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    • 1. 发明授权
    • Intermediates for oligonucleotide synthesis
    • 寡核苷酸合成中间体
    • US06329519B1
    • 2001-12-11
    • US09202294
    • 1999-03-15
    • Stephen Paul CollingwoodHeinz Ernst MoserKarl-Heinz AltmannMark Edward Douglas
    • Stephen Paul CollingwoodHeinz Ernst MoserKarl-Heinz AltmannMark Edward Douglas
    • C07H1920
    • C07H19/04Y02P20/55
    • A compound of formula (I) wherein B1 is a radical of a nucleoside base, R1 is hydrogen or a hydroxy-protecting group, R2 is hydrogen, hydroxy or a 2′-nucleoside-modifying atom or group, R3 is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, and Z is halogen or a group of formula (II) where R4 and R5 are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, or R4 is said group and R5 is hydrogen or R4 and R5 together with the nitrogen atom to which they are attached denote a five- to thirteen-membered heterocyclic ring, or Z is a group of formula (III): Nuc-O—, where Nuc is the residue of a natural or synthetic nucleoside or oligonucleotide after removal of a 5′-hydroxyl group therefrom attached through a 5′-methylene thereof to the indicated oxygen atom.
    • 式(I)的化合物,其中B1是核苷碱基的基团,R1是氢或羟基保护基,R2是氢,羟基或2'-核苷修饰的原子或基团,R3是未取代或取代的 C1至C10烷基,C2至C10烯基,C4至C10环烷基烷基,C6至C10芳基或C7至C13芳烷基,Z为卤素或式(Ⅱ)基团,其中R4和R5各自独立地为未取代或取代的C1 C 10至C 10链烯基,C 4至C 10环烷基烷基,C 6至C 10芳基或C 7至C 13芳烷基,或R 4为所述基团,R 5为氢或R 4和R 5与它们所连接的氮原子一起表示 5至13元杂环,或Z为式(III)的基团:Nuc-O-,其中Nuc是除去其中的5'-羟基之后天然或合成的核苷或寡核苷酸的残基,其通过 其指示氧原子的5'-亚甲基。
    • 3. 发明授权
    • Oligonucleotide analogues
    • 寡核苷酸类似物
    • US06562960B1
    • 2003-05-13
    • US09142212
    • 1998-10-09
    • Anthony David BaxterStephen Paul CollingwoodMark Edward DouglasRoger John Taylor
    • Anthony David BaxterStephen Paul CollingwoodMark Edward DouglasRoger John Taylor
    • C07H2100
    • C07H21/00
    • An oligonucleotide analogue having 10 to 200 natural and/or synthetic nucleoside units, linked by internucleoside linkages, at least one of the internucleoside linkages being of formula where the indicated methylene group is attached to a 3′ carbon atom of a nucleoside, the indicated oxygen atom is attached to a 5′-carbon atom of an adjacent nucleside, R1 is hydrogen, hydroxy, O—, thiol, S—, —NH2 or a group of formula R1a, —OR1a, —SR1a, —NHR1b, or —NR1bR1c wherein R1a is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group; and R1b and R1c are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C3 to C8 cycloalkyl, C6 to C10 aryl or C7 to C13 aralkyl group or R1b and R1c together with the nitrogen atom to which they are attached denote a five- or six-membered heterocyclic ring, and X is oxygen or sulfur.
    • 具有10至200个天然和/或合成的核苷单位的寡核苷酸类似物,通过核苷间键连接,至少一个位于所指定的亚甲基上的核苷间键与核苷的3'碳原子连接,所指示的氧原子 连接在相邻核苷酸的5'-碳原子上,R 1是氢,羟基,O-,硫醇,S-,-NH 2或式R1a,-OR1a,-SR1a,-NHR1b或-NR1bR1c的基团,其中 R1a是未取代或取代的C1至C10烷基,C2至C10烯基,C3至C8环烷基,C6至C10芳基或C7至C13芳烷基; R1b和R1c各自独立地为未取代或取代的C1至C10烷基,C2至C10烯基,C3至C8环烷基,C6至C10芳基或C7至C13芳烷基或R1b和R1c与它们所连接的氮原子一起 表示五元或六元杂环,X是氧或硫。