114 results about "Dipeptidylpeptidase iv" patented technology

The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.

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 novel methods and compositions for detection and isolation of cancer cells with metastatic potential. The invention further relates to assays for measuring the metastatic potential of such cancer cells and drug screening assays for the identification of agents having anti-metastatic potential. The present invention further provides methods and compositions for inhibiting the metastatic potential of cancer cells by modulating the activity of serine integral membrane proteases [(SIMP) consisting of seprase and dipedidyl peptidase IV (DPPIV)]expressed on the surface of metastasizing cancer cells.

Method for preparing 8-(3-aminopiperidin-1-yl)-xanthine derivatives (I) and their enantiomers and salts. Method for preparing 8-(3-aminopiperidin-1-yl)-xanthine derivatives of formula (I) and their enantiomers and salts by: (a) reacting an 8-X-xanthine (III) with 3-phthalimidopiperidine (A), or its enantiomer; (b) deprotecting the product (II); and (c) optionally conversion to salt. X : halo or sulfonate ester, especially bromo; R 1>phenylcarbonylmethyl, benzyl, naphthylmethyl, pyridinylmethyl, pyrimidinylmethyl, (iso)quinolinylmethyl, quinazolinylmethyl, quinoxalinylmethyl, naphthyridinylmethyl or phenanthridinylmethyl, all optionally substituted by one or two, same or different, Ra; R 2>1-3C alkyl, cyclopropyl or phenyl; R 3>2-buten-1-yl, 3-methyl-2-buten-1-yl, 2-butyn-1-yl, or 2-(fluoro, chloro, bromo, iodo, methyl, trifluoromethyl or cyano)-benzyl; Ra : hydrogen, fluoro, chloro, bromo, cyano, methyl, trifluoromethyl, ethyl, phenyl, methoxy, di- or tri-fluoromethoxy, or two Ra on adjacent C atoms complete OCH 2O or OCH 2CH 2O Independent claims are also included for the following: (1) (R) and (S)-3-phthalimidopiperidine as new compounds; and (2) methods for preparing the compounds of (1). [Image] [Image] - ACTIVITY : Antidiabetic; Antiarthritic; Anorectic; Osteopathic. No details of tests for these activities are given. - MECHANISM OF ACTION : Inhibition of dipeptidylpeptidase IV.

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 relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula:

wherein X, Y, a, R¹, and R² are as defined herein.

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.

The present invention relates to solid forms of trelagliptin, a preparation method therefor and applications thereof, and relates specifically to six new solid forms of the dipeptidyl peptidase-4 inhibitor trelagliptin and preparation methods therefor, as well as to pharmaceutical compositions comprising said solid forms of trelagliptin, and uses of same in the preparation of medicines for the treatment of diseases mediated by dipeptidyl peptidase-4.

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 invention relates to an amino six-membered ring derivative and an application thereof in medicines, and in particular, the invention relates to an amino six-membered ring derivative represented as the general formula (I), or a stereisomer thereof, a pharmaceutically-acceptable salt thereof, a pre-drug thereof, a drug composition comprising the derivative, and the application in a medicine of preparing a dipeptidyl peptidase IV (DPP-IV) inhibitor, wherein the substituent groups in the general formula (I) are defined as same as that in the specification.

The invention provides an inhibitor of dipeptidyl peptidase IV shown in formula (I). In the formula, R1 is hydrogen, chlorine, fluorine, bromine, hydroxide radical or alkoxy radical of C1-C6; R2 is hydrogen, fluorine, bromine or hydroxide radical; but R1 can not be the hydroxide or the alkoxy radical of C1-C6 when R2 is hydrogen; and R3 is hydrogen or fluorine. The compound can be used for treating or preventing diseases related with the dipeptidyl peptidase IV, such as diabetes mellitus, obesity and hyperlipoidemia. The invention also provides a method for preparing a compound shown in the formula (I), a preparation method of a pharmaceutically acceptable salt and a pharmaceutical composition thereof, and an application of the compound, the pharmaceutically acceptable salt and the pharmaceutical composition thereof in medicines used for treating or preventing the diseases related with the dipeptidyl peptidase IV.

The present invention describes a synergistic composition comprising of one or more statins, or one or more dipeptidyl peptidase IV (DPP IV) inhibitor or one or more biguanide antihyperglycaemic agent and a PPAR agonist of formula (Ia)

for the treatment of diabetes, especially non-insulin dependent diabetes (NIDDM) or Type 2 diabetes and conditions associated with diabetes mellitus and to compositions suitable for use in such method. The invention also describes the preparation of such compositions. The present invention also relates to certain novel salts of the PPAR agonist of formula (I):

processes for the preparation of these novel salts and use thereof.