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公开(公告)号：US6124271A
公开(公告)日：2000-09-26
申请号：US12198
申请日：1998-01-23
IPC分类号： A61K31/7088 , A61K47/48 , A61P31/04 , A61K31/70 , C07H21/00
CPC分类号： A61K47/48092 , A61K47/48023 , A61K47/48315
摘要： A method and comjugate for treating H. pylori infection in a subject are disclosed. The conjugate is composed of (a) a nuclease-resistant antisense oligomer effective to inhibit H. pylori infection in the subject by base-specific Watson-Crick binding to an H. pylori mRNA transcript, and (b) a transport moiety conjugated to the oligomer. The transport moiety is effective to facilitate uptake of the conjugate from the environment of the stomach into the cytoplasm of H. pylori cells by active transport or by pH-gradient transport across of the cell membrane of H. pylori. The conjugate is administered by oral route, preferably in a swellable polymer bolus designed to release the conjugate in sustained release.
摘要翻译： 公开了用于治疗受试者中幽门螺杆菌感染的方法和共轭物。 缀合物由（a）通过碱基特异性Watson-Crick结合幽门螺杆菌mRNA转录物有效抑制幽门螺杆菌感染的核酸酶抗性反义寡聚体，和（b）与 低聚物。 运输部分有利于通过主动转运或通过幽门螺旋杆菌的细胞膜上的pH梯度转运来促进缀合物从胃的环境吸收到幽门螺杆菌细胞的细胞质中。 缀合物通过口服途径施用，优选在可膨胀聚合物推注中，其设计用于释放持续释放的缀合物。
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公开(公告)号：US08785410B2
公开(公告)日：2014-07-22
申请号：US12983798
申请日：2011-01-03
IPC分类号： C07H21/00
CPC分类号： C12N15/1136 , A61K31/675 , A61K47/645 , C07H21/00 , C07K7/08 , C12N2310/11 , C12N2310/31 , C12N2310/3145 , C12N2310/3233 , C12N2310/3513 , C12N2320/30 , C12Q1/6876 , C12Q2600/158 , Y10T436/143333
摘要： A method and compound for treating skeletal muscle mass deficiency in a human subject are disclosed. The composition is an oligomer of morpholino subunits and phosphorus-containing intersubunit linkages joining a morpholino nitrogen of one subunit to a 5′ exocyclic carbon of an adjacent subunit, contains between 10-40 nucleotide bases, has a base sequence effective to hybridize to an expression-sensitive region of processed or preprocessed human myostatin RNA transcript, identified, in its processed form, by SEQ ID NO:6, and is capable of uptake by target muscle cells in the subject. In practicing the method, the compound is administered in an amount and at a dosage schedule to produce an overall reduction in the level of serum myostatin measured in the patient, and preferably to bring the myostatin level within the a range determined for normal, healthy individuals.
摘要翻译： 公开了一种用于治疗人类受试者骨骼肌质量不足的方法和化合物。 该组合物是吗啉代亚基的低聚物和将一个亚基的吗啉代氮连接到相邻亚单位的5'环外碳的含磷亚基间键，含有10-40个核苷酸碱基之间，具有有效地与表达杂交的碱基序列 经处理或预处理的人肌生成抑制素RNA转录物的敏感区域，以其加工形式由SEQ ID NO：6鉴定，并且能够被摄体中的靶肌细胞摄取。 在实施该方法中，化合物以量和剂量方案施用以产生在患者体内测量的血清肌生成抑制素水平的总体降低，优选使肌生成抑制素水平在正常健康个体确定的范围内 。
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3.发明授权Antisense oligomers and methods for inducing immune tolerance and immunosuppression 有权反义寡聚体和诱导免疫耐受和免疫抑制的方法公开(公告)号：US08415313B2
公开(公告)日：2013-04-09
申请号：US11433033
申请日：2006-05-11
CPC分类号： A61K31/675 , C12N15/1138 , C12N2310/11 , C12N2310/3233 , C12N2310/3513
摘要： A method and composition for inducing human dendritic cells to a condition of reduced capacity for antigen-specific activation of T cells, and, in mature dendritic cells, increased production of extracellular IL-10 is disclosed. A population of dendritic cells is exposed to a substantially uncharged antisense compound, including partially positively charged, containing 12-40 subunits and a base sequence effective to hybridize to a target region within the sequence identified by SEQ ID NO:9, to form a duplex structure between the compound and transcript having a Tm of at least 45° C. Formation of the duplex blocks expression of full-length CD86 in the cells, which in turn leads to reduced capacity for antigen-specific activation of T cells, and, in mature dendritic cells, increased production of extracellular IL-10.
