Novel inhibitors of dipeptidyl peptidase I
AssigneeProbiodrug AG
InventorsAndre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
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AssigneeProbiodrug AG
InventorsAndre Niestroj, Ulrich Heiser, Hans-Ulrich Demuth
Estimating the term…
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 1 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.
Compounds of the general formula (I)
Compounds according to any one of the preceding claims, wherein the residue R′ may be mono-, di-, or poly-substituted by C1-C6 alkoxy, C1-C6 alkyl, C1-C6 thioether, NO2, NH2, F, Cl, Br, I atoms or groups, except when R′ is H.
Compounds according to any one of the preceding claims, characterised in that they are in the form of prodrugs.
A pharmaceutical composition, characterised in that it contains a compound according to any one of the preceding claims optionally in combination with pharmaceutically acceptable carriers and/or adjuncts.
Dependencies are inferred from the claim text.