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1.发明授权公开(公告)号：US09243038B2
公开(公告)日：2016-01-26
申请号：US14130336
申请日：2012-06-29
CPC分类号： A61K38/12 , A61K31/395 , A61K38/00 , C07K5/0215 , C07K7/54
摘要： Macrocyclic compounds that specifically inhibit insulin degrading enzyme (IDE) are provided. Pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, polymorphs, tautomers, isotopically enriched forms, and prodrugs of the macrocyclic IDE inhibitors are also described. Pharmaceutical compositions are also provided. In vivo and in vitro methods of using the IDE inhibitor, and pharmaceutical compositions comprising the IDE inhibitor, for example, for the inhibition of IDE in a subject exhibiting aberrant IDE activity, impaired insulin signaling, or insulin resistance, for example, a subject having diabetes, are also provided.
摘要翻译： 提供特异性抑制胰岛素降解酶（IDE）的大环化合物。 还描述了大环IDE抑制剂的药学上可接受的盐，溶剂合物，水合物，立体异构体，多晶型物，互变异构体，同位素富集形式和前药。 还提供药物组合物。 使用IDE抑制剂的体内和体外方法以及包含IDE抑制剂的药物组合物，例如用于抑制表现出异常IDE活性的受试者，受损的胰岛素信号传导或胰岛素抵抗的IDE，例如具有 也提供糖尿病。
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2.发明申请公开(公告)号：US20140213515A1
公开(公告)日：2014-07-31
申请号：US14130336
申请日：2012-06-29
IPC分类号： C07K7/54
CPC分类号： A61K38/12 , A61K31/395 , A61K38/00 , C07K5/0215 , C07K7/54
摘要： Macrocyclic compounds that specifically inhibit insulin degrading enzyme (IDE) are provided. Pharmaceutically acceptable salts, solvates, hydrates, stereoisomers, polymorphs, tautomers, isotopically enriched forms, and prodrugs of the macrocyclic IDE inhibitors are also described. Pharmaceutical compositions are also provided. In vivo and in vitro methods of using the IDE inhibitor, and pharmaceutical compositions comprising the IDE inhibitor, for example, for the inhibition of IDE in a subject exhibiting aberrant IDE activity, impaired insulin signaling, or insulin resistance, for example, a subject having diabetes, are also provided.
摘要翻译： 提供特异性抑制胰岛素降解酶（IDE）的大环化合物。 还描述了大环IDE抑制剂的药学上可接受的盐，溶剂合物，水合物，立体异构体，多晶型物，互变异构体，同位素富集形式和前药。 还提供药物组合物。 使用IDE抑制剂的体内和体外方法以及包含IDE抑制剂的药物组合物，例如用于抑制表现出异常IDE活性的受试者，受损的胰岛素信号传导或胰岛素抵抗的IDE，例如具有 也提供糖尿病。
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公开(公告)号：US08975232B2
公开(公告)日：2015-03-10
申请号：US13812431
申请日：2011-07-29
申请人： David R. Liu , Ralph E. Kleiner
发明人： David R. Liu , Ralph E. Kleiner
CPC分类号： C07K5/02 , A61K38/12 , C07K5/1016
摘要： The present invention provides macrocyclic compounds of Formula (I): pharmaceutically acceptable salts thereof; and pharmaceutical compositions thereof, wherein R1, R2, R3, R4, RE, RF, RG, RH, RI, f, g, h, n, and m are as defined herein. The present invention further provides methods of synthesizing these macrocyclic compounds, and methods of their use and treatment. Certain aspects of the present invention relate to modulation of kinase activity, and in the treatment of kinase-associated diseases or disorders.
摘要翻译： 本发明提供式（I）的大环化合物：其药学上可接受的盐; 及其药物组合物，其中R1，R2，R3，R4，RE，RF，RG，RH，RI，f，g，h，n和m如本文所定义。 本发明还提供了合成这些大环化合物的方法及其使用和处理方法。 本发明的某些方面涉及激酶活性的调节和激素相关疾病或病症的治疗。
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公开(公告)号：US20130178429A1
公开(公告)日：2013-07-11
申请号：US13812431
申请日：2011-07-29
申请人： David R. Liu , Ralph E. Kleiner
发明人： David R. Liu , Ralph E. Kleiner
IPC分类号： C07K5/02
CPC分类号： C07K5/02 , A61K38/12 , C07K5/1016
摘要： The present invention provides macrocyclic compounds of Formula (I): pharmaceutically acceptable salts thereof; and pharmaceutical compositions thereof, wherein R1, R2, R3, R4, RE, RF, RG, RH, RI, f, g, h, n, and m are as defined herein. The present invention further provides methods of synthesizing these macrocyclic compounds, and methods of their use and treatment. Certain aspects of the present invention relate to modulation of kinase activity, and in the treatment of kinase-associated diseases or disorders.
摘要翻译： 本发明提供式（I）的大环化合物：其药学上可接受的盐; 及其药物组合物，其中R1，R2，R3，R4，RE，RF，RG，RH，RI，f，g，h，n和m如本文所定义。 本发明还提供了合成这些大环化合物的方法及其使用和处理方法。 本发明的某些方面涉及激酶活性的调节和激素相关疾病或病症的治疗。
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