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公开(公告)号：US20120208819A1
公开(公告)日：2012-08-16
申请号：US13499835
申请日：2010-10-05
申请人： Joseph Arndt , Timothy Chan , Kevin Guckian , Gnanasambandam Kumaravel , Wen-Cherng Lee , Edward Yin-Shiang Lin , Daniel Scott , Lihong Sun , Jermaine Thomas , Kurt van Vloten , Deping Wang , Lei Zhang , Daniel Erlanson
发明人： Joseph Arndt , Timothy Chan , Kevin Guckian , Gnanasambandam Kumaravel , Wen-Cherng Lee , Edward Yin-Shiang Lin , Daniel Scott , Lihong Sun , Jermaine Thomas , Kurt van Vloten , Deping Wang , Lei Zhang , Daniel Erlanson
IPC分类号： A61K31/53 , C07D401/14 , C07D409/14 , A61P35/00 , A61K31/444 , A61K31/519 , A61K31/4439 , A61K31/517 , C07D471/04 , C07D401/12
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/452 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/517 , A61K31/519 , A61K31/53 , A61K31/5377 , A61K31/5383 , C07D213/82 , C07D213/85 , C07D241/26 , C07D241/28 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D417/14 , C07D473/34 , C07D487/04 , C07D491/052 , C07D498/04 , C07D519/00
摘要： The present invention provides compounds useful as inhibitors of PDK1. The present invention also provides compositions thereof, and methods of treating PDK1-mediated diseases.
摘要翻译： 本发明提供了可用作PDK1抑制剂的化合物。 本发明还提供了其组合物，以及治疗PDK1介导的疾病的方法。
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公开(公告)号：US20100166819A1
公开(公告)日：2010-07-01
申请号：US12086954
申请日：2006-12-22
申请人： Wen-Cherng Lee , Lihong Sun , Michael Hoemann , Deqiang Niu , Dingxue Yan , Claudio Chuaqui , Russell Petter , Helen (Xiaomei) Feng
发明人： Wen-Cherng Lee , Lihong Sun , Michael Hoemann , Deqiang Niu , Dingxue Yan , Claudio Chuaqui , Russell Petter , Helen (Xiaomei) Feng
IPC分类号： A61K31/55 , A61K9/00 , A61K31/502 , A61K31/517 , A61K31/438 , C07D487/10 , C07D401/14 , C07D403/14 , A61P35/00 , A61P9/12 , A61P9/10 , A61P27/02 , A61P1/16 , A61P13/12
CPC分类号： C07D487/10 , C07D471/10
摘要： The invention is related to compounds of formula (I) that can be used as antagonists of the TGFβ family type I receptors, Alk5 and/or Alk4, compositions and methods of use. The compounds of formula (I) can be employed in the prevention and/or treatment of diseases such as fibrosis (e.g., renal fibrosis, pulmonary fibrosis, and hepatic fibrosis), progressive cancers, or other diseases for which reduction of TGFβ family signaling activity is desirable.
