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    • 3. 发明申请
    • Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    • 核苷类,其制备和用作RNA病毒聚合酶的抑制剂
    • US20050080053A1
    • 2005-04-14
    • US10928177
    • 2004-08-30
    • Yarlagadda BabuPooran ChandYahya El-KattanPravin KotianMinwan Wu
    • Yarlagadda BabuPooran ChandYahya El-KattanPravin KotianMinwan Wu
    • A61K31/675C07F9/6561
    • C07F9/65616
    • Compounds represented by the formula: Wherein A is —(CH2)n—R, —CH═CH2, —CH2—CH═CH2, —O—(CH2)n—R, —CH(OH)CH3, —CH(OH)—CH2OH, —CH2—CH(OH)CH3, —CH2—CH(OH)—CH2OH, —CH(OH)—CH(OH)—CH3; R is H, OH, F, N3, NH2, CO2H, SH, alkyl, S-alkyl, O-acyl, CONH2, CONH-alkyl; Z and Z′ independently is OR′, OR2, O—(CH2)n—O-alkyl or aminoacids and esters thereof; R1 and R2 independently is H, alkyl, aryl, pivaloyloxymethyl, phthalyl or substituted phthalyl, C(R3)2OC(O) X (R4)a, R3 is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, or —OR5; R4 is —H, C1-C12 alkyl, C5-C12 aryl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 alkenylaryl, C7-C12 alkynylaryl, or C6-C12 alkaryl, any of which is unsubstituted or is substituted with 1 or 2 halo, cyano, azido, nitro, —N(R6)2 or —OR5; R5 is C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl or C5-C12 aryl; provided that at least one R4 is not H; and a is 1 when X is CH2, or direct bond, or 1 or 2 when X is N with the proviso that when a is 2 and X is N, (a) two N-linked R groups can be taken together to form a carbocyclic or oxygen containing heterocycle, (b) one N-linked R4 additionally can be —OR5 or (c) both N-linked R4 groups can be —H; R6 is H or C1-C8 alkyl; R7 is selected from H, alkyl, alkenyl, alkynyl, aryl, acyloxyalkyl, and pivaloyloxyalkyl; n is 1-3; Y is O, S or NH; W is O or S; B is selected from the group consisting of adenine, guanine, and modified purines are provided.
    • 由下式表示的化合物:其中A是 - (CH2)nR,-CH = CH2,-CH2-CH = CH2,-O-(CH2)nR,-CH(OH)CH3,-CH(OH)-CH2OH, -CH 2 -CH(OH)CH 3,-CH 2 -CH(OH)-CH 2 OH,-CH(OH)-CH(OH)-CH 3; R是H,OH,F,N 3,NH 2,CO 2 H,SH,烷基,S-烷基,O-酰基,CONH 2,CONH-烷基; Z和Z'独立地是OR',OR 2,O-(CH 2)n -O-烷基或其氨基酸及其酯; R 1和R 2独立地是H,烷基,芳基,新戊酰氧基甲基,邻苯二甲酰基或取代的邻苯二甲酰基,C(R 3)2 OC(O)X(R 4)a,R 3是 - H,C 1 -C 12烷基,C 5 -C 12芳基,C 2 -C 12烯基,C 2 -C 12炔基,C 7 -C 12链烯基芳基,C 7 -C 12炔基芳基或C 6 -C 12烷芳基,其中任何一个是未取代的或被1或2 卤素,氰基,叠氮基,硝基或-OR 5; R 4是-H,C 1 -C 12烷基,C 5 -C 12芳基,C 2 -C 12烯基,C 2 -C 12炔基,C 7 -C 12链烯基芳基,C 7 -C 12炔基芳基或C 6 -C 12烷芳基,其中任何一个是未取代的或 被1或2个卤素,氰基,叠氮基,硝基,-N(R 6)2或-OR 5取代; R 5是C 1 -C 12烷基,C 5