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公开(公告)号：US5663321A
公开(公告)日：1997-09-02
申请号：US474810
申请日：1995-06-07
IPC分类号： C07H21/00 , C07H21/04 , C07H19/073 , C07K16/28
CPC分类号： C07H21/00
摘要： Homo-oligomeric 5-fluorouridine and 5-fluorodeoxyuridine (FrU.sub.n and FdU.sub.n, n=oligomer length) are synthesized and used as a polymeric drug delivery system for production of FdUMP, the potent inhibitor of thymidylate synthase (TS) and an important target in cancer chemotherapy. Disclosed are methods of both preparing and utilizing said compositions.
摘要翻译： 合成了低聚5-氟尿苷和5-氟脱氧尿苷（FrUn和FdUn，n =寡聚体长度），并用作产生FdUMP的聚合物药物递送系统，其是胸苷酸合酶（TS）的有效抑制剂和癌症中的重要靶标 化疗。 公开了制备和利用所述组合物的方法。
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22.发明授权Synthetic oligonucleotides which mimic telomeric sequences for use in treatment of cancer and other diseases 失效模仿用于治疗癌症和其他疾病的端粒序列的合成寡核苷酸
公开(公告)号：US5643890A
公开(公告)日：1997-07-01
申请号：US381097
申请日：1995-01-31
申请人： Patrick L. Iversen , John E. Mata
发明人： Patrick L. Iversen , John E. Mata
IPC分类号： A61K38/00 , C12N15/113 , A61K48/00 , C07H21/04 , C12N5/10
CPC分类号： A61K31/711 , C12N15/1137 , C12Y207/07049 , A61K38/00 , C12N2310/13 , C12N2310/315
摘要： A method of inhibiting proliferation of immortal cells or cells that express telomerase is disclosed. The method includes introduction of synthetic oligonucleotides which mimic telomere motifs. Quite surprisingly applicant has demonstrated that a single telomere motif, TTAGGG exhibits greater cellular uptake and higher inhibition of proliferation than longer oligonucleotides, which were previously thought to be necessary to achieve sequence specific interaction with telomerase.
摘要翻译： 公开了抑制表达端粒酶的永生细胞或细胞增殖的方法。 该方法包括引入模拟端粒基序的合成寡核苷酸。 非常令人惊讶的是，申请人已经证明，单链端粒基序TTAGGG与较长的寡核苷酸相比表现出更大的细胞吸收和更高的增殖抑制，其先前被认为是实现与端粒酶的序列特异性相互作用所必需的。
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23.发明授权
公开(公告)号：US5641754A
公开(公告)日：1997-06-24
申请号：US179655
申请日：1994-01-10
申请人： Patrick L. Iversen
发明人： Patrick L. Iversen
CPC分类号： C12N15/1135 , A61K41/0038 , A61K48/00 , A61K38/00 , C12N2310/315
摘要： The present invention relates to methods and compositions for the treatment of cancer using an oligonucleotide and an hydroxyl radical up-regulator. The oligonucleotide is characterized by its ability to down-regulate the path by which the cell repairs oxidative damage to its DNA. Thus, the oligonucleotide renders the tumor cells more susceptible to eradication upon exposure to the hydroxyl radical up-regulator administered substantially concomitantly with or subsequent to administration of the oligonucleotide. This novel treatment, preferentially inhibits the proliferation or kills malignant cells but not normal cells. Preferably, the oligonucleotide is antisense to the gene which encodes protein p53, although other antisense oligonucleotides can also be used. The invention also includes novel conjugates of the oligonucleotide and the hydroxyl up-regulator, as well as new oligonucleotides.
