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公开(公告)号:US20080119512A1
公开(公告)日:2008-05-22
申请号:US12019045
申请日:2008-01-24
申请人: Adnan Mjalli , Robert Andrews , Ramosh Gopalaswamy , Chris Wysong
发明人: Adnan Mjalli , Robert Andrews , Ramosh Gopalaswamy , Chris Wysong
IPC分类号: A61K31/4704 , A61K31/165 , A61K31/4462
CPC分类号: C07D231/12 , C07C235/38 , C07C237/20 , C07C271/22 , C07C2601/08 , C07C2603/18 , C07D207/16 , C07D211/34 , C07D217/26 , C07D233/56 , C07D249/08 , C07D309/04
摘要: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
摘要翻译: 本发明提供某些化合物,其制备方法,包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物(RAGE)的受体与其配体如晚期糖基化终产物(AGE),S100 /钙粒蛋白/ EN-RAGE,β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ,以及由RAGE引起的人类疾病的管理,治疗,控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症,糖尿病晚期并发症的发展,例如血管通透性增加,肾病,动脉粥样硬化和视网膜病变,阿尔茨海默病的发展,勃起功能障碍和肿瘤侵袭和转移。
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公开(公告)号:US20100286197A1
公开(公告)日:2010-11-11
申请号:US12839877
申请日:2010-07-20
IPC分类号: A61K31/472 , A61P3/10 , A61P9/10 , A61P13/12 , A61K31/167 , A61K31/27 , A61K31/351 , A61K31/401 , A61K31/4174 , A61K31/4465
CPC分类号: C07D231/12 , C07C235/38 , C07C237/20 , C07C271/22 , C07C2601/08 , C07C2603/18 , C07D207/16 , C07D211/34 , C07D217/26 , C07D233/56 , C07D249/08 , C07D309/04
摘要: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
摘要翻译: 本发明提供某些化合物,其制备方法,包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物(RAGE)的受体与其配体如晚期糖基化终产物(AGE),S100 /钙粒蛋白/ EN-RAGE,淀粉样蛋白和 两性霉素,以及由RAGE引起的人类疾病的管理,治疗,控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症,糖尿病晚期并发症的发展,例如血管通透性增加,肾病,动脉粥样硬化和视网膜病变,阿尔茨海默病的发展,勃起功能障碍和肿瘤侵袭和转移。
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公开(公告)号:US07423177B2
公开(公告)日:2008-09-09
申请号:US10091759
申请日:2002-03-05
IPC分类号: C07C237/00 , C07C233/00 , C07C235/00 , A01N37/18
CPC分类号: C07D231/12 , C07C235/38 , C07C237/20 , C07C271/22 , C07C2601/08 , C07C2603/18 , C07D207/16 , C07D211/34 , C07D217/26 , C07D233/56 , C07D249/08 , C07D309/04
摘要: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.
摘要翻译: 本发明提供某些化合物,其制备方法,包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物(RAGE)的受体与其配体如晚期糖基化终产物(AGE),S100 /钙粒蛋白/ EN-RAGE,β-淀粉样蛋白和两性蛋白之间相互作用的调节剂 ,以及由RAGE引起的人类疾病的管理,治疗,控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症,糖尿病晚期并发症的发展,例如血管通透性增加,肾病,动脉粥样硬化和视网膜病变,阿尔茨海默病的发展,勃起功能障碍和肿瘤侵袭和转移。
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公开(公告)号:US20110039714A1
公开(公告)日:2011-02-17
申请号:US12901133
申请日:2010-10-08
申请人: Adnan M. M. Mjalli , Chris Wysong , Jerome Baudry , Thomas Scott Yokum , Rob Andrews , William K. Banner
发明人: Adnan M. M. Mjalli , Chris Wysong , Jerome Baudry , Thomas Scott Yokum , Rob Andrews , William K. Banner
CPC分类号: C07D231/56 , A61K31/416 , A61K31/454 , C07C229/34 , C07C235/20 , C07C235/52 , C07C237/08 , C07C237/20 , C07C237/22 , C07C237/24 , C07C237/52 , C07C271/22 , C07C271/24 , C07C271/26 , C07C275/24 , C07C275/26 , C07C275/30 , C07C275/42 , C07C307/08 , C07C311/06 , C07C311/16 , C07C311/19 , C07C311/20 , C07C323/60 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D207/09 , C07D231/12 , C07D237/04 , C07D243/08 , C07D243/14 , C07D249/12 , C07D277/38 , C07D307/20 , C07D307/52 , C07D309/10 , C07D309/14 , C07D335/02 , C07D407/12 , C07D409/12 , C07D417/04 , C40B40/04 , C40B50/14 , G01N33/53 , G01N33/94 , G01N2500/00 , G16B15/00 , G16B30/00 , G16C20/50
摘要: Aspects of the present invention include probes, methods, systems that have stand alone utility and may comprise features of a drug discovery system or method. The present invention also includes pharmaceutical compositions.In more detail, the present invention provides molecular probes and methods for producing molecular probes. The present invention provides also provides systems and methods for new drug discovery. An embodiment of the present invention utilizes sets of probes of the present invention and a new approach to computational chemistry in a drug discovery method having increased focus in comparison to heretofore utilized combinatorial chemistry. The present invention also provides computer software and hardware tools useful in drug discovery systems. In an embodiment of a drug discovery method of the present invention in silico methods and in biologico screening methods are both utilized to maximize the probability of success while minimizing the time and number of wet laboratory steps necessary to achieve the success.
摘要翻译: 本发明的方面包括具有独立效用并且可以包括药物发现系统或方法的特征的探针,方法,系统。 本发明还包括药物组合物。 更详细地,本发明提供了用于产生分子探针的分子探针和方法。 本发明还提供了用于新药物发现的系统和方法。 与迄今使用的组合化学相比,本发明的一个实施例利用了本发明的探针组合和新的药物发现方法中的计算化学方法,其具有增加的焦点。 本发明还提供了在药物发现系统中有用的计算机软件和硬件工具。 在本发明的药物发现方法的一个实施方案中,在计算机方法和生物鉴别筛选方法中都被用来最大化成功的可能性,同时最小化实现成功所需的湿实验室步骤的时间和数量。
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