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1. 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.

2. 发明申请

US20090263405A1 CpG OLIGONUCLEOTIDE PRODRUGS, COMPOSITIONS THEREOF AND ASSOCIATED THERAPEUTIC METHODS 有权
标题翻译： CpG寡核苷酸产物，其组合物及相关治疗方法
公开(公告)号：US20090263405A1
公开(公告)日：2009-10-22
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： A61K39/00 , A61K31/7088 , C07H21/00
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.
摘要翻译：本发明提供了CpG寡核苷酸前药，其在其至少一个核苷酸上包含热不稳定取代基。本发明还提供了包含载体和治疗有效量的至少一种CpG寡核苷酸前药的组合物。本发明进一步提供了使用这种耐热不稳定CpG寡核苷酸前药及其组合物的治疗方法。本发明还提供了通过用一个或多个不耐热取代基官能化CpG寡核苷酸来抑制CpG寡核苷酸中的四聚体形成的方法。

3. 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。

4. 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。

5. 发明授权

US07355037B2 Thermolabile hydroxyl protecting groups and methods of use 有权
标题翻译：耐热不饱和羟基保护基和使用方法
公开(公告)号：US07355037B2
公开(公告)日：2008-04-08
申请号：US10497416
申请日：2002-12-03
申请人： Serge L. Beaucage , Andrzej Grajkowski , Andrzej Wilk
发明人： Serge L. Beaucage , Andrzej Grajkowski , Andrzej Wilk
IPC分类号： C07H21/00
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： Provided is a hydroxyl-protected alcohol of the formula R—O—Pg, wherein Pg is a protecting group of the formula: wherein Y, Z, W, R1, R1a, R2, R2a, R3, R3a, R4, R4a, a, b, c, d, e and f are defined herein and R is a nucleosidyl group, an oligonucleotidyl group with 2 to about 300 nucleosides, or an oligomer with 2 to about 300 nucleosides. Also provided is a deprotection method, which includes heating the hydroxyl-protected alcohol at a temperature effective to cleave thermally the hydroxyl-protecting group therefrom.
摘要翻译：提供式RO-Pg的羟基保护的醇，其中Pg是下式的保护基：其中Y，Z，W，R 1，R 1a， R 2，R 2，R 3，R 3，R 4，R 4， R 4a，a，b，c，d，e和f如本文所定义，R为核苷基，具有2至约300个核苷的寡聚核苷酸或具有2至约300个核苷还提供了脱保护方法，其包括在有效地将羟基保护基从其上裂解的温度下加热羟基保护的醇。

6. 发明授权

US5512668A Solid phase oligonucleotide synthesis using phospholane intermediates 失效
标题翻译：使用磷脂中间体的固相寡核苷酸合成
公开(公告)号：US5512668A
公开(公告)日：1996-04-30
申请号：US826929
申请日：1992-01-23
申请人： Wojciech J. Stec , Andrzej Grajkowski , Bogdan Uznanski
发明人： Wojciech J. Stec , Andrzej Grajkowski , Bogdan Uznanski
IPC分类号： C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/04 , C07H21/02
CPC分类号： C07H21/00 , C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20
摘要： Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O- 1,3,2-dichalcogen-substituted-phospholane! synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O- 1,3,2-dichalcogen-substituted-phospholane! synthons, and P-chiral oligonucleotides and related P-chiral polymers.
摘要翻译：提供方法和化合物用于通过在催化碱存在下缩合受保护的单体-O- [1,3,2-二硫化物取代的 - 磷脂]合成子来固相合成寡核苷酸和相关聚合物。本发明的化合物包括上述合成子的2-N-取代-1,3,2-二硫代磷酸酯前体，被保护的单体-O- [1,3,2-二硫代碳原子取代的 - 磷脂]合成子，和 P-手性寡核苷酸和相关的P-手性聚合物。

7. 发明授权

US5646267A Method of making oligonucleotides and oligonucleotide analogs using phospholanes and enantiomerically resolved phospholane analogues 失效
标题翻译：使用磷脂和对映体解析的磷脂类似物制备寡核苷酸和寡核苷酸类似物的方法
公开(公告)号：US5646267A
公开(公告)日：1997-07-08
申请号：US462418
申请日：1995-06-05
申请人： Wojciech J. Stec , Andrzej Grajkowski , Bogdan Uznanski
发明人： Wojciech J. Stec , Andrzej Grajkowski , Bogdan Uznanski
IPC分类号： C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H21/00 , C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20
摘要： Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons, and P-chiral oligonucleotides and related P-chiral polymers.
摘要翻译：提供方法和化合物用于通过在催化碱存在下缩合受保护的单体-O- [1,3,2-二硫化物取代的 - 磷脂]合成子来固相合成寡核苷酸和相关聚合物。本发明的化合物包括上述合成子的2-N-取代-1,3,2-二硫代磷酸酯前体，被保护的单体-O- [1,3,2-二硫代碳原子取代的 - 磷脂]合成子，和 P-手性寡核苷酸和相关的P-手性聚合物。

