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    Dinucleoside phosphinates and their pharmaceutical compositions
    21.
    发明授权
    Dinucleoside phosphinates and their pharmaceutical compositions 失效
    二核苷次膦酸盐及其药物组合物

    公开(公告)号：US5466677A

    公开(公告)日：1995-11-14

    申请号：US204020

    申请日：1994-02-28

    申请人： Anthony D. Baxter ,  Eric K. Baylis ,  Stephen P. Collingwood ,  Roger J. Taylor ,  Alain De Mesmaeker ,  Chantal Schmit

    发明人： Anthony D. Baxter ,  Eric K. Baylis ,  Stephen P. Collingwood ,  Roger J. Taylor ,  Alain De Mesmaeker ,  Chantal Schmit

    IPC分类号： G01N33/569 ,  A61K31/665 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7064 ,  A61K31/7072 ,  A61K31/7076 ,  A61P31/12 ,  A61P31/16 ,  C07F9/6512 ,  C07F9/655 ,  C07F9/6561 ,  C07H19/04 ,  C07H19/06 ,  C07H19/16 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04

    CPC分类号： C07H21/00 ,  C07H19/04

    摘要： A dinucleotide analogue of formula ##STR1## where B.sup.1 and B.sup.2 are each independently a monovalent nucleoside base radical;R.sup.1 is R.sup.1.sub.a or Z;R.sup.1.sub.a, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, halogen or hydroxy;R.sup.5 is R.sup.5.sub.a or Z;R.sup.6 is hydrogen or R.sup.6.sub.a ;R.sup.7 is hydrogen, alkyl-N,N-dialkylphosphoramidyl or R.sup.7.sub.a, R.sup.8 is R.sup.8.sub.a or Z, or the indicated R.sup.7 O and R.sup.8 together denote an isopropylidenedioxy group;R.sup.5.sub.a and R.sup.8.sub.a are each independently hydrogen, halogen, hydroxy, --OR.sup.10, --OCOR.sup.10 or silyloxy substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.6.sub.a and R.sup.7.sub.a are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.30 araliphatic radical, --COR.sup.11, --SO.sub.2 R.sup.11 or silyl substituted by three C.sub.1 -C.sub.15 hydrocarbyl groups;R.sup.9 is hydrogen, a C.sub.1 -C.sub.8 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical, a C.sub.7 -C.sub.13 araliphatic radical, an alkali metal ion or an ammonium ion;R.sup.10 and R.sup.11 are each independently a C.sub.1 -C.sub.10 aliphatic radical, a C.sub.3 -C.sub.8 cycloaliphatic radical, a C.sub.6 -C.sub.15 aromatic radical or a C.sub.7 -C.sub.16 araliphatic radical;R.sup.x and R.sup.y are independently hydrogen, halogen, hydroxy, a C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl, C.sub.7 -C.sub.16 aralkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.10 alkenoxy, C.sub.6 -C.sub.10 aryloxy or C.sub.7 -C.sub.16 aralkyloxy group, which is substituted or unsubstituted, or --OCOR.sup.z ;R.sup.z is a substituted or unsubstituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.15 aryl or C.sub.7 -C.sub.16 aralkyl group; andZ is C.sub.6 -C.sub.10 aryloxythiocarbonyloxy, the C.sub.6 -C.sub.10 aryl group being substituted or unsubstituted.

    摘要翻译： 式Ⅰ的二核苷酸类似物，其中B1和B2各自独立地是一价核苷碱基; R1为R1a或Z; R1a，R2，R3和R4各自独立地为氢，卤素或羟基; R5为R5a或Z; R6是氢或R6a; R7是氢，烷​​基-N，N-二烷基磷酰胺基或R7a，R8是R8a或Z，或者所指示的R7O和R8一起表示异丙烯二氧基; R5a和R8a各自独立地为氢，卤素，羟基，-OR10，-OCOR10或被三个C1-C15烃基取代的甲硅烷氧基; R6a和R7a各自独立地为C1-C10脂族基团，C6-C15芳族基团，C7-C30芳脂族基团，-COR11，-SO2R11或被三个C1-C15烃基取代的甲硅烷基基团; R9是氢，C1-C8脂族基团，C3-C8脂环族基团，C6-C15芳族基团，C7-C13芳脂族基团，碱金属离子或铵离子; R 10和R 11各自独立地为C 1 -C 10脂族基团，C 3 -C 8脂环族基团，C 6 -C 15芳族基团或C 7 -C 16芳脂族基团; Rx和Ry独立地是氢，卤素，羟基，C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基，C7-C16芳烷基，C1-C10烷氧基，C2-C10链烯氧基，C6-C10芳氧基 或取代或未取代的C 7 -C 16芳烷氧基或-OCOR z; Rz是取代或未取代的C1-C10烷基，C2-C10烯基，C3-C8环烷基，C6-C15芳基或C7-C16芳烷基; Z为C6-C10芳氧基硫代羰氧基，C6-C10芳基为取代或未取代的。