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21. 发明申请

WO1993010820A1 ENHANCED TRIPLE-HELIX AND DOUBLE-HELIX FORMATION WITH OLIGOMERS CONTAINING MODIFIED PYRIMIDINES 审中-公开
标题翻译：增强的三螺旋和双螺旋形成与含改性吡啶的低聚物
公开(公告)号：WO1993010820A1
公开(公告)日：1993-06-10
申请号：PCT/US1992010115
申请日：1992-11-24
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , FROEHLER, Brian , WAGNER, Rick , MATTEUCCI, Mark , JONES, Robert, J. , GUTIERREZ, Arnold, J. , PUDLO, Jeff
IPC分类号： A61K48/00
CPC分类号： C07H19/06 , C07H19/10 , C07H19/20 , C07H21/00 , C12Q1/6839 , Y02P20/55 , C12Q2525/101
摘要： Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention. Compositions of the invention can be used as pharmaceutical agents to treat various diseases such as those caused by viruses and can be used for diagnostic purposes in order to detect viruses or disease conditions.
摘要翻译：公开了与仅含有常规碱的低聚物相比，具有增强形成双链体或三链体的能力的新型低聚物。低聚物含有5-（1-丙炔基）尿嘧啶，5-（1-丙炔基）胞嘧啶或相关类似物的碱基。本发明的寡聚体能够（i）通过在生理pH下偶联到目标DNA双链体的主要沟槽中或（ii）通过结合单链DNA形成双链体，形成具有各种靶序列的病毒或致癌基因序列的三链体或由靶基因编码的RNA。本发明的寡聚体可以并入药学上可接受的载体中，并且可以被构建成具有任何所需的序列，条件是序列通常包括用本发明的类似物代替的一个或多个碱基。本发明的组合物可以用作药剂来治疗由病毒引起的各种疾病，并且可以用于诊断目的以检测病毒或疾病状况。

22. 发明申请

WO1993009127A1 ENHANCED TRIPLE-HELIX FORMATION DIRECTED BY OLIGONUCLEOTIDES COMPOSED OF 2'-DEOXY-7-DEAZAXANTHOSINE AND 2'-DEOXY-7-DEAZAGUANOSINE AND RELATED ANALOGS 审中-公开
标题翻译：由2'-脱氧-7-二氮杂和2'-脱氧-7-哒嗪酮组成的寡核苷酸与相关模拟物的增强三重螺旋形成
公开(公告)号：WO1993009127A1
公开(公告)日：1993-05-13
申请号：PCT/US1992009195
申请日：1992-10-21
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , MATTEUCCI, Mark , KRAWCZYK, Steve , MILLIGAN, John
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H19/14 , C12Q1/6839
摘要： Oligomers containing deazapurine bases have enhanced ability with respect to forming triplexes as compared with oligomers containing only conventional bases. The deazapurine bases are substituted and unsubstituted forms of 7-deazaxanthine and 7-deazaguanine. The oligomers of the invention are capable of forming triplexes with various target sequences such as HER-2 and HIV sequences by coupling into the major groove of a target DNA duplex at physiological pH. The oligomers of the invention may be incorporated into pharmaceutically acceptable carriers and may be constructed to have any desired sequence, provided the sequence includes at least one deazapurine which enhances the ability of the oligomer to form a triplex with the target sequence. Compositions of the invention can be used as pharmaceuticals to treat various diseases linked to genetic material and can be used for diagnostic purposes in order to detect various disease conditions.
摘要翻译：含有脱氮嘌呤碱的低聚物与仅含有常规碱的低聚物相比，具有增强形成三链体的能力。脱氮嘌呤碱基是7-脱氧黄嘌呤和7-脱氮鸟嘌呤的取代和未取代的形式。本发明的寡聚体能够通过在生理pH下连接到目标DNA双链体的主要沟槽中而与各种靶序列如HER-2和HIV序列形成三链体。本发明的寡聚体可以并入药学上可接受的载体中，并且可以构建成具有任何所需的序列，条件是该序列包括至少一种脱氮嘌呤，其增强寡聚体与靶序列形成三链体的能力。本发明的组合物可用作药物以治疗与遗传物质相关的各种疾病，并且可用于诊断目的以检测各种疾病状况。