8. 发明申请

US20050020827A1 Thermolabile hydroxyl protecting groups and methods of use 有权
标题翻译：耐热不饱和羟基保护基和使用方法
公开(公告)号：US20050020827A1
公开(公告)日：2005-01-27
申请号：US10497416
申请日：2002-12-03
申请人： Serge Beaucage , Andrzej Grajkowski , Andrzej Wilk
发明人： Serge Beaucage , Andrzej Grajkowski , Andrzej Wilk
IPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C08B37/00 , C07C69/88
CPC分类号： C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , Y02P20/55
摘要： Provided are a hydroxyl-protected alcohol of the formula R—O-Pg, wherein Pg is a protecting group of the Formulae (I), (II), wherein Y is R1, OR1, or NR1R1a; Z is O, NR2 or CR2R2a; W is CO or SO; R1, R1a, R2, R2a, R3, R3a, R4 and R4a include H, a saturated or unsaturated alkyl, an aryl, and a saturated or unsaturated alkyl comprising an aryl; a, b, c, d, e and f include H, a halogen, a saturated or unsaturated alkyl, a hydroxyl, an alkoxy, an aryloxy, an aralkoxy, a cyano, a nitro, a sulfhydryl, an alkyl or aryl sulfoxy, are alkyl or aryl sulfonyl, a keto, a thioketo, an ester, an amide, an amino, an alkylamino or a dialkylamino; and R represents the organic residue of the hydroxyl-protected alcohol; a hydroxyl-protected alcohol which includes a thermally cleavable 2-amidoethoxycarbonyl hydroxyl-protecting group; and a deprotection method, which includes heating the hydroxyl-protected alcohol at a temperature effective to cleave thermally the hydroxyl-protecting group therefrom.
摘要翻译：提供式RO-Pg的羟基保护的醇，其中Pg是式（I），（II）的保护基，其中Y是R 1，OR 1或NR 1 R <1a>; Z是O，NR 2或CR 2 R 2a; W是CO或SO; R 1，R 1a，R 2，R 2a，R 3，R 3a，R 4和R 4a包括H，饱和或不饱和的烷基，芳基和包含芳基的饱和或不饱和烷基; a，b，c，d，e和f包括H，卤素，饱和或不饱和的烷基，羟基，烷氧基，芳氧基，芳烷氧基，氰基，硝基，巯基，烷基或芳氧基，烷基或芳基磺酰基，酮基，硫代酮，酯，酰胺，氨基，烷基氨基或二烷基氨基; R表示羟基保护的醇的有机残基; 羟基保护的醇，其包括可热切割的2-酰氨基乙氧基羰基羟基保护基; 和脱保护方法，其包括在有效地将羟基保护基从其上裂解的温度下加热羟基保护的醇。

9. 发明授权

US5883237A Oligonucleotides having R.sub.p and S.sub.p linkages at predetermined locations 失效
标题翻译：在预定位置具有Rp和Sp键的寡核苷酸
公开(公告)号：US5883237A
公开(公告)日：1999-03-16
申请号：US108878
申请日：1993-08-18
申请人： Wojciech J. Stec , Andrzej Grajkowski , Bogdan Uznanski
发明人： Wojciech J. Stec , Andrzej Grajkowski , Bogdan Uznanski
IPC分类号： C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C07H21/00 , C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20
摘要： Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O-�1,3,2-dichalcogen-substituted-phospholane! synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O-�1,3,2-dichalcogen-substituted-phospholane! synthons, and P-chiral oligonucleotides and related P-chiral polymers.
摘要翻译：提供方法和化合物用于通过在催化碱存在下缩合受保护的单体-O- [1,3,2-二硫化物取代的 - 磷脂]合成子来固相合成寡核苷酸和相关聚合物。本发明的化合物包括上述合成子的2-N-取代-1,3,2-二硫代磷酸酯前体，被保护的单体-O- [1,3,2-二硫代碳原子取代的 - 磷脂]合成子，和 P-手性寡核苷酸和相关的P-手性聚合物。

10. 发明授权

US5359052A Chalcophospholanes useful in the synthesis of oligonucleoside phosphorothioates, phosphorodithioates and related selenates 失效
标题翻译：可用于合成寡核苷酸硫代磷酸酯，二硫代磷酸酯和相关硒酸盐的茶聚糖
公开(公告)号：US5359052A
公开(公告)日：1994-10-25
申请号：US883622
申请日：1992-05-12
申请人： Wojciech J. Stee , Andrzej Grajkowski , Bogdan Uznanski
发明人： Wojciech J. Stee , Andrzej Grajkowski , Bogdan Uznanski
IPC分类号： C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20 , C07H21/00
CPC分类号： C07H21/00 , C07F9/6564 , C07F9/6578 , C07H19/10 , C07H19/20
摘要： Methods and compounds are provided for solid phase synthesis of oligonucleotides and related polymers by condensing protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons in the presence of a catalytic base. Compounds of the invention include 2-N-substituted-1,3,2-dichalcogen-substituted-phospholane precursors of the above synthons, the protected monomer-O-[1,3,2-dichalcogen-substituted-phospholane] synthons, and P-chiral oligonucleotides and related P-chiral polymers.
摘要翻译：提供方法和化合物用于通过在催化碱存在下缩合受保护的单体-O- [1,3,2-二硫化物取代的 - 磷脂]合成子来固相合成寡核苷酸和相关聚合物。本发明的化合物包括上述合成子的2-N-取代-1,3,2-二硫代磷酸酯前体，被保护的单体-O- [1,3,2-二硫代碳原子取代的 - 磷脂]合成子，和 P-手性寡核苷酸和相关的P-手性聚合物。

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