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    SELECTIVE SOLVENT FREE PHOSPHORYLATION
    3.
    发明申请
    SELECTIVE SOLVENT FREE PHOSPHORYLATION 审中-公开
    选择性溶剂免费磷化

    公开(公告)号：WO2016196941A1

    公开(公告)日：2016-12-08

    申请号：PCT/US2016/035729

    申请日：2016-06-03

    Applicant: CHROMADEX, INC. ,  THE QUEEN'S UNIVERSITY OF BELFAST

    Inventor： MIGAUD, Marie Eugenie ,  REDPATH, Philip ,  CROSSEY, Kerri ,  CUNNINGHAM, Richard ,  RHONEMUS, Troy ,  VENKATARAMAN, Sylesh

    IPC: A01N43/40 ,  A61K31/44

    CPC classification number: C07H19/048 ,  C07F9/582 ,  C07F9/65583 ,  C07F9/65616 ,  C07H1/04 ,  C07H19/04 ,  C07H19/20

    Abstract: A synthetic process is provided for the preparation of phosphorylated analogs of nicotinamide riboside ("NR") having the formula (I), or salts thereof, and reduced or modified derivatives thereof, having the formula (II), wherein X - , Y 1 , Y 2 , Z 1 , Z 2 , n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined herein. The present disclosure also relates to the preparation of phosphorylated analogs of nicotinic acid riboside ("NAR") having the formula (I), or salts thereof, and reduced or modified derivatives thereof, having the formula (II). Generally solvent-free conditions are employed using appropriate mechano-chemical techniques as described. (I) (II)

    Abstract translation: 提供了一种合成方法，用于制备具有式（I）的烟酰胺核苷（“NR”）或其盐以及具有式（II）的还原或修饰的衍生物的磷酸化类似物，其中X，Y 1， Y2，Z1，Z2，n，R1，R2，R3，R4，R5，R6和R7如本文所定义。 本公开还涉及具有式（I）的烟酸核糖苷（“NAR”）的磷酸化类似物或其盐以及具有式（II）的还原或修饰的衍生物的制备。 一般使用无溶剂条件，使用所述的适当的机械化学技术。 （一）（二）

    NICOTINIC ACID RIBOSIDE OR NICOTINAMIDE RIBOSIDE COMPOSITIONS, REDUCED DERIVATIVES THEREOF, AND THE USE THEREOF
    4.
    发明申请
    NICOTINIC ACID RIBOSIDE OR NICOTINAMIDE RIBOSIDE COMPOSITIONS, REDUCED DERIVATIVES THEREOF, AND THE USE THEREOF 审中-公开
    非甾体类抗坏血酸或尼罗替尼组合物，其减少的衍生物及其用途

    公开(公告)号：WO2016149395A1

    公开(公告)日：2016-09-22

    申请号：PCT/US2016/022682

    申请日：2016-03-16

    Applicant: CHROMADEX INC. ,  THE QUEEN'S UNIVERSITY OF BELFAST

    Inventor： DELLINGER, Ryan ,  MIGAUD, Marie, Eugenie ,  REDPATH, Philip ,  RHONEMUS, Troy ,  CUNNINGHAM, Richard

    IPC: C07H19/048 ,  A61K31/706

    CPC classification number: C07H19/048 ,  A61K8/675 ,  A61Q19/00 ,  A61Q19/004 ,  A61Q19/007 ,  A61Q19/08

    Abstract: Derivatives of nicotinic acid riboside (NAR), nicotinamide riboside (NR), and reduced NAR and NR, including 1-(2', 3', 5'-triacetyl-beta-D-ribofuranosyl)-1,4-dihydronicotinic acid (4a), and compositions containing the same and/or reduced derivative forms of nicotinamide riboside including 1-(2',3',5'-triacetyl-beta-D-ribofuranosyl)-1,4-nicotinamide (2), are provided for use in the care of treatment of skin and skin conditions. In some embodiments, the invention relates to pharmaceutical compositions and cosmetic compositions containing one or more NR, NAR, NRH, or NARH derivatives, or prodrugs or salts thereof. In further embodiments, the invention relates to methods of using one or more NR, NAR, NRH, or NARH derivatives, or prodrugs, solvates, or salts thereof, to promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for improving cell and tissue survival and overall cell and tissue health.

    Abstract translation: 烟碱苷（NAR）衍生物，烟酰胺核苷（NR）和还原的NAR和NR，包括1-（2'，3'，5'-三乙酰基-β-D-呋喃核糖基）-1,4-二氢烟酸 提供了含有相同和/或还原的衍生物形式的包括1-（2'，3'，5'-三乙酰基-β-D-呋喃核糖基）-1,4-烟酰胺（2）的烟酰胺核苷的组合物 用于护理皮肤和皮肤状况的治疗。 在一些实施方案中，本发明涉及含有一种或多种NR，NAR，NRH或NARH衍生物或其前药或盐的药物组合物和化妆品组合物。 在进一步的实施方案中，本发明涉及使用一种或多种NR，NAR，NRH或NARH衍生物或其前药，溶剂合物或其盐来促进细胞中烟酰胺腺嘌呤二核苷酸（NAD +）的细胞内水平的增加的方法，以及 用于改善细胞和组织存活的组织以及整个细胞和组织的健康。

    METHODS OF PREPARING NICOTINAMIDE RIBOSIDE AND DERIVATIVES THEREOF
    5.
    发明申请
    METHODS OF PREPARING NICOTINAMIDE RIBOSIDE AND DERIVATIVES THEREOF 审中-公开
    制备尼古丁酰胺及其衍生物的方法

    公开(公告)号：WO2015014722A1

    公开(公告)日：2015-02-05

    申请号：PCT/EP2014/065971

    申请日：2014-07-24

    Applicant: THE QUEEN'S UNIVERSITY OF BELFAST

    Inventor： MIGAUD, Marie ,  REDPATH, Philip ,  CROSSEY, Kerri ,  DOHERTY, Mark

    IPC: C07H19/048

    CPC classification number: C07H19/048 ,  C07H1/00 ,  C07H1/06 ,  C07H19/04 ,  Y02P20/582

    Abstract: The invention relates to methods of preparing nicotinamide riboside and derivatives thereof. In an aspect, the invention relates to a method of preparing a compound of formula (I), wherein n is 0 or 1; m is 0 or 1; Y is O or S; R 1 is selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted primary or secondary amino, and substituted or unsubstituted azido; R 2 - R 5 , which may be the same or different, are each independently selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, and substituted or unsubstituted aryl; and X - is an anion, selected from an anion of a substituted or unsubstituted carboxylic acid, a halide, a substituted or unsubstituted sulfonate, a substituted or unsubstituted phosphate, a substituted or unsubstituted sulfate, a substituted or unsubstituted carbonate, and a substituted or unsubstituted carbamate.

    Abstract translation: 本发明涉及制备烟酰胺核苷及其衍生物的方法。 一方面，本发明涉及制备式（I）化合物的方法，其中n为0或1; m为0或1; Y为O或S; R 1选自H，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基，取代或未取代的伯或仲氨基，以及取代或未取代的叠氮基; R 2 -R 5可以相同或不同，各自独立地选自H，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的炔基和取代或未取代的芳基; 并且X是阴离子，其选自取代或未取代的羧酸的阴离子，卤化物，取代或未取代的磺酸酯，取代或未取代的磷酸酯，取代或未取代的硫酸酯，取代或未取代的碳酸酯， 未取代的氨基甲酸酯。

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