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US 2003/0166572 A1Published application
2-Amino-3-hydroxy-4-tert-leucyl-amino-5 phenyl-pentanoic acid amide derivatives
OwnerPascal Furet, Carlos Garcia-Echeverria +3inventors
InventorsPascal Furet, Carlos Garcia-Echeverria, Patricia Imbach, Marc Lang, Johann Zunnernann
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Abstract
The invention relates to compounds of formula (I), wherein the substituents and symbols are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.
Claims16
A compound of formula I
- 12
- wherein
- n is 0 or 1;
- R1 and R2 are independently of the other an aliphatic radical, or an aromatic, aromatic-aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, heterocyclic or heterocyclic-aliphatic radical, each radical having not more than 20 carbon atoms;
- R3 is hydrogen, oxa-alkyl, an aliphatic radical or a radical with up to 20 carbon atoms of the formula —(Y)m—R6, wherein Y is alkyl, m is 0 or 1 and R6 is an unsubstituted or substituted monocyclic radical with 5 or 6 ring members containing up to 3 hetero atoms selected from the group consisting of nitrogen, oxygen and sulfur, wherein said monocyclic radical can also be fused to a benzo ring;
- R4 and R5 are independently selected from the group consisting of hydrogen;
- an aliphatic radical;
- free, etherified or esterified hydroxy;
- free or esterified carboxy;
- formyl;
- alkanoyl;
- unsubstituted, mono- or di-substituted amino;
- mercapto;
- sulfo;
- alkyl-thio;
- carbamoyl;
- N-alkyl-carbamoyl;
- N,N-di-alkyl-carbamoyl;
- cyano and nitro;
- wherein carbon containing radicals R4 and R5 have up to 12 carbon atoms, with the proviso that R4 and R5 are not both hydrogen if n is 1, R1 is benzyl or tert-butyl, R2 is benzyl or 4-methoxy-benzyl, R3 is isopropyl and X is oxygen and that R4 is not methoxy if n is 0 or 1, R2 is 4-methoxy-benzyl, R3 is isopropyl or tert-butyl, R5 is hydrogen and X is oxygen;
- and
- X is nitrogen, oxygen or sulfur;
- or a salt thereof.
20 more elements
Dependencies are inferred from the claim text.