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公开(公告)号：US09227969B2
公开(公告)日：2016-01-05
申请号：US14451563
申请日：2014-08-05
IPC分类号： C07D471/04 , A61K31/53 , A61K31/4745 , A61K31/506 , A61K31/513 , A61K31/437 , A61K45/06
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4745 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/53 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
摘要翻译： 本发明涉及式I化合物：其中n，R1，R2，R3a，R4和R5定义在发明概述中; 能够抑制MEK的活性。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来控制过度增殖性疾病如癌症的方法。
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公开(公告)号：US20130053346A1
公开(公告)日：2013-02-28
申请号：US13592511
申请日：2012-08-23
申请人： Aranapakam Venkatesan , Roger Astbury Smith , Subramanya Hosahalli , Vijay Potluri , Sunil Kumar Panigrahi , Vishnu Basetti , Karunasree Kunta
发明人： Aranapakam Venkatesan , Roger Astbury Smith , Subramanya Hosahalli , Vijay Potluri , Sunil Kumar Panigrahi , Vishnu Basetti , Karunasree Kunta
IPC分类号： A61K31/519 , A61K31/5377 , C07D519/00 , A61K31/541 , A61K31/55 , A61K31/551 , C07F9/6561 , A61K31/675 , A61P29/00 , A61P19/08 , A61P3/00 , A61P11/06 , A61P5/00 , A61P37/08 , A61P25/00 , C07D487/04
CPC分类号： C07D487/04 , C07D519/00 , C07F9/6561
摘要： The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
摘要翻译： 本申请提供了新的嘧啶并哒嗪酮化合物及其制备和使用方法。 这些化合物可用于通过向患者施用一种或多种化合物来治疗患者的炎症。 在一个实施方案中，新的嘧啶并哒嗪酮化合物具有式（I），并且R 1和R 2在本文中定义。
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公开(公告)号：US08729079B2
公开(公告)日：2014-05-20
申请号：US13592511
申请日：2012-08-23
申请人： Aranapakam Venkatesan , Roger Astbury Smith , Subramanya Hosahalli , Vijay Potluri , Sunil Kumar Panigrahi , Vishnu Basetti , Karunasree Kunta
发明人： Aranapakam Venkatesan , Roger Astbury Smith , Subramanya Hosahalli , Vijay Potluri , Sunil Kumar Panigrahi , Vishnu Basetti , Karunasree Kunta
IPC分类号： C07D487/04 , C07D519/00 , A61K31/519 , A61P29/00
CPC分类号： C07D487/04 , C07D519/00 , C07F9/6561
摘要： The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
摘要翻译： 本申请提供了新的嘧啶并哒嗪酮化合物及其制备和使用方法。 这些化合物可用于通过向患者施用一种或多种化合物来治疗患者的炎症。 在一个实施方案中，新的嘧啶并哒嗪酮化合物具有式（I），并且R 1和R 2在本文中定义。
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公开(公告)号：US08440662B2
公开(公告)日：2013-05-14
申请号：US13285227
申请日：2011-10-31
申请人： Roger Astbury Smith , Scott Kevin Thompson , Subramanya Hosahalli , Mallesham Bejugam , Srinivas Nanduri , Sunil Kumar Panigrahi , Natarajan Mahalingam
发明人： Roger Astbury Smith , Scott Kevin Thompson , Subramanya Hosahalli , Mallesham Bejugam , Srinivas Nanduri , Sunil Kumar Panigrahi , Natarajan Mahalingam
IPC分类号： A61K31/535 , C07D413/04 , C07D413/14
CPC分类号： C07D239/72 , A61K31/535 , C07D239/42 , C07D295/155 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
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公开(公告)号：US20120129851A1
公开(公告)日：2012-05-24
申请号：US13285227
申请日：2011-10-31
申请人： Roger Astbury Smith , Scott Kevin Thompson , Subramanya Hosahalli , Mallesham Bejugam , Srinivas Nanduri , Sunil Kumar Panigrahi , Natarajan Mahalingam
发明人： Roger Astbury Smith , Scott Kevin Thompson , Subramanya Hosahalli , Mallesham Bejugam , Srinivas Nanduri , Sunil Kumar Panigrahi , Natarajan Mahalingam
IPC分类号： A61K31/5377 , C07D413/04 , C07D471/04 , A61P29/00 , A61P35/02 , A61P11/00 , A61P9/10 , A61P1/00 , A61P35/00 , C07D413/14 , A61P19/02
CPC分类号： C07D239/72 , A61K31/535 , C07D239/42 , C07D295/155 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
摘要翻译： 本申请提供新的取代喹唑啉和吡啶并嘧啶化合物及其药学上可接受的盐。 还提供了制备这些化合物的方法。 通过向患者施用治疗有效量的一种或多种化合物，这些化合物可用于共同调节PI3K和/或mTOR活性。 通过这样做，这些化合物在治疗与PI3K / AKT / mTOR途径失调相关的病症中是有效的。 有利地，这些化合物表现为双重PI3K / mTOR抑制剂。 可以使用这些化合物治疗各种病症，并且包括以炎症或异常细胞增殖为特征的疾病。 在一个实施方案中，该疾病是癌症。
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