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1. 发明申请

US20100234386A1 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：US20100234386A1
公开(公告)日：2010-09-16
申请号：US12599544
申请日：2008-05-08
申请人： Amita Chaudhari , Dashyant Dhanak , Carla Ann Donatelli , Thomas H. Faitg , Yanhong Feng , Steven David Knight , Cynthia A. Parrish , Jeffrey M. Ralph , Martha A. Sarpong , Domingos J. Silva
发明人： Amita Chaudhari , Dashyant Dhanak , Carla Ann Donatelli , Thomas H. Faitg , Yanhong Feng , Steven David Knight , Cynthia A. Parrish , Jeffrey M. Ralph , Martha A. Sarpong , Domingos J. Silva
IPC分类号： A61K31/498 , C07D401/02 , A61P29/00 , A61P9/00 , A61P25/00 , A61P11/06 , A61P13/12 , A61P35/00 , A61P15/00
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/14
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。

2. 发明申请

US20080081808A1 AZAINDOLE INHIBITORS OF AURORA KINASES 有权
公开(公告)号：US20080081808A1
公开(公告)日：2008-04-03
申请号：US11855183
申请日：2007-09-14
申请人： Martha Sarpong , Nicholas Adams , Jeffrey Axten , Amita Chaudhari , Dashyant Dhanak , Toshihiro Hamajima , Kenneth Newlander , Cynthia Parrish , Jerry Adams , Domingos Silva , Jun Tang
发明人： Martha Sarpong , Nicholas Adams , Jeffrey Axten , Amita Chaudhari , Dashyant Dhanak , Toshihiro Hamajima , Kenneth Newlander , Cynthia Parrish , Jerry Adams , Domingos Silva , Jun Tang
IPC分类号： A61K31/437 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/54 , A61P35/00 , C07D471/04
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.

3. 发明申请

US20080293706A1 QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS 失效
标题翻译：喹啉衍生物作为PI3激酶抑制剂
公开(公告)号：US20080293706A1
公开(公告)日：2008-11-27
申请号：US12117127
申请日：2008-05-08
申请人： Amita CHAUDHARI , Dashyant DHANAK , Carla Ann DONATELLI , Thomas H. FAITG , Yanhong FENG , Steven David KNIGHT , Cynthia A. PARRISH , Jeffrey M. RALPH
发明人： Amita CHAUDHARI , Dashyant DHANAK , Carla Ann DONATELLI , Thomas H. FAITG , Yanhong FENG , Steven David KNIGHT , Cynthia A. PARRISH , Jeffrey M. RALPH
IPC分类号： A61K31/498 , C07D413/14 , C07D241/36 , A61K31/541 , A61P35/02 , A61P35/00 , C07D279/12 , A61K31/5377
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07D417/14
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。

4. 发明申请

US20070265345A1 Novel Biphenyl Compounds And Their Use 审中-公开
标题翻译：新型联苯化合物及其用途
公开(公告)号：US20070265345A1
公开(公告)日：2007-11-15
申请号：US11632331
申请日：2005-07-27
申请人： Amita Chaudhari , Dashyant Dhanak , Steven Knight , David Morgans , Cynthia Parrish
发明人： Amita Chaudhari , Dashyant Dhanak , Steven Knight , David Morgans , Cynthia Parrish
IPC分类号： A61K31/17 , A61K31/165 , A61P35/00 , A61P37/00 , A61P43/00 , A61P9/00 , C07C233/00 , C07C273/18 , C07C275/00
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。具体地说，本发明涉及式Ⅰ化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和Y如下所定义，及其药学上可接受的盐。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，免疫疾病，真菌病症和炎症。因此，本发明进一步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。在另一方面，本发明提供筛选将结合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结合竞争的化合物。所述方法包括组合本发明的标记化合物，KSP驱动蛋白和至少一种候选试剂，并确定候选生物活性剂与KSP驱动蛋白的结合。另一方面，本发明提供筛选KSP驱动蛋白活性调节剂的方法。所述方法包括组合本发明的化合物，KSP驱动蛋白和至少一种候选试剂，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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