摘要翻译： 本发明涉及使用寡核苷酸和羟基自由基上调的治疗癌症的方法和组合物。 寡核苷酸的特征在于其下调细胞修复其DNA的氧化损伤的途径的能力。 因此，寡核苷酸使得肿瘤细胞在暴露于与施用寡核苷酸基本上同时或之后施用的羟基自由基上调节剂时更易于根除。 这种新型治疗优先抑制增殖或杀死恶性细胞而不是正常细胞。 优选地，寡核苷酸与编码蛋白质p53的基因反义，尽管也可以使用其他反义寡核苷酸。 本发明还包括寡核苷酸和羟基上调的新型缀合物，以及新的寡核苷酸。
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24.发明授权Metal binding oligonucleotide and methods and compositions for their use to treat metal toxicity 失效金属结合寡核苷酸及其用于治疗金属毒性的方法和组合物
公开(公告)号：US5618796A
公开(公告)日：1997-04-08
申请号：US759841
申请日：1991-09-12
申请人： Patrick L. Iversen
发明人： Patrick L. Iversen
CPC分类号： C07H21/00
摘要： The present invention discloses novel methods and compositions useful for removing toxic heavy metals from a host organism containing detectable levels of such heavy metals. The method comprises administering to the host organism a therapeutically effective amount of a heavy-metal binding agent which, when saturated with heavy metal atoms, is readily excreted from the body. In a preferred embodiment of the present invention, the binding agent is an oligomeric phosphorothioate oligonucleotide.
摘要翻译： 本发明公开了可用于从含有可检测水平的这种重金属的宿主生物中除去有毒重金属的新方法和组合物。 该方法包括向宿主生物体施用治疗有效量的重金属结合剂，其当被重金属原子饱和时容易从体内排出。 在本发明的优选实施方案中，结合剂是寡聚硫代磷酸酯寡核苷酸。
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25.发明授权Method of treating cancer with homo-oligonuleotides of 5-FU 5'-monophosphate 失效用5-FU 5'-单磷酸的同源寡核苷酸治疗癌症的方法
公开(公告)号：US5614505A
公开(公告)日：1997-03-25
申请号：US526337
申请日：1995-09-11
CPC分类号： C07H21/00
摘要： Homo-oligomeric 5-fluorouridine and 5-fluorodeoxyuridine (FrU.sub.n and FdU.sub.n, n=oligomer length) are synthesized and used as a polymeric drug delivery system for production of FdUMP, the potent inhibitor of thymidylate synthase (TS) and an important target in cancer chemotherapy. Disclosed are methods of both preparing and utilizing said compositions.
摘要翻译： 合成了低聚5-氟尿苷和5-氟脱氧尿苷（FrUn和FdUn，n =寡聚体长度），并用作产生FdUMP的聚合物药物递送系统，其是胸苷酸合酶（TS）的有效抑制剂和癌症中的重要靶标 化疗。 公开了制备和利用所述组合物的方法。
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26.发明授权公开(公告)号：US08524684B2
公开(公告)日：2013-09-03
申请号：US13469892
申请日：2012-05-11
CPC分类号： C12N15/113 , A61K31/675 , A61K31/713 , C12N15/1131 , C12N2310/11 , C12N2310/3233
摘要： The present invention provides antisense antiviral compounds, compositions, and methods of their use and production, mainly for inhibiting the replication of viruses of the Filoviridae family, including Ebola and Marburg viruses. The compounds, compositions, and methods also relate to the treatment of viral infections in mammals including primates by Ebola and Marburg viruses. The antisense antiviral compounds include phosphorodiamidate morpholino oligonucleotides (PMOplus) having a nuclease resistant backbone, about 15-40 nucleotide bases, at least two but typically no more than half piperazine-containing intersubunit linkages, and a targeting sequence that is targeted against the AUG start site region of Ebola virus VP35, Ebola virus VP24, Marburg virus VP24, or Marburg virus NP, including combinations and mixtures thereof.
