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1. 发明授权

US4415732A Phosphoramidite compounds and processes 失效
标题翻译：亚磷酰胺化合物和方法
公开(公告)号：US4415732A
公开(公告)日：1983-11-15
申请号：US248450
申请日：1981-03-27
申请人： Marvin H. Caruthers , Serge L. Beaucage
发明人： Marvin H. Caruthers , Serge L. Beaucage
IPC分类号： C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04 , C07H17/00
CPC分类号： C07H21/00
摘要： A new class of nucleoside phosphoramidites which are relatively stable to permit isolation thereof and storage at room temperature. The phosphoramidites are derivatives of saturated secondary amines.
摘要翻译：一类新的核苷亚磷酰胺，其相对稳定以允许其在室温下分离并储存。亚磷酰胺是饱和仲胺的衍生物。

2. 发明授权

US4973679A Process for oligonucleo tide synthesis using phosphormidite intermediates 失效
标题翻译：使用亚磷酰胺中间体进行寡核苷酸合成的方法
公开(公告)号：US4973679A
公开(公告)日：1990-11-27
申请号：US909070
申请日：1986-09-18
申请人： Marvin H. Caruthers , Serge L. Beaucage
发明人： Marvin H. Caruthers , Serge L. Beaucage
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A new class of nucleoside phosphoramidites which are relatively stable to permit isolation thereof and storage at room temperature. The phosphoramidites are derivatives of saturated secondary amines.
摘要翻译：一类新的核苷亚磷酰胺，其相对稳定以允许其在室温下分离并储存。亚磷酰胺是饱和仲胺的衍生物。

3. 发明授权

US4668777A Phosphoramidite nucleoside compounds 失效
标题翻译：亚磷酰胺核苷化合物
公开(公告)号：US4668777A
公开(公告)日：1987-05-26
申请号：US637927
申请日：1984-08-06
申请人： Marvin H. Caruthers , Serge L. Beaucage
发明人： Marvin H. Caruthers , Serge L. Beaucage
IPC分类号： C07H21/00 , C07H17/00
CPC分类号： C07H21/00
摘要： A new class of nucleoside phosphoramidites which are relatively stable to permit isolation thereof and storage at room temperature. The phosphoramidites are derivatives of saturated secondary amines.
摘要翻译：一类新的核苷亚磷酰胺，其相对稳定以允许其在室温下分离并储存。亚磷酰胺是饱和仲胺的衍生物。

4. 发明授权

US5003097A Method for the sulfurization of phosphorous groups in compounds 失效
标题翻译：化合物中磷基硫化的方法
公开(公告)号：US5003097A
公开(公告)日：1991-03-26
申请号：US415710
申请日：1989-10-02
申请人： Serge L. Beaucage , Judith B. Regan , Radhakrishnan P. Iyer
发明人： Serge L. Beaucage , Judith B. Regan , Radhakrishnan P. Iyer
IPC分类号： C07D339/04 , C07D339/08 , C07H19/10 , C07H19/20 , C07H21/00
CPC分类号： C07H21/00 , C07D339/04 , C07D339/08 , C07H19/10 , C07H19/20
摘要： A method is disclosed for the sulfurization of a phosphorus containing compound, which comprises: solubilizing the phosphorous containing compound and then contacting the phosphorous containing compound, with a sulfur containing compound of the solution formula: ##STR1## wherein, B is selected from the group consisting of --CH.sub.2 --, --C(O)-- or --C(S)--;Q is a non-interfering moiety or radical; andm and n, same or different, are selected from the group consisting of zero or one.
摘要翻译：公开了一种含磷化合物硫化的方法，该方法包括：使含磷化合物溶解，然后使含磷化合物与含硫化合物的式I化合物反应：其中B选自由-CH 2 - ， - C（O） - 或-C（S） - 组成的基团; Q是非干扰部分或基团; 并且m和n相同或不同，选自零或一个。

5. 发明授权

US09284343B2 2′-O-aminooxymethyl nucleoside derivatives for use in the synthesis and modification of nucleosides, nucleotides and oligonucleotides 有权
标题翻译：用于核苷，核苷酸和寡核苷酸的合成和修饰的2'-O-氨氧基甲基核苷衍生物
公开(公告)号：US09284343B2
公开(公告)日：2016-03-15
申请号：US14008805
申请日：2012-03-29
申请人： Serge L. Beaucage , Jacek Cieslak
发明人： Serge L. Beaucage , Jacek Cieslak
IPC分类号： C07H21/00 , C07H19/16 , C07H19/00 , C07H19/06 , C07H23/00 , C07H1/00 , C07H19/048
CPC分类号： C07H19/16 , C07H1/00 , C07H19/048 , C07H19/06 , C07H23/00 , Y02P20/55
摘要： Disclosed are O-protected compounds of the formula (I): wherein B is an optionally protected nucleobase, and R1-R3 are as described herein, wherein at least one of R1-R3 is —CH2—O—N═CHR. The compounds are useful as intermediates in oligonucleotide synthesis. Also disclosed is a method of preparing the compounds from nucleosides via a process comprising conversion of a hydroxyl group to a methylthiomethoxy group, and a method of preparing oligonucleotides such as RNA starting from the compounds. The —CH2—O—N═CHR group is stable during oligonucleotide synthesis and can be easily removed after synthesis via, for example, treatment with a base.
摘要翻译：公开了式（I）的O-保护的化合物：其中B是任选保护的核碱基，并且R 1 -R 3如本文所述，其中R 1 -R 3中的至少一个是-CH 2 -O-N = CHR。该化合物可用作寡核苷酸合成中的中间体。还公开了通过包括将羟基转化为甲基硫代甲氧基的方法从核苷制备化合物的方法，以及从化合物开始制备寡核苷酸例如RNA的方法。 -CH 2 -O-N = CHR基团在寡核苷酸合成期间是稳定的，并且可以通过例如用碱处理在合成后容易地除去。

