Abstract: Prodrug compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The Prodrug compounds can be used in the treatment of impaired glucose tolerance, glucosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy.
Abstract: 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.
Abstract: 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.
Type:
Grant
Filed:
September 6, 2002
Date of Patent:
January 18, 2005
Assignee:
Probiodrug AG
Inventors:
Andre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
Abstract: The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula 1 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.
Abstract: The invention relates to a simple and industrially readily executable method of producing thiazolidine base and salts thereof. In particular, the invention relates to a process for the production of thiazolidine base and salts thereof which is characterized in that hexamethylenetetramine of formula (I)
is caused to react with cysteamine or salts thereof of formula (II)
in which X(−) represents an acid residue, X(−) being preferably a halide or sulfate.
Abstract: Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.
Type:
Grant
Filed:
November 28, 2000
Date of Patent:
April 15, 2003
Assignee:
Probiodrug AG
Inventors:
Hans-Ulrich Demuth, Konrad Glund, Dagmar Schlenzig, Susanne Kruber
Abstract: The present invention discloses a method for therapeutically treating mammals, including but not limited to humans, to increase the relative insulin producing performance of endogenous pancreatic &bgr;-cells and to cause differentiation of pancreatic epithelial cells into insulin producing &bgr;-cells. Oral administration a DP IV inhibitor causes the active form of GLP-1 to be preserved longer under physiological conditions. The extended presence of GLP-1, in particular in the pancreatic tissue facilitates differentiation and regeneration of the &bgr;-cells already present that are in need of repair. These repaired insulin producing cells can contribute to the correction and maintenance of normal physiological glycemic levels.