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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：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：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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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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公开(公告)号：US20170035751A1
公开(公告)日：2017-02-09
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 , A61K31/495 , A61K31/4985 , A61K31/55 , A61K31/551 , A61K31/40 , A61K31/4709 , A61K31/4725 , A61K31/4545 , A61K31/454
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.
摘要翻译： 对映异构体，非对映异构体，前药，溶剂合物，代谢物或其药学上可接受的盐，其中在此提供组成变量。 式I和II的化合物是金属蛋白酶的调节剂，并且可用于治疗与金属蛋白酶活性相关的疾病，例如关节炎，癌症，心血管疾病，皮肤病，炎症和变态反应。
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公开(公告)号：US20180362546A1
公开(公告)日：2018-12-20
申请号：US15959942
申请日：2018-04-23
发明人： Yun-Long Li , Brian W. Metcalf , Andrew P. Combs
IPC分类号： C07D519/00 , C07D487/04 , C07D471/04 , 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：US20170334847A1
公开(公告)日：2017-11-23
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： C07D207/06 , A61K31/407 , C07D495/04 , C07D493/10 , C07D491/20 , C07D491/107 , C07D491/10 , C07D487/10 , C07D487/08 , C07D487/04 , C07D471/10 , 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 , C07D498/20 , C07D513/10
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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