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    • 7. 发明公开
    • NUCLEOSIDES PREPARATION THEREOF AND USE AS INHIBITORS OF RNA VIRAL POLYMERASES
    • 核苷酸,IHRE HERSTELLUNG UND VERWENDUNG ALS HEMMER VON RNA-VIRUSPOLYMERASEN
    • EP1450809A2
    • 2004-09-01
    • EP02807245.2
    • 2002-11-14
    • Biocryst Pharmaceuticals, Inc.
    • BABU, Yarlagadda, S.CHAND, PooranEL-KATTAN, YahyaWU, Minwan
    • A61K31/505A61K31/51A61K31/513A61K31/52C07D239/36C07D473/34
    • C07F9/65616A61K31/13A61K31/66A61K36/28A61K38/20A61K38/208A61K38/21A61K38/212C07F9/10C07F9/65121C07F9/65122Y02A50/393Y02A50/465A61K2300/00
    • 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 , OR , O-(CH2)n-O-alkyl or aminoacids and esters thereof; R and R independently is H, alkyl, aryl, pivaloyloxymethyl, phthalyl or substituted phthalyl, C(R )2OC(O)X(R )a, R 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 -OR ; R 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(R )2 or -OR ; R is C1-C12
    • 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为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'独立地为OR 1,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