process of developing substances as potent and selective inhibitors of phosphodiesterase isoforms of types 1 to 5 (pde1, pde2, pde3, pde4, pde5) based on diocleine, fluranol or analogs and their pharmaceutical compositions for the study and treatment of cardiovascular disease and associated products

摘要

"DEVELOPMENT PROCESS OF SUBSTANCES AS POTENTIAL AND SELECTIVE INHIBITORS OF TYPES 1 TO 5 PHOSPHODYESTERASES (PDE1, PED3, PDE4, PDE5) ON THE DIOCLEIN, FLORANOL OR ANALOGUE OF THE PHOSOPHESES AND COMPOSES OF THE COMPOSIENTS CARDIOVASCULAR AND ASSOCIATED PRODUCTS ". The present invention is characterized by the process of developing substances as potent and selective inhibitors of the types 1 to 5 phosphodiesterase isoforms (PDE1, PED2, PED3, PDE4, PDE5) 5 based on dioclein, floranol or the like; whether or not associated with inclusion compounds with cyclodextrins and controlled release devices using biodegradable polymers or not, such as PLGA, PLA, PGA or mixtures; their respective pharmaceutical compositions for the study and treatment of cardiovascular disease and associated products. The substances developed in the present invention were tested for their ability to inhibit different PDE isoforms. They are also the first substances and their pharmaceutical compositions in the therapeutic arsenal capable of potently and selectively inhibiting the phosphodiesterase type 1 (PDE1) isoform. The present invention utilizes two flavonoids as type 1 to 5 phosphodiasterase inhibiting forms: dioclein and floranol, as well as their analogues and pharmaceutical compositions using cyclodextrins and their inclusion compounds as well as pharmaceutically and pharmacologically acceptable excipients.