Hoechst Aktiengesellschaft

Abbott Laboratories Corporation

Dieter Ruppert

Hansjorg Urbach

Bernward Scholkens

Rainer Henning

Wolfgang Ruger

Karl-Heinz Budt

Wolf-Ulrich Nickel

Heinz-Werner Kleemann

Jochen Knolle

Anuschirwan Peyman

Holger Heitsch

Arnold Paessens

Wolfgang Linz

Adalbert Wagner

Jutta Hansen

Wilhelm Stahl

Christoph Meichsner

Bernd Stowasser

Heinz-Werner Kleeman

Henning Schussler

Konrad Wagner

The present invention relates to compounds of the formula I ##STR1## wherein A, Y, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, l, m and the corresponding radicals labeled with * are defined as stated in the description, a process for their preparation and their use for the inhibition of retroviral proteases.

Inhibitors of retroviral proteases

Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.

Phosphinic acid derivatives, their preparation and their use

Amino acid derivatives with renin-inhibiting properties, a process for the preparation thereof, agents containing these, and the use thereof The invention relates to renin-inhibiting amino acid derivatives of the formula ##STR1## in which R.sup.1 is a radical of a substituted nitrogen-containing heterocycle such as piperidine, X is CO, CS, SO.sub.2 or SO, Y is CH.sub.2, O or S, B is the radical of an amino acid of the formula H--B--OH, and R.sup.3, R.sup.4 and R.sup.5 are as defined in the description, a process for the preparation thereof, agents containing these, and the use thereof.

Amino acid derivatives with renin-inhibiting properties, a process for

The invention relates to compounds of the formula I ##STR1## in which A denotes a radical of the formula II ##STR2## in which E denotes a CH.sub.2 group or an NR.sup.9 radical,

Renin-inhibiting aminodiol derivatives

Dipeptide derivatives having an enzyme inhibitory action Compounds of the formula I ##STR1## in which R.sup.1 represents a (substituted) heterocyclyl-alkyl, -alkoxy, -cycloalkyl or -cycloalkoxy and the corresponding heterocyclylmercapto radicals, A and B independently of one another denote an amino acid, R.sup.2 is hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl, aryl or aryl-alkyl, R.sup.3 represents hydrogen, alkyl, aryl, aryl-alkyl or hydroxyl and R.sup.4 denotes a radical (CH.sub.2).sub.0-4 CHR.sup.5 -D where R.sup.5 =hydrogen, alkyl, alkoxy, alkylthio, alkylamino, hydroxyl, azido or halogen and D=(substituted) heterocyclyl, have enzyme-inhibiting properties. Processes for the preparation of compounds of the formula I and their use in the treatment of hypertension and viral diseases are described.

Dipeptide derivatives having an enzyme inhibitory action

The invention relates to compounds of the formula I ##STR1## in which A represents a substituted thio-, sulfinyl- or sulfonyl-alkanoyl radical or a four- to eleven-membered heterocycle, B is an amino acid residue, R.sup.1 denotes hydrogen (substituted) alkyl, (substituted)cycloalkyl or aryl, R.sup.2 represents hydrogen, (substituted)alkyl or aryl, R.sup.3 denotes a radical of the formula --(CH.sub.2).sub.q --(X).sub.r --(CH.sub.2).sub.s --R.sup.6 with X denoting CF.sub.2, CO or CHR.sup.8, R.sup.6 denoting a (substituted)heteroaromatic, R.sup.8 denoting alkyl, alkoxy, alkylthio, alkylamino, hydroxyl, azide or halogen, q and s denoting 1 to 4, and r denoting 0 or 1, and R.sup.9 is hydrogen, (substituted)alkyl, alkanoyl, cycloalkanoyl, (substituted) aroyl or (substituted)aryl, and to the salts thereof. In addition, processes for the preparation of these compounds, and the use thereof as renin inhibitors are described.

Renin-inhibiting amino acid derivatives

The present invention relates to compounds of the general formula I ##STR1## in which A denotes a radical from the group comprising S, SO, SO.sub.2, O, CO, CS or a direct bond,

Enzyme-inhibiting amino acid derivatives, a process for the preparation

The invention relates to compounds of the formula 1 ##STR1## in which A.sup.1 denotes a radical of the formulae ##STR2## A.sup.2 is absent or represents a radical of the formula ##STR3## R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and X and Y, independently of one another, represent --O-- or --NR.sup.13 --, and to the salts thereof. Also described is a process for the preparation of the compounds of the formula 1, corresponding pharmaceutical products, and the use thereof as medicines, and intermediates for the preparation of these compounds.

Renin inhibitors

Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof. The present invention relates to compounds of the formula I ##STR1## in which A and B denote, indpendently of one another, an amino acid,

Enzyme-inhibiting urea derivatives of dipeptides, a process for the

The invention relates to compounds of the formula ##STR1## in which R.sup.1 is absent or denotes hydrogen, alkyl or acyl, A denotes an acyl radical or an amino acid residue, B denotes an amino acid residue, and R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification, and to their salts, to a process for their preparation, to pharmaceutical products containing them, and to their use as medicaments, and intermediates for the preparation of these compounds.

Growing community of inventors

Kronberg/Taunus, Germany

Dieter Ruppert