73 results about "Dipeptidyl peptidase-4 inhibitor" 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 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.

Abstract of Disclosure The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain;B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g/mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.

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.

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.

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 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 present invention provides new uses of DPIV-inhibitors of the present invention, and their corresponding pharmaceutically acceptable acid addition salt forms, for lowering blood pressure levels.

Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (Formula I) are inhibitors of the dipep tidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus.

The invention relates to beta-amino tetrahydropyrazine, tetrahydropyrimidine and tetrahydropyridine used as dipeptidy peptidase inhibitors for curing or preventing diabetes. Each variable quantity is defined as the application specification. The compounds are the inhibitors of dipeptidy peptidase-IV enzyme ('DP-IV inhibitors') and can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete. The invention also relates to a medicinal composition comprising the compounds and application of the compounds and the composition in preventing or curing the diseases relevant to the dipeptidy peptidase-IV enzyme.

The invention discloses a novel crystal form of oxalate of dipeptidyl peptidase inhibitor, namely, (s)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxo-1-imidazolidinyl)ethylamino)acetyl)-2-cyanpyrrolidine oxalate. In X-ray powder diffraction of the crystal form, characteristic peaks occur at 2 theta diffraction angles of 4.5+/-0.1, 5.5+/-0.1, 9.0+/-0.1, 10.9+/-0.1, 16.4+/-0.1, 17.7+/-0.1, 18.1+/-0.1, 22.0+/-0.1, 22.7+/-0.1, 25.6+/-0.1, 28.1+/-0.1, 28.4+/-0.1 and 32.0+/-0.1. The crystal form disclosed by the invention is superior to the original oxalate in stability, and is more stable for light, heat and humidity and convenient to store and transport; the cost of the DPP-IV (dipeptidyl peptidase-IV) inhibitor in transportation and preservation processes is decreased; and the safety of the product is further guaranteed.

The present invention is directed to novel pharmaceutical compositions comprising fixed dose combinations of a dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor), or a pharmaceutically acceptable salt thereof, and simvastatin, or pharmaceutically acceptable salt thereof, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes and hypercholesterolemia with such pharmaceutical compositions. In particular, the invention is directed to pharmaceutical compositions comprising fixed-dose combinations of sitagliptin phosphate and simvastatin.

The invention provides piperazinoltriazole derivatives, in particular dipeptidyl peptidase IV inhibitors shown by a formula (I) below. The substituents in the formula are defined in the description. The compounds can be used for treating or preventing diseases associated with dipeptidyl peptidase IV, such as diabetes, obesity and hyperlipidemia. The invention also provides methods for preparing the compounds shown by the formula (I), pharmaceutically acceptable salts of the compounds and medicinal compositions and the use of the compounds, the pharmaceutically acceptable salts of the compounds and the medicinal compositions in the preparation of medicaments for treating or preventing diseases associated with dipeptidyl peptidase IV.

Compounds having Formula I, including pharmaceutically acceptable salts and prodrugs thereof: (I) are inhibitors of the dipeptidyl peptidase-IV enzyme (DP-IV), and are useful in the treatment of DP-IV mediated diseases and conditions, such as non-insulin dependent diabetes mellitus

The invention provides a drug for treating hepatocellular carcinoma. The drug comprises a glucagon-like peptide-1 receptor stimulant and/or a dipeptidyl peptidase 4 inhibitor. The invention further provides application of the glucagon-like peptide-1 receptor stimulant and/or dipeptidyl peptidase 4 inhibitor to preparation of a drug for preventing or treating hepatocellular carcinoma, to preparation of a drug for liver function recovery after liver transplantation, and to preparation of a drug for preventing liver cancer relapse after liver transplantation. The glucagon-like peptide-1 receptor stimulant and/or dipeptidyl peptidase 4 inhibitor generates a differential effect in a tissue specificity way, so as to inhibit cancer cell proliferation and promote cancer cell apoptosis, meanwhile, liver cells are protected against apoptosis, so that obesity-dependent liver cancer or non-dependent liver cancer can be treated or weakened.

The invention relates to a reagent for detection of biological activity of glucagon-like peptide-1 (GLP-1). Each 100 microliters of the reagent mainly comprises 20 micrograms of a gene recombinant GLP-1 acceptor, a dipeptidyl peptidase-4 inhibitor of which the weight is 1% of the weight of a blood plasma sample, 480 micrograms of triphosadenine, 10 micrograms of guanosine triphosphate, 0.5 milligrams of 3-isobutyl-1-methylxanthine and 100 microliters of a membrane reaction solution. The GLP-1 acceptor is obtained by genetic recombination, is convenient for purification and reduces batch difference of the reagent. The GLP-1 acceptor is used as a probe for capturing GLP-1 so that detection sensitivity is improved, biological activity can be directly determined, sensitivity is high, and practicality is strong.