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公开(公告)号：US20140148494A1
公开(公告)日：2014-05-29
申请号：US14170101
申请日：2014-01-31
发明人： Shaomeng Wang , Yujun Zhao , Wei Sun , Sanjeev Kumar , Lance Leopold , Laurent Debussche , Cedric Barriere , Jean-Christophe Carry , Kwame Amaning
IPC分类号： C07D487/10 , A61K31/407 , A61N5/10 , A61K45/06
CPC分类号： A61N5/10 , A61K31/407 , A61K45/06 , C07D487/10 , A61K2300/00
摘要： Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
摘要翻译： 本文提供了药物化学领域中的化合物，组合物和方法。 本文提供的化合物和组合物涉及用作p53和MDM2之间相互作用的拮抗剂的螺 - 羟基吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。
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公开(公告)号：US20170281773A1
公开(公告)日：2017-10-05
申请号：US15619671
申请日：2017-06-12
发明人： Shaomeng Wang , Xu Ran , Yujun Zhao , Chao-Yie Yang , Liu Liu , Longchuan Bai , Donna McEachern , Jeanne Stuckey , Jennifer Lynn Meagher , Duxin Sun , Xiaoqin Li , Bing Zhou , Hacer Karatas , Ruijuan Luo , Arul Chinnaiyan , Irfan A. Asangani
IPC分类号： A61K45/06 , C07D487/04 , C07D471/04 , C07D491/056
CPC分类号： A61K45/06 , C07D471/04 , C07D487/04 , C07D491/056
摘要： Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
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公开(公告)号：US09675697B2
公开(公告)日：2017-06-13
申请号：US14204076
申请日：2014-03-11
发明人： Shaomeng Wang , Xu Ran , Yujun Zhao , Chao-Yie Yang , Liu Liu , Longchuan Bai , Donna McEachern , Jeanne Stuckey , Jennifer Lynn Meagher , Duxin Sun , Xiaoqin Li , Bing Zhou , Hacer Karatas , Ruijuan Luo , Arul Chinnaiyan , Irfan A. Asangani
IPC分类号： A61K31/519 , C07D471/04 , A61K45/06 , C07D487/04 , C07D491/056
CPC分类号： A61K45/06 , C07D471/04 , C07D487/04 , C07D491/056
摘要： Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
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公开(公告)号：US10391175B2
公开(公告)日：2019-08-27
申请号：US15619671
申请日：2017-06-12
发明人： Shaomeng Wang , Xu Ran , Yujun Zhao , Chao-Yie Yang , Liu Liu , Longchuan Bai , Donna McEachern , Jeanne Stuckey , Jennifer Lynn Meagher , Duxin Sun , Xiaoqin Li , Bing Zhou , Hacer Karatas , Ruijuan Luo , Arul Chinnaiyan , Irfan A. Asangani
IPC分类号： A61K31/519 , C07D471/04 , A61K45/06 , C07D487/04 , C07D491/056
摘要： Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
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![9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS](/abs-image/US/2015/09/03/US20150246923A1/abs.jpg.150x150.jpg)
5.发明申请9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS 有权9H-PYRIMIDO [4,5-B]吲哚和相关模拟物作为BROMODOMAIN抑制剂公开(公告)号：US20150246923A1
公开(公告)日：2015-09-03
申请号：US14633360
申请日：2015-02-27
发明人： Shaomeng Wang , Yujun Zhao , Bing Zhou , Angelo Aguilar , Liu Liu , Longchuan Bai , Donna McEachern , Duxin Sun , Bo Wen , Ruijuan Luo , Ting Zhao , Arul Chinnaiyan , Irfan A. Asangani , Jeanne Stuckey , Jennifer Lynn Meagher , Xu Ran
IPC分类号： C07D487/04 , C07D487/14 , C07D519/00
CPC分类号： C07D519/00 , A61K31/437 , A61K31/519 , A61K31/5377 , A61K31/538 , C07D487/04 , C07D487/14
摘要： The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
摘要翻译： 本公开提供取代的9H-嘧啶并[4,5-b]吲哚和5H-吡啶并[4,3-b]吲哚和由式I表示的相关类似物及其药学上可接受的盐，水合物和溶剂合物，其中R1a A，B1，B2，G，X1，Y1，Y2和Y3如说明书中所述。 本公开还涉及式I化合物用于治疗对抑制BET溴结构域有反应的病症或病症。 本公开的化合物特别可用于治疗癌症。
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公开(公告)号：US20130296303A1
公开(公告)日：2013-11-07
申请号：US13944587
申请日：2013-07-17
发明人： Shaomeng Wang , Shanghai Yu , Wei Sun , Sanjeev Kumar , Duxin Sun , Peng Zou , Donna McEachern , Yujun Zhao
IPC分类号： C07D487/10 , A61K31/5377 , A61K31/454 , A61K31/496 , A61K31/407 , A61K45/06
CPC分类号： C07D487/10 , A61K31/407 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D471/20 , C07D491/107 , C07D495/10 , C07F9/6561 , A61K2300/00
摘要： Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