23. 发明申请

WO1992019637A1 OLIGONUCLEOTIDE ANALOGS CONTAINING THIOFORMACETAL LINKAGES 审中-公开
标题翻译：含有连接子的寡核苷酸模拟物
公开(公告)号：WO1992019637A1
公开(公告)日：1992-11-12
申请号：PCT/US1992003385
申请日：1992-04-24
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , MATTEUCCI, Mark , JONES, Bob , LIN, Kuei-Ying
IPC分类号： C07H19/00
CPC分类号： C07H19/06 , C07H19/16 , C07H21/00
摘要： Modified oligomers containing at least one internucleoside linkage of the formula Y CX2Y wherein at least one of Y and Y is sulfur and the other is oxygen and wherein each X is the same or different and is a stabilizing substituent are disclosed. These oligomers show superior binding properties and are thus useful for binding target substances in therapeutic and analytical uses. Also disclosed are improved methods for synthesis of oligomers containing linkages of the general formula -YCX2Y- wherein each Y may be independently oxygen or sulfur.
摘要翻译：含有至少一个式Y 1 CX 2 Y 2的核苷间键的修饰低聚物，其中Y 1和Y 2中的至少一个是硫，另一个是氧，并且其中每个X相同或不同，是一种稳定取代基。这些低聚物显示出优异的结合性，因此可用于在治疗和分析用途中结合靶物质。还公开了用于合成含有通式-YCX 2 Y-的键的低聚物的改进方法，其中每个Y可以独立地为氧或硫。

24. 发明申请

WO1991014696A1 OLIGONUCLEOTIDE-TRANSPORT AGENT DISULFIDE CONJUGATES 审中-公开
标题翻译：寡核苷酸运输代理商无关联
公开(公告)号：WO1991014696A1
公开(公告)日：1991-10-03
申请号：PCT/US1991002224
申请日：1991-03-29
申请人： GILEAD SCIENCES, INC. , LATHAM, John, A. , LIN, Kuei-Ying , MATTEUCCI, Mark
发明人： GILEAD SCIENCES, INC.
IPC分类号： C07H17/00
CPC分类号： C12Q1/6841 , A61K47/554 , C12N15/87 , C12Q1/6813
摘要： The invention relates to compositions and methods for enhancing the delivery of an oligonucleotide into a cell. The compositions of the invention comprise oligonucleotide conjugates which consist of an oligonucleotide, conjugated via a molecular linker containing at least one disulfide bond, to an agent (termed herein "transport agent") which facilitates transport across an outer cell membrane, or across the blood-brain barrier. In a preferred aspect, the disulfide linkage is cleaved upon uptake of the composition by the cell. Pharmaceutical compositions comprising an oligonucleotide conjugate of the invention may be used to treat a wide variety of diseases and disorders. Methods for inhibiting the expression of a nucleic acid sequence within a cell, and methods for detecting a nucleic acid sequence within a cell are also provided. In a specific embodiment, an oligonucleotide conjugated to cholesterol via a linker containing a disulfide linkage can be used for therapeutic or diagnostic purposes, by hybridization of the oligonucleotide to a complementary nucleic acid sequence in a procaryotic or eucaryotic cell.
摘要翻译：本发明涉及用于增强寡核苷酸向细胞递送的组合物和方法。本发明的组合物包含寡核苷酸缀合物，其由通过含有至少一个二硫键的分子接头缀合的寡核苷酸组成，其有助于穿过外细胞膜或穿过血液的药剂（称为“转运剂”））脑屏障在优选的方面，当细胞摄取组合物时，二硫键被切割。包含本发明的寡核苷酸缀合物的药物组合物可用于治疗多种疾病和病症。还提供了抑制细胞内核酸序列表达的方法，以及用于检测细胞内的核酸序列的方法。在一个具体实施方案中，通过将寡核苷酸与原核或真核细胞中的互补核酸序列杂交，通过含有二硫键的接头与胆固醇缀合的寡核苷酸可用于治疗或诊断目的。

