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    Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases
    18.
    发明申请
    Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases 审中-公开
    核苷类，其制备和用作RNA病毒聚合酶的抑制剂

    公开(公告)号：US20050080053A1

    公开(公告)日：2005-04-14

    申请号：US10928177

    申请日：2004-08-30

    申请人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Pravin Kotian ,  Minwan Wu

    发明人： Yarlagadda Babu ,  Pooran Chand ,  Yahya El-Kattan ,  Pravin Kotian ,  Minwan Wu

    IPC分类号： A61K31/675 ,  C07F9/6561

    CPC分类号： C07F9/65616

    摘要： 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.

    摘要翻译： 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