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1. 发明专利

ZA201206925B MINOR GROOVE BINDER (MGB)-OLIGONUCLEOTIDE MIRNA ANTAGONISTS 未知
公开(公告)号：ZA201206925B
公开(公告)日：2013-06-26
申请号：ZA201206925
申请日：2012-09-14
申请人： ELITECH HOLDINGS B V , DHARMACON INC
发明人： KHVOROVA ANASTASIA , KAISER ROB , VERMEULEN NICOLAAS , VERMEULEN ANNALEEN , KARPILOW JON , MAHONEY WALT
IPC分类号： C12N20060101

2. 发明专利

ES2574625T3 Antagonistas de miARN de oligonucleótido conjugado con aglutinante del surco menor (MGB) 未知
公开(公告)号：ES2574625T3
公开(公告)日：2016-06-21
申请号：ES10788176
申请日：2010-11-23
申请人： ELITECHGROUP B V , DHARMACON INC
发明人： KHVOROVA ANASTASIA , VERMEULEN ANNALEEN , KAISER ROB , KARPILOW JON , VERMEULEN NICOLAAS , MAHONEY WALT
IPC分类号： C12N15/113
摘要： Una composición inhibidora para inhibir ARN no codificantes que comprende: un oligonucleótido; y un aglutinante del surco menor (MGB), en la que el oligonucleótido comprende nucleótidos, en la que todos los nucleótidos del oligonucleótido comprenden ribofuranosa que tiene la siguiente estructura:**Fórmula** en la que Rz es -OCH3, en la que B es una base normal o una base modificada; y en la que el MGB está conjugado con el extremo 5' o con el extremo 3' del oligonucleótido; y en la que el oligonucleótido es esencialmente complementario a una secuencia de miARN o ARNpi madura endógena.

3. 发明专利

CA2687336C MICRO-RNA SCAFFOLDS AND NON-NATURALLY OCCURRING MICRO-RNAS 未知
公开(公告)号：CA2687336C
公开(公告)日：2014-12-23
申请号：CA2687336
申请日：2008-05-22
申请人： DHARMACON INC
发明人： KELLEY MELISSA , BIRMINGHAM AMANDA , KARPILOW JON , KHVOROVA ANASTASIA , SULLIVAN KEVIN
IPC分类号： C12N15/113 , A61K31/7105 , A61K48/00 , C07H21/02 , C12N5/10 , C12N15/63 , C12Q1/68
摘要： The present disclosure provides a non-naturally occurring miRNA having a stem-loop structure comprising a scaffold derived from a first endogenous miRNA (e.g., miR-196a-2 or miR-204), a mature strand derived from a second endogenous miRNA, and a star strand sequence that is at least partially complementary to the mature strand sequence. The present disclosure also provides a non-naturally occurring miRNA having a stem-loop structure comprising a scaffold derived from an endogenous miRNA (e.g., miR-196a-2 or miR-204), a mature strand designed t be at least partially complementary to a target RNA, and a star strand sequence that is at least partially complementary to the mature strand sequence. The methods and compositions of the disclosure may be used to mediate gene silencing via the RNAi pathway.

4. 发明专利

AU2008256886B2 Micro-RNA scaffolds and non-naturally occurring micro-RNAs 未知
公开(公告)号：AU2008256886B2
公开(公告)日：2013-02-28
申请号：AU2008256886
申请日：2008-05-22
申请人： DHARMACON INC
发明人： BIRMINGHAM AMANDA , KHVOROVA ANASTASIA , SULLIVAN KEVIN , KARPILOW JON , KELLEY MELISSA
IPC分类号： C12Q1/68
摘要： The present disclosure provides a non-naturally occurring miRNA having a stem-loop structure comprising a scaffold derived from a first endogenous miRNA (e.g., miR-196a-2 or miR-204), a mature strand derived from a second endogenous miRNA, and a star strand sequence that is at least partially complementary to the mature strand sequence. The present disclosure also provides a non-naturally occurring miRNA having a stem-loop structure comprising a scaffold derived from an endogenous miRNA (e.g., miR-196a-2 or miR-204), a mature strand designed t be at least partially complementary to a target RNA, and a star strand sequence that is at least partially complementary to the mature strand sequence. The methods and compositions of the disclosure may be used to mediate gene silencing via the RNAi pathway.

