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公开(公告)号：US10961239B2
公开(公告)日：2021-03-30
申请号：US16475413
申请日：2018-01-03
发明人： Robert M. Borzilleri , Upender Velaparthi , Chetan Padmakar Darne , Peiying Liu , Manjunatha Narayana Rao Kamble , Balaji Seshadri , Raju Mannoori , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号： C07D487/04 , C07D401/14 , C07D471/04 , A61K45/06 , C07K16/28
摘要： The invention relates generally to compounds of formula (I) that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：US10399987B2
公开(公告)日：2019-09-03
申请号：US15747843
申请日：2016-07-27
发明人： Lalgudi S. Harikrishnan , Brian E. Fink , Robert M. Borzilleri , Gopikishan Tonukunuru , Jayakumar Sankara Warrier
IPC分类号： C07D487/04 , A61P35/00 , A61K31/519
摘要： The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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3.发明授权公开(公告)号：US09822112B2
公开(公告)日：2017-11-21
申请号：US15587679
申请日：2017-05-05
发明人： Ivar M. McDonald , Naidu S. Chowdari , Walter Lewis Johnson , Yong Zhang , Robert M. Borzilleri , Sanjeev Gangwar
IPC分类号： C07D487/04 , C07D519/00 , C07D471/04
CPC分类号： C07D471/04 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07D487/04 , C07D519/00 , C07K5/06052
摘要： Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
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4.发明申请公开(公告)号：US20170233392A1
公开(公告)日：2017-08-17
申请号：US15587679
申请日：2017-05-05
发明人： Ivar M. MCDONALD , Naidu S. Chowdari , Walter Lewis Johnson , Yong Zhang , Robert M. Borzilleri , Sanjeev Gangwar
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07D487/04 , C07D519/00 , C07K5/06052
摘要： Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
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5.发明授权Heteroarylene-bridged benzodiazepine dimers, conjugates thereof, and methods of making and using 有权异亚芳基桥连的苯并二氮杂二聚体，其共轭物，以及制备和使用方法公开(公告)号：US09526801B2
公开(公告)日：2016-12-27
申请号：US14994378
申请日：2016-01-13
发明人： Ivar M. McDonald , Naidu S. Chowdari , Walter Lewis Johnson , Yong Zhang , Robert M. Borzilleri , Sanjeev Gangwar
IPC分类号： C07D487/04 , C07D519/00 , A61K47/48 , C07K5/062
CPC分类号： C07D471/04 , A61K47/6803 , A61K47/6851 , A61K47/6889 , C07D487/04 , C07D519/00 , C07K5/06052
摘要： Benzodiazepine dimers having a structure represented by wherein X comprises a heteroaromatic moiety and is as further defined in the application; R1 is and the other variables in formulae (I), (Ia), and (Ib) are as defined in the application. Such dimers are useful as anti-cancer agents, especially when used in an antibody-drug conjugate (ADC).
摘要翻译： 并且式（I），（Ia）和（Ib）中的其它变量如申请中所定义。 这种二聚体可用作抗癌剂，特别是当用于抗体 - 药物偶联物（ADC）时。
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公开(公告)号：US09453048B2
公开(公告)日：2016-09-27
申请号：US14419975
申请日：2013-08-06
IPC分类号： A61K38/06 , C07K5/09 , C07D401/12 , C07D207/16 , C07K5/062 , C07K5/083 , A61K45/06
CPC分类号： C07K5/0815 , A61K38/06 , A61K45/06 , C07D207/16 , C07D401/12 , C07K5/06026 , C07K5/0806
摘要： There are disclosed compounds of formula (I) that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing said compounds.
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公开(公告)号：US20160264553A1
公开(公告)日：2016-09-15
申请号：US15043729
申请日：2016-02-15
发明人： Pingyu Ding , Marina Gelman , Todd Kinsella , Rajinder Singh , Somasekhar Bhamidipati , Upender Velaparthi , Robert M. Borzilleri , Hasibur Rahaman , Jayakumar Sankara Warrier
IPC分类号： C07D401/14 , C07B59/00 , C07D471/04 , C07D487/04 , C07C53/18 , C07C53/06
CPC分类号： C07D401/14 , C07B59/002 , C07B2200/05 , C07C53/06 , C07C53/18 , C07D471/04 , C07D487/04
摘要： Disclosed are 2,2′-bipyridyl compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein R1, Z and n are as described herein. In certain embodiments, a compound disclosed herein inhibits GDF8, and can be used to treat disease by blocking GDF8 signaling.
摘要翻译： 和其药学上可接受的盐，前药和N-氧化物（及其溶剂化物和水合物），其中R1，Z和n如本文所述。 在某些实施方案中，本文公开的化合物抑制GDF8，并且可以用于通过阻断GDF8信号传导来治疗疾病。
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公开(公告)号：US20150080440A1
公开(公告)日：2015-03-19
申请号：US14553081
申请日：2014-11-25
IPC分类号： C07D491/044 , C07D417/06
CPC分类号： C07D491/044 , C07D417/06 , C07D491/04 , C07D493/04
摘要： The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1-R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.
摘要翻译： 本发明涉及下列化合物，其中变量G，W，Q，X，Y，B1，B2，Z1，Z2和R1-R7如本文所定义，衍生物及其中间体的制备方法 。
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公开(公告)号：US20130338081A1
公开(公告)日：2013-12-19
申请号：US13921467
申请日：2013-06-19
CPC分类号： A61K38/08 , A61K45/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D413/14 , C07K7/02
摘要： There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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公开(公告)号：US20190292179A1
公开(公告)日：2019-09-26
申请号：US16316714
申请日：2017-07-19
发明人： Robert M. Borzilleri , Peiyung Liu , Andrew J. Tebben , Upender Velaparthi , Hasibur Rahaman , Gopikishan Tonukunuru , Jayakumar Sankara Warrier
IPC分类号： C07D471/04 , A61K31/437 , A61K31/5383 , A61K31/416 , A61K31/5025 , A61K39/395 , C07D403/04 , C07D487/04 , C07D498/04
摘要： The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
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