Novel heterocyclic compounds having a six membered ring structure fused to
a five membered ring structure are found to be useful for the treatment
and prevention of symptoms or manifestations associated with disorders
affected by Interleukin-12 ("IL-12") intracellular signaling, such as, for
example, Th1 cell-mediated disorders. The therapeutic compounds,
pharmaceutically acceptable derivatives (e.g., resolved enantiomers,
diastereomers, tautomers, salts and solvates thereof) or prodrugs thereof,
have the following general formula:
##STR1##
Each X, Y and Z are independently selected from a member of the group
consisting of C(R.sub.3), N, N(R.sub.3) and S. Each R.sub.1, R.sub.2 and
R.sub.3 is substituted or unsubstituted and is independently selected from
a member of the group consisting of hydrogen, halo, oxo, C.sub.(1-20)
alkyl, C.sub.(1-20) hydroxyalkyl, C.sub.(1-20) thioalkyl, C.sub.(1-20)
alkylamino, C.sub.(1-20) alkylaminoalkyl, C.sub.(1-20) aminoalkyl,
C.sub.(1-20) aminoalkoxyalkenyl, C.sub.(1-20) aminoalkoxyalkynyl,
C.sub.(1-20) diaminoalkyl, C.sub.(1-20) triaminoalkyl, C.sub.(1-20)
tetraaminoalkyl, C.sub.(5-15) aminotrialkoxyamino, C.sub.(1-20)
alkylamido, C.sub.(1-20) alkylamidoalkyl, C.sub.(1-20) amidoalkyl,
C.sub.(1-20) acetamidoalkyl, C.sub.(1-20) alkenyl, C.sub.(1-20) alkynyl,
C.sub.(3-8) alkoxyl, C.sub.(1-11) alkoxyalkyl, and C.sub.(1-20)
dialkoxyalkyl.
Le roman les composés qu'hétérocycliques ayant des six la structure membered anneau fondue à des cinq membered la structure d'anneau s'avèrent utile pour le traitement et la prévention des symptômes ou des manifestations liés aux désordres affectés par la signalisation intracellulaire d'Interleukin-12 ("IL-12"), comme, par exemple, les désordres Th1 communiqués par les cellules. Les composés thérapeutiques, pharmaceutiquement les dérivés acceptables (par exemple, énantiomères, diastereomers, tautomers, sels et solvates résolus en) ou les prodrogues en, ont la formule générale suivante : ## du ## STR1 Chaque X, Y et Z sont indépendamment choisis parmi un membre du groupe se composant de C(R.sub.3), de N, de N(R.sub.3) et de S. Chaque R.sub.1, R.sub.2 et R.sub.3 est substitué ou non substitué et est indépendamment choisi parmi un membre de l'hydrogène de groupe, du halo, des oxo se composants, C.sub.(1-20) alkyl, C.sub.(1-20) hydroxyalkylique, C.sub.(1-20) thioalkyl, C.sub.(1-20) alkylamino, C.sub.(1-20) alkylaminoalkyl, C.sub.(1-20) aminoalkyle, C.sub.(1-20) aminoalkoxyalkenyl, C.sub.(1-20) aminoalkoxyalkynyl, C.sub.(1-20) diaminoalkyl, C.sub.(1-20) triaminoalkyl, C.sub.(1-20) tetraaminoalkyl, C.sub.(5-15) aminotrialkoxyamino, C.sub.(1-20) alkylamido, C.sub.(1-20) alkylamidoalkyl, C.sub.(1-20) amidoalkyl, C.sub.(1-20) acetamidoalkyl, C.sub.(1-20) alkényle, C.sub.(1-20) alkynyl, C.sub.(3-8) alcoxyle, C.sub.(1-11) alkoxyalkyl, et C.sub.(1-20) dialkoxyalkyl.
