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US 8,283,366 B2Granted
Derivatives of pyridoxine for inhibiting HIV integrase
AssigneeAmbrilia Biopharma Inc.
InventorsBrent Richard Stranix, Guy Milot, Jean-Emmanuel Bouchard
Life of this patent
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Abstract
The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, solvates or formulations thereof. Compounds of Formula I inhibit HIV-integrase enzyme and are useful for preventing and treating of HIV infection, acquired immune deficiency syndrome (AIDS), AIDS-related complex (ARC), hepatitis C, and other diseases and conditions caused or mediated by HIV infection.
Claims11
A compound of formula I,
- wherein:
- X is H or OH;
- Y is H or OH;
- R1 is H or halogen (F, Cl, Br, I);
- R2 is H or halogen (F, Cl, Br, I);
- R3 is H, C1-6 alkyl, C1-6 fluoroalkyl, or benzyl;
- R4 is H, C1-6 alkyl, or benzyl;
- and
- R5 is H or C1-6 alkyl;
- or
- pharmaceutically acceptable salts thereof.
8 more elements
A compound of formula Ic,
- wherein:
- X is O or N—OH;
- Y is H or OH;
- R1 is H or halogen (F, Cl, Br, I);
- R2 is H or halogen (F, Cl, Br, I);
- R3 is H, C1-6 alkyl or benzyl;
- R4 is H, C1-6 alkyl or benzyl;
- and
- R5 is H or C1-6 alkyl;
- or
- pharmaceutically acceptable salts thereof.
8 more elements
A compound selected from:
- (R)-5-((3-Chloro-4-fluorophenyl)(hydroxy)methyl)-N,3-dihydroxy-4-(hydroxymethyl)picolinamide;
- 5-(4-fluorobenzyl)-N,3-dihydroxy-4-(hydroxymethyl)picolinamide;
- 5-((4-fluorophenyl)(hydroxy)methyl)-N,3-dihydroxy-4-(hydroxymethyl)picolinamide;
- 5-((4-fluorophenyl)(hydroxy)methyl)-N-hydroxy-N,2,2-trimethyl-4H-[1,3]dioxino[4,5-c]pyridine-8-carboxamide;
- 5-((4-fluorophenyl)(hydroxy)methyl)-N,3-dihydroxy-4-(hydroxymethyl)-N-methylpicolinamide;
- 5-((4-fluorophertyl)(hydroxy)methyl)-3-hydroxy-4-(hydroxymethyl)-N-methoxypicolinamide;
- 5-(4-fluorobenzyl)-N,3-dihydroxy-4-methylpicolinamide;
- 5-((4-fluorophenyl)(hydroxy)methyl)-N,3-dihydroxy-4-methylpicolinamide;
- 5-(4-fluorobenzoyl)-N,3-dihydroxy-4-methylpicolinamide;
- (E)-5-((4-fluorophenyl)(hydroxyimino)methyl)-N,3-dihydroxy-4-methylpicolinamide;
- and
- (S)-5-((3-Chloro-4-fluorophenyl)(hydroxy)methyl)-N,3-dihydroxy-4-(hydroxymethyl)picolinamide;
- or
- pharmaceutically acceptable salts thereof.
11 more elements
Dependencies are inferred from the claim text.