Multibinding inhibitors of hmg-coa reductase

Details Multibinding inhibitors of hmg-coa reductase Multibinding inhibitors of hmg-coa reductase

A - Human Necessities

61

K

A61K 31/35 (2006.01) A61K 31/00 (2006.01) A61K 31/365 (2006.01) A61K 38/00 (2006.01) A61K 39/00 (2006.01) A61K 39/395 (2006.01) A61K 39/44 (2006.01) A61K 47/48 (2006.01) A61K 51/00 (2006.01) C07C 233/36 (2006.01) C07C 233/78 (2006.01) C07C 237/24 (2006.01) C07C 271/20 (2006.01) C07C 321/04 (2006.01) C07C 323/12 (2006.01) C07D 207/333 (2006.01) C07D 207/34 (2006.01) C07D 209/12 (2006.01) C07D 211/58 (2006.01) C07D 215/56 (2006.01) C07D 233/90 (2006.01) C07D 235/30 (2006.01) C07D 309/30 (2006.01) C07D 401/06

Patent

CA 2319761

Disclosed are multibinding compounds which inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate limiting enzyme in cholesterol biosynthesis. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is a moiety capable of binding to HMG-CoA reductase and the distance between ligands is at least 10 .ANG.. The multibinding compounds of this invention are useful in the treatment and prevention of hypercholesterolemia, hyperlipidemia, atherosclerosis and the like.

L'invention concerne des composés de multiliaison inhibant la 3-hydroxy-3-méthylglutaryle coenzyme A réductase (HMG-CoA réductase), l'enzyme limitant le taux dans la biosynthèse du cholestérol. Les composés de multiliaison de cette invention contiennent 2 à 10 ligands fixés de manière covalente à un ou plusieurs lieurs. Chaque ligand est une fraction capable de se lier à la HMG-CoA réductase et la distance entre les ligands est d'au moins 10 .ANG.. Les composés de multiliaison de cette invention sont utiles dans le traitement et la prévention de l'hypercholestérolémie, de l'hyperlipidémie, de l'athérosclérose et analogue.

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