25. 发明申请

WO1991006626A2 TRIPLE HELIX FORMATION IN OLIGONUCLEOTIDE THERAPY 审中-公开
标题翻译：寡核苷酸治疗中的三联螺旋形成
公开(公告)号：WO1991006626A2
公开(公告)日：1991-05-16
申请号：PCT/US1990006128
申请日：1990-10-23
申请人： GILEAD SCIENCES, INC. , FROEHLER, Brian , TOOLE, John, J.
发明人： GILEAD SCIENCES, INC.
IPC分类号： C12N0
CPC分类号： C12Q1/6813 , C12N15/113 , C12N2310/15 , C12N2310/317 , C12N2310/318 , C12N2310/32 , C12N2310/321 , C12Q1/6839 , Y10S435/81
摘要： Oligonucleotides having tandem sequences of inverted polarity, i.e., oligonucleotides comprising regions of the formula: 3'-----5'--C--5'-----3' or 5'-----3'--C--3'-----5', wherein -C- symbolizes any method of coupling the nucleotide sequence of opposite polarity, are useful for forming an extended triple helix with a double-helical nucleotide duplex. Single or mixed motif oligomers may be used. The inverted polarity also stabilizes the single-strand oligonucleotides to exonuclease degradation.
摘要翻译：具有反向极性的串联序列的寡核苷酸，即包含下式的区域的寡核苷酸：3' - 5'-C 5' - 3'或5' - 3' -C 3'----- 5'，其中-C表示任何偶联相反极性的核苷酸序列的方法，可用于形成具有双螺旋核苷酸双链体的延伸三螺旋。可以使用单个或混合基序寡聚体。反向极性还使单链寡核苷酸稳定到外切核酸酶降解。

26. 发明公开

EP1809277A2 PHOSPHONATE DERIVATIVES OF MYCOPHENOLIC ACID 审中-公开
标题翻译：膦酸酯OFF霉酚酸
公开(公告)号：EP1809277A2
公开(公告)日：2007-07-25
申请号：EP05822599.6
申请日：2005-10-26
申请人： GILEAD SCIENCES, INC. , Watkins, William J. , Cho, Aesop
发明人： GILEAD SCIENCES, INC. , Watkins, William J. , Cho, Aesop
IPC分类号： A61K31/335 , C07F9/40
CPC分类号： C07F9/65517 , C07F9/65586
摘要： Phosphorus substituted mycophenolate oxime derivatives with anti-cancer, anti-viral, anti-inflammatory and anti-tissue/organ transplant rejection properties having use as therapeutics and for other industrial purposes are disclosed. The compositions inhibit tumor growth, viral growth, inflammation, and tissue/organ transplant rejection and/or are useful therapeutically for the treatment or prevention of cancer, viral infection, inflammation and tissue/organ transplant rejection, as well as in assays for the detection of cancer, viral infection, inflammation and tissue/organ transplant rejection.

