Compounds and compositions for use in ingibting endoparasitic fatty acid biosynthesis

Use according to any preceding claim, wherein R3 is C1-6 alkyl or C3-6cycloalkyl.

Use according to any preceding claim, wherein R4 is hydrogen or C1-6alkyl.

Use according to any preceding claim, wherein R1 is selected from the group consisting of hydrogen, C1-20alkyl, (cyano)C1-20 alkylene, C2-20 alkenyl, C2-20 alkynyl, (C1-10alkoxy)C1-20alkylene, (C1-10alkoxy) C2-20alkenylene, (C1-10alkoxy) C2-20alkynylene, C3-8cycloalkyl, (C3-6cycloalkyl) C1-20alkylene, (C3-8cycloalkyl) C2-20alkenylene, (C3-8cycloalkyl)C2-20alkynylene, heterocycle, (heterocycle) C1-20alkylene, (heterocycle) C2-20alkenylene, (heterocycle) C2-20alkynylene, aryl, (aryl) C1-20alkylene, (aryl)C2-20alkenylene, (aryl)C2-20alkynylene, (arylcarbonylarylene) C1-20alkylene, (arylcarbonylarylene)C2-20alkenylene and (arylcarbonylarylene) C2-20alkynylene.

Use according to any preceding claim, wherein heterocycle represents a 3 to 8 membered ring containing at least one heteroatom selected from oxygen, nitrogen and sulphur.

Use according to any preceding claim, wherein aryl represents phenyl.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (IA)

• 15
• where Ra is (cyano)C1-3alkylene.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (IB)

• 16
• where Rb is hydrogen or C3-12alkyl.

Use of at least one thiclactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (IC)

• 17
• where Rc is C2-16 alkenyl, but excluding the racemic mixture of a chiral compound of formula (IC) in which Rc is CH2═CH—C(CH3)═CH—.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (ID)

• 18
• where Rd is (heterocycle)C1-3alkylene.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (IE)

• 19
• where Re is (aryl)C1-6alkylene or (aryl)C2-6alkenylene.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (IF)

• 20
• where Rf is (arylcarbonylarylene)C1-6alkylene.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is of formula (IG)

• 21
• where Rg is (C1-6alkoxy)C1-6alkylene.

Use of at least one thiolactomycin analogue, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one β-ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which thiolactomycin analogue is selected from compounds A to S:

• 22 23 24

Use according to any preceding claim, wherein the endoparasites are of the phylum Apicomplexa.