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11. 发明公开

KR1020050083891A 신규 2', 5'-올리고아데닐산 유사체 失效
标题翻译： 2'，5'-寡氨酸类似物
公开(公告)号：KR1020050083891A
公开(公告)日：2005-08-26
申请号：KR1020057009011
申请日：2003-11-19
申请人： 상꾜 가부시키가이샤
发明人： 고이즈미마코토 , 모리타고지
IPC分类号： C07H21/00 , C07H21/02
CPC分类号： C12N15/113 , C07H21/00 , C12N2310/11 , C12N2310/315 , C12N2310/319 , C12N2310/321 , C12N2310/3231 , C12N2310/3515 , Y02P20/55 , C12N2310/3521 , C07H21/02
摘要： 2-5A Analogues represented by the general formula (1) and pharmacologically acceptable salts thereof: (1) wherein m is 0 or 1; n is 0 to 2; R1 is optionally substituted C1-6 alkoxy, mercapto, mercapto blocked with a protecting group for synthesis of nucleic acid, or optionally substituted C1-4 alkylthio; R2, R3, R4, R5 and R6 are each hydroxyl, hydroxyl blocked with a protecting group for synthesis of nucleic acid, optionally substituted C1-6 alkoxy, mercapto, mercapto blocked with a protecting group for synthesis of nucleic acid, or optionally substituted C1-4 alkylthio; R7 is oxygen or -O(CH2CH2O)q- (wherein q is 2 to 6); R 8 is hydrogen, optionally substituted C1-6 alkyl, or a 5'-phosphorylated oligonucleotide analogue lacking one hydroxyl group on the 5'-phosphate group; and E1, E 2, E3 and E4 are each a natural or modified nucleic acid unit.
摘要翻译： 2-5A由通式（1）表示的类似物及其药理学上可接受的盐：（1）其中m为0或1; n为0〜2; R1是任选被取代的C 1-6烷氧基，巯基，用用于合成核酸的保护基封端的巯基，或任选取代的C 1-4烷硫基; R 2，R 3，R 4，R 5和R 6各自为羟基，用用于合成核酸的保护基封闭羟基，任选取代的C 1-6烷氧基，巯基，用用于合成核酸的保护基封端的巯基或任选取代的C 1 -4-烷硫基; R7是氧或-O（CH2CH2O）q-（其中q是2-6）; R 8为氢，任意取代的C 1-6烷基或5'-磷酸基上缺少一个羟基的5'-磷酸化寡核苷酸类似物; E1，E2，E3和E4各自为天然或修饰的核酸单元。

12. 发明公开

KR1020020013519A 보편적 및/또는 축퇴성 염기를 포함하는 안티센스올리고뉴클레오티드 无效
标题翻译：包含通用和/或简并碱基的反义寡核苷酸
公开(公告)号：KR1020020013519A
公开(公告)日：2002-02-20
申请号：KR1020017012777
申请日：2000-04-07
申请人： 오아시스 바이오사이언시즈 인코포레이티드
发明人： 브라운,밥,디. , 릴리티모씨,에이.
IPC分类号： C07H21/04
CPC分类号： C12N15/113 , A61K38/00 , C12N15/1135 , C12N15/1137 , C12N2310/18 , C12N2310/31 , C12N2310/319 , C12N2310/331 , C12N2310/345 , C12Y207/11013
摘要： 하나이상의축퇴성및/또는보편적염기및 하나이상의변형된백본링키지를포함하는안티센스올리고뉴클레오티드및 표적 RNA 분자절단에의그 이용.

