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公开(公告)号：US20210188872A1
公开(公告)日：2021-06-24
申请号：US17118891
申请日：2020-12-11
IPC分类号： C07D498/06 , C07D498/16 , C07D471/06 , A61P35/00 , C07D519/00
摘要： The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
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公开(公告)号：US10442803B2
公开(公告)日：2019-10-15
申请号：US15688313
申请日：2017-08-28
申请人： Incyte Corporation
发明人： James D. Rodgers , Stacey Shepard , Haisheng Wang , Lixin Shao
IPC分类号： C07D471/14 , A61K31/437
摘要： The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
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![Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors](/abs-image/US/2019/09/03/US10398699B2/abs.jpg.150x150.jpg)
33.发明授权公开(公告)号：US10398699B2
公开(公告)日：2019-09-03
申请号：US15960069
申请日：2018-04-23
发明人： James D. Rodgers , Stacey Shepard
IPC分类号： A61K31/519 , A61P35/04 , C07D487/04 , C07D471/04 , A61K45/06 , C07D417/04 , C07B59/00 , A61K9/00 , A61K9/20 , A61K31/573
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
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![Heteroaryl substituted pyrrolo[2,3-B] pyridines and pyrrolo[2,3-B] pyrimidines as janus kinase inhibitors](/abs-image/US/2018/05/22/US09974790B2/abs.jpg.150x150.jpg)
34.发明授权公开(公告)号：US09974790B2
公开(公告)日：2018-05-22
申请号：US15356957
申请日：2016-11-21
发明人： James D. Rodgers , Stacey Shepard
IPC分类号： A61K31/519 , A61P17/06 , A61P17/14 , C07D471/04 , C07D487/04 , A61K45/06 , C07D417/04 , C07B59/00 , A61K9/00 , A61K9/20 , A61K31/573 , A61K31/437
CPC分类号： A61K31/519 , A61K9/0014 , A61K9/0053 , A61K9/20 , A61K31/573 , A61K45/06 , C07B59/002 , C07B2200/05 , C07D417/04 , C07D471/04 , C07D487/04
摘要： The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
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![Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile](/abs-image/US/2016/12/06/US09512161B2/abs.jpg.150x150.jpg)
35.发明授权Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-D]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile 有权3-（4-（7H-吡咯并[2,3-D]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的羟基，酮基和葡糖苷酸衍生物公开(公告)号：US09512161B2
公开(公告)日：2016-12-06
申请号：US14263476
申请日：2014-04-28
发明人： James D. Rodgers , Adam Shilling , Argyrios G. Arvanitis , Stacey Shepard , Laurine G. Galya , Mei Li , Frank M. Nedza
IPC分类号： A61K31/519 , C07H17/02 , C07D403/04 , C07D405/12 , C07D487/04
CPC分类号： C07H17/02 , A61K31/519 , C07D403/04 , C07D405/12 , C07D487/04
摘要： The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.
摘要翻译： 本发明提供3-（4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的羟基，酮基和葡糖苷酸衍生物。
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![SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE](/abs-image/US/2016/11/24/US20160339031A1/abs.jpg.150x150.jpg)
36.发明申请SALTS OF THE JANUS KINASE INHIBITOR (R)-3-(4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE 有权甘油激酶抑制剂（R）-3-（4-（7H-吡咯烷并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙烯酸的盐公开(公告)号：US20160339031A1
公开(公告)日：2016-11-24
申请号：US15164518
申请日：2016-05-25
发明人： James D. Rodgers , Hui-Yin Li
IPC分类号： A61K31/519 , A61K9/20 , A61K9/00
CPC分类号： A61K31/519 , A61K9/0053 , A61K9/20 , C07B2200/07 , C07B2200/13 , C07D487/04
摘要： The present invention provides salt forms of (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile that are useful in the modulation of Janus kinase activity and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
摘要翻译： 本发明提供（R）-3-（4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的盐形式，其可用于 Janus激酶活性的调节，并且可用于治疗与Janus激酶活性相关的疾病，包括例如免疫相关疾病，皮肤病，骨髓增生性疾病，癌症和其它疾病。
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公开(公告)号：US09309246B2
公开(公告)日：2016-04-12
申请号：US14575284
申请日：2014-12-18
申请人： Incyte Corporation
发明人： James D. Rodgers , Stacey Shepard , Haisheng Wang , Lixin Shao
IPC分类号： C07D471/14
CPC分类号： C07D471/14 , A61K31/437
摘要： The present invention relates to tricyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
摘要翻译： 本发明涉及作为BET蛋白如BRD2，BRD4，BRD4和BRD-t的抑制剂的三环杂环，可用于治疗诸如癌症的疾病。
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公开(公告)号：US09227985B2
公开(公告)日：2016-01-05
申请号：US14212721
申请日：2014-03-14
申请人： Incyte Corporation
IPC分类号： C07D498/16 , C07D471/06 , C07D498/06
CPC分类号： C07D498/06 , C07D471/06 , C07D498/16 , C07D519/00
摘要： The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
摘要翻译： 本发明涉及式（I）的三环杂环：其是BET蛋白如BRD2，BRD3，BRD4和BRD-t的抑制剂，可用于治疗疾病如癌症。
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39.发明申请CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES AS JANUS KINASE INHIBITORS 审中-公开作为JANUS KINASE抑制剂的CYCLOBUTANE AND METHYLCYCLOBUTANE DERIVATIVES公开(公告)号：US20150087662A1
公开(公告)日：2015-03-26
申请号：US14499916
申请日：2014-09-29
申请人： Incyte Corporation
发明人： Yun-Long Li , James D. Rodgers
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to cyclobutane and methylcyclobutane derivatives, as well as their salts, compositions, and methods of use, which are Janus kinase (JAK) inhibitors useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer and myeloproliferative disorders.
摘要翻译： 本发明涉及环丁烷和甲基环丁烷衍生物，以及它们的盐，组合物和使用方法，其是可用于治疗JAK相关疾病的Janus激酶（JAK）抑制剂，包括例如炎性和自身免疫性疾病， 以及癌症和骨髓增生性疾病。
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![HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE](/abs-image/US/2014/12/25/US20140378400A1/abs.jpg.150x150.jpg)
40.发明申请HYDROXYL, KETO, AND GLUCURONIDE DERIVATIVES OF 3-(4-(7H-PYRROLO[2,3-d]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-3-CYCLOPENTYLPROPANENITRILE 有权3-（4-（7H-吡咯烷并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环丙基丙烯酸的羟基，羟甲基和羟基胆碱衍生物公开(公告)号：US20140378400A1
公开(公告)日：2014-12-25
申请号：US14263476
申请日：2014-04-28
申请人： Incyte Corporation
发明人： James D. Rodgers , Adam Shilling , Argyrios G. Arvanitis , Stacey Shepard , Laurine G. Galya , Mei Li , Frank M. Nedza
IPC分类号： C07H17/02 , C07D487/04
CPC分类号： C07H17/02 , A61K31/519 , C07D403/04 , C07D405/12 , C07D487/04
摘要： The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.
摘要翻译： 本发明提供3-（4-（7H-吡咯并[2,3-d]嘧啶-4-基）-1H-吡唑-1-基）-3-环戊基丙腈的羟基，酮基和葡糖苷酸衍生物。
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