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1. 发明授权

US09695210B2 C1-phostphonate analogue of UDP-GlcNAc for inhibition of O-GlcNAc transferase 有权
公开(公告)号：US09695210B2
公开(公告)日：2017-07-04
申请号：US14969136
申请日：2015-12-15
申请人： SOONCHUNHYANG UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
发明人： Jungkyun Im
IPC分类号： C07H19/00 , C07H19/10 , C07H1/02 , C07H19/06 , C07H1/04 , C07H19/067
CPC分类号： C07H19/10 , C07H1/02 , C07H1/04 , C07H19/06 , C07H19/067
摘要： A novel C1-phosphate log of uridine-5′-diphosphate (UDP)-GlcNAc as an effective OGT (O-linked N-acetylglucosamine (O-GlcNAc) transferase) inhibitor, and a preparation method for the same provides a compound having an OGT inhibitory effect that can be used as a useful tool in the studies on various vital phenomena in association with the protein modification by O-GlcNAc within cells and furthermore as a candidate substance in the treatment or research of diseases related to the protein modification by O-GlcNAc, such as cancers, diabetes, or degenerative neurological diseases.

2. 发明申请

US20160355539A1 SELECTIVE SOLVENT FREE PHOSPHORYLATION 审中-公开
标题翻译：选择性溶剂免费磷化
公开(公告)号：US20160355539A1
公开(公告)日：2016-12-08
申请号：US15172662
申请日：2016-06-03
申请人： ChromaDex, Inc. , The Queen's University of Belfast
发明人： Marie Eugenie Migaud , Philip Redpath , Kerri Crossey , Richard Cunningham , Troy Rhonemus , Sylesh Venkataraman
IPC分类号： C07H19/048 , C07F9/58 , C07H19/20 , C07F9/6558
CPC分类号： C07H19/048 , C07F9/58 , C07F9/65583 , C07F9/65616 , C07H1/04 , C07H19/04 , C07H19/20
摘要： 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−, Y1, Y2, Z1, Z2, n, R1, R2, R3, R4, R5, R6, and R7 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.
摘要翻译：提供了一种合成方法，用于制备具有式（I）的烟酰胺核苷（“NR”）或其盐的磷酸化类似物及其还原或修饰的衍生物，其具有式（II），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。通常使用如所述的适当的机械化学技术无溶剂条件。（一）（二）

3. 发明申请

US20150368288A1 METHOD OF PREPARING OLIGOMERIC COMPOUNDS USING MODIFIED COUPLING PROTOCOLS 有权
标题翻译：使用改性的偶联方法制备低分子化合物的方法
公开(公告)号：US20150368288A1
公开(公告)日：2015-12-24
申请号：US14764655
申请日：2014-01-30
申请人： Isis Pharmaceuticals, Inc.
发明人： Isaiah E. Cedillo , Michael T. Migawa , W. Brad Wan
IPC分类号： C07H21/02
CPC分类号： C07H21/02 , C07H1/00 , C07H1/02 , C07H1/04 , C07H19/06 , C07H19/16 , C07H21/00
摘要： Provided herein are methods for the synthesis of oligomeric compounds wherein the standard coupling protocols are modified when coupling bicyclic nucleosides of Formula I. More particularly, the modified coupling protocols provide for a decrease in the ratio of phosphoramidite solution to activator solution in the coupling reagent with an increased contact time. The modified coupling protocols provide for oligomeric compounds having comparable yields to similar oligomeric compounds having modified nucleosides other than bicyclic nucleosides of Formula I.
摘要翻译：本文提供了合成寡聚化合物的方法，其中当偶联式I的双环核苷时，标准偶联方案被修饰。更具体地，修饰的偶联方案提供了亚磷酰胺溶液与偶联试剂中活化剂溶液的比例的降低，增加接触时间。修饰的偶联方案提供具有与具有式I的双环核苷以外的修饰的核苷的类似寡聚化合物具有相当产率的低聚化合物。

