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    • 1. 发明申请
    • COMPOUNDS AND COMPOSITIONS FOR USE IN INHIBITING ENDOPARASITIC FATTY ACID BIOSYNTHESIS
    • 用于抑制内毒素脂肪酸生物合成的化合物和组合物
    • WO0149278A3
    • 2002-04-11
    • PCT/GB0100082
    • 2001-01-08
    • UNIV CARDIFFBERRY COLINHARWOOD JOHN L
    • BERRY COLINHARWOOD JOHN L
    • C07D333/32A61K31/381A61K45/00A61P33/00A61P33/02A61P33/06A61P43/00C07D409/06A61K31/38
    • A61K31/381
    • Use of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, as an inhibitor of at least one beta -ketoacyl acyl carrier protein synthase operable in the fatty acid biosynthesis of endoparasites, which compound is of the general formula (I) where R1 is selected from the group consisting of hydrogen, alkyl, (cyano)alkylene, alkenyl, alkynyl, (alkoxy)alkylene, (alkoxy)alkenylene, (alkoxy)alkynylene, cycloalkyl, (cycloalkyl)alkylene, (cycloalkyl)alkenylene, (cycloalkyl)alkynylene, (heterocycle)alkylene, (heterocycle)alkenylene, (heterocycle)alkynylene, aryl, (aryl)alkylene, (aryl)alkenylene, (aryl)alkynylene, (arylcarbonylarylene)alkylene, (arylcarbonylarylene)alkenylene and (arylcarbonylarylene)alkynylene; R2 is alkyl or cycloalkyl; R3 is alkyl or cycloalkyl; and R4 is hydrogen or alkyl; including racemic mixtures and enantiomers of said compound when the latter is chiral, but excluding the racemic mixture of a chiral compound of formula (I) in which R1 is CH2=CH-C(CH3)=CH-, R2 is methyl, R3 is methyl and R4 is hydrogen.
    • 至少一种化合物或其药学上可接受的盐或前药作为至少一种可在内寄生虫的脂肪酸生物合成中操作的β-酮酰酰基载体蛋白合成酶的抑制剂的用途,该化合物具有通式(I),其中R 1 (烷氧基)亚烷基,(烷氧基)亚烯基,(烷氧基)亚炔基,环烷基,(环烷基)亚烷基,(环烷基)亚烯基,(环烷基) 亚芳基,(亚芳基)亚烷基,(芳基)亚烯基,(芳基羰基亚芳基)亚烷基,(芳基羰基亚芳基)亚烯基和(芳基羰基亚芳基)亚炔基) R2是烷基或环烷基; R3是烷基或环烷基; 和R4是氢或烷基; 包括当后者为手性时所述化合物的外消旋混合物和对映异构体,但不包括其中R 1为CH 2 = CH-C(CH 3)= CH-的式(I)的手性化合物的外消旋混合物,R 2为甲基,R 3为 甲基,R4为氢。