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1. 发明公开

EP1928847A4 THERAMUTEIN MODULATORS 审中-公开
标题翻译： THERAMUTEINMODULATOREN
公开(公告)号：EP1928847A4
公开(公告)日：2011-08-10
申请号：EP06824860
申请日：2006-08-29
申请人： HOUSEY GERARD M
发明人： HOUSEY GERARD M
IPC分类号： C07D265/00 , A01N43/58 , A61K31/535 , C07D237/02
CPC分类号： C07D239/48 , C07D213/77 , C07D215/38 , C07D253/07 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D417/14

2. 发明公开

EP1581307A4 IRS MODULATORS 失效转让
标题翻译： IRS调节剂
公开(公告)号：EP1581307A4
公开(公告)日：2009-02-11
申请号：EP03808631
申请日：2003-12-31
申请人： HOUSEY GERARD M , WHITE MORRIS F
发明人： HOUSEY GERARD M , WHITE MORRIS F
IPC分类号： A61K20060101 , A61P5/00 , C07K14/47 , C12Q1/68 , A61K38/22 , A61K38/26 , A61K45/00 , A61K48/00
CPC分类号： A61K38/26 , A61K38/00 , A61K38/22 , A61K48/00 , C07K14/47 , G01N33/68 , G01N33/74 , G01N2500/04 , G01N2800/042
摘要： This invention is directed to a general method for the chronic treatment, potential cure, or prevention of various metabolic and related diseases in people, including diabetes, by modulating IRS2 activity in cells and tissues in the body. IRS1 and IRS2 are part of the insulin or insulin-like growth factor signaling pathway. By upregulating the levels or functional activity of IRS2, insuling is used more efficiently by the body to control nutrient levels. By upregulating IRS2 levels or functional activity in pancreatic β-cells, glucose sensing and insulin secretion are enhanced.

3. 发明公开

EP1960535A4 COMPOUNDS AND METHODS OF IDENTIFYING, SYNTHESIZING, OPTIMIZING AND PROFILING PROTEIN MODULATORS 有权
标题翻译：化合物和鉴定，合成，优化和蛋白调节剂的创建方法
公开(公告)号：EP1960535A4
公开(公告)日：2011-04-06
申请号：EP06838389
申请日：2006-11-24
申请人： HOUSEY GERARD M
发明人： HOUSEY GERARD M
IPC分类号： G01N33/50 , C12Q1/50
CPC分类号： G01N33/5008 , G01N33/5011 , G01N33/502
摘要： This invention relates to methods of identifying, synthesizing, optimizing and profiling compounds that are inhibitors or activators of proteins, both naturally occurring endogenous proteins as well as certain variant forms of endogenous proteins, and novel methods of identifying such variants. The method accelerates the identification and development of compounds as potential therapeutically effective drugs by simplifying the pharmaceutical discovery and creation process through improvements in hit identification, lead optimization, biological profiling, and rapid elimination of toxic compounds. Implementation results in overall cost, reductions in the drug discovery process resulting from the corresponding increases in efficiency.
摘要翻译：本发明涉及鉴定，合成，优化和建档的化合物的方法是抑制剂或激活剂那样的蛋白，天然存在的内源蛋白质，以及内源性蛋白质的某些变体形式，和识别检测变体的新方法。该方法通过命中鉴定，先导优化，生物分析和快速消除有毒化合物的改进，简化药品发现和创造进程的加快为潜在的治疗有效的药物化合物的鉴定和发展。实施效果总体费用，在药物发现过程从效率的相应升幅则所得的减少。

4. 发明公开

EP1751115A4 THERAMUTEIN MODULATORS 审中-公开
标题翻译： THERAMUTEINMODULATOREN
公开(公告)号：EP1751115A4
公开(公告)日：2010-10-20
申请号：EP05754265
申请日：2005-05-23
申请人： HOUSEY GERARD M
发明人： HOUSEY GERARD M
IPC分类号： C07D213/81 , C07D213/87 , C07D215/50 , C07D231/14 , C07D237/02 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D401/12 , C07D405/12 , C07D409/12
CPC分类号： A61K31/5377 , A61K31/166 , A61K31/175 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/4196 , A61K31/44 , A61K31/4436 , A61K31/444 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/53 , C07C243/38 , C07D213/77 , C07D213/81 , C07D213/86 , C07D213/87 , C07D215/38 , C07D215/50 , C07D231/14 , C07D239/42 , C07D239/48 , C07D239/84 , C07D253/065 , C07D253/075 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , G01N33/5011 , G01N33/502 , G01N33/5041 , G01N33/573 , G01N33/574 , G01N2500/00 , G01N2500/10
摘要： This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

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