申请人:Medivir AB
公开号:US07795270B2
公开(公告)日:2010-09-14
Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is —NHCO—, —CONH—, -0-, —C(═O)—, —CH═CH, —C≡C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(═O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH; —OHR11 is H, F, —CH3, —CH2NH2, —CH2OH, —CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.
公式(I)中的脱氧尿嘧啶衍生物,其中R1是氢或各种取代基;D是—NHCO—,—CONH—,-0-,—C(═O)—,—CH═CH,—C≡C—,—NR5—;R4是氢或各种取代基;R5是H,C1-C4烷基,C1-C4烷酰基;E是Si或C;R6,R7和R8分别选择自C1-C8烷基,C2-C8烯基,C2-C8炔基或稳定的单环,双环或三环环系统;G是—O—,—S—,—CHR10—,—C(═O)—;J是—CH2—,或当G是CHR10时也可以是—O—或—NH—;R10是H,F,—CH3,—CH2NH2,—CH2OH;—OHR11是H,F,—CH3,—CH2NH2,—CH2OH,—CH(OH)CH3,CH(NH3)CH3;或R10和R11一起定义一个烯丙基键,或一起形成一个—CH2基团,从而定义一个顺式或反式环丙基基团;在预防或治疗疟疾等原虫病方面具有用途。