[EN] COMPOUNDS IN THE FORM OF HOMODIMERIC, HETERODIMERIC AND/OR HOMO AND HETEROMULTIMERIC PRO-DRUGS; PROCESS FOR OBTAINING THESE PRO-DRUGS AND THEIR ACCEPTABLE PHARMACEUTICAL SALTS AND USE OF COMPOUNDS IN THE TREATMENT OF PHOSPHODIESTERASIS-MEDIATED DISEASES OR DYSFUNCTION<br/>[FR] COMPOSES SOUS FORME DE PROMEDICAMENTS HOMODIMERIQUES, HETERODIMERIQUES ET/OU HOMO ET HETEROMULTIMERIQUES; PROCEDES PERMETTANT D'OBTENIR CES PROMEDICAMENTS AINSI QUE LEURS SELS PHARMACEUTIQUEMENT ACCEPTABLES; UTILISATION DE CES COMPOSES DANS LE TRAITEMENT DU DYSFONCTIONNEMENT ET/OU DES MALADIES INDUITS PAR LA PHOSPHODIESTERA
申请人:CRISTALIA PRODUTOS QUIMICOS E
公开号:WO2002012241A1
公开(公告)日:2002-02-14
Present invention describes the obtainment of new compounds, synthesized in the form of homodimeric, heterodimeric, and /or homo and heteromultimeric pro-drugs, which present activity of phosphodiesterasis inhibition, being useful for the treatment of diseases and dysfunctions mediated by this class of enzyme or where the inhibition of these enzymes cause the desired therapeutic effects. These compounds, sinthesized as pro-drugs, are activated by the organism by means of natural biochemical processes, being this activation effected by means of cleavage of their labile bond bridges. The availability of the active drugs, derivative of these pro-drugs, is made in a natural way in the organism, positively influencing on its effect, increasing the bioavailability of these active drugs, being this increment followed by decreased side effects, due to the reduced degradation of the active drugs by the pre-systemic metabolism.
本发明描述了新化合物的获得,以同源二聚体、异源二聚体和/或同源和异源多聚体前药的形式合成,这些化合物具有磷酸二酯酶抑制活性,适用于治疗由该类酶介导的疾病和功能障碍或酶抑制引起所需的治疗效果的疾病。这些作为前药合成的化合物通过自然生化过程被机体激活,这种激活通过其不稳定的键桥的断裂来实现。这些前药的衍生活性药物在机体中以自然方式可获得,这对其效果具有积极影响,增加了这些活性药物的生物利用度,这种增加随之而来的是减少了由于前系统代谢导致的活性药物降解的副作用。