Compounds for use in the treatment of fascioliasis
AssigneeMerck Patent GmbH
InventorsJohn Mark Francis Gardner, Andrew Simon Bell
Life of this patent
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Abstract
The present invention relates to compounds and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such novel compounds, salts or solvates and to the use of such novel compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
Claims33
A method for treating or preventing fascioliasis comprising administering a therapeutically effective amount of a compound of formula (1a), (1b), (1c), (1d) or (1e) or a pharmaceutically acceptable salt or solvate thereof to a patient in need thereof,
- wherein:
- R1 is C1-C4 alkyl optionally substituted with up to five F atoms, C3-C6 cycloalkyl optionally substituted with one methyl group, or C4-C7 cycloalkylmethyl;
- R2 is H, F, Cl or OMe;
- R3 is H, OH, OMe, OPO(OH)OH or OCH2OPO(OH)OH;
- R4 is H, OH, OMe, OPO(OH)OH or OCH2OPO(OH)OH;
- provided that R3 and R4 cannot both be H;
- or R3 and R4 combine, together with the phenyl ring to which they are attached, to form an indazole group as shown below
- R5 is H, F, Cl or OMe;
- R6 is H, F, Cl or OMe;
- X is N or C—R7, wherein R7 is H or F;
- R8 is SF5, Br, C1-C3 alkyl optionally substituted with up to seven F atoms, C3-C4 cycloalkyl, OCH2C≡CH or OC1-C3 alkyl optionally substituted with up to seven F atoms;
- R9 is H;
- and
- R10 is H, F or Me.
2-3. (canceled)
A compound of formula (1e)
- or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is C1-C4 alkyl optionally substituted with up to five F atoms, C3-C6 cycloalkyl optionally substituted with one methyl group, or C4-C7 cycloalkylmethyl;
- R2 is H, F, Cl or OMe;
- R3 is H, OH, OMe, OPO(OH)OH or OCH2OPO(OH)OH;
- R4 is H, OH, OMe, OPO(OH)OH or OCH2OPO(OH)OH;
- provided that R3 and R4 cannot both be H;
- or R3 and R4 combine, together with the phenyl ring to which they are attached, to form an indazole group as shown below
- R5 is H, F, Cl or OMe;
- R6 is H, F, Cl or OMe;
- X is N or C—R7, wherein R7 is H or F;
- R8 is SF5, Br, C1-C3 alkyl optionally substituted with up to seven F atoms, C3-C4 cycloalkyl, OCH2C≡CH or OC1-C3 alkyl optionally substituted with up to seven F atoms;
- R9 is H;
- and
- R10 is H, F or Me.
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21-23. (canceled)
Dependencies are inferred from the claim text.