Pyrazinones compound
A technology of compounds and medicinal salts, applied in the field of pyrazinone compounds, can solve problems such as GLP-1 deficiency, achieve the effect of increasing the level and prolonging the half-life
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Problems solved by technology
Another study showed that the postprandial GIP level of patients with type 2 diabetes was comparable to that of healthy people, but the level of GLP-1 was significantly lower than that of healthy people, indicating that these patients have GLP-1 deficiency
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Embodiment 1
[0035] The present embodiment provides a compound represented by formula (II):
[0036]
Embodiment 2
[0038] This embodiment provides a compound represented by formula (III)
[0039]
Embodiment 3
[0041] The present embodiment provides a compound represented by formula (IV):
[0042]
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The invention relates to a pyrazinones compound which can be used as a dipeptidyl peptidase-4 (DDP-4) inhibitor. The pyrazinones compound has high activity and selectivity to the dipeptidyl peptidase-4. The compound provided by the invention can raise the level of endogenous incretin through inhibiting the DDP-4 and prolonging a half-life period of GLP-1 (Glucagonlike Peptide-1) and can completely perform the beneficial effects on adjusting the blood sugar so that the corresponding pharmacological effects are achieved. The pyrazinones compound or a pharmacological composition comprising the compound can be used for preventing or treating diabetes mellitus, especially II type diabetes mellitus, hyperglycemia, syndrome X, hyperinsulinemia, adiposity, atherosclerosis and various immunomodulatary diseases.
Description
technical field [0001] The present invention relates to pyrazinone compounds and their pharmaceutical applications. Background technique [0002] Diabetes mellitus is an endocrine system disease characterized by blood glucose metabolism disorder caused by the interaction of various environmental factors and genetic factors. Type II diabetes is caused by insulin resistance of tissue cells (that is, cells no longer combine with insulin, so that the glucose entering the cell to participate in the generation of heat decreases, and the glucose remaining in the blood increases), β cell function decline or other reasons. , is the result of the joint action of genetic and environmental factors, accounting for more than 90% of the total number of people with diabetes. . Type II diabetes is more common in overweight or obese middle-aged and elderly people, and has obvious family heredity. [0003] Incretins are intestinal hormones, which mainly include glucose-dependent insulinotro...
Claims
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IPC IPC(8): C07D487/04C07F9/6561A61K31/4985A61K31/675A61P3/10A61P5/50A61P3/04A61P9/10
Inventor 殷建明朱惠霖