Protease inhibitors and their pharmaceutical uses
OwnerEmerson Poley Pecanha, Luciana J.O. Figueiredo +4inventors
InventorsEmerson Poley Pecanha, Luciana J.O. Figueiredo, Vera Bongertz, Octavio Augusto Ceva Antunes, Amilcar Tanuri, Rodrigo de Moraes Brindeiro
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Abstract
The present invention refers to synthetic protease inhibitors having an axis of symmetry C2 or pseudo-C2 characterised by possessing, in the central portion: (1) preferably, a dihydroxyethylene function, which is isosteric with a peptidic bond; (2) a peptidemimetic bridge between the two nitrogens of the main chain and (3) radicals capable of mimetising amino acids. These new protease inhibitors are a base for the preparation of anti-viral formulations capable of inhibiting HIV virus proliferation.
Claims30
Compound characterised by possessing the following formula:
- 137
- where:
- Z and Y are independently selected from CHR2R3;
- CHR4COOR5;
- CHR4CONHR6 and CHR4C(O)NHN═CR7R8
- R6 is selected from (NH2), CHR4COOR5, hydrogen, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycles, alkyl heterocycles and lower alkyl
- R2, R3, R4, R7, R8 are independently selected from hydrogen, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heterocycles, alkyl heterocycles and lower alkyl
- R5 is a lower alkyl or hydrogen
- W and W2 are independently selected from hydrogen, lower alkyl, carbonylalkyl, carbonylaryl, alkylsulphone, arylsulphone, substituted arylsulphone
- R is hydrogen or a protecting group and
- X and X2 are independently selected from CH2 and CO,
- or a pro drug or a pharmaceutically acceptable salt of said compound.
Dependencies are inferred from the claim text.