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    PROCESS FOR PRODUCING MULTIPLE OLIGONUCLEOTIDES ON A SOLID SUPPORT
    2.
    发明公开
    PROCESS FOR PRODUCING MULTIPLE OLIGONUCLEOTIDES ON A SOLID SUPPORT 审中-公开
    用于生产固相多种寡核苷酸

    公开(公告)号：EP1319012A1

    公开(公告)日：2003-06-18

    申请号：EP01966905.0

    申请日：2001-09-05

    申请人： University Technologies International Inc.

    发明人： PON, Richard, T. ,  SANGHVI, Yogesh ,  YU, Shuyuan

    IPC分类号： C07H21/00

    CPC分类号： C07H21/00 ,  C07B2200/11

    摘要： A process for the production of the two or more molecules of interest. The present process may be advantageously used to produce two, three, four or more molecules of interest (the same or different from one another) on a single support material. A preferred embodiment comprises use of the present process to produce two or more oligonucleotides of interest. The process can be readily extended to other applications such as combinatorial chemistry, peptide synthesis and the like. Various novel intermediates in the process are also disclosed.

    LINKER ARM FOR SOLID SUPPORT OLIGONUCLEOTIDE SYNTHESIS AND PROCESS FOR PRODUCTION THEREOF
    3.
    发明公开
    LINKER ARM FOR SOLID SUPPORT OLIGONUCLEOTIDE SYNTHESIS AND PROCESS FOR PRODUCTION THEREOF 失效
    连接臂固体支持寡核苷酸合成和方法及其生产

    公开(公告)号：EP0877751A1

    公开(公告)日：1998-11-18

    申请号：EP96940965.0

    申请日：1996-12-13

    申请人： UNIVERSITY TECHNOLOGIES INTERNATIONAL INC.

    发明人： PON, Richard, T. ,  YU, Shuyuan

    IPC分类号： C07B61 ,  C07H19 ,  C07H21 ,  G01N33 ,  G01N37

    CPC分类号： C07H21/00 ,  C07B2200/11 ,  C07H19/06

    摘要： A linker arm for solid support oligonucleotide synthesis, the linker arm comprising formula (1), wherein: X1 is selected from the group consisting of -O-, -S-, -S(O)¿2?-, -C(O)- and -N(R?12)-; R12¿ is selected from the group comprising hydrogen, a substituted or unsubstituted C¿1?-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkaryl group, X?3¿ is -O- or -N(H)-; R?1, R2, R3, R4 and R5¿ are the same or different and are selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C¿1?-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group; n is 0, 1 or 2; and one of A' and B' is selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C1-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group, and the other of A' and B' has formula (2), wherein X?2¿ is selected from the group consisting of -O-, -S-, -S(O)¿2?- and -N(R?13)-; R13¿ is selected from the group comprising hydrogen, a substituted or unsubstituted C¿1?-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkaryl group; R?6 and R7¿ are the same or different and are selected from the group consisting of hydrogen, halide, a substituted or unsubstituted C¿1?-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group; p is 0 or 1; and m is 0, 1 or 2. A process for producing the linker arm is also disclosed. The linker arm is useful in solid support oligonucleotide synthesis and is characterized by a desirable combination of stability against spontaneous hydrolysis and ease of intentional cleavage of the synthesized oligonucleotide from the linker arm.

    LINKER PHOSPHORAMIDITES FOR OLIGONUCLEOTIDE SYNTHESIS
    4.
    发明公开
    LINKER PHOSPHORAMIDITES FOR OLIGONUCLEOTIDE SYNTHESIS 审中-公开
    LEFT亚磷酰胺用于生产寡核苷酸

    公开(公告)号：EP1319013A2

    公开(公告)日：2003-06-18

    申请号：EP01971543.2

    申请日：2001-09-10

    申请人： University Technologies International Inc.

    发明人： PON, Richard, T. ,  YU, Shuyuan

    IPC分类号： C07H21/00 ,  C07H19/06 ,  C07H19/16

    CPC分类号： C07H19/10 ,  C07B2200/11 ,  C07H19/00 ,  C07H19/20 ,  C07H21/00 ,  C40B40/00

    摘要： A novel approach for combining the ease of cleavage of carboxylic acid linker arms with the single phosphoramidite coupling chemistry of the universal supports useful in oligonucleotide synthesis. There is disclosed a new class of phosphoramidite reagents, linker phosphoramidites, which contain a bifunctional linker arm with a protected nucleoside linked through a 3'-ester bond on one end and a reactive phosphoramidite group or other phosphate precursor group on the other end. The phosphoramidite group on the linker phosphoramidite may be activated under the same conditions and has similar reactivity as conventional nucleoside-3'-phosphoramidite reagents lacking the intermediate linker arm. The 3'-ester linkage contained within the linker phosphoramidite has similar properties to the linkages on prederivatized supports. The ester linkage is stable to all subsequent synthesis steps, but upon treatment with a cleavage reagent, such as ammonium hydroxide, the ester linkage is hydrolyzed. This releases the oligonucleotide product with the desired 3'-hydroxyl terminus and leaves the phosphate portion of the reagent attached to the support, which is subsequently discarded.

    REUSABLE SOLID SUPPORT FOR OLIGONUCLEOTIDE SYNTHESIS, PROCESS FOR PRODUCTION THEREOF AND PROCESS FOR USE THEREOF
    5.
    发明公开
    REUSABLE SOLID SUPPORT FOR OLIGONUCLEOTIDE SYNTHESIS, PROCESS FOR PRODUCTION THEREOF AND PROCESS FOR USE THEREOF 失效
    可重复使用FESTTÄGER寡核苷酸合成，制造及其方法及其使用方法

    公开(公告)号：EP0876390A1

    公开(公告)日：1998-11-11

    申请号：EP96940964.0

    申请日：1996-12-13

    申请人： UNIVERSITY TECHNOLOGIES INTERNATIONAL INC.

    发明人： PON, Richard, T. ,  YU, Shuyuan

    IPC分类号： C07B61 ,  C07H19 ,  C07H21 ,  G01N33 ,  G01N37

    CPC分类号： C07H21/00 ,  C07B2200/11 ,  C07H19/06

    摘要： A solid support for oligonucleotide synthesis is disclosed. The solid support has formula (1) wherein: R8 is selected from the group consisting of a substituted or unsubstituted C¿1?-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group; X?3 and X4¿ are the same or different and are selected from the group consisting of -O-, -S-, -S(O)¿2?- and -N(R?12)-; R12¿ is selected from the group consisting of a substituted or unsubstituted C¿1?-C20 alkyl group, a substituted or unsubstituted C5-C30 aryl group and a substituted or unsubstituted C5-C40 alkylaryl group; and Y is selected from the group consisting of: -CH2-CH2-; -CH2-; -CH2-O-CH2-; -CH2-CH2-CH2-; -CH=CH-; -CH=C(CH3)-; -C(CH3)=C(CH3)-; -CH2-C(=CH2)-; and -CH2-S-CH2-; wherein when Y is -CH2-CH2-, at least one of X?3 and X4¿ is -O-. An aspect of the invention also relates to a linker arm for oligonucleotide synthesis based on the solid support. Process for producing of the solid support and the linker arm, respectively, are also disclosed. The linker arm is characterized by being reusable in an otherwise conventional oligonucleotide production protocol.