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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.

15. 发明申请

US20160076031A1 PHOSPHOROUS-LINKED OLIGOMERIC COMPOUNDS AND THEIR USE IN GENE MODULATION 有权
标题翻译：磷酸二酯化合物及其在基因调控中的应用
公开(公告)号：US20160076031A1
公开(公告)日：2016-03-17
申请号：US14834873
申请日：2015-08-25
申请人： Isis Pharmaceuticals, Inc.
发明人： Brenda F. Baker , Anne B. Eldrup , Muthiah Manoharan , Balkrishen Bhat , Richard H. Griffey , Eric E. Swayze , Thazha P. Prakash
IPC分类号： C12N15/113
CPC分类号： C12N15/111 , C12N2310/14 , C12N2310/315 , C12N2310/317 , C12N2310/319 , C12N2310/3341 , C12N2310/341 , C12N2310/342 , C12N2310/343 , C12N2310/346 , C12N2310/321 , C12N2310/3525 , C12N2310/3521
摘要： Oligonucleotide compositions comprising first and second oligonucleotides are provided wherein at least a portion of the first oligonucleotide is capable of hybridizing with at least a portion of the second oligonucleotide, at least a portion of the first oligonucleotide is complementary to and capable of hybridizing to a selected target nucleic acid, and at least one of the first or second oligonucleotides includes at least one nucleotide having a modified phosphorous-containing internucleoside linkage. Oligonucleotide/protein compositions are also provided comprising an oligonucleotide complementary to and capable of hybridizing to a selected target nucleic acid and at least one protein comprising at least a portion of an RNA-induced silencing complex (RISC), wherein at least one nucleotide of the oligonucleotide has a modified phosphorous-containing internucleoside linkage.
摘要翻译：提供了包含第一和第二寡核苷酸的寡核苷酸组合物，其中至少一部分第一寡核苷酸能够与至少一部分第二寡核苷酸杂交，第一寡核苷酸的至少一部分与选定的靶核酸，并且第一或第二寡核苷酸中的至少一个包含至少一个具有修饰的含磷核苷间键的核苷酸。还提供了寡核苷酸/蛋白质组合物，其包含与选定的靶核酸互补并且能够与选定的靶核酸杂交的寡核苷酸和至少一种包含至少一部分RNA诱导的沉默复合物（RISC）的蛋白质，其中至少一个核苷酸寡核苷酸具有修饰的含磷核苷键。

16. 发明授权

US09284551B2 RNAi sequence-independent modification formats, and stabilized forms thereof 有权
标题翻译：与RNAi序列无关的修饰形式及其稳定形式
公开(公告)号：US09284551B2
公开(公告)日：2016-03-15
申请号：US13782441
申请日：2013-03-01
申请人： APPLIED BIOYSYSTEMS, LLC
发明人： Nitin Puri , Irudaya Charles , Susan Magdaleno , Alexander Vlassov , Chris Burnett
IPC分类号： C07H21/02 , C07H21/04 , A61K31/70 , C12N15/113 , C12N15/11 , C12Q1/68
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.
摘要翻译：提供了具有修饰的核苷酸的修饰形式用于siRNA。具有修饰形式的短干扰RNA和本文提供的经修饰的核苷酸减少RNA干扰内源基因的脱靶效应。证明进一步修饰格式化的siRNA被稳定到富含核酸酶的环境中。意外的是，增加或维持链偏倚，同时必需保持内源性RNA干扰的效力，不足以减少细胞生物学测定中的脱靶效应。

17. 发明授权

US08987221B2 Potentiation of autoimmune and inflammatory disease treatments by immune regulatory oligonucleotide (IRO) antagonists of TLR7 and TLR9 有权
标题翻译： TLR7和TLR9的免疫调节寡核苷酸（IRO）拮抗剂对自身免疫和炎性疾病治疗的加强
公开(公告)号：US08987221B2
公开(公告)日：2015-03-24
申请号：US12791636
申请日：2010-06-01
申请人： Fu-Gang Zhu , Ekambar Kandimalla , Sudhir Agrawal
发明人： Fu-Gang Zhu , Ekambar Kandimalla , Sudhir Agrawal
IPC分类号： A61K48/00 , C12N15/11 , A61K31/7088 , A61K38/17 , A61K45/06 , C12N15/117
CPC分类号： C12N15/117 , A61K31/7088 , A61K38/1793 , A61K45/06 , A61K2300/00 , C12N2310/17 , C12N2310/3183 , C12N2310/319 , C12N2310/321 , C12N2310/332 , C12N2310/336 , C12N2310/3521 , C12N2310/51 , C12N2320/31 , Y02A50/463
摘要： The invention provides the use of immune regulatory oligonucleotides (IRO) as antagonist of TLRs and potentiators of anti-inflammatory agents that inhibit TNF for the prevention and treatment of inflammatory and autoimmune diseases.
摘要翻译：本发明提供免疫调节寡核苷酸（IRO）作为TLR的拮抗剂和抗炎剂的增强剂的用途，所述抗炎药抑制TNF用于预防和治疗炎性和自身免疫性疾病。

