230 results about "Dipeptidyl peptidase-4" patented technology

The invention discloses certain N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

The invention discloses certain N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-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 relates to new compounds that act as specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I). Those compounds are represented by the general formula and the pharmaceutical salts thereof, in which R is an acyl-residue including urethane and peptide, or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues may be optionally substituted, or is H, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R' is a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 cycloalkenyl, C2-C9 heterocycloalkyl, C3-C9 heterocycloalkenyl, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues my be optionally substituted, or is H.

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, β-cell failure, obesity, satiety disorders, atherosclerosis, and various immunomodulatory diseases.

Pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound with the formula: where the labeled substituents are as described herein.

Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C═NR4, and L, X, Z, R2 and R3 are as defined herein.

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 pyrrolidinylaminoacetyl pyrrolidine boronic acid compounds that display selective, potent dipeptidyl peptidase IV inhibitory activity. These compounds are useful for the treatment of disorders that can be regulated or normalized via inhibition of DPP-IV including those characterized by impaired glycemic control such as Diabetes Mellitus and related conditions. The compounds can be administered alone or with another medicament that displays pharmacological activity for treatment of these and other diseases.

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 present invention relates to specific inhibitors of the cysteine protease dipeptidyl peptidase I (DP I), which can be used in the treatment of malignant cell degeneration, immune deseases impaired wound healing and metabolic diseases of humans and are represented by the general formula in which R is a peptide or a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 carbocyclic, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, all of the above residues optionally being substituted, the residue AS—AS is a dipeptide or a mimetic thereof, AS is an amino acid or a peptide mimetic thereof. The amino acid is peptide bound with R and R′ is a branched or unbranched C1-C9 alkyl chain, a branched or unbranched C2-C9 alkenyl chain, a branched or unbranched C2-C9 alkynyl chain, a C3-C9 cycloalkyl, C4-C9 cycloalkenyl, C2-C9 heterocycloalkyl, C3-C9 heterocycloalkenyl, C5-C14 aryl, C3-C9 heteroaryl, C3-C9 heterocyclic, whereas the heterocycloalkyl, heterocycloalkenyl, heteroaryl, heterocyclic residue can have up to 6 hetero ring atoms, an amino acid or a peptide mimetic thereof, all of the above residues may be optionally substituted, or is H.

Compounds that selectively inhibit dipeptidyl peptidase-IV over closely related dipeptidyl peptidases are those of Formula (I):as well as pharmaceutically acceptable salts thereof, cyclic isomers thereof, prodrugs thereof, and solvates thereof, where all the variables are defined herein. These compounds can be used, alone or in combination with other drugs, for the treatment of diabetes and related diseases.

The present invention is related to novel compounds of the general formula A, their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.

The present invention relates to compounds that 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.