摘要翻译： 本发明涉及可用作TGFβb拮抗剂的式（I）化合物; 家族I型受体，Alk5和/或Alk4，组合物和使用方法。 式（I）化合物可用于预防和/或治疗诸如纤维化（例如肾纤维化，肺纤维化和肝纤维化），进行性癌症或其它TGFβb的降低的疾病; 家庭信号传导活动是可取的。
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公开(公告)号：US20100144730A1
公开(公告)日：2010-06-10
申请号：US12307104
申请日：2007-07-02
申请人： Kenneth Egnard Lind , Kathy Cao , Edward Yin-shiang Lin , Thinh Ba Nguyen , Bradley T. Tangonan , Daniel A. Erlanson , Kevin Guckian , Robert Lowell Simmons , Wen-cherng Lee , Lihong Sun , Stig Hansen , Nuzhat Pathan , Lei Zhang
发明人： Kenneth Egnard Lind , Kathy Cao , Edward Yin-shiang Lin , Thinh Ba Nguyen , Bradley T. Tangonan , Daniel A. Erlanson , Kevin Guckian , Robert Lowell Simmons , Wen-cherng Lee , Lihong Sun , Stig Hansen , Nuzhat Pathan , Lei Zhang
IPC分类号： A61K31/437 , C07D471/04 , C07D487/04 , C07D413/14 , A61K31/519 , A61K31/5377 , A61P35/00
CPC分类号： C07D471/04 , A61K31/4412 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4985 , A61K31/506 , A61K31/519 , A61K31/5377 , C07D211/86 , C07D213/64 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04
摘要： The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
摘要翻译： 本发明提供吡啶基PDK1抑制剂和使用其制备癌症的方法。
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公开(公告)号：US07691865B2
公开(公告)日：2010-04-06
申请号：US10526839
申请日：2003-09-05
申请人： Wen-Cherng Lee , Mary Beth Carter , Lihong Sun , Paul Lyne , Claudio Chuaqui , Zhongli Zheng , Juswinder Singh , Paula Boriack-Sjodin
发明人： Wen-Cherng Lee , Mary Beth Carter , Lihong Sun , Paul Lyne , Claudio Chuaqui , Zhongli Zheng , Juswinder Singh , Paula Boriack-Sjodin
IPC分类号： A61K31/519 , C07D471/02 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04
摘要： Compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I:
摘要翻译： 式I的化合物对Alk 5和/或Alk 4具有出人意料的高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化疾病在内的许多疾病。 在一个实施方案中，本发明的特征在于式I的化合物：
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公开(公告)号：US07612094B2
公开(公告)日：2009-11-03
申请号：US10510459
申请日：2003-04-04
申请人： Wen-Cherng Lee , Lihong Sun , Feng Shan , Claudio Chuaqui , Zhongli Zheng , Russell C. Petter
发明人： Wen-Cherng Lee , Lihong Sun , Feng Shan , Claudio Chuaqui , Zhongli Zheng , Russell C. Petter
IPC分类号： A61K31/4545 , C07D401/14
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/00 , C07D487/08
摘要： Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders.In one embodiment, the invention features a compound of the general formula (I).
摘要翻译： 式（I）化合物对Alk 5和/或Alk 4具有出人意料的高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化疾病在内的许多疾病。 在一个实施方案中，本发明的特征在于通式（I）的化合物。
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公开(公告)号：US20080171755A1
公开(公告)日：2008-07-17
申请号：US11661531
申请日：2005-08-24
申请人： Wen-Cherng Lee , Lihong Sun , Claudio Chuaqui , Mark Comebise , Juswinder Singh , Feng Shan
发明人： Wen-Cherng Lee , Lihong Sun , Claudio Chuaqui , Mark Comebise , Juswinder Singh , Feng Shan
IPC分类号： A61K31/506 , C07D405/14 , C12N5/06 , A61P35/00 , A61P35/02 , A61P25/28
CPC分类号： C07D471/04 , C07D401/14 , C07D403/14 , C07D405/14
摘要： The invention is based on the discovery that compounds of formula (I) possess high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. The invention features a compound of formula (I) and uses thereof: formula (I).
摘要翻译： 本发明基于以下发现：式（I）化合物对Alk 5和/或Alk 4具有高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化疾病在内的许多疾病。 本发明的特征在于式（I）化合物及其用途：式（I）。
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公开(公告)号：US20060063809A1
公开(公告)日：2006-03-23
申请号：US10510459
申请日：2003-04-04
申请人： Wen-Cherng Lee , Lihong Sun , Feng Shan , Claudio Chuaqui , Zhongli Zheng , Russell Petter
发明人： Wen-Cherng Lee , Lihong Sun , Feng Shan , Claudio Chuaqui , Zhongli Zheng , Russell Petter
IPC分类号： A61K31/4545 , A61K31/4439 , C07D403/14
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D453/00 , C07D487/08
摘要： Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of the general formula (I).
