Amandine , KULAGOWSKI, Janusz, Jozef , NADIN, Alan, John , PRICE, Stephen
发明人： HANCOX, Timothy, Colin , PEGG, Neil, Anthony , BESWICK, Mandy, Christine , BLENCH, Toby, Jonathan , DECHAUX, Elsa, Amandine , KULAGOWSKI, Janusz, Jozef , NADIN, Alan, John , PRICE, Stephen
IPC分类号： C07D513/04 , A61K31/519 , A61P35/00
CPC分类号： C07D513/04
摘要： Thiazolopyrimidines of formula (I): wherein W represents a thiazole ring; R 1 and R 2 form, together with the N atom to which they are attached, a group of the following formula (IIa): in which A is a ring system; m is 0, 1 or 2; R 3 is H or C 1 -C 6 alkyl; and R 4 is an indole group which is unsubstituted or substituted; and the pharmaceutically acceptable salts thereof are inhibitors of PI3K and are selective for the p110δ isoform, which is a class Ia PD kinase, over both other class Ia and class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
摘要翻译：式（I）的噻唑并嘧啶：其中W表示噻唑环; R1和R2与它们所连接的N原子一起形成下式（IIa）的基团：其中A是环系; m为0,1或2; R3是H或C1-C6烷基; R4是未取代或取代的吲哚基; 其药学上可接受的盐是PI3K的抑制剂，并且对于其它Ia类和1b类激酶对p110d亚型是Ia Ia激酶的选择性。该化合物可用于治疗与PI3激酶例如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌功能障碍和神经障碍相关的异常细胞生长，功能或行为引起的疾病和障碍。

5. 发明申请

WO2008125839A3 PYRIMIDINE DERIVATIVES AS INHIBITORS OF PHOSPHATIDYLINOSITOL-3-KINASE 审中-公开
公开(公告)号：WO2008125839A3
公开(公告)日：2008-10-23
申请号：PCT/GB2008/001301
申请日：2008-04-14
申请人： PIRAMED LIMITED , THE INSTITUTE OF CANCER RESEARCH , GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
发明人： GOLDSMITH, Paul, John , HANCOX, Timothy, Colin , PEGG, Neil, Anthony , SHUTTLEWORTH, Stephen, Joseph , DECHAUX, Elsa, Amandine , PRICE, Stephen , LARGE, Jonathan, Martin , MCDONALD, Edward
IPC分类号： C07D403/04 , C07D401/14 , C07D417/14 , A61K31/506 , A61P35/00
摘要： The invention provides compounds which are pyrimidines for formula (i): wherein R 1, R 2 are as described herein, and/or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of PI3K and may thus be used to treat diseases and disorders arising form abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.

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