Dipeptidyl peptidase iv inhibiting fluorinated cyclic amides

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 207/22 (2006.01) A61K 31/401 (2006.01) A61P 3/10 (2006.01)

Patent

CA 2502068

The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for treating diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, hyperglycemia, impaired glucose tolerance, metabolic syndrome (Syndrome X or insulin resistance syndrome), glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of identifying an insulin secretagogue agent for diabetes.

Cette invention concerne de nouveaux inhibiteurs sélectifs et thérapeutiquement actifs de l'enzyme dipeptidyl peptidase IV; des compositions comprenant ces composés; et l'utilisation de ces composés pour traiter des maladies associées à des protéines soumises à un traitement par DPP-IV, telles que le diabète non insulino-dépendant, l'hyperglycémie, l'intolérance au glucose, le syndrome métabolique (syndrome X ou syndrome de résistance l'insuline), la glucosurie, l'acidose métabolique, les cataractes, la neuropathie diabétique, la rétinopathie diabétique, la cardiomyopathie diabétique, le diabète insulino-dépendant, l'obésité, les affections exacerbées par l'obésité, l'hypertension, l'hyperlipidémie, l'athérosclérose, l'ostéoporose, l'ostéopénie, la fragilité, la perte osseuse, la fracture de l'os, le syndrome coronaire aigu, l'infertilité due au syndrome des ovaires polykystiques, le syndrome de l'intestin court, l'anxiété, la dépression, l'insomnie, la fatigue chronique, l'épilepsie, les troubles de la nutrition, la douleur chronique, l'alcoolisme, les maladies associées à la motilité intestinale, les ulcères, le syndrome du côlon irritable, la maladie intestinale inflammatoire; et pour enrayer l'évolution du diabète non insulino-dépendant. L'invention concerne en outre une méthode permettant d'identifier un agent sécrétagogue de l'insuline contre le diabète.

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