摘要翻译： 本发明提供反义抗病毒化合物，组合物及其使用和生产方法，主要用于抑制丝状病毒科病毒的复制，包括埃博拉病毒和马尔堡病毒。 化合物，组合物和方法还涉及治疗包括埃博拉和马尔堡病毒在内的哺乳动物中的病毒感染。 反义抗病毒化合物包括具有核酸酶抗性主链的磷酸二亚胺吗啉代寡核苷酸（PMOplus），约15-40个核苷酸碱基，至少两个但通常不超过一半的含哌嗪的亚单位间连接，以及针对AUG起始靶向序列 埃博拉病毒VP35的位点区域，埃博拉病毒VP24，马尔堡病毒VP24或马尔堡病毒NP，包括其组合和混合物。
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公开(公告)号：US08501704B2
公开(公告)日：2013-08-06
申请号：US12267437
申请日：2008-11-07
CPC分类号： C12N15/1138 , C12N15/113 , C12N2310/11 , C12N2310/314 , C12N2310/3233 , C12N2310/3513
摘要： Provided are methods and antisense oligonucleotide analogs for suppressing an immune response in a mammalian subject, for the treatment or prevention of an autoimmune condition or transplantation rejection. The oligonucleotide analogs provided herein comprise a targeting sequence complementary to a preprocessed CTLA-4 mRNA region that spans the splice junction between intron 1 and exon 2 of the preprocessed CTLA-4 mRNA. Also provided are methods of use, in which the oligonucleotides are effective, when administered to a subject, to form within host cells, a heteroduplex structure (i) composed of the preprocessed CTLA-4 mRNA and the oligonucleotide compound, (ii) characterized by a Tm of dissociation of at least 45° C., and (iii) resulting in an increased ratio of processed mRNA encoding ligand-independent CTLA-4 to processed mRNA encoding full-length CTLA-4.
摘要翻译： 提供了用于抑制哺乳动物受试者的免疫应答的方法和反义寡核苷酸类似物，用于治疗或预防自身免疫病症或移植排斥反应。 本文提供的寡核苷酸类似物包含与预处理的CTLA-4 mRNA的内含子1和外显子2之间的剪接连接的预处理的CTLA-4mRNA区域互补的靶向序列。 还提供了使用方法，其中当给受试者施用时，寡核苷酸是有效的，以在宿主细胞内形成异源双链结构（i）由预处理的CTLA-4mRNA和寡核苷酸化合物组成，（ii）其特征在于 解离的Tm至少为45℃，和（iii）增加编码不依赖配体的CTLA-4的加工mRNA与编码全长CTLA-4的加工mRNA的比例增加。
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28.发明申请PEPTIDE CONJUGATED, INOSINE-SUBSTITUTED ANTISENSE OLIGOMER COMPOUND AND METHOD 有权肽联合，非取代的抗原寡聚化合物和方法公开(公告)号：US20130131312A1
公开(公告)日：2013-05-23
申请号：US13243341
申请日：2011-09-23
IPC分类号： C12N15/113
CPC分类号： C12N15/113 , A61K48/0008 , C12N15/111 , C12N15/1135 , C12N2310/11 , C12N2310/3145 , C12N2310/3233 , C12N2310/331 , C12N2310/3513 , C12N2320/32
摘要： A therapeutic oligomer-peptide conjugate, and methods of using the conjugate are disclosed. The conjugate includes (a) a substantially uncharged oligonucleotide analog compound having a base sequence that includes a string of bases that are complementary to four or more contiguous cytosine bases in a target nucleic acid region to which the compound is intended to bind, and (b) conjugated to the compound, an arginine-rich peptide effective to enhance the uptake of the compound into target cells. The string of bases in the compound includes at least one inosine base positioned in the string so as to limit the number of contiguous guanine bases in said string to three or fewer. The conjugate has greater cellular uptake than the compound alone, by virtue of the arginine-rich peptide, and substantially greater antisense activity greater activity than the conjugate in the absence of inosine-for guanine substitutions.