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8.发明申请Novel CD40:CD154 binding interruptor compounds and use thereof to treat immunological complications 审中-公开新型CD40：CD154结合阻断剂及其用于治疗免疫并发症的药物公开(公告)号：US20070249682A1
公开(公告)日：2007-10-25
申请号：US11701983
申请日：2007-02-02
申请人： Zhongli Zheng , Mary Carter , YuSheng Liao , Lihong Sun , Leonid Kirkovsky , Susan Mrose , Yen-Ming Hsu , David Thomas , Gerald Shipps , Satish Jindal , George Lenz , Huw Nash
发明人： Zhongli Zheng , Mary Carter , YuSheng Liao , Lihong Sun , Leonid Kirkovsky , Susan Mrose , Yen-Ming Hsu , David Thomas , Gerald Shipps , Satish Jindal , George Lenz , Huw Nash
IPC分类号： A61K31/44 , A61P37/08 , C07C303/00 , C07D213/44
CPC分类号： A61K31/444 , C07C311/47 , C07D401/14 , F25B9/10 , F25B9/145 , F25B2309/1408 , F25B2309/1411 , F25B2309/1418 , F25B2309/1424 , F25B2309/14241
摘要： The present invention relates to novel CD40:CD154 binding interrupter compounds and use of these compounds and pharmaceutical compositions comprising them, to treat conditions associated with inappropriate CD154 activation in a subject. Specifically, this invention provides compounds which are identified by screening a library of small molecules for those that are capable of specifically binding CD154 and interrupting CD40:CD154 interaction.
摘要翻译： 本发明涉及新的CD40：CD154结合中断剂化合物，以及这些化合物和包含它们的药物组合物的用途，以治疗与受试者中不适当的CD154活化相关的病症。 具体地，本发明提供了通过筛选能够特异性结合CD154并中断CD40：CD154相互作用的那些的小分子文库来鉴定的化合物。
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公开(公告)号：US20060264440A1
公开(公告)日：2006-11-23
申请号：US10545179
申请日：2004-02-12
申请人： Wen-Cherng Lee , Lihong Sun , Feng Shan , Claudio Chuaqui , Mark Cornebise , Timothy Pontz , Mary Carter , Juswinder Singh , Paula Boriack-Sjodin , Leona Ling , Russell Petter
发明人： Wen-Cherng Lee , Lihong Sun , Feng Shan , Claudio Chuaqui , Mark Cornebise , Timothy Pontz , Mary Carter , Juswinder Singh , Paula Boriack-Sjodin , Leona Ling , Russell Petter
IPC分类号： A61K31/522 , A61K31/52 , A61K31/519 , A61K31/517 , C07D473/02 , C07D487/04
CPC分类号： C07D401/14 , C07D401/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention is based on the discovery that compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I (I).
摘要翻译： 本发明基于以下发现：式I化合物对Alk 5和/或Alk 4具有出人意料的高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化病症在内的许多疾病。 在一个实施方案中，本发明的特征在于式I（I）的化合物。
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公开(公告)号：US20060135517A1
公开(公告)日：2006-06-22
申请号：US10526653
申请日：2003-09-05
申请人： Wen-Cherng Lee , Mary Carter , Lihong Sun , Claudio Chuaqui , Juswinder Singh , Paula Boriack-Sjodin , Michael Choi
发明人： Wen-Cherng Lee , Mary Carter , Lihong Sun , Claudio Chuaqui , Juswinder Singh , Paula Boriack-Sjodin , Michael Choi
IPC分类号： A61K31/5377 , C07D471/02 , A61K31/506
CPC分类号： C07D471/04 , C07D471/02 , C07D487/04
摘要： Compounds of formula I possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of formula I:
摘要翻译： 式I的化合物对Alk 5和/或Alk 4具有出人意料的高亲和力，并且可用作其拮抗剂，用于预防和/或治疗包括纤维化疾病在内的许多疾病。 在一个实施方案中，本发明的特征在于式I的化合物：
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