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39 条记录 (耗时 0.034 秒)

    2-deoxy-isoguanosines isosteric analogues and isoguanosine derivatives as well as their synthesis
    11.
    发明授权
    2-deoxy-isoguanosines isosteric analogues and isoguanosine derivatives as well as their synthesis 失效
    2-脱氧 - 异鸟嘌呤等位基因类似物和异鸟苷衍生物及其合成

    公开(公告)号：US06498241B1

    公开(公告)日：2002-12-24

    申请号：US09712454

    申请日：2000-11-13

    申请人： Frank Seela ,  Zigmunt Kasimierczuk ,  Klaus Mühlegger ,  Herbert Von Der Eltz

    发明人： Frank Seela ,  Zigmunt Kasimierczuk ,  Klaus Mühlegger ,  Herbert Von Der Eltz

    IPC分类号： C07H2104

    CPC分类号： C07H21/00 ,  C07H19/04

    摘要： 2′-Deoxyisoguanosine, isosteric analogues and isoguanosine derivatives of formulae I-V, processes for their production via compounds of the general formulae a or b and reaction with aroyl isocyanates or from compounds of the general formulae VI-IX by photochemical irradiation. A further production process is the conversion of deoxyguanosines or guanosines by means of persilylation, reaction with ammonia and deamination in the 2 position. The compounds are suitable as pharmaceutical agents with antiviral efficacy.

    摘要翻译： 2-脱氧异鸟苷，式I-V的异构体类似物和异鸟嘌呤衍生物，其通过通式a或b的化合物生产并通过光化学辐射与芳酰基异氰酸酯或通式VI-IX的化合物反应。 进一步的生产过程是通过去硅藻土或鸟氨酸的转化，通过与二氨基反应和脱氨作用。 该化合物适合作为具有抗病毒功效的药剂。

    Nucleosides and nucleoside derivatives containing enzymatically cleavable protecting groups
    13.
    发明授权
    Nucleosides and nucleoside derivatives containing enzymatically cleavable protecting groups 失效
    含有酶切割保护基团的核苷和核苷衍生物

    公开(公告)号：US5756704A

    公开(公告)日：1998-05-26

    申请号：US844127

    申请日：1997-04-18

    申请人： Herbert Waldman ,  Armin Reidel ,  Axel Heuser ,  Klaus Muehlegger ,  Herbert Von Der Eltz ,  Christian Birkner

    发明人： Herbert Waldman ,  Armin Reidel ,  Axel Heuser ,  Klaus Muehlegger ,  Herbert Von Der Eltz ,  Christian Birkner

    IPC分类号： C12Q1/68 ,  C07H19/04 ,  C07H19/073 ,  C07H19/173 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/70 ,  C07H1/00 ,  C07H1/02

    CPC分类号： C07H21/00 ,  C07H19/04 ,  Y02P20/55

    摘要： Process for the production of oligonucleotides of formula II, in which the exocyclic amino groups of the bases adenine, guanine, cytosine, 7-deazaadenine and 7-deazaguanine carry N-phenylacetyl groups, are used for oligonucleotide synthesis, wherein in a first step a starting nucleotide is bound to a solid carrier, subsequently the desired oligonucleotide is synthesized by stepwise coupling with appropriately activated further monomeric nucleotide building blocks of the general formula I with the above-mentioned meanings, if desired, trivalent phosphorus is oxidized to pentavalent phosphorus during and after the synthesis, the oligonucleotide is cleaved from the carrier and the 5' protecting groups are cleaved off. The phenylacetyl functional groups that protect exocyclic NH.sub.2 groups of the bases can be cleaved off in a mild way with penicillin amidohydrolase (EC 3.5.1.11).

    摘要翻译： 用于生产式II寡核苷酸的方法，其中碱基腺嘌呤，鸟嘌呤，胞嘧啶，7-脱氮鸟嘌呤和7-脱氮鸟嘌呤的环外氨基携带N-苯乙酰基用于寡核苷酸合成，其中在第一步中 起始核苷酸与固体载体结合，随后所需的寡核苷酸通过与适当活化的具有上述含义的通式I的其它单体核苷酸结构单元逐步偶联来合成，如果需要，三价磷被氧化成五价磷， 合成后，将寡核苷酸从载体上切下，5'保护基被切掉。 保护碱基的环外NH2基团的苯乙酰基官能团可以用青霉素酰胺水解酶（EC 3.5.1.11）以温和的方式裂解。

    Oligo-2′-deoxynucleotides and their use as pharmaceutical agents with antiviral activity
    18.
    发明授权
    Oligo-2′-deoxynucleotides and their use as pharmaceutical agents with antiviral activity 失效
    寡脱氧核苷酸及其作为具有抗病毒活性的药物的用途

    公开(公告)号：US06329346B1

    公开(公告)日：2001-12-11

    申请号：US08991183

    申请日：1997-12-16

    申请人： Klasu Muhlegger ,  Herbert Von Der Eltz ,  Frank Seela ,  Helmut Rosemeyer

    发明人： Klasu Muhlegger ,  Herbert Von Der Eltz ,  Frank Seela ,  Helmut Rosemeyer

    IPC分类号： A01N4304

    CPC分类号： C07H19/10 ,  C07H19/20 ,  C07H21/00

    摘要： Oligodeoxyribonucleotides in which at least two 2′-deoxy-&bgr;-D-erythro-pentofuranosyl groups are replaced by 2′-deoxy-&bgr;-D-threo-pentofuranosyl groups at both the 5′ end and 3′ end, and oligodeoxyribonucleotides in which at least 20% of the 2′-deoxy-&bgr;-D-erythro-pentofuranosyl groups in consecutive nucleotide building blocks are replaced by 2′-deoxy-&bgr;-D-threo-pentofuranosyl groups and which are composed of 6 to 100 nucleotide building blocks, are suitable for the inhibition of the expression of viral genes and oncogenes by the antisense principle and can be used for the production of pharmaceutical agents with antiviral activity.

    摘要翻译： 在5'末端和3'末端两个脱氧-β-D-赤 - 呋喃糖基被2'-脱氧-β-D-苏 - 戊呋喃糖基取代的寡脱氧核糖核苷酸和其中的寡脱氧核糖核苷酸 连续核苷酸构建单元中2'-脱氧-β-D-赤型 - 戊呋喃糖基的至少20％被2'-脱氧-β-D-苏糖 - 呋喃糖基取代，它们由6至100个核苷酸构建 适用于通过反义原理抑制病毒基因和癌基因的表达，并可用于生产具有抗病毒活性的药剂。