6. 发明授权

US06965041B1 N-acylphosphoramidites and their use in oligonucleotide synthesis 有权
标题翻译： N-酰基亚磷酰胺及其在寡核苷酸合成中的应用
公开(公告)号：US06965041B1
公开(公告)日：2005-11-15
申请号：US09937292
申请日：2000-02-16
申请人： Serge L. Beaucage , Andrzej Wilk , Andrzej Grajkowski
发明人： Serge L. Beaucage , Andrzej Wilk , Andrzej Grajkowski
IPC分类号： C07D407/12 , C07H19/10 , C07H19/20 , C07H21/00
CPC分类号： C07H21/00 , C07H19/10 , C07H19/20 , Y02P20/55
摘要： The present invention provides a compound of formula (I), (II), or (III), wherein R1, R2, R2′, R3, and R3′ are the same or different and each is H an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl, or an aralkyl. Alternatively, either of R2 or R2′ combined with either of R3 or R3′ comprises a ring. R4 is a protecting group or a solid support R5 is H or an alkyl. R6 is a protecting group, an amidoalkyl, an alkyl, an alkyl ketone, an alkenyl, an alkynyl, a cycloalkyl, an aryl, or an aralkyl. R15 is H or a protecting group. Q and Q1 are the same or different and each is a nucleoside, an oligonucleotide comprising a nucleoside, or an oligomer comprising a nucleoside, which is of formula (a) or (b), wherein B is a labeling group, an alkyl, an alkenyl, an alkynyl, a cyclic group optionally containing one or more heteroatoms, or an amino; and, E is H, a halogen, a hydroxy, an alkoxy, an ester, an amino or a protecting group. X and X1 are independently O, S, or Se, and n is an integer from 1 to about 300. Each Q in each monomeric unit defined by n can be the same or different. The present invention further provides a method of preparing a polymer using the N-acylphosphoramidite of formula (I) or (II).
摘要翻译：本发明提供式（I），（II）或（III）的化合物，其中R 1，R 2，R 2， R 3，R 3和R 3'相同或不同，并且各自为烷基，烯基，炔基，环烷基，芳基或芳烷基。或者，与R 3或R 3或R 3'中的任一个组合的R 2或R 2'2'中的任一个包括环。 R 4是保护基或固体载体R 5是H或烷基。 R 6是保护基，酰氨基烷基，烷基，烷基酮，烯基，炔基，环烷基，芳基或芳烷基。 R 15是H或保护基。 Q和Q 1相同或不同，并且各自为核苷，包含核苷的寡核苷酸或包含式（a）或（b）的核苷的寡聚体，其中B为标记基团，烷基，烯基，炔基，任选含有一个或多个杂原子的环状基团或氨基; 并且，E是H，卤素，羟基，烷氧基，酯，氨基或保护基。 X和X 1独立地为O，S或Se，n为1至约300的整数。由n定义的每个单体单元中的每个Q可以相同或不同。本发明还提供使用式（I）或（II）的N-酰基亚磷酰胺制备聚合物的方法。

7. 发明公开

US20230271998A1 SOLID SUPPORT FOR SYNTHESIZING NUCLEIC ACID SEQUENCES AND METHODS FOR MAKING AND USING 审中-公开
公开(公告)号：US20230271998A1
公开(公告)日：2023-08-31
申请号：US18003404
申请日：2021-06-28
申请人： Serge L. Beaucage , Andrzej M. Grajkowski
发明人： Serge L. Beaucage , Andrzej M. Grajkowski
IPC分类号： C07H21/04 , C40B50/18
CPC分类号： C07H21/04 , C40B50/18
摘要： Disclosed herein are embodiments of a solid support suitable for synthesizing nucleic acid sequences. The solid support may have a structure according to Formula I, where CPG is controlled pore glass, and m, n, x, y, R1 and R2 are as defined herein.

Also disclosed are methods for making and using the solid support, kits including solid support, and a universal linker phosphoramidite suitable for use in the solid support.

