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US 2011/0237577 A1Published application
Bicyclic peptidomimetic inhibitors of aspartyl-proteases for the treatment of infectious diseases
AssigneesIstituto Superiore di Sanita, Universita' Degli Studi Di Firenze
InventorsAntonio Cassone, Flavia De Bernardis, Enrico Garaci, Andrea Trabocchi, Antonio Guarna
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Abstract
The present invention refers to 3-aza-bicyclo[3.2.1]octane derivatives of general formula (I) their preparation, use and pharmaceutical compositions useful in the treatment of pathologies associated with microbial pathogens expressing aspartyl-protease activity.
Claims13
A compounds of formula (I)
- wherein:
- R1 is —CH(R)COR5;
- R is an α-amino acid side chain;
- R2 is H, alkyl, aryl, alkylaryl;
- R3 and R4 are independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, alkylaryl, aryl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, and —CH(α-amino acid side chain)CH2OH;
- R3 and R4 together with the nitrogen atom to which they are connected can form a 5 to 8 membered cycle, optionally substituted;
- R5 is selected from the group consisting of —Oalkyl, —Oaryl, —NHalkyl, NHaryl, amino acid, and peptide;
- comprising all the possible combination of stereoisomers.
5 more elements
A method of treating infectious diseases in a patient in need thereof wherein a compound of formula (I) is administered,
- wherein:
- R1 is selected from the group consisting of benzyl, phenyl, and —CH(R)COR5;
- R is a α-amino acid side chain;
- R2 is H, alkyl, aryl, alkylaryl;
- R3 and R4 are independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, cycloalkyl, alkylaryl, aryl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, and —CH(α-amino acid side chain)CH2OH;
- R3 and R4 together with the nitrogen atom they are bonded to can form a 5 to 8 membered cyclic compound, optionally substituted;
- R5 is selected from the group consisting of —Oalkyl, —Oaryl, —NHalkyl, NHaryl, amino acid, and peptide;
- comprising all the possible combination of stereoisomers.
5 more elements
Dependencies are inferred from the claim text.