13. 发明公开

KR1020170007492A 장기에서의 허혈 재관류 손상 방지 방법 및 방지용 조성물 审中-实审
标题翻译：用于预防器官缺血再灌注损伤的方法和组合物
公开(公告)号：KR1020170007492A
公开(公告)日：2017-01-18
申请号：KR1020167037012
申请日：2015-05-27
申请人： 쿠아크 파마수티칼스 인코퍼레이티드
发明人： 엘리자베스씨스퀴어스 , 샤이엘리히 , 다니엘로덴스타인 , 니르샤론 , 다니엘제이오덴하이머 , 엘레나파인스타인
IPC分类号： A61K48/00 , A61K31/712 , A61K39/395 , A61K31/436 , C12N15/113
CPC分类号： C12N15/1135 , A61K9/0019 , A61K31/713 , A61K45/06 , C12N2310/14 , C12N2310/317 , C12N2310/319 , C12N2310/321 , C12N2310/3515 , C12N2320/30 , C12N2310/3521
摘要： 본발명은, 일부구체예들에서, 장기에서의허혈재관류손상 (IRI) 방지, 특히 35세및 그이상의연령의장기에서의 IRI 방지를위한화합물및 방법에관한것이다. 구체적인용도들에는 35세및 그이상의연령의공여자장기의재이식및 이식에있어서본래의장기에서의 IRI 방지가포함된다. 추가구체예들에는사망공여자신장이식의수혜자에서의지연성이식신기능 (DGF)의예방및 투석빈도, 투석양및 투석기간의감소가포함된다. 상기방법들은장기를또는에서한시적 p53 억제제와접촉시키는것을수반한다. 신규한한시적 dsNA p53 억제제들또한제공된다.
摘要翻译：在一些实施方案中，本发明涉及用于预防器官中的局部缺血再灌注损伤（IRI）的化合物和方法，尤其涉及35岁及以上器官中IRI的化合物和方法。具体用途包括在体内天然器官中预防IRI，在35岁及以上的供体器官的再植入和移植中。另外的实施方案包括预防延迟移植物功能（DGF）以及减少受试者接受者死亡供体肾移植的频率，数量和持续时间。该方法需要使体内或离体的器官与临时p53抑制剂接触。还提供了新的临时dsNA p53抑制剂。

14. 发明公开

EP3149172A1 METHODS AND COMPOSITIONS FOR PREVENTING ISCHEMIA REPERFUSION INJURY IN ORGANS 有权
标题翻译： VERFAHREN UND ZUSAMMENSETZUNGEN ZUR PRENVENTION VONISCHÄMISCHENREPERFUSIONSSCHÄDENIN ORGANEN
公开(公告)号：EP3149172A1
公开(公告)日：2017-04-05
申请号：EP15729289.7
申请日：2015-05-27
申请人： Quark Pharmaceuticals, Inc.
发明人： SQUIERS, Elizabeth C. , ERLICH, Shai , ROTHENSTEIN, Daniel , SHARON, Nir , ODENHEIMER, Daniel J. , FEINSTEIN, Elena
IPC分类号： C12N15/113 , A61K31/712
CPC分类号： C12N15/1135 , A61K9/0019 , A61K31/713 , A61K45/06 , C12N2310/14 , C12N2310/317 , C12N2310/319 , C12N2310/321 , C12N2310/3515 , C12N2320/30 , C12N2310/3521
摘要： The invention, in some embodiments, relates to compounds and methods for the prevention of ischemia reperfusion injury (IRI) in organs, and in particular to IRI in organs aged 35 years and older. Specific uses include prevention of IRI in native organs in vivo, in reimplantations and in transplantations of donor organs aged 35 years and older. Additional embodiments include the prophylaxis of delayed graft function (DGF) and reduction in the frequency, amount and duration of dialysis in recipients of deceased donor kidney transplantations. The methods entail contacting the organ in vivo or ex vivo with a temporary p53 inhibitor. Novel temporary dsNA p53 inhibitors are further provided.
摘要翻译：在一些实施方案中，本发明涉及用于预防器官中的局部缺血再灌注损伤（IRI）的化合物和方法，特别是涉及年龄在35岁及以上的器官中的IRI的化合物和方法。具体用途包括在体内天然器官中预防IRI，在35岁及以上的供体器官的再植入和移植中。另外的实施方案包括预防延迟移植物功能（DGF）以及减少受试者在接受死亡供体肾移植的频率，数量和持续时间。该方法需要使体内或离体的器官与临时p53抑制剂接触。还提供了新的临时dsNA p53抑制剂。