摘要翻译： 公开了一种用于将人树突状细胞诱导到T细胞的抗原特异性激活能力降低的条件下，并且在成熟树突状细胞中细胞外IL-10的产生增加的方法和组合物。 将一群树突状细胞暴露于包含部分带正电荷的基本上不带电荷的反义化合物，其含有12-40个亚单位和碱基序列，其有效地与SEQ ID NO：9所鉴定的序列内的靶区域杂交以形成双链体 化合物和具有至少45℃的Tm的转录物之间的结构。双链体阻断细胞中全长CD86的表达，这又导致T细胞抗原特异性激活的能力降低，并且在 成熟的树突状细胞，细胞外IL-10的产生增加。
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4.发明授权公开(公告)号：US08030291B2
公开(公告)日：2011-10-04
申请号：US12402455
申请日：2009-03-11
CPC分类号： C12N15/1131 , C12N2310/11 , C12N2310/31 , C12N2310/32 , C12N2310/3513
摘要： The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Filoviridae family, and in the treatment of a viral infection. The compounds and methods relate to the treatment of viral infections in mammals including primates by Ebola and Marburg viruses. The antisense antiviral compounds are morpholino oligonucleotides having: a) a nuclease resistant backbone, b) 15-40 nucleotide bases, and c) a targeting sequence of at least 15 bases in length that hybridizes to a target region selected from the following: i) the Ebola virus AUG start site region of VP24; ii) the Ebola virus AUG start site region of VP35; iii) the Marburg virus AUG start site region of VP24; or iv) the Marburg virus AUG start site region of NP.
摘要翻译： 本发明提供了反义抗病毒化合物及其在抑制丝状病毒科病毒生长和用于病毒感染治疗中的用途和生产方法。 该化合物和方法涉及哺乳动物中的病毒感染的治疗，包括埃博拉和马尔堡病毒的灵长类动物。 反义抗病毒化合物是吗啉代寡核苷酸，其具有：a）核酸酶抗性主链，b）15-40个核苷酸碱基，和c）长度为至少15个碱基的靶向序列与选自以下的靶区域杂交：i） 埃博拉病毒AUG起始站点区域VP24; ii）VP35的埃博拉病毒AUG起始区域; iii）马尔堡病毒AUG VP24的起始区域; 或iv）Marburg病毒AUG起始地点的NP。
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公开(公告)号：US20110166082A1
公开(公告)日：2011-07-07
申请号：US12983798
申请日：2011-01-03
IPC分类号： A61K31/675 , A61K38/00 , A61K38/10 , C07D413/14 , C07K9/00 , G01N33/48 , A61P21/00
CPC分类号： C12N15/1136 , A61K31/675 , A61K47/645 , C07H21/00 , C07K7/08 , C12N2310/11 , C12N2310/31 , C12N2310/3145 , C12N2310/3233 , C12N2310/3513 , C12N2320/30 , C12Q1/6876 , C12Q2600/158 , Y10T436/143333
摘要： A method and compound for treating skeletal muscle mass deficiency in a human subject are disclosed. The composition is an oligomer of morpholino subunits and phosphorus-containing intersubunit linkages joining a morpholino nitrogen of one subunit to a 5′ exocyclic carbon of an adjacent subunit, contains between 10-40 nucleotide bases, has a base sequence effective to hybridize to an expression-sensitive region of processed or preprocessed human myostatin RNA transcript, identified, in its processed form, by SEQ ID NO:6, and is capable of uptake by target muscle cells in the subject. In practicing the method, the compound is administered in an amount and at a dosage schedule to produce an overall reduction in the level of serum myostatin measured in the patient, and preferably to bring the myostatin level within the a range determined for normal, healthy individuals.
摘要翻译： 公开了一种用于治疗人类受试者骨骼肌质量不足的方法和化合物。 该组合物是吗啉代亚基的低聚物和将一个亚基的吗啉代氮连接到相邻亚单位的5'环外碳的含磷亚基间连接，含有10-40个核苷酸碱基之间，具有有效地与表达杂交的碱基序列 经处理或预处理的人肌生成抑制素RNA转录物的敏感区域，以其加工形式由SEQ ID NO：6鉴定，并且能够被摄体中的靶肌细胞摄取。 在实施该方法中，化合物以量和剂量方案施用以产生在患者体内测量的血清肌生成抑制素水平的总体降低，优选使肌生成抑制素水平在正常健康个体确定的范围内 。
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6.发明授权公开(公告)号：US07507196B2
公开(公告)日：2009-03-24
申请号：US11433840
申请日：2006-05-11
CPC分类号： C12N15/1131 , C12N2310/11 , C12N2310/31 , C12N2310/32 , C12N2310/3513
摘要： The invention provides antisense antiviral compounds and methods of their use and production in inhibition of growth of viruses of the Filoviridae family, and in the treatment of a viral infection. The compounds and methods relate to the treatment of viral infections in mammals including primates by Ebola and Marburg viruses. The antisense antiviral compounds are morpholino oligonucleotides having: a) a nuclease resistant backbone, b) 15-40 nucleotide bases, and c) a targeting sequence of at least 15 bases in length that hybridizes to a target region selected from the following: i) the AUG start site region of VP35, as exemplified by SEQ ID NOS:67-71 or ii) the AUG start site region of VP24, as exemplified by SEQ ID NOS:72-76.
摘要翻译： 本发明提供了反义抗病毒化合物及其在抑制丝状病毒科病毒生长和用于病毒感染治疗中的用途和生产方法。 该化合物和方法涉及哺乳动物中的病毒感染的治疗，包括埃博拉和马尔堡病毒的灵长类动物。 反义抗病毒化合物是吗啉代寡核苷酸，其具有：a）核酸酶抗性主链，b）15-40个核苷酸碱基，和c）长度为至少15个碱基的靶向序列与选自以下的靶区域杂交：i） VP35的AUG起始位点区域，如SEQ ID NO：67-71所示，或ii）VP24的AUG起始位点区域，如SEQ ID NO：72-76所例示。
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7.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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9.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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10.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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