摘要翻译： 公开了治疗性低聚物 - 肽缀合物和使用该缀合物的方法。 缀合物包括（a）具有碱基序列的基本上不带电的寡核苷酸类似物化合物，其碱基序列包括与化合物所要结合的靶核酸区域中的四个或更多个连续胞嘧啶碱基互补的碱基序列，和（b ），富含精氨酸的肽有效地增强化合物进入靶细胞的摄取。 所述化合物中的碱基串包括位于所述串中的至少一个肌苷碱基，以将所述串中的连续鸟嘌呤碱基的数目限制为三个或更少。 通过富含精氨酸的肽，缀合物比单独的化合物具有更大的细胞摄取，并且在不存在肌苷 - 用于鸟嘌呤取代的情况下，具有比缀合物更大的反义活性。
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29.发明申请ANTISENSE ANTIVIRAL COMPOUND AND METHOD FOR TREATING ssRNA VIRAL INFECTION 有权抗体抗病毒化合物和用于治疗ssRNA病毒感染的方法公开(公告)号：US20120322847A1
公开(公告)日：2012-12-20
申请号：US13335450
申请日：2011-12-22
CPC分类号： C12N15/1131 , C07K19/00 , C12N15/111 , C12N2310/11 , C12N2310/314 , C12N2310/3233 , C12N2310/3513 , C12N2310/531 , C12N2320/11 , C12N2770/00011 , C12N2770/10011 , C12N2770/12011 , C12N2770/16011 , C12N2770/20011 , C12N2770/24011 , C12N2770/28011 , C12N2770/32011 , C12N2770/36011
摘要： The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Flaviviridae, Picornoviridae, Caliciviridae, Togaviridae, Arteriviridae, Coronaviridae, Astroviridae and Hepeviridae families in the treatment of a viral infection. The antisense antiviral compounds are substantially uncharged morpholino oligonucleotides having a sequence of 12-40 subunits, including at least 12 subunits having a targeting sequence that is complementary to a region associated with stem-loop secondary structure within the 5′-terminal end 40 bases of the positive-sense RNA strand of the virus.
摘要翻译： 本发明提供反义抗病毒化合物及其在抑制黄病毒科，细小病毒科，杯状病毒科，披膜病毒科，动脉病毒科，科罗亚病毒科，蛔虫科和乙肝病毒科的病毒生长中的用途和生产方法。 反义抗病毒化合物是具有12-40个亚基序列的基本上不带电荷的吗啉代寡核苷酸，包括至少12个亚基，其具有与在5'-末端40个碱基内的茎环二级结构相关的区域互补的靶向序列 病毒的正义RNA链。
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30.发明授权Antisense antiviral compound and method for treating picornavirus infection 失效反义抗病毒化合物及治疗小RNA病毒感染的方法公开(公告)号：US08329668B2
公开(公告)日：2012-12-11
申请号：US11518058
申请日：2006-09-08
CPC分类号： C12N15/1131 , C12N2310/11 , C12N2310/3145 , C12N2310/3233 , C12N2310/3513 , C12N2770/32311 , C12N2770/32711
摘要： The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Picornaviridae family and in the treatment of a viral infection. The compounds are particularly useful in the treatment of Enterovirus and/or Rhinovirus infection in a mammal. The antisense antiviral compounds are substantially uncharged, including partially positively charged, morpholino oligonucleotides have a sequence of 12-40 subunits, including at least 12 subunits having a targeting sequence that is complementary to a region associated with viral RNA sequences within a 32 nucleotide region of the viral 5′ untranslated region identified by SEQ ID NO:4.
摘要翻译： 本发明提供反义抗病毒化合物及其在抑制小核糖核酸病毒科家族病毒生长和用于病毒感染治疗中的用途和生产方法。 所述化合物特别可用于治疗哺乳动物中的肠病毒和/或鼻病毒感染。 反义抗病毒化合物是基本上不带电的，包括部分带正电荷的吗啉代寡核苷酸具有12-40个亚基的序列，包括至少12个亚基，其具有与与32个核苷酸区域内的病毒RNA序列相关的区域互补的靶向序列 由SEQ ID NO：4鉴定的病毒5'非翻译区。
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