Flourinated cyclic amides as dipeptidyl peptidase iv inhibitors

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 207/08 (2006.01) A61K 31/397 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61P 3/10 (2006.01) C07D 205/04 (2006.01) C07D 211/38 (2006.01) C12Q 1/37 (2006.01)

Patent

CA 2487636

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.

L'invention de nouveaux inhibiteurs thérapeutiquement actifs et sélectifs de l'enzyme dipeptidyl peptidase-IV (DPP-IV), des compositions pharmaceutiques comprenant les composés et l'utilisation de ces composés pour traiter des maladies associées à des protéines soumises à un traitement par la DPP-IV, telles que le diabète sucré de type 2, l'hyperglycémie, la tolérance au glucose altérée, un syndrome métabolique (syndrome X ou syndrome de résistance à l'insuline), la glycosurie, l'acidose métabolique, la cataracte, la neuropathie diabétique, la néphropathie diabétique, la rétinopathie diabétique, la cardiomyopathie diabétique, le diabète de type 1, l'obésité, les états exacerbés par l'obésité, l'hypertension, l'hyperlipidémie, l'athérosclérose, l'ostéoporose, l'ostéopénie, la fragilité, la perte osseuse, les fractures osseuses, le syndrome coronaire aiguë, l'infertilité due au syndrome polycystique ovarien, le syndrome de l'intestin court, l'anxiété, la dépression, l'insomnie, la fatigue chronique, l'épilepsie, les troubles de l'alimentation, les douleurs chroniques, l'addiction à l'alcool, les maladies associées à la motilité intestinale, les ulcères, le syndrome de l'intestin irritable, le syndrome de l'intestin inflammatoire; et pour prévenir l'évolution d'une maladie dans le diabète de type 2. L'invention concerne également une méthode permettant d'identifier un agent sécrétagogue de l'insuline dans le diabète.

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