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    2'-Substituted nucleosides and oligonucleotide derivatives
    4.
    发明申请
    2'-Substituted nucleosides and oligonucleotide derivatives 审中-公开
    2'-取代的核苷和寡核苷酸衍生物

    公开(公告)号：US20050159374A1

    公开(公告)日：2005-07-21

    申请号：US10696488

    申请日：2003-10-29

    申请人： Bernard Cuenoud ,  Karl-Heinz Altmann ,  Pierre Martin ,  Heinz Moser

    发明人： Bernard Cuenoud ,  Karl-Heinz Altmann ,  Pierre Martin ,  Heinz Moser

    IPC分类号： C12N15/09 ,  C07H21/00 ,  A61K48/00 ,  C07H21/02 ,  C12Q1/68

    CPC分类号： C07H21/00

    摘要： The invention relates to an oligonucleotide derivative which comprises at least one nucleoside building block of the formula (I) The invention furthermore relates to nucleoside building blocks, intermediates and processes for preparing the oligonucleotide derivatives and the nucleoside building blocks. The invention also relates to pharmaceutical compositions and to uses of the oligonucleotide derivatives and the nucleoside building blocks.

    摘要翻译： 本发明涉及包含至少一种式（I）核苷结构单元的寡核苷酸衍生物。本发明还涉及核苷结构单元，中间体和制备寡核苷酸衍生物和核苷结构单元的方法。 本发明还涉及药物组合物以及寡核苷酸衍生物和核苷结构单元的用途。

    Intermediates for oligonucleotide synthesis
    5.
    发明授权
    Intermediates for oligonucleotide synthesis 有权
    寡核苷酸合成中间体

    公开(公告)号：US06329519B1

    公开(公告)日：2001-12-11

    申请号：US09202294

    申请日：1999-03-15

    申请人： Stephen Paul Collingwood ,  Heinz Ernst Moser ,  Karl-Heinz Altmann ,  Mark Edward Douglas

    发明人： Stephen Paul Collingwood ,  Heinz Ernst Moser ,  Karl-Heinz Altmann ,  Mark Edward Douglas

    IPC分类号： C07H1920

    CPC分类号： C07H19/04 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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。

    Phthalazines with angiogenesis inhibiting activity
    10.
    发明授权
    Phthalazines with angiogenesis inhibiting activity 失效
    具有血管生成抑制活性的酞嗪类

    公开(公告)号：US06710047B2

    公开(公告)日：2004-03-23

    申请号：US10338062

    申请日：2003-01-07

    申请人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

    发明人： Guido Bold ,  Jörg Frei ,  Peter Traxler ,  Karl-Heinz Altmann ,  Helmut Mett ,  David Raymond Stover ,  Jeanette Marjorie Wood

    IPC分类号： A61K31495

    CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

    摘要： The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etheritied or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are either single or double bonds; or an N-oxide of said compound with the stipulation that, if Y is pyridyl or unsubstituted cycloalkyl, X is imino, and the remaining radicals are as defined, then G is selected from the group comprising lower alkylene, —CH2—O—, —CH2—S—, oxa and thia; or a salt thereof. The compounds inhibit angiogenesis.

    摘要翻译： 本发明涉及式I化合物，其中r为0至2，n为0至2; m为0〜4; R1和R2（i）在每种情况下都是低级烷基，或（ii）一起在子式I *中形成桥，或（iii）一起形成子式I **中的桥，其中一个或两个环成员T1，T2 ，T3和T4是氮，余数分别为CH; A，B，D和E是N或CH，其中不多于2个这些基团是N; G是低级亚烷基，酰氧基或羟基 - 低级亚烷基，-CH 2 -O-，-CH 2 -S-，-CH 2 -NH-，氧杂，硫杂或亚氨基; Q是甲基; R是H或低级烷基; X是亚氨基，氧杂或硫杂; Y是芳基，吡啶基或（未）取代的环烷基; 羟基，醚基或酯化的羟基，硝基，氰基，羧基，酯化的羧基，烷酰基，氨基甲酰基，N-单或N，N-二取代的氨基甲酰基，脒基， 胍基，巯基，磺基，苯硫基，苯基 - 低级烷硫基，烷基苯硫基，苯基亚磺酰基，苯基 - 低级烷基亚磺酰基，烷基苯基亚磺酰基，苯基磺酰基，苯基 - 低级烷基磺酰基或烷基苯基磺酰基。 并且其中以波浪线表征的键是单键或双键; 或所述化合物的N-氧化物，其规定如果Y是吡啶基或未取代的环烷基，则X是亚氨基，剩余的基团如所定义，则G选自低级亚烷基，-CH 2 -O-， -CH 2 -S-，氧杂和硫杂; 或其盐。 该化合物抑制血管发生。