发明名称 Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
摘要 Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.
申请公布号 US9409879(B2) 申请公布日期 2016.08.09
申请号 US201214007172 申请日期 2012.03.29
申请人 CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE 发明人 Davioud-Charvet Elisabeth;Lanfranchi Don Antoine;Johann Laure;Williams David Lee;Cesar Rodo Elena
分类号 A61K31/47;C07D311/86;A61K31/352;C07D213/44;C07D215/20;C07D311/78;C07D311/82;C07C46/00;C07C49/84;C07C50/24;C07C50/32;C07D213/50;C07D215/24 主分类号 A61K31/47
代理机构 Young & thompson 代理人 Young & thompson
主权项 1. A method of treating a subject suffering from a blood-feeding parasite of genus Eimeria, Babesia, or Schistosoma, comprising administering to said subject an effective amount of a compound of formula (Ia):wherein: each of X1, X2, X3 and X4 represents a carbon atom, or either one of X1, X2, X3 and X4 represents a nitrogen atom, and each of the three others of X1, X2, X3 and X4 represents a carbon atom, or each of X1 and X4 represents a nitrogen atom and each of X2 and X3 represents a carbon atom; X5 represents CO, CH2 or CHOH; each of X6, X7, X8, X9 and X10 represents a carbon atom, or one of X6, X7, X8, X9 and X10 represents a nitrogen atom and each of the four others of X6, X7, X8, X9 and X10 represents a carbon atom; X1, X2, X3, and X4, when they are carbon atoms optionally being substituted with a hydrogen atom,a halogen atom,a hydroxy group,a triflate group,a phosphate group,a linear or branched (C1-C4)alkyl group,a linear or branched (C1-C4)alkoxy group,a thio(C1-C4)alkoxy group,a pentafluorosulfanyl group,—SCF3,—SCH2F,a trifluoromethyl group, ora trifluoromethoxy group, and X6, X7, X8, X9, X10, when they are carbon atoms optionally being substituted by a hydrogen atom,a halogen atom,a hydroxy group,a linear or branched (C1-C4)alkyl group,a linear or branched (C1-C4)alkoxy group,a thio(C1-C4)alkoxy group,a pentafluorosulfanyl group,a trifluoromethyl group,a trifluoromethoxy group,a difluoromethoxy group,a difluoromethyl group,COOH,COO(C1-C4) alkyl group,CONR1(CH2)mCN with R1 being a hydrogen atom or a linear or branched (C1-C4)alkyl group and m=1, 2 or 3,CSNR1(CH2)mCN with R1 being a hydrogen atom or a linear or branched (C1-C4)alkyl group m=1, 2 or 3,CONR1Het with R1 being a hydrogen atom or a linear or branched (C1-C4) alkyl group and Het representing a pyridine-2-yl group, said pyridine-2-yl group optionally substituted by an amino group in -6 or by a —CONH2 group in -5,NO2,CN,NR2R3 with R2 and R3 each independently representing a hydrogen atom, an amino protecting group that is a Boc group or a (C1-C4) alkyl group, or R2 and R3 forming with the nitrogen atom which bears them a cyclic group selected from the group consisting of morpholine, piperidine, and piperazine groups, said cyclic groups being optionally substituted,an aryl group or an aryl group substituted by one or more substituents selected from the group consisting of a (C1-C4) alkyl group, a —NO2 group, a —COOR4 with R4 being a hydrogen atom or a linear or branched (C1-C4) alkyl group, a —NR5R6 with R5 and R6 independently being a hydrogen atom or a linear or branched (C1-C4) alkyl group, ora heterocyclic group selected from the group consisting of a morpholinyl group, a piperidinyl group, and a piperazinyl group, each of said heterocyclic groups being optionally substituted by one or more substituents selected from the group consisting of a linear or branched (C1-C4)alkyl group, —COOCH2CH3, and a group, and pharmaceutically acceptable derivatives thereof.
地址 Paris FR