5. 发明专利

CA2687336A1 MICRO-RNA SCAFFOLDS AND NON-NATURALLY OCCURRING MICRO-RNAS 未知
公开(公告)号：CA2687336A1
公开(公告)日：2008-12-04
申请号：CA2687336
申请日：2008-05-22
申请人： DHARMACON INC
发明人： KARPILOW JON , KHVOROVA ANASTASIA , SULLIVAN KEVIN , BIRMINGHAM AMANDA , KELLEY MELISSA
IPC分类号： C12Q1/68
摘要： The present disclosure provides a non-naturally occurring miRNA having a stem-loop structure comprising a scaffold derived from a first endogenous mi RNA (e.g., miR-196a-2 or miR-204), a mature strand derived from a second end ogenous miRNA, and a star strand sequence that is at least partially complem entary to the mature strand sequence. The present disclosure also provides a non-naturally occurring miRNA having a stem-loop structure comprising a sca ffold derived from an endogenous miRNA (e.g., miR-196a-2 or miR-204), a matu re strand designed t be at least partially complementary to a target RNA, an d a star strand sequence that is at least partially complementary to the mat ure strand sequence. The methods and compositions of the disclosure may be u sed to mediate gene silencing via the RNAi pathway.

6. 发明专利

AU2008256886A1 Micro-RNA scaffolds and non-naturally occurring micro-RNAs 未知
公开(公告)号：AU2008256886A1
公开(公告)日：2008-12-04
申请号：AU2008256886
申请日：2008-05-22
申请人： DHARMACON INC
发明人： BIRMINGHAM AMANDA , KHVOROVA ANASTASIA , KARPILOW JON , KELLEY MELISSA , SULLIVAN KEVIN
IPC分类号： C12Q1/68

7. 发明专利

AU2010324860A1 Minor groove binder (MGB)-oligonucleotide miRNAs antagonists 未知
公开(公告)号：AU2010324860A1
公开(公告)日：2012-06-14
申请号：AU2010324860
申请日：2010-11-23
申请人： DHARMACON INC , ELITECH HOLDING BV
发明人： KHVOROVA ANASTASIA , VERMEULEN ANNALEEN , KAISER ROB , KARPILOW JON , VERMEULEN NICOLAAS , MAHONEY WALT
IPC分类号： C12N15/113
摘要： Compositions and methods for inhibiting the actions of non- coding RNAs such as miRNAs are provided. The compositions comprise single or double stranded oligonucleotides conjugated with Minor Groove Binders ("MGBs"). The oligonucleotides can vary in length, can contain nucleotides having one or more modifications, and have regions that are substantially complementary to one or more mature miRNAs or piRNAs.

8. 发明专利

CA2781618A1 MINOR GROOVE BINDER (MGB)-OLIGONUCLEOTIDE MIRNA ANTAGONISTS 未知
公开(公告)号：CA2781618A1
公开(公告)日：2011-06-03
申请号：CA2781618
申请日：2010-11-23
申请人： ELITECH HOLDING BV , DHARMACON INC
发明人： KHVOROVA ANASTASIA , VERMEULEN ANNALEEN , KAISER ROB , KARPILOW JON , VERMEULEN NICOLAAS , MAHONEY WALT
IPC分类号： C12N15/113
摘要： Compositions and methods for inhibiting the actions of non- coding RNAs such as miRNAs are provided. The compositions comprise single or double stranded oligonucleotides conjugated with Minor Groove Binders ("MGBs"). The oligonucleotides can vary in length, can contain nucleotides having one or more modifications, and have regions that are substantially complementary to one or more mature miRNAs or piRNAs.

