Pyrido(3,2-d)pyrimidines and pharmaceutical compositions...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/519 (2006.01) A61P 37/00 (2006.01)

Patent

CA 2594241

This invention relates to substituted pyrido(3,2-d)pyrimidine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, pro-drugs and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These derivatives are also useful in preventing or treating cardiovascular disorders, disorders of the central nervous system, TNF-.alpha. related disorders, viral diseases (including hepatitis C), erectile dysfunction and cell proliferative disorders.

L'invention se rapporte à des dérivés substitués pyrido(3,2-d)pyrimidine, à leurs sels pharmaceutiquement acceptables, leurs N-oxydes, leurs solvates, leurs promédicaments et leurs énantiomères, qui possèdent des propriétés pharmaceutiques souhaitées inattendues, et qui s'avèrent en particulier être des agents immunosuppresseurs fortement actifs, et sont utiles pour cette raison dans le traitement du phénomène de rejet après transplantation et/ou dans le traitement de certaines maladies inflammatoires. Ces dérivés sont également utiles pour prévenir ou traiter les troubles cardio-vasculaires, les troubles du système nerveux central, les troubles associés au TNF-.alpha., les maladies virales (notamment l'hépatite C), la dysérection, et les troubles de prolifération cellulaire.

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