PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM
    5.
    发明公开
    PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM 有权
    吡唑并三唑基核苷类似物和包含它们的寡核苷酸

    公开(公告)号:EP2854813A1

    公开(公告)日:2015-04-08

    申请号:EP13798069.4

    申请日:2013-05-30

    申请人: Bio-lab Ltd.

    IPC分类号: A61K31/53

    摘要: The present invention relates to pyrazolotriazolyl nucleoside analogues, oligonucleotide comprising them, and uses thereof. Further the invention relates to a method for reducing gene expression in a cell comprising transfecting the cell with such an oligonucleotide. It has been found, in accordance with the present invention, that certain pyrazolotriazolyl-based nucleoside analogues such as 8-[3′-(2-cyanoethyl)-(N,Ndiisopropyl)]-phosphoramidite-(2′-deoxy-5′-dimethoxytrity 1-13-D-ribofuranozyl)-4-{N-benzoylamino)-pyrazolo[1,5a]-1,3,5-triazine, can be incorporated into oligonucleotides, substituting natural purine nucleosides and imparting acid stability and nuclease stability to the oligonucleotide. Furthermore, oligonucleotides comprising one or more such nucleoside analogues are capable of hybridizing with oligonucleotides having complementary sequences thereto in which no such analogues are incorporated.

    摘要翻译: 本发明涉及吡唑并三唑基核苷类似物,包含它们的寡核苷酸及其用途。 此外,本发明涉及用于减少细胞中基因表达的方法,包括用这种寡核苷酸转染细胞。 已经发现,根据本发明,某些基于吡唑并三唑基的核苷类似物如8- [3' - (2-氰乙基) - (N,N-二异丙基)] - 亚磷酰胺 - (2'-脱氧-5' - 二甲氧基特定1-13-D-ri呋喃丙酰基)-4- {N-苯甲酰氨基) - 吡唑并[1,5a] -1,3,5-三嗪可以掺入寡核苷酸中,取代天然嘌呤核苷并赋予酸稳定性 和寡核苷酸的核酸酶稳定性。 此外,包含一个或多个此类核苷类似物的寡核苷酸能够与其中不含有此类类似物的具有互补序列的寡核苷酸杂交。

    LACTOBACILLUS HAVING ABILITY TO INDUCE IL-12 PRODUCTION, AND METHOD FOR CULTURING SAME
    6.
    发明公开
    LACTOBACILLUS HAVING ABILITY TO INDUCE IL-12 PRODUCTION, AND METHOD FOR CULTURING SAME 审中-公开
    具有诱导IL-12产生和方法文化它的能力LACTOBACILLUS

    公开(公告)号:EP2930235A4

    公开(公告)日:2016-08-17

    申请号:EP13860196

    申请日:2013-07-22

    IPC分类号: C12N1/04 C12N1/20 C12N1/38

    摘要: The present invention provides a novel technology which is capable of producing a large volume of Lactobacillus bacteria and increasing the activity of the obtained Lactobacillus. The Lactobacillus is prepared by culturing in a culture medium and adding an alkaline chemical while controlling the pH, and sterilizing the Lactobacillus by applying stress in the later stage of the cultivation so as to produce Lactobacillus having the ability to induce IL-12 production. Applying stress is preferably selected from the group consisting of: (a) cultivating without adding an alkaline chemical; (b) cultivating at a temperature range in which propagation is suppressed; (c) cultivating by adding 1 % by weight or more of salt; and/or (d) cultivating at pH of 5 or below.

    摘要翻译: 本发明提供一种新颖的技术全部是能够产生大体积的乳杆菌属细菌的和提高所获得的乳杆菌的活性。 乳杆菌是通过在培养基中培养并加入到碱性化学物质,同时控制pH值,并通过在培养的后期阶段施加应力杀菌乳杆菌,以便具有诱导IL-12产生的能力,以产生乳杆菌制备。 施加应力,优选选自下组中选择:不添加到碱性化学试剂(a)培养; (B)在温度范围中传播培养被抑制; (C)由(重量)或更多的盐的加入1%培养; 和/或(d)培养在5或以下的pH。

    PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM
    9.
    发明公开
    PYRAZOLOTRIAZOLYL NUCLEOSIDE ANALOGUES AND OLIGONUCLEOTIDES COMPRISING THEM 有权
    吡唑并三唑核苷寡核苷酸与寡核苷酸的关系

    公开(公告)号:EP2854813A4

    公开(公告)日:2016-01-27

    申请号:EP13798069

    申请日:2013-05-30

    申请人: BIO LAB LTD

    IPC分类号: A61K31/53 C07D487/04

    摘要: The present invention relates to pyrazolotriazolyl nucleoside analogues, oligonucleotide comprising them, and uses thereof. Further the invention relates to a method for reducing gene expression in a cell comprising transfecting the cell with such an oligonucleotide. It has been found, in accordance with the present invention, that certain pyrazolotriazolyl-based nucleoside analogues such as 8-[3′-(2-cyanoethyl)-(N,Ndiisopropyl)]-phosphoramidite-(2′-deoxy-5′-dimethoxytrity 1-13-D-ribofuranozyl)-4-{N-benzoylamino)-pyrazolo[1,5a]-1,3,5-triazine, can be incorporated into oligonucleotides, substituting natural purine nucleosides and imparting acid stability and nuclease stability to the oligonucleotide. Furthermore, oligonucleotides comprising one or more such nucleoside analogues are capable of hybridizing with oligonucleotides having complementary sequences thereto in which no such analogues are incorporated.

    摘要翻译: 本发明涉及吡唑并三唑基核苷类似物,包含它们的寡核苷酸及其应用。 此外,本发明涉及一种减少细胞中基因表达的方法,包括用这种寡核苷酸转染细胞。 已经发现,根据本发明,某些基于吡唑并三唑基的核苷类似物如8- [3' - (2-氰基乙基) - (N,N-二异丙基)] - 亚磷酰胺 - (2'-脱氧-5' -4'-硝基乙酰基)-4- {N-苯甲酰基氨基] - 吡唑并[1,5a] -1,3,5-三嗪可以掺入寡核苷酸中,用天然嘌呤核苷取代并赋予酸稳定性和核酸酶 对寡核苷酸的稳定性。 此外,包含一个或多个这样的核苷类似物的寡核苷酸能够与其中没有引入这样的类似物的具有互补序列的寡核苷酸杂交。