18. 发明申请

US20130324591A1 DOUBLE STRANDED OLIGONUCLEOTIDE COMPOUNDS COMPRISING POSITIONAL MODIFICATIONS 审中-公开
标题翻译：包含位置修饰的双重拉链寡核苷酸化合物
公开(公告)号：US20130324591A1
公开(公告)日：2013-12-05
申请号：US13991610
申请日：2011-12-06
申请人： Sharon Avkin-Nachum , Elena Feinstein , Leonid Beigelman
发明人： Sharon Avkin-Nachum , Elena Feinstein , Leonid Beigelman
IPC分类号： C12N15/113
CPC分类号： C12N15/1137 , C12N15/111 , C12N2310/14 , C12N2310/31 , C12N2310/314 , C12N2310/317 , C12N2310/319 , C12N2310/321 , C12N2310/323 , C12N2310/332 , C12N2310/335 , C12N2320/51 , C12N2310/3521
摘要： Disclosed herein are double stranded RNA molecules which have been modified to exhibit one of the following, increased activity, enhanced nuclease stability, reduced off target activity and or reduced immunogenicity, to pharmaceutical compositions comprising such compounds and to methods of use. Further disclosed is a method for the synthesis of threose nucleic acid phosphoramidites and methods of use thereof.
摘要翻译：本文公开了双链RNA分子，其被修饰以显示下列之一，增加的活性，增强的核酸酶稳定性，降低的靶活性和/或降低的免疫原性，包括这些化合物的药物组合物和使用方法。进一步公开了一种合成苏氨酸核酸亚磷酰胺的方法及其使用方法。

19. 发明申请

US20110257248A1 RNAi-RELATED INHIBITION OF TNFa SIGNALING PATHWAY FOR TREATMENT OF OCULAR ANGIOGENESIS 有权
标题翻译：肿瘤坏死因子信号通路治疗眼内血管生成的RNAi相关性抑制
公开(公告)号：US20110257248A1
公开(公告)日：2011-10-20
申请号：US13169549
申请日：2011-06-27
申请人： Jon E. Chatterton , Abbot F. Clark , David P. Bingaman , Martin B. Wax , Adrian M. Timmers
发明人： Jon E. Chatterton , Abbot F. Clark , David P. Bingaman , Martin B. Wax , Adrian M. Timmers
IPC分类号： A61K31/713 , A61P27/02 , C07H21/02
CPC分类号： C12N15/1138 , C12N15/113 , C12N15/1136 , C12N15/1137 , C12N2310/111 , C12N2310/14 , C12N2310/141 , C12N2310/31 , C12N2310/319 , C12N2310/32 , C12N2310/321 , C12N2310/53 , C12N2310/531
摘要： RNA interference is provided for inhibition of tumor necrosis factor α (TNFα) by silencing TNFα cell surface receptor TNF receptor-1 (TNFR1) mRNA expression, or by silencing TNFα converting enzyme (TACE/ADAM17) mRNA expression. Silencing such TNFα targets, in particular, is useful for treating patients having a TNFα-related condition or at risk of developing a TNFα-related condition, such as ocular angiogenesis, retinal ischemia, and diabetic retinopathy.
摘要翻译：通过沉默TNFα细胞表面受体TNF受体-1（TNFR1）mRNA表达或沉默TNFα转化酶（TACE / ADAM17）mRNA表达，提供RNA干扰抑制肿瘤坏死因子α（TNFα）。特别是使TNFα靶标沉默可用于治疗患有TNFα相关病症或出现TNFα相关病症如眼血管生成，视网膜缺血和糖尿病性视网膜病变的风险的患者。

20. 发明申请

US20110105591A1 siRNA COMPOUNDS FOR INHIBITING NRF2 有权
标题翻译：用于抑制NRF2的siRNA化合物
公开(公告)号：US20110105591A1
公开(公告)日：2011-05-05
申请号：US12988307
申请日：2009-04-06
申请人： Elena Feinstein , Igor Mett , Hagar Kalinski
发明人： Elena Feinstein , Igor Mett , Hagar Kalinski
IPC分类号： A61K31/7052 , C07H21/00 , A61P35/00
CPC分类号： C12N15/113 , C12N2310/14 , C12N2310/317 , C12N2310/319 , C12N2310/321 , C12N2310/3231 , C12N2310/332 , C12N2310/343 , C12N2310/344 , C12N2310/3521
摘要： The present invention provides chemically modified siRNA compounds that target the Nrf2 gene and pharmaceutical compositions comprising same useful for treating or preventing the incidence or severity of a cancerous disease, particularly various lung cancers.
摘要翻译：本发明提供靶向Nrf2基因的化学修饰的siRNA化合物和包含用于治疗或预防癌性疾病，特别是各种肺癌的发病率或严重程度的药物组合物。

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