Dimeric inhibitors of influenza neuraminidase
AssigneeBiota Scientific Management Pty Ltd.
InventorsWen-Yang Wu, Betty Jin
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Abstract
This invention relates to novel dimeric compounds, methods for their preparation, pharmaceutical formulations thereof, and their use as antiviral agents. The compounds are particularly useful against influenza virus. In particular the invention provides a dimeric compound which comprises two neuraminidase binding groups attached to a spacer or linking group. Preferably the dimeric molecule comprises two neuraminidase-binding neuraminic acid (sialic acid) or cyclopentyl or cyclohexenyl carboxylic acid derivatives covalently attached to a common spacer group. Pharmaceutical compositions and methods of treatment, prophylaxis and diagnosis are disclosed and claimed.
Claims20
A compound of General Formula I:
- wherein
- R represents an azido group, a hydroxy group, an unsubstituted or substituted guanidino group, or an unsubstituted or substituted amino group;
- R2 represents COCH3,COCF3,SO2CH3 or SO2CF3;
- X represents O, O(C═O), NH, NHCO, O(C═O)NH, O(C═S)NH, NH(C═O)NH, or NH(C═S)NH;
- and the spacer group Y is an optionally substituted straight, or branched or cyclic group or combination thereof, of up to 100 atoms in length, with the backbone atoms selected from the group consisting of carbon, nitrogen, oxygen and sulphur;
- or a pharmaceutically-acceptable derivative thereof.
A method for the treatment of a mammal suffering from a viral infection, comprising the step of administration of an effective amount of a compound of General Formula (I):
- or a pharmaceutically acceptable derivative thereof, wherein:
- R is an amino or guanidino group, which may optionally be substituted;
- R2 is acetyl or trifluoroacetyl;
- X is O(C═O)NH;
- and
- Y is a group of between 10 and 50 atoms in length;
- wherein said administration occurs once.
Dependencies are inferred from the claim text.