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公开(公告)号：US20200123176A1
公开(公告)日：2020-04-23
申请号：US16545070
申请日：2019-08-20
发明人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
IPC分类号： C07D519/00 , C07D513/04 , C07D487/04 , C07D471/04
摘要： The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
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公开(公告)号：US10226459B2
公开(公告)日：2019-03-12
申请号：US15719949
申请日：2017-09-29
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Fenglei Zhang , Brian W. Metcalf
IPC分类号： A61K31/496 , A61K31/40 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/4985 , A61K31/55 , A61K31/551 , C07D487/04 , C07D495/04 , C07D221/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , A61K31/495
摘要： The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
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公开(公告)号：US20180258105A1
公开(公告)日：2018-09-13
申请号：US15980400
申请日：2018-05-15
申请人： Incyte Corporation
发明人： Yun-Long Li , Brian W. Metcalf , Hui-Yin Li
IPC分类号： C07D519/00 , C07D473/34 , C07D513/04
CPC分类号： C07D519/00 , C07B2200/13 , C07D473/34 , C07D513/04
摘要： The present invention is related to crystalline forms of (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one which is a PI3K inhibitor useful in the treatment of cancer and other diseases.
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公开(公告)号：US20170050987A1
公开(公告)日：2017-02-23
申请号：US15221163
申请日：2016-07-27
发明人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
IPC分类号： C07D519/00
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
摘要翻译： 本发明提供调节磷酸肌醇3-激酶（PI3K）的活性的嘧啶酮，并且可用于治疗与PI3Ks的活性相关的疾病，包括例如炎症性疾病，基于免疫的疾病，癌症和其它疾病。
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公开(公告)号：US09067921B2
公开(公告)日：2015-06-30
申请号：US14176781
申请日：2014-02-10
申请人： Incyte Corporation
发明人： Chu-Biao Xue , Ganfeng Cao , Taisheng Huang , Lihua Chen , Ke Zhang , Anlai Wang , David J. Meloni , Rajan Anand , Joseph Glenn , Brian W. Metcalf
IPC分类号： A61K31/497 , C07D401/14 , A61K31/496 , A61K45/06 , C07D401/06 , C07D417/14 , C07D471/04 , A61K31/502 , A61K31/506
CPC分类号： C07D401/14 , A61K31/496 , A61K31/502 , A61K31/506 , A61K45/06 , C07D401/06 , C07D417/14 , C07D471/04 , A61K2300/00
摘要： The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.
摘要翻译： 本发明涉及式I化合物：其中可变取代基在本文中定义，其调节趋化因子受体如CCR5的活性或与其结合。 在一些实施方案中，本发明的化合物对CCR5是选择性的。 该化合物可用于例如治疗与趋化因子受体表达或活性相关的疾病，例如炎性疾病，免疫疾病和病毒感染。
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公开(公告)号：US20210253601A1
公开(公告)日：2021-08-19
申请号：US17038165
申请日：2020-09-30
发明人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
IPC分类号： C07D519/00 , C07D471/04 , C07D513/04 , C07D487/04
摘要： The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
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![SALTS OF (S)-7-(1-(9H-PURIN-6-YLAMINO)ETHYL)-6-(3-FLUOROPHENYL)-3-METHYL-5H-THIAZOLO[3,2-A]PYRIMIDIN-5-ONE](/abs-image/US/2019/07/04/US20190202840A1/abs.jpg.150x150.jpg)
7.发明申请公开(公告)号：US20190202840A1
公开(公告)日：2019-07-04
申请号：US16295435
申请日：2019-03-07
申请人： Incyte Corporation
发明人： Yun-Long Li , Brian W. Metcalf , Hui-Yin Li
IPC分类号： C07D519/00 , C07C309/04 , C07C65/03 , C07C55/14 , C07D473/34 , A61K45/06 , A61K31/52 , C07D513/04
CPC分类号： C07D519/00 , A61K31/52 , A61K45/06 , C07B2200/13 , C07C55/14 , C07C65/03 , C07C309/04 , C07D473/34 , C07D513/04
摘要： The present invention relates to salt forms of the phosphoinositide 3-kinase (PI3K) inhibitor (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one, pharmaceutical compositions comprising the same, and methods of using the salts and compositions for the treatment of PI3K-associated diseases such as cancer.
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公开(公告)号：US09975907B2
公开(公告)日：2018-05-22
申请号：US15221163
申请日：2016-07-27
发明人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
IPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D513/04
CPC分类号： C07D519/00 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
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公开(公告)号：US09957229B2
公开(公告)日：2018-05-01
申请号：US15602693
申请日：2017-05-23
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Colin Zhang , Brian W. Metcalf , Chunhong He , Ding-Quan Qian
IPC分类号： C07D471/10 , C07D207/06 , A61K31/407 , C07D491/107 , C07D513/10 , C07D498/20 , C07D495/04 , C07D493/10 , C07D491/20 , C07D491/10 , C07D487/10 , C07D487/08 , C07D487/04 , C07D471/04 , C07D417/04 , C07D413/14 , C07D413/10 , C07D405/14 , C07D405/04 , C07D403/04 , C07D401/14 , C07D401/10 , C07D401/06 , C07D401/04 , C07D333/34 , C07D295/185 , C07D221/20 , C07D217/26 , C07D217/06 , C07D213/38 , C07D211/70 , C07D211/66 , C07D211/64 , C07D211/58 , C07D211/52 , C07D211/48 , C07D211/46 , C07D211/34 , C07D211/22 , C07D211/18 , C07D211/16 , C07D209/70 , C07D209/62 , C07D209/52 , C07D209/44 , C07D209/42 , C07D209/08 , C07D207/27 , C07D207/16 , C07D207/14 , C07D207/12 , C07D207/10 , C07D207/08 , A61K31/4439
CPC分类号： C07D207/06 , A61K31/407 , A61K31/4439 , C07D207/08 , C07D207/10 , C07D207/12 , C07D207/14 , C07D207/16 , C07D207/27 , C07D209/08 , C07D209/42 , C07D209/44 , C07D209/52 , C07D209/62 , C07D209/70 , C07D211/16 , C07D211/18 , C07D211/22 , C07D211/34 , C07D211/46 , C07D211/48 , C07D211/52 , C07D211/58 , C07D211/64 , C07D211/66 , C07D211/70 , C07D213/38 , C07D217/06 , C07D217/26 , C07D221/20 , C07D295/185 , C07D333/34 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/10 , C07D413/14 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D493/10 , C07D495/04 , C07D498/20 , C07D513/10
摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
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公开(公告)号：US09801877B2
公开(公告)日：2017-10-31
申请号：US15204423
申请日：2016-07-07
发明人： Wenqing Yao , Jincong Zhuo , Meizhong Xu , Fenglei Zhang , Brian W. Metcalf
IPC分类号： A61K31/496 , A61K31/4545 , A61K31/4985 , A61K31/454 , A61K31/551 , C07D417/14 , C07D471/04 , C07D487/04 , C07D221/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D221/20 , C07D401/06 , C07D401/14 , C07D409/14 , C07D495/04 , A61K31/40 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/55
CPC分类号： A61K31/496 , A61K31/40 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/4985 , A61K31/55 , A61K31/551 , C07D221/20 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
摘要： The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
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