| abstract |
The present invention relates to the field of organic chemistry and pharmaceutics, and more particularly to ligands of the cysteinyl leukotriene receptors CysLT 1 R and CysLT 2 R, having the given formulae, where R 1 , R 2 , R 3 and R 4 have the values given in the claims, and to pharmaceutically acceptable derivatives thereof, and further relates to pharmaceutical compositions of such compounds or their pharmaceutically acceptable derivatives, which can be used for treating inflammatory, cardiovascular and oncological diseases linked to the type I or type II cysteinyl leukotriene receptor, as well as oncological disorders and diseases linked to a mutant form of the type II cysteinyl leukotriene receptor containing the single nucleotide polymorphism L129Q, and still further relates to a method for treating said diseases using a therapeutically effective amount of one of the proposed compounds or its pharmaceutically acceptable derivative, or a therapeutically effective amount of a pharmaceutical composition containing one of the proposed compounds or its pharmaceutically acceptable derivative together with a pharmaceutically acceptable carrier, diluent, filler and/or other excipient. The technical results of the invention include: providing novel type I or type II cysteinyl leukotriene receptor ligands which are effective in the treatment of diseases linked to cysteinyl leukotriene receptors, and which have novel chemical structures and do not cause the undesirable effects on the gastrointestinal tract or the neuropsychiatric side effects characteristic of known cysteinyl leukotriene receptor ligands; providing cysteinyl leukotriene receptor ligands that are inverse agonists for a mutant L129Q form of the type II receptor, which can be used in medicine for treating cancer types, the pathogenesis of which involves a mutant from of the CysLT 2 R receptor containing the single nucleotide polymorphism L129Q; providing cysteinyl leukotriene receptor ligands which can be used in medicine for treating inflammatory, cardiovascular and oncological diseases, the pathogenesis of which involves cysteinyl leukotrienes; and providing type I and type II cysteinyl leukotriene receptor ligands that exhibit greater solubility by comparison with known ligands available on the market. |