4. 发明公开

US20230303614A1 CAPPING COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20230303614A1
公开(公告)日：2023-09-28
申请号：US18048407
申请日：2022-10-20
申请人： Gritstone bio, Inc.
发明人： Karin Jooss , Amy Rachel Rappaport , Ciaran Daniel Scallan , Leonid Gitlin , Sue-Jean Hong , Arvin Akoopie
IPC分类号： C07H21/02 , C07H21/00 , C07H1/04 , A61K47/54 , A61K39/12 , C12N15/86
CPC分类号： C07H21/02 , C07H21/00 , C07H1/04 , A61K47/549 , A61K39/12 , C12N15/86 , A61K2039/53
摘要： The present disclosure includes, among other things, non-natural nucleotides useful as 5′ caps for RNA nucleotides. The present disclosure also includes, among other things, compositions and methods using delivery and vaccine RNA nucleotide compositions that include non-natural nucleotides as 5′ caps.

5. 发明申请

US20160208313A1 SYNTHESIS OF FOUR-COLOR 3'-O-ALLYL MODIFIED PHOTOCLEAVABLE FLUORESCENT NUCLEOTIDES AND RELATED METHODS 审中-公开
标题翻译：四色素3'-O-全变体可光化荧光核苷的合成及相关方法
公开(公告)号：US20160208313A1
公开(公告)日：2016-07-21
申请号：US14992784
申请日：2016-01-11
申请人： Jingyue Ju , Qinglin Meng , Dae H Kim , Lanrong Bi , Xiaopeng Bai , Nicholas J Turro
发明人： Jingyue Ju , Qinglin Meng , Dae H Kim , Lanrong Bi , Xiaopeng Bai , Nicholas J Turro
IPC分类号： C12Q1/68 , C07H19/14 , C07H19/10 , C07H1/04
CPC分类号： C12Q1/6806 , C07H1/04 , C07H19/067 , C07H19/10 , C07H19/14 , C12Q1/6869 , C12Q1/6874 , C12Q2521/101 , C12Q2525/117 , C12Q2525/186 , C12Q2563/107
摘要： This invention provides a process for making 3′-O-allyl-dGTP-PC-Biodopy-FL-510, 3′-O-allyl-dATP-PC-ROX, 3′-O-allyl-dCTP-PC-Bodipy-650 and 3′-O-allyl-dUTP-PC-R6G, and related methods.
摘要翻译：本发明提供了制备3'-O-烯丙基-dGTP-PC-生物反应-FL-510,3'- O-烯丙基-DATP-PC-ROX，3'-O-烯丙基-dCTP-PC- 650和3'-O-烯丙基-dUTP-PC-R6G及相关方法。

6. 发明授权

US09255292B2 Synthesis of four-color 3′-O-allyl modified photocleavable fluorescent nucleotides and related methods 有权
标题翻译：四色3'-O-烯丙基修饰的可透光荧光核苷酸的合成及相关方法
公开(公告)号：US09255292B2
公开(公告)日：2016-02-09
申请号：US13186353
申请日：2011-07-19
申请人： Jingyue Ju , Qinglin Meng , Dae H. Kim , Lanrong Bi , Xiaopeng Bai , Nicholas J. Turro
发明人： Jingyue Ju , Qinglin Meng , Dae H. Kim , Lanrong Bi , Xiaopeng Bai , Nicholas J. Turro
IPC分类号： C12Q1/68 , C12P19/34 , C07H19/067 , C07H19/04
CPC分类号： C12Q1/6806 , C07H1/04 , C07H19/067 , C07H19/10 , C07H19/14 , C12Q1/6869 , C12Q1/6874 , C12Q2521/101 , C12Q2525/117 , C12Q2525/186 , C12Q2563/107
摘要： This invention provides a process for making 3′-O-allyl-dGTP-PC-Biodopy-FL-510, 3′-O-allyl-dATP-PC-ROX, 3′-O-allyl-dCTP-PC-Bodipy-650 and 3′-O-allyl-dUTP-PC-R6G, and related methods.
摘要翻译：本发明提供了制备3'-O-烯丙基-dGTP-PC-生物反应-FL-510,3'- O-烯丙基-DATP-PC-ROX，3'-O-烯丙基-dCTP-PC- 650和3'-O-烯丙基-dUTP-PC-R6G及相关方法。