15. 发明公开

EP2958998A4 SHORT INTERFERING NUCLEIC ACID (siNA) MOLECULES CONTAINING A 2' INTERNUCLEOSIDE LINKAGE 有权
标题翻译：具有'2核苷酸连接的新生分子
公开(公告)号：EP2958998A4
公开(公告)日：2016-07-13
申请号：EP14754069
申请日：2014-02-20
申请人： SIRNA THERAPEUTICS INC
发明人： CHANG WONSUK , GUIDRY ERIN N , STANTON MATTHEW G , ZEWGE DANIEL
IPC分类号： C12N15/11 , C07H21/00 , C07H21/02 , C07H21/04
CPC分类号： C12N15/113 , C07H19/10 , C07H21/00 , C07H21/02 , C07H21/04 , C12N15/111 , C12N2310/11 , C12N2310/14 , C12N2310/319
摘要： The present invention relates to RNAi molecules, and compositions thereof, comprising a 2′ internucleoside linkage connecting the nucleotide at position 1 and the nucleotide at position 2 at the 5′ end of the antisense strand. Specifically, the invention relates to single- and double-stranded short interfering nucleic acid (siNA) molecules that are capable of mediating RNA interference comprising 5′ modified nucleotides that comprise, among other potential modifications, a 2′ internucleoside linkage. The invention further relates to 5′ modified nucleotides used as reagents to generate the RNAi molecules of the invention and methods of using the disclosed RNAi molecules.

16. 发明公开

EP2195428A2 SiRNA SEQUENCE-INDEPENDENT MODIFICATION FORMATS FOR REDUCING OFF-TARGET PHENOTYPIC EFFECTS IN RNAi, AND STABILIZED FORMS THEREOF 有权
标题翻译：为了降低目标违规RNAi的表型效应的siRNA序列独立改性FORMATS及其的稳定形式
公开(公告)号：EP2195428A2
公开(公告)日：2010-06-16
申请号：EP08831316.8
申请日：2008-09-17
申请人： Applied Biosystems, LLC
发明人： PURI, Nitin , CHARLES, Irudaya , MAGDALENO, Susan , VLASSOV, Alexander , BURNETT, Chris
IPC分类号： C12N15/11
CPC分类号： C12N15/113 , C12N15/111 , C12N15/1137 , C12N15/1138 , C12N2310/14 , C12N2310/319 , C12N2310/321 , C12N2310/3231 , C12N2310/343 , C12N2320/53 , C12N2310/3521
摘要： Modification formats having modified nucleotides are provided for chemically synthesised RNA, in particular duplex RNA. RNA having modification formats and modified nucleotides provided herein reduce off-target effects in RNA interference of endogenous genes. Further modification formatted RNAs are demonstrated to be stabilized to nuclease-rich environments. Unexpectedly, increasing or maintaining strand bias, while necessary to maintain potency for endogenous RNA interference, is not sufficient for reducing off-target effects in cell biology assays.

17. 发明公开

EP2157182A2 Modified short interfering RNA 审中-公开
标题翻译： Modifizierte kurz干扰RNA
公开(公告)号：EP2157182A2
公开(公告)日：2010-02-24
申请号：EP09008116.7
申请日：2006-03-08
申请人： Qiagen GmbH
发明人： Pitsch, Stefan , Muller, Evelyne , Reymond, Luc , Andreou, Ionna
IPC分类号： C12N15/113 , C07H21/00 , C07H19/04
CPC分类号： C12N15/111 , C07H19/04 , C07H19/10 , C07H19/20 , C07H21/00 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/318 , C12N2310/319 , C12N2310/321 , C12N2310/322 , C12N2320/51 , C12Y207/11024 , C12N2310/3521 , C12N2310/3525
摘要： The present invention pertains to a double-stranded siRNA molecule comprising a nucleotide modified at the 2'-position by a -O-CH 2 -O-(CH 2 ) 2 -OH group and related technologies.
摘要翻译：本发明涉及包含通过-O-CH 2 -O-（CH 2）2 -OH基团在2位修饰的核苷酸的双链siRNA分子及相关技术。

