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1. 发明申请

WO2011103546A1 TRIAZOLONES AS FATTY ACID SYNTHASE INHIBITORS 审中-公开
标题翻译：三唑酮作为脂肪酸合成酶抑制剂
公开(公告)号：WO2011103546A1
公开(公告)日：2011-08-25
申请号：PCT/US2011/025661
申请日：2011-02-22
申请人： GLAXOSMITHKLINE LLC , ADAMS, Nicholas, D. , AQUINO, Christopher, Joseph , CHAUDHARI, Amita, M. , GHERGUROVICH, Jonathan, M. , KIESOW, Terence, John , PARRISH, Cynthia, A. , REIF, Alexander, Joseph , WIGGALL, Kenneth
发明人： ADAMS, Nicholas, D. , AQUINO, Christopher, Joseph , CHAUDHARI, Amita, M. , GHERGUROVICH, Jonathan, M. , KIESOW, Terence, John , PARRISH, Cynthia, A. , REIF, Alexander, Joseph , WIGGALL, Kenneth
IPC分类号： A01N43/64 , A61K31/41
CPC分类号： C07D403/14 , A61K31/397 , A61K31/4196 , C07D401/14 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
摘要翻译：本发明涉及三唑酮衍生物用于调节，特别是抑制脂肪酸合酶（FAS）活性或功能的用途。合适地，本发明涉及三唑酮在治疗癌症中的用途。

2. 发明申请

WO2009021083A1 QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为PI3激酶抑制剂
公开(公告)号：WO2009021083A1
公开(公告)日：2009-02-12
申请号：PCT/US2008/072401
申请日：2008-08-07
申请人： SMITHKLINE BEECHAM CORPORATION , KNIGHT, Steven, David , PARISH, Cynthia, A. , RIDGERS, Lance, H. , SARPONG, Martha, A. , CHAUDHARI, Amita, M.
发明人： KNIGHT, Steven, David , PARISH, Cynthia, A. , RIDGERS, Lance, H. , SARPONG, Martha, A. , CHAUDHARI, Amita, M.
IPC分类号： A61K31/535
CPC分类号： C07D405/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D495/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.
摘要翻译：发明的是使用喹喔啉衍生物抑制PI3激酶的活性/功能的方法。还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应，通过施用喹喔啉衍生物的移植排斥和肺部损伤。

3. 发明申请

WO2008150827A1 NAPHTHYRIDINE, DERIVATIVES AS P13 KINASE INHIBITORS 审中-公开
标题翻译：萘啶，衍生物作为P13激酶抑制剂
公开(公告)号：WO2008150827A1
公开(公告)日：2008-12-11
申请号：PCT/US2008/065021
申请日：2008-05-29
申请人： SMITHKLINE BEECHAM CORPORATION , ADAMS, Nicholas, D. , BURGESS, Joelle, L. , CHAUDHARI, Amita, M. , KNIGHT, Steven, David , PARRISH, Cynthia, A.
发明人： ADAMS, Nicholas, D. , BURGESS, Joelle, L. , CHAUDHARI, Amita, M. , KNIGHT, Steven, David , PARRISH, Cynthia, A.
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： Invented is a method of inhibiting the activity/function of PB kinases using naphthyridine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of naphthyridine derivatives.
摘要翻译：本发明是使用萘啶衍生物抑制PB激酶的活性/功能的方法。还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应，通过施用萘啶衍生物的移植物排斥和肺损伤。

4. 发明申请

WO2012064642A1 FATTY ACID SYNTHASE INHIBITORS 审中-公开
标题翻译：脂肪酸合成酶抑制剂
公开(公告)号：WO2012064642A1
公开(公告)日：2012-05-18
申请号：PCT/US2011/059563
申请日：2011-11-07
申请人： GLAXOSMITHKLINE LLC , ADAMS, Nicholas, D. , CHAUDHARI, Amita, M. , KIESOW, Terence, John , PARRISH, Cynthia, Ann , REIF, Alexander, Joseph , RIDGERS, Lance, Howard , SCHMIDT, Stanley, J. , WIGGALL, Kenneth
发明人： ADAMS, Nicholas, D. , CHAUDHARI, Amita, M. , KIESOW, Terence, John , PARRISH, Cynthia, Ann , REIF, Alexander, Joseph , RIDGERS, Lance, Howard , SCHMIDT, Stanley, J. , WIGGALL, Kenneth
IPC分类号： A61K31/44
CPC分类号： C07D498/10 , A61K31/44 , A61K31/4709 , A61K31/499 , A61K31/5386 , A61K45/06 , C07D471/10 , C07D519/00
摘要： This invention relates to the use of spirocyclic piperidine derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of spirocyclic piperidines in the treatment of cancer.
摘要翻译：本发明涉及螺环哌啶衍生物用于调节，特别是抑制脂肪酸合成酶（FAS）活性或功能的用途。合适地，本发明涉及螺环哌啶在治疗癌症中的用途。

