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US 6,673,783 B2Granted
Fusidic acid derivatives
AssigneeLeo Pharmaceutical Products Ltd. A/S
InventorTore Duvold
Life of this patent
Estimating the term…
Abstract
Novel 17,20-methanofusidic acid derivatives are used in pharmaceutical compositions for the treatment of infections, in particular in topical compositions for the treatment of skin or eye infections.
Claims19
A compound of the general formula I
- wherein
- Q1, Q2 and Q3 are the same or different and independently represent a —(CO)— group;
- a —(CHOH)— group;
- a —(CHOR)— group;
- a —(CHSH)— group;
- a —(CHNH2)— group;
- a —(C—X)— group, wherein X represents halogen;
- or a —(CHNHR)— group, wherein R represents an alkyl radical having 1 to 4 carbon atoms or an acyl radical having 1 to 4 carbon atoms;
- and wherein Q2 and Q3 may also independently represent a —(CH2)— group;
- Y represents hydrogen, hydroxy, an alkyl radical having 1 to 4 carbon atoms, or an acyl radical having 1 to 4 carbon atoms;
- A represents an oxygen or sulphur atom;
- R1 represents an alkyl radical having 1 to 4 carbon atoms, an olefinic group having 2 to 4 carbon atoms, a (C1-C6)acyl group, a (C3-C7)cycloalkylcarbonyl group or a benzoyl group, R1 being optionally substituted with one or more halogen atoms and/or hydroxy, alkoxy or azido groups;
- and pharmaceutically acceptable salts and easily hydrolysable esters thereof.
10 more elements
A compound of formula I selected from the group consisting of
- 17S,20S-Methanofusidic acid, Compound 101
- 24,25-Dihydro-17S,20S-methanofusidic acid, Compound 102
- 11-Dehydro-17S,20S-methanofusidic acid, Compound 103
- 3-dehydro-17S,20S-methanofusidic acid, Compound 104
- 16-Deacetoxy-16β-propionyloxy-17S,20S-methanofusidic acid, Compound 105
- 16-Deacetoxy-16β-cyclohexylcarbonyloxy-17S,20S-methanofusidic acid, Compound 106
- 16-Deacetoxy-16β-(isopropionyloxy)-17S,20S-methanofusidic acid, Compound 107
- 16-Deacetoxy-16β-(4′-fluorobenzoyloxy)-17S,20S-methanofusidic acid, Compound 108
- 16-Deacetoxy-16β-furfuryloxy-17S,20S-methanofusidic acid, Compound 109
- 16-Deacetoxy-16β-ethoxy-17S,20S-methanofusidic acid, Compound 110
- 16-Deacetoxy-16β-(1′,1′,1′-trifluoroethoxy)-17S,20S-methanofusidic acid, Compound 111
- 16-Deacetoxy-16β-(methoxymethyl-17S,20S-methanofusidic acid, Compound 112
- 3-Dehydro-3β-bromo-17S,20S-methanofusidic acid, Compound 113
- 3-Dehydro-3β-chloro-17S,20S-methanofusidic acid, Compound 114
- and their pharmaceutically acceptable salts and easily hydrolysable esters.
12 more elements
A stereoisomer of a compound of formula I or Ia in pure form;
- or a mixture of such stereoisomers.
Dependencies are inferred from the claim text.