226 results about "Dipeptidyl peptidase-4" patented technology

The present invention relates to novel compounds, their use for inhibiting serine proteases, such as dipeptidyl peptidases, such as dipeptidyl peptidase IV (DPP-IV) and to methods for their production and their therapeutic utility.

The present invention relates to a method of making novel dipeptidyl peptidase-IV ("DPP-IV') inhibitor compounds useful for treating, inter alia, diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes mellitus, metabolic syndrome (Syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of making 3,3,4,4-tetrafluoropyrrolidine, a starting material utilized in the afore-mentioned method for preparing DPP-IV compounds.

The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

A dipeptidyl peptidase IV inhibitor which is satisfactory in respect of activity, stability and safety and has an excellent action as a pharmaceutical agent. A compound represented by the following general formula or a pharmaceutically acceptable salt thereof:

wherein R¹ and R² each represents hydrogen, an optionally substituted C1-6 alkyl group, or —COOR⁵ whereupon R⁵ represents hydrogen or an optionally substituted C1-6 alkyl group, or R¹, R², and a carbon atom together represent a 3- to 6-membered cycloalkyl group, R³ represents hydrogen or an optionally substituted C6-10 aryl group, R⁴ represents a hydrogen or a cyano group, D represents —CONR⁶—, —CO— or —NR⁶CO—, R⁶ represents hydrogen or an optionally substituted C1-6 alkyl group, E represents —(CH₂)_m— whereupon m is 1 to 3, —CH₂OCH₂—, or —SCH₂—, n is 0 to 3, and A represents an optionally substituted bicyclic heterocyclic group or bicyclic hydrocarbon group.

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

The invention relates to thiadiazole derivatives which are shown as a formula I and have DPP-IV (dipeptidyl peptidase IV) inhibition activity, a preparation method of the thiadiazole derivatives and drug compositions of the thiadiazole derivatives, and application of the thiadiazole derivatives to treatment of diseases beneficial from DPP-IV inhibition, especially application to treatment of diabetes mellitus type 2. The thiadiazole derivatives provided by the invention have very good DPP-IV inhibition activity, have a very good in-vivo metabolic level and a very proper in-vivo half-life period and are expected to be used as proper DPP-IV inhibitor drugs.

The present invention is directed to novel substituted aminotetrahydropyrans of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Disclosed are pharmaceutical compositions comprising fixed-dose combinations of an extended-release form of metformin, or a pharmaceutically acceptable salt thereof, coated with an immediate-release form of the DPP-4 inhibitor sitagliptin, or a pharmaceutically acceptable salt thereof.

The invention belongs to the technical field of medicines, and in particular relates to a compound taking thieno-pyrimidone as mother nuclide or a salt thereof, a preparation method and a combination of the compound and application of the compound used as a DPP-IV (dipeptidyl peptidase) inhibitor in preventing or treating diseases benefiting from the DPP-IV inhibition. The compound provided by the invention has the advantages that the preparation process is simple, the raw material is easily available, the compound is suitable for large-scale production, and in-vitro experiment verifies that the compound has good selective inhibition action on the DPP-IV, and hardly has any influence on the activities of DPP-VIII and DPP-IX while effectively inhibiting the activity of the DDP-IV, thereby predicting that the medicine prepared from the compound has very low toxicity and an outstanding advantage.

The invention discloses a method for preparing a DPP-IV inhibitory peptide through using hairtail. The method is characterized in that the method comprises the following steps: adding water to hairtail, and rubbing to form a uniform fish flesh pulp; putting the fish flesh pulp in an enzymatic hydrolysis tank, adding endo protease, and carrying out stirring hydrolysis for 4-12h to obtain a hydrolysate; heating to 95-100DEG C, and maintaining the temperature unchanged for 10-15min for enzyme killing; cooling the hydrolysate to 40-60DEG C, adding exoproteinase, and carrying out stirring hydrolysis for 2-8h; heating to 95-100DEG C, and maintaining the temperature unchanged for 10-15min for enzyme killing; centrifuging the obtained enzyme-killed hydrolysate, and taking the obtained supernatant; adding the supernatant to an ultrafilter membrane separator, adjusting the pressure and the interception molecular weight of the ultrafilter membrane to 0.05-0.1MPa and 3000Da respectively, and collecting an ultrafilter membrane permeate liquid; and separating and purifying the DPP-IV inhibitory peptide through adopting an affinity chromatography process. The method has the advantages of simple technology, low production cost and short production period.

The present invention relates to compounds of formula (I),

which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Disclosed are pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and metformin, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.

The invention provides a method for preparing a dipeptidyl peptidase-IV inhibitor, and in particular relates to a method for preparing 7-[3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-trifluoromethyl-1,2,4-triazol[4,3-a]pyrazine raceme or an optically pure (R) or (S) compound thereof. The method comprises the following steps of: (1) performing hydrogenation reduction to obtain racemate; (2) reacting the racemate with camphorsulfonic acid or tartaric acid; and (3) converting a salt obtained in the step 2 into a corresponding alkali. The method has low cost and can be applied to industrial production.