摘要翻译： 本文提供了药物化学领域中的化合物，组合物和方法。 本文提供的化合物和组合物涉及用作p53和MDM2之间相互作用的拮抗剂的螺 - 羟基吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。
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![9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors](/abs-image/US/2017/02/28/US09580430B2/abs.jpg.150x150.jpg)
7.发明授权9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors 有权9H-嘧啶并[4,5-B]吲哚和相关类似物作为BET溴代寡核苷酸抑制剂公开(公告)号：US09580430B2
公开(公告)日：2017-02-28
申请号：US14633360
申请日：2015-02-27
发明人： Shaomeng Wang , Yujun Zhao , Bing Zhou , Angelo Aguilar , Liu Liu , Longchuan Bai , Donna McEachern , Duxin Sun , Bo Wen , Ruijuan Luo , Ting Zhao , Arul Chinnaiyan , Irfan A. Asangani , Jeanne Stuckey , Jennifer Lynn Meagher , Xu Ran , Yang Hu
IPC分类号： A01N43/54 , A61K31/505 , C07D491/00 , C07D487/04 , A61K31/519 , C07D487/14 , C07D519/00
CPC分类号： C07D519/00 , A61K31/437 , A61K31/519 , A61K31/5377 , A61K31/538 , C07D487/04 , C07D487/14
摘要： The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
摘要翻译： 本公开提供取代的9H-嘧啶并[4,5-b]吲哚和5H-吡啶并[4,3-b]吲哚和由式I表示的相关类似物及其药学上可接受的盐，水合物和溶剂合物，其中R1a A，B1，B2，G，X1，Y1，Y2和Y3如说明书中所述。 本公开还涉及式I化合物用于治疗对抑制BET溴结构域有反应的病症或病症。 本公开的化合物特别可用于治疗癌症。
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公开(公告)号：US09079913B2
公开(公告)日：2015-07-14
申请号：US14485054
申请日：2014-09-12
发明人： Shaomeng Wang , Shanghai Yu , Wei Sun , Sanjeev Kumar , Duxin Sun , Peng Zou , Donna McEachern , Yujun Zhao
IPC分类号： C07D487/10 , A61K31/407 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D491/107 , C07D495/10 , C07D471/20 , C07F9/6561
CPC分类号： C07D487/10 , A61K31/407 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/675 , A61K45/06 , C07D471/20 , C07D491/107 , C07D495/10 , C07F9/6561 , A61K2300/00
摘要： Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
摘要翻译： 本文提供了药物化学领域中的化合物，组合物和方法。 本文提供的化合物和组合物涉及用作p53和MDM2之间相互作用的拮抗剂的螺 - 羟基吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。
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9.发明申请BET BROMODOMAIN INHIBITORS AND THERAPEUTIC METHODS USING THE SAME 审中-公开BET BROMODOMAIN INHIBITORS AND THERAPEUTIC METHODS WITH THE SAME公开(公告)号：US20140256706A1
公开(公告)日：2014-09-11
申请号：US14204076
申请日：2014-03-11
发明人： Shaomeng Wang , Xu Ran , Yujun Zhao , Chao-Yie Yang , Liu Liu , Longchuan Bai , Donna McEachern , Jeanne Stuckey , Jennifer Lynn Meagher , Duxin Sun , Xiaoqin Li , Bing Zhou , Hacer Karatas , Ruijuan Luo , Arul Chinnaiyan , Irfan A. Asangani
IPC分类号： A61K31/5377 , A61K31/437 , A61K45/06 , C07D471/04 , C07D491/056 , A61K31/519 , C07D487/04
CPC分类号： A61K45/06 , C07D471/04 , C07D487/04 , C07D491/056
摘要： Inhibitors of BET bromodomains and compositions containing the same are disclosed. Methods of using the BET bromodomain inhibitors in the treatment of diseases and conditions wherein inhibition of BET bromodomain provides a benefit, like cancers, also are disclosed.
摘要翻译： 公开了BET溴结构域的抑制剂和含有它们的组合物。 还公开了使用BET溴域结构域抑制剂治疗其中抑制BET溴结构域提供益处的疾病和病症的方法，如癌症。
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![9H-pyrimido [4,5-B] indoles as BET bromodomain inhibitors](/abs-image/US/2019/06/04/US10307407B2/abs.jpg.150x150.jpg)
公开(公告)号：US10307407B2
公开(公告)日：2019-06-04
申请号：US15553593
申请日：2016-02-26
发明人： Shaomeng Wang , Yujun Zhao , Bing Zhou , Angelo Aguilar
IPC分类号： C07D487/04 , C07D487/14 , A61K31/437 , A61K31/519 , C07D231/38 , C07D261/06 , C07D471/04
摘要： The present disclosure provides substituted 9H-pyrimido [4,5-b] indoles and 5H-pyrido [4,3-b] indoles and related analogs represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, W, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains such as cancer. The present disclosure is also directed to the use of compound of Formula I as synthetic intermediates.
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