7. 发明申请

US20150112053A1 OLIGONUCLEOTIDE SYNTHESIS METHOD USING HIGHLY DISPERSIBLE LIQUID-PHASE SUPPORT 有权
标题翻译：使用高分散液相支持的寡核苷酸合成方法
公开(公告)号：US20150112053A1
公开(公告)日：2015-04-23
申请号：US14404562
申请日：2012-05-30
申请人： Shokaku Kim , Masanori Matsumoto
发明人： Shokaku Kim , Masanori Matsumoto
IPC分类号： C07H21/00 , C07H1/00
CPC分类号： C07H21/00 , C07H1/00 , C07H1/02 , C07H1/04 , C07H19/073 , C07H21/02 , C07H21/04 , Y02P20/55
摘要： A nucleic acid synthesis method enabling a reaction in a fluid (flow) with a highly dispersible liquid-phase support to improve coupling efficiency is provided.The method for synthesizing an oligonucleotide comprising: sequentially condensing and oxidizing a nucleoside phosphoramidite compound in the presence of an acid/azole complex compound using a starting raw material, i.e., hydrophobic group-bonded nucleoside represented by Formula (1):where R1: an alkylene group having 1 to 12 carbon atoms, R2: an alkylene group having 1 to 22 carbon atoms, R3 and R4 each independently represent an alkyl group having 1 to 22 carbon atoms or the like, R5: a single bond or an alkylene group having 1 to 22 carbon atoms, R6: each independently an alkyl group having 6 to 30 carbon atoms, n represents an integer of 2 to 6, X represents a hydrogen atom, hydroxyl group, or the like, Y: a protecting group deprotectable under an acidic condition, and Z: an adenyl group, a guanyl group, or the like having a polar group optionally protected by a protecting group, wherein a condensation reaction is performed by preliminarily dissolving the hydrophobic group-bonded nucleoside or hydrophobic group-bonded oligonucleotide and the nucleoside phosphoramidite compound in a non-polar solvent, and contacting the resulting solution with the acid/azole complex compound or a solution containing the complex compound.
摘要翻译：提供了一种使流体（流动）与高度分散的液相载体反应以提高耦合效率的核酸合成方法。合成寡核苷酸的方法，其包括：使用起始原料，即由式（1）表示的疏水性基团键合的核酸，在酸/唑配合物的存在下，顺序地使核苷亚磷酰胺化合物缩合和氧化：其中R1：具有1至12个碳原子的亚烷基，R 2：具有1至22个碳原子的亚烷基，R 3和R 4各自独立地表示具有1至22个碳原子的烷基等，R 5：单键或亚烷基，其具有 1〜22个碳原子，R6各自独立地为碳原子数6〜30的烷基，n表示2〜6的整数，X表示氢原子，羟基等，Y表示可以在酸性条件，Z：具有任选被保护基保护的极性基团的腺苷基，脒基等，其中通过预先将疏水性基团键合的核苷或疏水基键合的寡核苷酸和核苷亚磷酰胺化合物在非极性溶剂中，并使所得溶液与酸/唑配合物或含有配合物的溶液接触。