5. 发明申请

WO2011066211A1 AZABENZIMIDAZOLES AS FATTY ACID SYNTHASE INHIBITORS 审中-公开
标题翻译： AZABENZIMIDAZOLES作为脂肪酸合成酶抑制剂
公开(公告)号：WO2011066211A1
公开(公告)日：2011-06-03
申请号：PCT/US2010/057594
申请日：2010-11-22
申请人： GLAXOSMITHKLINE LLC , CHAUDHARI, Amita, M. , HALLMAN, Jason , LAUDEMAN, Christopher, P. , MUSSO, David, Lee , PARRISH, Cynthia, A.
发明人： CHAUDHARI, Amita, M. , HALLMAN, Jason , LAUDEMAN, Christopher, P. , MUSSO, David, Lee , PARRISH, Cynthia, A.
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D473/40 , C07D519/00
摘要： This invention relates to the use of azabenzimidazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of azabenzimidazoles in the treatment of cancer.
摘要翻译：本发明涉及氮杂苯并咪唑衍生物用于调节，特别是抑制脂肪酸合成酶（FAS）的活性或功能的用途。合适地，本发明涉及氮杂苯并咪唑在治疗癌症中的用途。

6. 发明申请

WO2009021083A8 QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS 审中-公开
标题翻译：喹喔啉衍生物作为PI3激酶抑制剂
公开(公告)号：WO2009021083A8
公开(公告)日：2009-04-09
申请号：PCT/US2008072401
申请日：2008-08-07
申请人： SMITHKLINE BEECHAM CORP , KNIGHT STEVEN DAVID , PARRISH CYNTHIA A , RIDGERS LANCE H , SARPONG MARTHA A , CHAUDHARI AMITA M
发明人： KNIGHT STEVEN DAVID , PARRISH CYNTHIA A , RIDGERS LANCE H , SARPONG MARTHA A , CHAUDHARI AMITA M
IPC分类号： A61K31/535
CPC分类号： C07D405/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D471/04 , C07D495/04
摘要： Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.
摘要翻译：本发明是使用喹喔啉衍生物来抑制PI3激酶的活性/功能的方法。还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经退行性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，喹喔啉衍生物的移植排斥和肺损伤。

7. 发明申请

WO2008144464A1 QUINOLINE DERIVATIVES AS P13 KINASE INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为P13激酶抑制剂
公开(公告)号：WO2008144464A1
公开(公告)日：2008-11-27
申请号：PCT/US2008/063821
申请日：2008-05-16
申请人： SMITHKLINE BEECHAM CORPORATION , ADAMS, Nicholas, D. , CHAUDHARI, Amita, M. , DONATELLI, Carla, A. , KNIGHT, Steven, David , NEWLANDER, Kenneth, Allen , PARRISH, Cynthia, A. , RIDGERS, Lance , SARPONG, Martha, A.
发明人： ADAMS, Nicholas, D. , CHAUDHARI, Amita, M. , DONATELLI, Carla, A. , KNIGHT, Steven, David , NEWLANDER, Kenneth, Allen , PARRISH, Cynthia, A. , RIDGERS, Lance , SARPONG, Martha, A.
IPC分类号： A61K31/47
CPC分类号： C07D498/04 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/5383 , A61K31/549 , A61K45/06 , C07D285/24 , C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Invented is a method of inhibiting the activity/function of PB kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.
摘要翻译：本发明是使用喹啉衍生物抑制PB激酶的活性/功能的方法。还发明了一种治疗选自以下的一种或多种疾病状态的方法：自身免疫性疾病，炎性疾病，心血管疾病，神经变性疾病，变态反应，哮喘，胰腺炎，多器官功能衰竭，肾脏疾病，血小板聚集，癌症，精子活力，移植排斥反应，通过给药喹啉衍生物的移植物排斥反应和肺损伤。

8. 发明申请

WO2007076348A3 AZAINDOLE INHIBITORS OF AURORA KINASES 审中-公开
标题翻译： AURORA KINASES的AZAINDOLE抑制剂
公开(公告)号：WO2007076348A3
公开(公告)日：2007-11-01
申请号：PCT/US2006062289
申请日：2006-12-19
申请人： SMITHKLINE BEECHAM CORP , ADAMS JERRY LEROY , ADAMS NICHOLAS D , AXTEN JEFFREY MICHAEL , CHAUDHARI AMITA M , DHANAK DASHYANT , HAMAJIMA TOSHIHIRO , NEWLANDER KENNETH ALLEN , PARRISH CYNTHIA A , SARPONG MARTHA A , SILVA DOMINGOS J , TANG JUN
发明人： ADAMS JERRY LEROY , ADAMS NICHOLAS D , AXTEN JEFFREY MICHAEL , CHAUDHARI AMITA M , DHANAK DASHYANT , HAMAJIMA TOSHIHIRO , NEWLANDER KENNETH ALLEN , PARRISH CYNTHIA A , SARPONG MARTHA A , SILVA DOMINGOS J , TANG JUN
IPC分类号： A61K31/335
CPC分类号： C07D471/04
摘要： The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.
摘要翻译：本发明涉及由式（I）表示的化合物及其药学上可接受的盐。本发明的化合物抑制Aurora激酶，使其特别适用于治疗许多疾病，包括实体瘤癌症和血液癌症。