8. 发明授权

US06762298B2 Thermolabile phosphorus protecting groups, associated intermediates and methods of use 有权
标题翻译：耐热磷保护基，相关中间体和使用方法
公开(公告)号：US06762298B2
公开(公告)日：2004-07-13
申请号：US09792799
申请日：2001-02-23
申请人： Serge L. Beaucage , Andrzej Wilk , Andrzej Grajkowski
发明人： Serge L. Beaucage , Andrzej Wilk , Andrzej Grajkowski
IPC分类号： C07H2100
CPC分类号： C07H21/00 , C07H19/10 , C07H19/20 , Y02P20/55
摘要： The invention provides a method of thermally deprotecting the internucleosidic phosphorus linkage of an oligonucleotide, which method comprises heating a protected oligonucleotide in a fluid medium at a substantially neutral pH, so as to deprotect the oligonucleotide. The present invention further provides a method of synthesizing an oligonucleotide using the thermal deprotection method described above, and novel oligonucleotides and intermediates that incorporate the thermolabile protecting group used in accordance with the present invention.
摘要翻译：本发明提供了一种对寡核苷酸的核苷间磷键进行热脱保护的方法，该方法包括在基本上中性的pH下在流体介质中加热受保护的寡核苷酸，以使寡核苷酸脱保护。本发明还提供了一种合成使用上述热去保护方法的寡核苷酸，以及掺入根据本发明使用的耐热不稳定保护基的新型寡核苷酸和中间体。

9. 发明授权

US09809824B2 CpG oligonucleotide prodrugs, compositions thereof and associated therapeutic methods 有权
公开(公告)号：US09809824B2
公开(公告)日：2017-11-07
申请号：US11721409
申请日：2005-12-13
申请人： Daniela Verthelyi , Serge L. Beaucage , Andrzej Grajkowski
发明人： Daniela Verthelyi , Serge L. Beaucage , Andrzej Grajkowski
IPC分类号： C07H21/00 , C12N15/117
CPC分类号： C12N15/117 , C07H21/00 , C12N2310/17 , C12N2310/315 , C12N2310/351
摘要： The present invention provides a CpG oligonucleotide prodrug that includes a thermolabile substituent on at least one nucleotide thereof. The present invention also provides compositions that include a carrier and a therapeutically effective amount of at least one CpG oligonucleotide prodrug. The present invention further provides therapeutic methods of using such thermolabile CpG oligonucleotide prodrugs and compositions thereof. The present invention further provides a method of inhibiting tetrad formation in a CpG oligonucleotide by functionalizing the CpG oligonucleotide with one or more thermolabile substituents.

10. 发明申请

US20140051846A1 2'-O-AMINOOXYMETHYL NUCLEOSIDE DERIVATIVES FOR USE IN THE SYNTHESIS AND MODIFICATION OF NUCLEOSIDES, NUCLEOTIDES AND OLIGONUCLEOTIDES 有权
标题翻译：用于合成和修饰核苷酸，核苷酸和寡核苷酸的2'-O-氨基甲基甲基衍生物
公开(公告)号：US20140051846A1
公开(公告)日：2014-02-20
申请号：US14008805
申请日：2012-03-29
申请人： Serge L. Beaucage , Jacek Cieslak
发明人： Serge L. Beaucage , Jacek Cieslak
IPC分类号： C07H19/16 , C07H1/00 , C07H19/048
CPC分类号： C07H19/16 , C07H1/00 , C07H19/048 , C07H19/06 , C07H23/00 , Y02P20/55
摘要： Disclosed are O-protected compounds of the formula (I): wherein B is an optionally protected nucleobase, and R1-R3 are as described herein, a method of preparing such compounds, and a method of preparing oligonucleotides such as RNA starting from such compounds. The O-protected compounds have one or more advantages, for example, the 2′-O-protected compound is stable during the various reaction steps involved in oligonucleotide synthesis; the protecting group can be easily removed after the synthesis of the oligonucleotide, for example, by reaction with tetrabutylammonium fluoride; and/or the O-protected groups do not generate DNA/RNA alkylating side products, which have been reported during removal of 2′-O-(2-cyanoethyl)oxymethyl or 2′-O-[2-(4-tolylsulfonyl)ethoxymethyl groups under similar conditions.
摘要翻译：公开了式（I）的O-保护的化合物：其中B是任选保护的核碱基，并且R 1 -R 3如本文所述，制备此类化合物的方法，以及从这些化合物开始制备寡核苷酸例如RNA的方法。 O保护的化合物具有一个或多个优点，例如，2'-O-保护的化合物在涉及寡核苷酸合成的各种反应步骤期间是稳定的; 在寡核苷酸的合成之后，可以容易地除去保护基，例如通过与四丁基氟化铵反应; 和/或O-保护基团不产生DNA / RNA烷基化副产物，其在除去2'-O-（2-氰基乙基）氧基甲基或2'-O- [2-（4-甲苯磺酰基）乙氧基甲基。

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