Synthesis of inhibitors of 11beta-hydroxysteroid...

C - Chemistry – Metallurgy – 07 – D

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C07D 265/10 (2006.01) C07D 413/06 (2006.01)

Patent

CA 2729993

Disclosed are syntheses of 11.beta.-HSD1 inhibitors and corresponding intermediates that are promising for the treatment of a variety of disease states including diabetes, metabolic syndrome, obesity, glucose intolerance, insulin resistance, hyperglycemia, hypertension, hypertension-related cardiovascular disorders, hyperlipidemia, deleterious gluco-corticoid effects on neuronal function (e.g. cognitive impairment, dementia, and/or depression), elevated intra-ocular pressure, various forms of bone disease ( e.g., osteoporosis), tuberculosis, leprosy (Hansen's disease), psoriasis, and impaired wound healing (e.g., in patients that exhibit impaired glucose tolerance and/or type 2 diabetes).

La présente invention concerne des synthèses d'inhibiteurs de la 11ß-HSD1 et des intermédiaires correspondants qui sont prometteurs pour traiter une variété d'états pathologiques comprenant le diabète, le syndrome métabolique, lobésité, l'intolérance au glucose, l'insulinorésistance, l'hyperglycémie, l'hypertension, des troubles cardiovasculaires liés à l'hypertension, l'hyperlipidémie, les effets délétères des gluco-corticoïdes sur la fonction neuronale (par exemple une incapacité cognitive, la démence, et/ou la dépression), une pression intraoculaire élevée, des formes diverses de la maladie des os (par exemple, l'ostéoporose), la tuberculose, la lèpre (maladie d'Hansen), le psoriasis, et une guérison altérée des plaies (par exemple, chez des patients présentant une tolérance altérée au glucose et/ou un diabète de type 2).

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