27. 发明申请

WO1998004575A2 LIPOPHILIC OLIGONUCLEOTIDE ANALOGS 审中-公开
公开(公告)号：WO1998004575A2
公开(公告)日：1998-02-05
申请号：PCT/US1996012530
申请日：1996-07-31
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , BISCHOFBERGER, Norbert, W. , KENT, Kenneth, M. , WAGNER, Richard, W. , BUHR, Chris, A. , LIN, Kuei-Ying
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： The invention discloses lipophilic oligonucleotide analogs that are capable of efficient passive diffusion across cell membranes. These oligonucleotides contain at least two nucleotide residues and have an octanol:water partition coefficient of about -0.3 to + 2.5 and a solubility in water of at least 0.001 mu g/mL. Invention embodiments which include lipophilic oligonucleotide analogs having either at least 60 % of the internucleotide linkages are lipophilic, or at least 60 % of the bases contain lipophilic substitutions, or at least 60 % of the sugars contain lipophilic substitutions, or a combination of these sums to 60 %. These oligonucleotides may be conjugated to a label and used to visualize cells or subcellular compartments.
摘要翻译：本发明公开了能够在细胞膜上有效被动扩散的亲脂性寡核苷酸类似物。这些寡核苷酸含有至少两个核苷酸残基并且具有约-0.3至+ 2.5的辛醇：水分配系数和在水中的溶解度至少为0.001μg/ mL。包括具有至少60％的核苷酸间键的亲脂寡核苷酸类似物的发明实施方案是亲脂性的，或至少60％的碱含有亲脂性取代，或至少60％的糖含有亲脂性取代，或这些和的组合至60％。这些寡核苷酸可以缀合到标签上并用于使细胞或亚细胞区室可视化。

28. 发明申请

WO1997049723A1 CATIONIC LIPIDS FOR DELIVERY OF NUCLEIC ACID TO CELLS 审中-公开
标题翻译：用于向细胞输送核酸的阳离子脂肪
公开(公告)号：WO1997049723A1
公开(公告)日：1997-12-31
申请号：PCT/US1997011225
申请日：1997-06-26
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , LIN, Kuei-Ying , MATTEUCCI, Mark, D.
IPC分类号： C07K05/08
CPC分类号： C07D233/64 , A61K38/00 , C07K5/06026 , C07K5/06147 , C07K5/0806 , Y10T436/207497
摘要： The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, or similar compounds, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.
摘要翻译：本发明涉及其合成中的新的阳离子脂质和中间体，其可用于将核酸或肽转染到原核或真核细胞中。脂质包含与亲油部分连接的一个或两个取代的组氨酸残基或类似化合物。当与聚阴离子例如核酸或肽混合时，脂质形成复合物。复合物允许聚阴离子有效转移到细胞中，通常对细胞没有显着的毒性。

29. 发明申请

WO1997024361A1 NUCLEOTIDE ANALOGS 审中-公开
标题翻译：核素类似物
公开(公告)号：WO1997024361A1
公开(公告)日：1997-07-10
申请号：PCT/US1996020226
申请日：1996-12-13
申请人： GILEAD SCIENCES, INC. , ARIMILLI, Murty, N. , BISCHOFBERGER, Norbert, W. , JONES, Robert, J. , LEE, William, A. , PRISBE, Ernest, J.
发明人： GILEAD SCIENCES, INC.
IPC分类号： C07F09/6571
CPC分类号： C07F9/657181
摘要： Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.
摘要翻译：公开了以与磷酸酯核苷酸类似物的磷原子结合的酯连接基团的存在为特征的核苷酸膦酸酯。类似物包括在体内水解以产生相应的膦酸酯核苷酸类似物的酯键。描述了其合成和使用的方法和中间体。

30. 发明申请

WO1996023801A2 NOVEL COMPOUNDS AND METHODS FOR MAKING AND USING SAME 审中-公开
标题翻译：新型化合物及其制备和使用方法
公开(公告)号：WO1996023801A2
公开(公告)日：1996-08-08
申请号：PCT/US1996001574
申请日：1996-01-31
申请人： GILEAD SCIENCES, INC.
发明人： GILEAD SCIENCES, INC. , ALEXANDER, Petr , PRISBE, Ernest, J.
IPC分类号： C07F09/6558
CPC分类号： C07F9/65586 , C07F9/65616
摘要： In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.
摘要翻译：根据本发明，提供了选自饱和和不饱和的吡喃和呋喃的新化合物，其被至少一个膦酸酯基和杂环碱取代。这些化合物可用作抗感染剂，阻燃剂，诊断性寡核苷酸和免疫原。

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