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    Cationic oligonucleotides, automated methods for preparing same and their uses
    76.
    发明授权
    Cationic oligonucleotides, automated methods for preparing same and their uses 有权

    公开(公告)号：US09676798B2

    公开(公告)日：2017-06-13

    申请号：US14745871

    申请日：2015-06-22

    申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  UNIVERSITE DE STRASBOURG ,  POLYPLUS TRANSFECTION

    发明人： Jean-Paul Behr ,  Mitsuharu Kotera ,  Benedicte Pons ,  Emilie Voirin ,  Jean-Serge Remy

    IPC分类号： C07H21/00 ,  C07F9/22 ,  A61K47/48 ,  A61K48/00 ,  C12N15/88

    CPC分类号： C07F9/22 ,  A61K47/59 ,  A61K48/0041 ,  C07H21/00 ,  C12N15/88

    摘要： The invention relates to oligonucleotide-oligocation molecules AiBjH that can be synthetized via automated phosphoramidite chemistry having oligonucleotides moieties Ai and oligocations moieties Bj, wherein .Ai is an i-mer oligonucleotide residue, with i=5 to 50, where nucleotide A is an oligomer with naturally or non naturally occurring nucleobases and/or pentafuranosyl groups and/or native phosphodiester bonds, for example selected from the group comprising deoxyribo, ribo, locked (LNA) nucleotides as well as their chemical modifications or substitutions such as phosphorothioate, 2′-fluoro, 2′-O-alkyl, or a marker group such as a fluorescent agent, .Bj is a j-mer organic oligocation moiety, with j=1 to 50, where B is selected from the group comprising .—HPO3—R1—(X—R2n)n1—X—R3—O—, where R1, R2n and R3, identical or different, are lower alkylene, X is NH or NC(NH2)2, n varies from 1 to 5 and n1=2 to 20, .—HPO3—R4—CH(R5X1)—R6—O—, where R4 is lower alkylene, R5 and R6, identical or different, are lower alkylene and X1 is putrescine, spermidine or spermine residue, .—HPO3—R7-(aa)n2-R8—O—, where R7 is lower alkylene and R8 is lower alkylene, serine, a natural aminoalcohol, (aa)n2 is a peptide containing natural aminoacids with cationic side chains, such as Arginine, Lysine, Ornithine, -Histidine, Diaminopropionic acid and n2=2 to 20.

    BORATE-BASED BASE GENERATOR, AND BASE-REACTIVE COMPOSITION COMPRISING SUCH BASE GENERATOR
    77.
    发明申请
    BORATE-BASED BASE GENERATOR, AND BASE-REACTIVE COMPOSITION COMPRISING SUCH BASE GENERATOR 审中-公开
    基于硼酸盐的基因发生器和包含这种基因发生器的基础反应性组合物

    公开(公告)号：US20160340374A1

    公开(公告)日：2016-11-24

    申请号：US15114048

    申请日：2015-01-22

    申请人： WAKO PURE CHEMICAL INDUSTRIES, LTD.

    发明人： Nobuhiko SAKAI ,  Kosuke YANABA

    IPC分类号： C07F9/22 ,  G03F7/004 ,  C07F5/02 ,  C07D487/04 ,  C07C279/26 ,  C07D233/50

    CPC分类号： C07F9/22 ,  C07C229/26 ,  C07C279/02 ,  C07C279/04 ,  C07C279/16 ,  C07C279/18 ,  C07C279/26 ,  C07C2601/14 ,  C07D233/50 ,  C07D487/04 ,  C07F5/027 ,  C07F9/065 ,  C07F9/5337 ,  C07F9/572 ,  C07F9/6584 ,  C07F9/65848 ,  G03F7/0045

    摘要： An object of the present invention is to provide a compound which is capable of attaining a composition having high storage stability without reacting with a base-reactive compound, even in the case of storage for a long period of time in a mixed state with the base-reactive compound, such as an epoxy-based compound, as well as capable of generating a strong base (guanidines, biguanides, phosphazenes or phosphoniums) by irradiation of light (active energy rays) or heating; a base generator comprising the compound; and a base-reactive composition comprising the base generator and the base-reactive compound.The present invention relates to the compound represented by the general formula (A); the base generator comprising the compound; and the base-reactive composition comprising the base generator and the base-reactive compound. (wherein R1 represents an alkyl group; an arylalkynyl group which may be substituted with a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group; an alkenyl group; a 2-furylethynyl group; a 2-thiophenylethynyl group; or a 2,6-dithianyl group; R2 to R4 each independently represent an alkyl group; an arylalkynyl group which may be substituted with a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group; the aryl group which may be substituted with a halogen atom, an alkyl group, an alkoxy group, or an alkylthio group; a furanyl group; a thienyl group; or an N-alkyl-substituted pyrrolyl group; Z+ represents an ammonium cation having a guanidinium group, a biguanidium group or a phosphazenium group, or a phosphonium cation.)

    摘要翻译： （其中R1表示烷基;可被卤素原子，烷基，烷氧基或烷硫基取代的芳基炔基;烯基; 2-糠基乙炔基; 2-噻吩基乙炔基;或 2,6-二噻吩基; R 2〜R 4各自独立地表示烷基;可被卤素原子，烷基，烷氧基或烷硫基取代的芳基炔基;可被取代的芳基 具有卤素原子，烷基，烷氧基或烷硫基;呋喃基;噻吩基或N-烷基取代的吡咯基; Z +表示具有胍基的铵阳离子，双胍基或 磷腈鎓基或磷鎓阳离子）

    Modified creatine compounds
    78.
    发明授权
    Modified creatine compounds 有权
    改性肌酸化合物

    公开(公告)号：US09434753B2

    公开(公告)日：2016-09-06

    申请号：US14345503

    申请日：2012-09-18

    申请人： Gencia Corporation

    发明人： Shaharyar M. Khan ,  Robert Gadwood ,  Arthur Glenn Romero

    IPC分类号： C07F9/54 ,  C07F9/655 ,  C07F9/6506 ,  C07F9/22

    CPC分类号： C07F9/5456 ,  C07F9/22 ,  C07F9/5442 ,  C07F9/6506 ,  C07F9/6552

    摘要： The invention discloses creatine derivatives that are represented by Formula (I), Formula (II), and Formula (III); wherein Z is a functional group; Y is a mitochondrial targeting agent, a cationic ammonium group, or a polypeptide containing at least one positively charged amino acid residue; each R1 is independently hydrogen, alkyl, or a phosphate group; R2 a linker; R3 is a spacer group; R4 is hydrogen, alkyl, aryl, or heterocyclic; or R4 and R1, or R4 and R3, together with the nitrogen atoms to which they are attached form a heterocyclic ring, and W is hydrogen or alkyl.