C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 237/42 (2006.01) A61K 31/166 (2006.01) A61K 31/167 (2006.01) A61K 31/17 (2006.01) A61K 31/27 (2006.01) A61K 31/277 (2006.01) A61K 31/4406 (2006.01) A61K 31/4709 (2006.01) C07C 235/40 (2006.01) C07C 235/46 (2006.01) C07C 237/30 (2006.01) C07C 237/44 (2006.01) C07C 255/57 (2006.01) C07C 271/28 (2006.01) C07C 275/34 (2006.01) C07C 275/42 (2006.01) C07D 209/46 (2006.01) C07D 213/82 (2006.01) C07D 215/08 (2006.01) C07D 217/06 (2006.01) C07D 223/16 (2006.01) C07D 265/36 (2006.01) C07D 307/68 (2006.01) C07D 3
Patent
CA 2513349
Compounds of the formula (I) provide pharmacological agents which lower intracellular glucocorticoid concentrations in mammals, in particular, intracellular cortisol levels in humans. Therefore, the compounds of the instant invention improve insulin sensitivity in the muscle and the adipose tissue, and reduce lipolysis and free fatty acid production in the adipose tissue. The compounds of the invention lower hepatic glucocorticoid concentration in mammals, in particular, hepatic cortisol concentration in humans, resulting in inhibition of hepatic gluconeogenesis and lowering of plasma glucose levels. Thus, the compounds of the instant invention may be particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which hyperglycemia and/or insulin resistance are implicated, such as type-2 diabetes. The compounds of the invention may also be used to treat other glucocorticoid associated disorders, such as Syndrome- X, dyslipidemia, hypertension and central obesity. The invention furthermore relates to the use of the compounds according to the invention for the preparation of medicaments, in particular of medicaments useful for the treatment and prevention of glucocorticoid associated disorders, by improving insulin sensitivity, reducing plasma glucose levels, reducing lipolysis and free fatty acid production, and by decreasing visceral adipose tissue formation.
L'invention porte sur des composés de formule (I), agents pharmacologiques: abaissant chez les mammifères la concentration en glucocorticoïdes intracellulaires en particulier celle du cortisol intracellulaire, augmentant la sensibilité à l'insuline des muscles et des tissus adipeux et réduisant la lipolyse et la production d'acides gras dans les tissus adipeux. En outre, lesdits composés abaissent la concentration en glucocorticoïdes hépatiques chez les mammifères, et en particulier en cortisol hépatique chez l'homme, d'où une inhibition de la glucogenèse et une diminution des niveaux de glucose dans le sang. Lesdits composés sont particulièrement utiles comme hypoglycémiants pour traiter et prévenir l'hyperglycémie et/ou la résistance à l'insuline, par exemple dans le diabète de type 2, ou pour traiter d'autres troubles associés aux glucocorticoïdes tels que le Syndrome-X, la dyslipidémie, l'hypertension et l'obésité centrale, en augmentant la sensibilité à l'insuline, en réduisant les niveaux de glucose du plasma, la lipolyse et la production d'acides gras libres, et en ralentissant la formation des tissus adipeux viscéraux.
Coppola Gary Mark
Damon Robert Edson
Kukkola Paivi Jaana
Stanton James Lawrence
Fetherstonhaugh & Co.
Novartis Ag
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