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1. 发明授权

US09605019B2 Methods for the synthesis of functionalized nucleic acids 有权
公开(公告)号：US09605019B2
公开(公告)日：2017-03-28
申请号：US14233579
申请日：2012-07-13
申请人： Gregory L. Verdine , Meena , Naoki Iwamoto , David Charles Donnell Butler
发明人： Gregory L. Verdine , Meena , Naoki Iwamoto , David Charles Donnell Butler
IPC分类号： C07H21/02 , C07H21/04 , C07H21/00 , C07H11/00 , C07H13/12 , C07D265/30 , C07D295/00 , C07C69/96 , C07C315/00 , C07C317/00 , C07C331/00 , C07C381/00 , A61K31/66 , A61K31/70 , C07C309/66 , C07D295/108 , C07H13/04
CPC分类号： C07H21/04 , A61K31/66 , A61K31/70 , C07C309/66 , C07D295/108 , C07H13/04
摘要： The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ic with a silylating reagent to provide a silyloxyphosphonate, reacting the silyloxyphosphonate with a bis(thiosulfonate) reagent of structure IVc to provide a phosphorothiotriester comprising a thiosulfonate group of structure Vc, and then reacting the phosphorothiotriester comprising a thiosulfonate group of structure Vc with a nucleophile of structure VIc to provide an oligonucleotide of structure IIIc.

2. 发明申请

US20180216108A1 OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF 审中-公开
公开(公告)号：US20180216108A1
公开(公告)日：2018-08-02
申请号：US15746220
申请日：2016-07-22
申请人： Chandra Vargeese , Meena , Nenad Svrzikapa , Susovan Mohapatra , Christopher J. Francis , Gregory L. Verdine , Anna Sokolovska
发明人： Chandra Vargeese , Meena , Nenad Svrzikapa , Susovan Mohapatra , Christopher J. Francis , Gregory L. Verdine , Anna Sokolovska
IPC分类号： C12N15/113 , A61P25/28
摘要： Among other things, the present disclosure relates to chirally controlled oligonucleotides of select designs, chirally controlled oligonucleotide compositions, and methods of making and using the same. In some embodiments, a provided chirally controlled oligonucleotide composition provides different cleavage patterns of a nucleic acid polymer than a reference oligonucleotide composition. In some embodiments, a provided chirally controlled oligonucleotide composition provides single site cleavage within a complementary sequence of a nucleic acid polymer. In some embodiments, a chirally controlled oligonucleotide composition has any sequence of bases, and/or pattern or base modifications, sugar modifications, backbone modifications and/or stereochemistry, or combination of these elements, described herein.

3. 发明授权

US08017762B2 Modified iRNA agents 有权
标题翻译：修饰的iRNA试剂
公开(公告)号：US08017762B2
公开(公告)日：2011-09-13
申请号：US12510050
申请日：2009-07-27
申请人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Meena
发明人： Muthiah Manoharan , Kallanthottathil G. Rajeev , Meena
IPC分类号： C07H21/04 , A61K31/70
CPC分类号： C07H21/02
摘要： The invention relates to iRNA agents, which preferably include a monomer in which the ribose moiety has been replaced by a moiety other than ribose that further includes a tether having one or more linking groups, in which at least one of the linking groups is a cleavable linking group. The tether in turn can be connected to a selected moiety, e.g., a ligand, e.g., a targeting or delivery moiety, or a moiety which alters a physical property. The cleavable linking group is one which is sufficiently stable outside the cell such that it allows targeting of a therapeutically beneficial amount of an iRNA agent (e.g., a single stranded or double stranded iRNA agent), coupled by way of the cleavable linking group to a targeting agent—to targets cells, but which upon entry into a target cell is cleaved to release the iRNA agent from the targeting agent.The inclusion of such a monomer can allow for modulation of a property of the iRNA agent into which it is incorporated, e.g., by using the non-ribose moiety as a point to which a ligand or other entity, e.g., a lipophilic moiety. e.g., cholesterol, is directly, or indirectly, tethered. The invention also relates to methods of making and using such modified iRNA agents.
摘要翻译：本发明涉及iRNA试剂，其优选包括其中核糖部分已被核糖替代的单体，其进一步包括具有一个或多个连接基团的系链，其中至少一个连接基团是可切割的连接组。系链又可以连接到所选择的部分，例如配体，例如靶向或递送部分，或改变物理性质的部分。可切割连接基团是在细胞外部足够稳定的连接基团，使得其允许靶向治疗有益量的iRNA试剂（例如，单链或双链iRNA试剂），其通过可切割连接基团连接至靶向细胞靶向细胞，但是在进入靶细胞时被切割以从靶向剂释放iRNA试剂。包含这样的单体可以允许调节掺入其中的iRNA试剂的性质，例如通过使用非核糖部分作为配体或其它实体例如亲油部分的点。例如胆固醇是直接或间接的系链。本发明还涉及制备和使用这种修饰的iRNA试剂的方法。

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