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1. 发明授权

US06329519B1 Intermediates for oligonucleotide synthesis 有权
标题翻译：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。

2. 发明授权

US06768005B2 Process 有权
标题翻译：处理
公开(公告)号：US06768005B2
公开(公告)日：2004-07-27
申请号：US09740031
申请日：2000-12-20
申请人： Ben James Mellor , Donald Alfred Wellings , Mark Edward Douglas
发明人： Ben James Mellor , Donald Alfred Wellings , Mark Edward Douglas
IPC分类号： C07H2100
CPC分类号： C07H21/00
摘要： A process for the synthesis of phosphorothioate oligonucleotides is provided which comprises assembling an oligonucleotide bound to a solid support in the presence of acetonitrile; prior to cleaving the oligonucleotide from the solid support removing the acetonitrile; and cleaving the oligonucleotide from the solid support. The process is particularly suited to the large scale synthesis of nucleotides.
摘要翻译：提供了一种合成硫代磷酸酯寡核苷酸的方法，其包括在乙腈存在下组装与固体支持物结合的寡核苷酸; 之前从固相支持物上切下寡核苷酸，除去乙腈; 并从固体支持物上切割寡核苷酸。该方法特别适用于大规模合成核苷酸。

3. 发明授权

US06562960B1 Oligonucleotide analogues 失效
标题翻译：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。

4. 发明授权

US07227017B2 Process for the preparation of phosphorothioate oligonucleotides 有权
标题翻译：硫代磷酸酯寡核苷酸的制备方法
公开(公告)号：US07227017B2
公开(公告)日：2007-06-05
申请号：US10454841
申请日：2003-06-05
申请人： Ben James Mellor , Donald Alfred Wellings , Mark Edward Douglas
发明人： Ben James Mellor , Donald Alfred Wellings , Mark Edward Douglas
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A process for the synthesis of phosphorothioate oligonucleotides is provided which comprises assembling an oligonucleotide bound to a solid support in the presence of acetonitrile; prior to cleaving the oligonucleotide from the solid support removing the acetonitrile; and cleaving the oligonucleotide from the solid support. The process is particularly suited to the large scale synthesis of nucleotides. The acetonitrile may be removed from the solid support by one or both of drying and by washing with solvents. Preferred washing solvents comprise trialkylamines.
摘要翻译：提供了一种合成硫代磷酸酯寡核苷酸的方法，其包括在乙腈存在下组装与固体支持物结合的寡核苷酸; 之前从固相支持物上切下寡核苷酸，除去乙腈; 并从固体支持物上切割寡核苷酸。该方法特别适用于大规模合成核苷酸。可以通过干燥和用溶剂洗涤一次或两次从固体支持物除去乙腈。优选的洗涤溶剂包括三烷基胺。

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