9. 发明申请

WO2007095387A3 COMPOSITIONS AND METHODS FOR INHIBITING GENE SILENCING BY RNA INTERFERENCE 审中-公开
标题翻译：通过RNA干扰抑制基因沉默的组合物和方法
公开(公告)号：WO2007095387A3
公开(公告)日：2008-11-27
申请号：PCT/US2007004223
申请日：2007-02-16
申请人： DHARMACON INC , VERMEULEN ANNALEEN , ROBERTSON BARBARA , BASKERVILLE SCOTT , YAMADA CHRISTINA , LEAKE DEVIN , FEDOROV YURIY , KARPILOW JON , KHVOROVA ANASTASIA
发明人： VERMEULEN ANNALEEN , ROBERTSON BARBARA , BASKERVILLE SCOTT , YAMADA CHRISTINA , LEAKE DEVIN , FEDOROV YURIY , KARPILOW JON , KHVOROVA ANASTASIA
IPC分类号： C07H21/02 , A01N43/04 , A61K31/70 , C07H21/04
CPC分类号： C12N15/111 , C12N15/113 , C12N2310/11 , C12N2310/321 , C12N2310/3515 , C12N2310/53 , C12N2320/50 , C12N2310/3521
摘要： The present invention provides compositions and methods for inhibiting gene silencing by the RNAi pathway. The RNAi inhibitors of the invention have a reverse complement (RC) region to the target molecule of interest (e.g., miRNA) in association with at least one flanking region coupled to either at the 3' or 5' end of the RC region. The flanking regions can be single-stranded or can have one or more regions of double stranded nucleic acid with or without a hairpin loop. The RNAi inhibitors described herein can inhibit endogenous targets, including but not limited to microRNAs, or piRNAs, or can be used to inhibit the effects of exogenously introduced molecules, such as synthetic siRNAs, siRNAs expressed from vector constructs (e.g., viral expression systems), or siRNAs generated by enzymatic methods. Inhibition is specific, potent, prolonged, and can be performed on a single target or multiple targets simultaneously.
摘要翻译：本发明提供了通过RNAi途径抑制基因沉默的组合物和方法。本发明的RNAi抑制剂与至少一个与RC区3'端或5'末端连接的侧翼区相关联，具有与目的靶分子（例如miRNA）的反向互补序列（RC）区。侧翼区可以是单链的，或者可以具有一个或多个具有或不具有发夹环的双链核酸区域。本文所述的RNAi抑制剂可抑制内源性靶标，包括但不限于微小RNA或piRNA，或可用于抑制外源引入分子（如合成siRNAs），由载体构建体表达的siRNA（例如病毒表达系统），或通过酶法产生的siRNA。抑制是具体的，有效的，延长的，并且可以同时在单个目标或多个靶上进行。

10. 发明申请

WO2005090606A2 IDENTIFICATION OF TOXIC NUCLEOTIDE SEQUENCES 审中-公开
标题翻译：鉴定毒素核苷酸序列
公开(公告)号：WO2005090606A2
公开(公告)日：2005-09-29
申请号：PCT/US2005003131
申请日：2005-01-21
申请人： DHARMACON INC
发明人： FEDOROV YURIY , KARPILOW JON , KHVOROVA ANASTASIA
IPC分类号： C07H21/02 , C07H21/04 , C12N15/11 , C12Q1/68 , G01N33/48 , G01N33/50 , G06F19/00
CPC分类号： C12Q1/6883 , C12N15/111 , C12N2310/14 , C12N2310/53 , C12N2320/10 , C12Q2600/142
摘要： Toxic nucleic acid sequences and methods for identifying, using, and screening libraries for them, including in silico screening, are provided. Compositions of the invention comprise unimolecular and double stranded polynucleotides comprising at least one toxicity region. Toxic sequences of the invention include A/G UUU A/G/U, G/C AAA G/C, and/or GCCA, NUUU, wherein N is any nucleotide, or complements thereof. The invention also provides a method of inducing a toxic response in a cell, comprising introducing into the cell a unimolecular or double stranded polynucleotide comprising at least one toxicity region comprising a sequence selected from the group consisting of A/G UUU A/G/U, G/C AAA G/C, GAAT, and GCCA, NUUU, wherein N is any nucleotide, or a complement of any of the foregoing, wherein said unimolecular or double stranded polynucleotide is at least 5 base pairs long and is comprises a sense and antisense region that are at least substantially complementary.
摘要翻译：提供了有毒的核酸序列和用于识别，使用和筛选其文库的方法，包括计算机筛选。本发明的组合物包含包含至少一个毒性区域的单分子和双链多核苷酸。本发明的毒性序列包括A / G UUU A / G / U，G / C AAA G / C和/或GCCA，NUUU，其中N是任何核苷酸或其互补序列。本发明还提供了在细胞中诱导毒性反应的方法，包括向细胞中引入单分子或双链多核苷酸，所述单分子或双链多核苷酸包含至少一个毒性区，其包含选自A / G UUU A / G / U ，G / C AAA G / C，GAAT和GCCA，NUUU，其中N是任何前述的任何核苷酸或补体，其中所述单分子或双链多核苷酸长至少5个碱基对，并且包含感觉和至少基本上互补的反义区。

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