8. 发明申请

US20130158249A1 Novel Synthesis of Nucleoside 5'-Triphosphates and Their Derivatives 审中-公开
标题翻译：核苷5'-三磷酸及其衍生物的新型合成
公开(公告)号：US20130158249A1
公开(公告)日：2013-06-20
申请号：US13817820
申请日：2011-08-19
申请人： Zhen Huang
发明人： Zhen Huang
IPC分类号： C07H1/04 , C07H19/10 , C07H19/20
CPC分类号： C07H1/04 , C07H19/10 , C07H19/20 , C07H21/00
摘要： Disclosed are compounds of nucleoside 5′-triphosphates of formula (I), or derivatives thereof, or pharmaceutically acceptable salts of said nucleoside 5′-triphosphates or said derivatives, wherein the Base of formula (I) is Adenine (A), Cytosine (C), Guanine (G), Thymine (T), Uracil (U), modified nucleobase or unnatural nucleobase; R1 is H or OH, R2 is H or OH, X is independently selected from the group consisting of O, S and Se; and Y is independently selected from the group consisting of O, B (borano, or BH3), S, and Se. Also disclosed are processes of preparing the compounds of formula (I), said process comprising steps according to Scheme A:
摘要翻译：公开了式（I）的核苷5'-三磷酸的化合物或其衍生物或所述核苷5'-三磷酸或所述衍生物的药学上可接受的盐，其中式（I）的碱是腺嘌呤（A），胞嘧啶 C），鸟嘌呤（G），胸腺嘧啶（T），尿嘧啶（U），修饰的核碱基或非天然核碱基; R1是H或OH，R2是H或OH，X独立地选自O，S和Se; 并且Y独立地选自O，B（硼烷或BH 3），S和Se。还公开了制备式（I）化合物的方法，所述方法包括根据方案A的步骤：

9. 发明申请

US20120156680A1 SYNTHESIS OF FOUR-COLOR 3'-O-ALLYL MODIFIED PHOTOCLEAVABLE FLUORESCENT NUCLEOTIDES AND RELATED METHODS 有权
标题翻译：四色素3'-O-全变体可光化荧光核苷的合成及相关方法
公开(公告)号：US20120156680A1
公开(公告)日：2012-06-21
申请号：US13186353
申请日：2011-07-19
申请人： Jingyue Ju , Qinglin Meng , Dae H. Kim , Lanrong Bi , Xiaopeng Bai , Nicholas J. Turro
发明人： Jingyue Ju , Qinglin Meng , Dae H. Kim , Lanrong Bi , Xiaopeng Bai , Nicholas J. Turro
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6806 , C07H1/04 , C07H19/067 , C07H19/10 , C07H19/14 , C12Q1/6869 , C12Q1/6874 , C12Q2521/101 , C12Q2525/117 , C12Q2525/186 , C12Q2563/107
摘要： This invention provides a process for making 3′-O-allyl-dGTP-PC-Biodopy-FL-510, 3′-O-allyl-dATP-PC-ROX, 3′-O-allyl-dCTP-PC-Bodipy-650 and 3′-O-allyl-dUTP-PC-R6G, and related methods.
摘要翻译：本发明提供了制备3'-O-烯丙基-dGTP-PC-生物反应-FL-510,3'- O-烯丙基-DATP-PC-ROX，3'-O-烯丙基-dCTP-PC- 650和3'-O-烯丙基-dUTP-PC-R6G及相关方法。

10. 发明申请

US20180162895A1 METHOD FOR PREPARING NICOTINAMIDE MONONUCLEOTIDE (NMN) 审中-公开
公开(公告)号：US20180162895A1
公开(公告)日：2018-06-14
申请号：US15574851
申请日：2016-07-30
申请人： BONTAC BIO-ENGINEERING(SHENZHEN) CO.,LTD
发明人： Rongzhao FU , Qi ZHANG
IPC分类号： C07H19/048 , C12P19/30 , C07H1/04
CPC分类号： C07H19/048 , C07H1/04 , C07H19/207 , C12N9/1077 , C12P19/30 , C12Y204/02012
摘要： The present invention provides a method for preparing nicotinamide mononucleotide (NMN) by biocatalysis. The method includes a step of catalytically reacting a plurality of raw materials including nicotinamide, ATP, and ribose in the presence of nicotinamide phosphoribosyltransferase (Nampt), ribose phosphate pyrophosphokinase, and ribokinase, to prepare the NMN.

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