Substituted pyrimidines for control of diabetic complications

Details Substituted pyrimidines for control of diabetic complications Substituted pyrimidines for control of diabetic complications

C - Chemistry, Metallurgy

07

D

C07D 403/00 (2006.01) A61K 31/505 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 239/42 (2006.01) C07D 401/00 (2006.01) C07D 405/00 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2145640

This invention relates to methods of inhibiting sorbitol dehydrogenase, lowering fructose levels, and treating or preventing diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic microangiopathy or diabetic macroangiopathy in a mammal using pyrimidine derivatives of formula (I) wherein R1, R2, R3, R4 and R5 are defined as below, and to pharmaceutical compositions containing such derivatives. It also relates to certain novel substituted pyrimidines having the above formula. It also relates to mutual prodrugs of compounds of above formula (I) and aldose reductase inhibiting compounds, and to pharmaceutical compositions comprising a compound of above formula (I) and an aldose reductase inhibitor.

Cette invention concerne les procédés pour inhiber la déshydrogénase de sorbitol, pour abaisser les niveaux de fructose, et pour traiter ou prévenir les complications diabétiques telles que la névropathie diabétique, la rétinopathie diabétique, la microangiopathie diabétique ou la microangiopathie chez un mammifère en utilisant des dérivés de la pyrimidine selon la formule (I) dans laquelle R1, R2, R3, R4 et R5 sont définis comme ci-dessous. Cette invention concerne aussi les compositions pharmaceutiques contenant de tels dérivés. Elle concerne également certaines nouvelles pyrimidines substituées ayant la formule ci-dessus. Elle concerne également les promédicaments mutuels selon les composés de la formule (I) et des composés inhibiteurs de la réductase aldose, et les compositions pharmaceutiques comprenant un composé de la formule (I) et un inhibiteur de réductase aldose.

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