18. 发明公开

EP2125852A1 5'-SUBSTITUTED-2'-F MODIFIED NUCLEOSIDES AND OLIGOMERIC COMPOUNDS PREPARED THEREFROM 有权
标题翻译： 5'-取代的2'-F修饰的核苷和由其制备的低聚化合物
公开(公告)号：EP2125852A1
公开(公告)日：2009-12-02
申请号：EP08729961.6
申请日：2008-02-15
申请人： Isis Pharmaceuticals, Inc.
发明人： MIGAWA, Michael, T. , SWAYZE, Eric, E. , BHAT, Balkrishen
IPC分类号： C07H19/06 , C07H19/16 , C07H21/00 , C12N15/11
CPC分类号： C07H19/06 , C07H19/16 , C07H21/00 , C12N15/111 , C12N15/1137 , C12N2310/11 , C12N2310/315 , C12N2310/319 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2320/51 , C12N2310/3525
摘要： The present invention provides 5'-substituted-2'-F nucleoside analogs and oligomeric compounds comprising these nucleoside analogs. In one preferred embodiment the nucleoside analogs have either (R) or (5)-chirality at the 5'-position. These nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance.

19. 发明授权

EP1252307B1 MODULATION OF OLIGONUCLEOTIDE CpG-MEDIATED IMMUNE STIMULATION BY POSITIONAL MODIFICATION OF NUCLEOSIDES 有权
标题翻译：调制所造成的免疫刺激的位置CpG寡核苷酸变更相关的核苷
公开(公告)号：EP1252307B1
公开(公告)日：2008-01-02
申请号：EP01903365.3
申请日：2001-01-26
申请人： Idera Pharmaceuticals, Inc.
发明人： AGRAWAL, Sudhir
IPC分类号： C12N15/11 , C07H21/00 , A61K31/7125
CPC分类号： C12N15/117 , A61K31/7125 , A61K2039/55561 , C12N2310/18 , C12N2310/31 , C12N2310/3125 , C12N2310/315 , C12N2310/319 , C12N2310/32
摘要： The invention provides methods for modulating the immune response caused by CpG-containing oligonucleotides. The methods according to the invention enable both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.

20. 发明授权

US09771583B2 siRNA sequence-independent modification formats for reducing off-target phenotypic effects in RNAI, and stabilized forms thereof 有权
公开(公告)号：US09771583B2
公开(公告)日：2017-09-26
申请号：US15015912
申请日：2016-02-04
申请人： APPLIED BIOSYSTEMS, LLC
发明人： Nitin Puri , Irudaya Charles , Susan Magdaleno , Alexander Vlassov , Christopher Burnett
IPC分类号： C12N15/113 , C12N15/11
CPC分类号： C12N15/113 , C12N15/111 , C12N15/1137 , C12N15/1138 , C12N2310/14 , C12N2310/319 , C12N2310/321 , C12N2310/3231 , C12N2310/343 , C12N2320/53 , C12N2310/3521
摘要： Modification formats having modified nucleotides are provided for siRNA. Short interfering RNA having modification formats and modified nucleotides provided herein reduce off-target effects in RNA interference of endogenous genes. Further modification formatted siRNAs are demonstrated to be stabilized to nuclease-rich environments. Unexpectedly, increasing or maintaining strand bias, while necessary to maintain potency for endogenous RNA interference, is not sufficient for reducing off-target effects in cell biology assays.

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