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    Intermediates for oligonucleotide synthesis
    1.
    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。

    Oligonucleotide analogues
    2.
    发明授权
    Oligonucleotide analogues 失效
    寡核苷酸类似物

    公开(公告)号：US06562960B1

    公开(公告)日：2003-05-13

    申请号：US09142212

    申请日：1998-10-09

    申请人： Anthony David Baxter ,  Stephen Paul Collingwood ,  Mark Edward Douglas ,  Roger John Taylor

    发明人： Anthony David Baxter ,  Stephen Paul Collingwood ,  Mark Edward Douglas ,  Roger John Taylor

    IPC分类号： C07H2100

    CPC分类号： C07H21/00

    摘要： 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.

    摘要翻译： 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。

    Combinations of Glycopyrrolate and Beta2 Adrenoceptor Agonists
    9.
    发明申请
    Combinations of Glycopyrrolate and Beta2 Adrenoceptor Agonists 审中-公开
    乙酰胆碱酯酶和β2肾上腺素受体激动剂的组合

    公开(公告)号：US20130237564A1

    公开(公告)日：2013-09-12

    申请号：US13862529

    申请日：2013-04-15

    申请人： Stephen Paul Collingwood

    发明人： Stephen Paul Collingwood

    IPC分类号： A61K31/4704 ,  A61K31/40

    CPC分类号： A61K31/4704 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/402 ,  A61K2300/00

    摘要： A medicament comprising, separately or together (A) glycopyrrolate; and (B) either a compound of formula I in free or salt or solvate form, wherein W, Rx, Ry, R1, R2, R3, R4, R5, R6 and R7 have the meanings as indicated in the specification, or a compound of formula II in free or salt or solvate form, wherein X has the meaning as indicated in the specification, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain (A) and (B) are also described.

    摘要翻译： 一种药物，其单独或一起（A）格隆溴铵; 和（B）游离或盐或溶剂化物形式的式I化合物，其中W，Rx，Ry，R 1，R 2，R 3，R 4，R 5，R 6和R 7具有如说明书中所示的含义，或化合物 式II的游离或盐或溶剂合物形式，其中X具有说明书中指出的含义，用于在治疗炎性或阻塞性气道疾病中同时，连续或分开施用。 还描述了含有（A）和（B）的药物组合物。