Abstract: The invention relates to a new (3R)-3-amino-4-carboxybutyraldehyde derivatives of general formula(I) wherein X represents a C1-4 alkyloxycarbonyl, an optionally substituted phenyl-(C1-2 alkyloxy)-carbonyl, a C1-4 alkylcarbonyl or an optionally substituted phenyl-(C1-3 alkyl)-carbonyl group, n represents 1 or 0, Y represents, in the case when n=1, a tetrapeptide of general formula Y4-Y3-Y2-Y1, a tripeptide of general formula Y3-Y2-Y1 or a dipeptide of general formula Y2-Y1 or an amino acid residue of general formula Y1, or in the case when n=0, an &agr;-hydroxyacyl-tripeptide of general formula Q4-Y3-Y2-Y1, an &agr;-hydroxyacyl-dipeptide of general formula Q3-Y2-Y1 or an &agr;-hydroxyacyl-aminoacyl residue of general formula Q2-Y1; wherein Y1-Y4 represent a residue selected from the group of the following L- or D-amino acids: alanine, alloisoleucine, cyclohexyl-glycine, phenyl-alanine, glutamine, histidine, isoleucine, leucine, lysine, methionine, pipecolic acid, proline, tyrosi

Abstract: The invention relates to new peptidyl-arginine aldehyde compounds of formula (I) Q-D-Xaa-Pro-Arg-H  (I) wherein Q represents an acyl group of formula Q′—OCO, wherein Q′ represents an alkyl-group with 1-3 carbon atoms, D-Xaa represents a 3-cyclobutyl-D-alanyl- or 3-cyclopentyl-D-alanyl group, Pro represents an L-prolyl group, and Arg represents an L-arginyl group, and acid-addition salts thereof, and pharmaceutical compositions comprising them, which are suitable for the prevention and cure of thrombosis and accelerated blood clotting.

Abstract: This invention relates to peptide aldehyde derivatives of formula (I): D-Xaa-Pro-Arg-H, wherein Xaa represent a 2-cycloheptyl-2-hydroxyacetyl or 2-cyclopentyl-2-hydroxyacetyl group, Pro represents an L-prolyl residue and Arg represents an L-arginyl residue, their acid-additon salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of formula (I) of the invention have therapeutic, particularly anticoagulant, antiplatelet and antithrombotic properties.

Abstract: This invention relates to new peptide derivatives of the general formula (I) A-Xaa-Arg-H, wherein A represents a D- or L-isochroman-1-carbonyl, D- or L-isochroman-3-carbonyl group, furthermore an acyl group of the general formula: D- or DL-A'--CH(OH)--CO, wherein A' represents a phenyl, benzyl, 1-naphthyl, 1-naphthylmethyl, 2-naphthyl, 2-naphthylmethyl, 9-fluorenyl, benzhydryl, cyclohexyl, cyclohexylmethyl, 2-pyridyl, 3-pyridyl or 4-pyridyl group, and Xaa represents an L-prolyl or an L-pipecolinic acid residue, and Arg stands for an L-arginine residue, their acid addition salts formed with an organic or inorganic acid and pharmaceutical compositions containing the same. Furthermore the invention relates to a process for preparing them. The compounds of the invention have valuable therapeutic, particularly anticoagulant, properties.

Abstract: The invention relates to new peptide-aldehydes and a process for the preparation thereof, furthermore to pharmaceutical compositions containing the same.According to a feature of the present invention there are provided new peptide-aldehyde derivatives corresponding to the general formula (I) ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1-6 alkyl group,R.sub.2 stands for C.sub.1-6 alkyl group, furthermore R.sub.1 and R.sub.2 are linked to the amino group of the Xxx alpha-amino acid,Xxx represents a D-phenylalanine residue or a D-alpha-amino acid group having in the side chain a C.sub.1-4 alkyl group,Pro stands for L-proline residue,Yyy stands for L-, D- or DL-arginine residue andA represents an acid residue.The new peptide-aldehyde derivatives of the invention possess valuable anticoagulant activity.

Abstract: The invention relates to t-butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate and D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate, which is highly stable in aqueous solution, and to a process for preparing D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate from D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate or N.sup.G -carboxy derivative containing an acid-sensitive protecting group at its amino terminal, wherein the acid sensitive amino terminal protecting group or optionally the N.sup.G -carboxy group is removed with 1 to 12 N sulfuric acid, applied in 1 to 12 equivalent amounts and the resulting free tripeptide aldehyde sulfate isolated. The D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate of the invention possesses valuable anti-coagulant activity.

Abstract: The invention relates to D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate, highly stable in aqueous solution, and to a process for preparing it from D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate or N.sup.G -carboxy derivative containing an acid-sensitive protecting group at its amino terminal, wherein the acid sensitive amino terminal protecting group or optionally the N.sup.G -carboxy group is removed with 1 to 12 N sulfuric acid, applied in 1 to 12 equivalent amounts and the resulting free tripeptide aldehyde sulfate is isolated. The D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate of the invention possesses valuable anticoagulant activity.

Abstract: Anti-coagulants of the formula X-Pro-Agm(HB) (.sub.n) whereinX is an alpha-amino acid moiety of the configuration having a phenyl, phenyl-(lower)-alkyl or phenyl-(heteroatom-containing) lower alkyl side chain,Agm is an agmatine group (1-amino-4-guanidino-butane),B is an acid residue, andn is an integer from 0-2, are disclosed.

Abstract: Novel peptidyl-arginine aldehyde derivatives and their salts of formula I, ##STR1## wherein X represents a hydrogen atom, benzoyl or tert-butyloxycarbonyl group, and Y is a D-phenylalanine, .beta.-phenyl-D-lactic acid or D-allo-isoleucine moiety, are prepared from peptidyl-arginine aldehydes protected by an urethane type protecting group on their N- or O-terminal and/or a guanidino group, by removing the protecting group in a mixture of lower alkanols and water by means of hydrogenolysis, and eventually converting the product formed into a salt.The compounds of formula I possess valuable antithrombin activity.