9. 发明申请

WO2007076348A2 AZAINDOLE INHIBITORS OF AURORA KINASES 审中-公开
标题翻译：恶唑酮的AZAINDOLE抑制剂
公开(公告)号：WO2007076348A2
公开(公告)日：2007-07-05
申请号：PCT/US2006/062289
申请日：2006-12-19
申请人： SMITHKLINE BEECHAM CORPORATION , ADAMS, Jerry, Leroy , ADAMS, Nicholas, D. , AXTEN, Jeffrey, Michael , CHAUDHARI, Amita, M. , DHANAK, Dashyant , HAMAJIMA, Toshihiro , NEWLANDER, Kenneth, Allen , PARRISH, Cynthia, A. , SARPONG, Martha, A. , SILVA, Domingos, J. , TANG, Jun
发明人： ADAMS, Jerry, Leroy , ADAMS, Nicholas, D. , AXTEN, Jeffrey, Michael , CHAUDHARI, Amita, M. , DHANAK, Dashyant , HAMAJIMA, Toshihiro , NEWLANDER, Kenneth, Allen , PARRISH, Cynthia, A. , SARPONG, Martha, A. , SILVA, Domingos, J. , TANG, Jun
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.
摘要翻译：本发明涉及由式（I）表示的化合物：及其药学上可接受的盐。本发明的化合物抑制极光激酶，使其特别适用于治疗许多疾病，包括实体肿瘤癌症和血液癌症。

10. 发明申请

WO2006020358A3 NOVEL BIPHENYL COMPOUNDS AND THEIR USE 审中-公开
标题翻译：新型联烯化合物及其用途
公开(公告)号：WO2006020358A3
公开(公告)日：2006-12-28
申请号：PCT/US2005026214
申请日：2005-07-27
申请人： SMITHKLINE BEECHAM CORP , CYTOKINETICS , CHAUDHARI AMITA M , DHANAK DASHYANT , KNIGHT STEVEN DAVID , MORGANS DAVID J JR , PARRISH CYNTHIA A
发明人： CHAUDHARI AMITA M , DHANAK DASHYANT , KNIGHT STEVEN DAVID , MORGANS DAVID J JR , PARRISH CYNTHIA A
IPC分类号： A61K31/335 , A61K31/167 , A61K31/17 , C07C233/15 , C07C275/28 , C07C275/32 , C07C275/40 , C07C335/16 , C07C335/20 , C07D319/06
CPC分类号： C07C275/28 , C07C233/15 , C07C233/43 , C07C259/06 , C07C275/30 , C07C275/40 , C07C275/42 , C07C275/64 , C07C317/24 , C07C317/42 , C07C323/44 , C07C335/16 , C07D209/02 , C07D307/79 , C07D317/66 , C07D319/18
摘要： The invention is directed to certain biphenyl compounds. Specifically, the invention is directed to compounds according to Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and Y are as defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are KSP inhibitors, particularly human KSP inhibitors, and can be useful for the treatment for a variety of diseases and conditions, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders, fungal disorders, and inflammation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting KSP and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. In an additional aspect, the invention provides methods of screening for compounds that will bind to a KSP kinesin, for example compounds that will displace or compete with the binding of the compounds of the invention. The methods comprise combining a labeled compound of the invention, a KSP kinesin, and at least one candidate agent and determining the binding of the candidate bioactive agent to the KSP kinesin. In a further aspect, the invention provides methods of screening for modulators of KSP kinesin activity. The methods comprise combining a compound of the invention, a KSP kinesin, and at least one candidate agent and determining the effect of the candidate bioactive agent on the KSP kinesin activity.
摘要翻译：本发明涉及某些联苯化合物。具体而言，本发明涉及式（I）的化合物及其药学上可接受的盐：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和Y如下定义。本发明的化合物是KSP抑制剂，特别是人KSP抑制剂，并且可用于治疗各种疾病和病症，例如癌症，增生，再狭窄，心脏肥大，免疫病症，真菌病症和炎症。因此，本发明还涉及包含本发明化合物的药物组合物。本发明还涉及使用本发明化合物或包含本发明化合物的药物组合物抑制KSP和治疗与其相关的病症的方法。另一方面，本发明提供了筛选结合KSP驱动蛋白的化合物的方法，例如将取代或与本发明化合物的结合竞争的化合物。该方法包括将标记的本发明化合物，KSP驱动蛋白和至少一种候选试剂组合并确定候选生物活性剂与KSP驱动蛋白的结合。另一方面，本发明提供了筛选KSP驱动蛋白活性调节剂的方法。该方法包括将本发明化合物，KSP驱动蛋白和至少一种候选试剂组合，并确定候选生物活性剂对KSP驱动蛋白活性的影响。

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