N 1-2-THIOPHENE-2-YLETHYL-N2-SUBSTITUTED BIGUANIDE DERIVATE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENTS
[EN] BENZIMIDAZOLES FOR THE TREATMENT OF CANCER<br/>[FR] BENZIMIDAZOLES POUR LE TRAITEMENT D'UN CANCER
申请人:MAX PLANCK GESELLSCHAFT
公开号:WO2014027053A1
公开(公告)日:2014-02-20
The present invention relates to novel substituted benzimidazoles and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these substituted benzimidazoles together with pharmaceutically acceptable carrier, excipient and/or diluents. Said novel substituted benzimidazoles binding to the prenyl binding pocket of PDEδ have been identified as useful for the prophylaxis and treatment of cancer by the inhibition of the binding of PDEδ to K-Ras and of oncogenic Ras signalling in cells by altering its localization leading to cell death or inhibition of proliferation.
N1-2-thiophene-2-ylethyl-N2-substituted biguanide derivate, preparation method thereof, and pharmaceutical composition containing the same as active ingredients
申请人:Kim Sung Wuk
公开号:US08648111B2
公开(公告)日:2014-02-11
The present invention provides an N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative of formula (I) or a pharmaceutically acceptable salt thereof, a method for preparing same, and a pharmaceutical composition comprising same as an active ingredient. The inventive N1-2-thiophen-2-ylethyl-N2-substituted biguanide derivative exhibits improved blood glucose level- and lipid level-lowering effects even with a reduced dosage as compared to conventional drugs, and thus, it is useful for preventing or treating diabetes, metabolic syndromes such as insulin-independent diabetes, obesity and atherosclerosis, or a P53 gene defect-related cancer.