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    Amide-based cationic lipids
    1.
    发明授权
    Amide-based cationic lipids 失效
    酰胺类阳离子脂质

    公开(公告)号：US06339173B1

    公开(公告)日：2002-01-15

    申请号：US09327392

    申请日：1999-06-07

    申请人： David Aaron Schwartz ,  William J. Daily ,  Brian Patrick Dwyer ,  Kumar Srinivasan ,  Bob Dale Brown

    发明人： David Aaron Schwartz ,  William J. Daily ,  Brian Patrick Dwyer ,  Kumar Srinivasan ,  Bob Dale Brown

    IPC分类号： C07C23305

    CPC分类号： B82Y5/00 ,  A61K9/1272 ,  C07C237/06 ,  C07C237/10 ,  C07C237/22 ,  C07K5/0215 ,  C07K5/06086 ,  C07K5/0815

    摘要： The present invention provides novel amide-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R1 is H or a lipophilic moiety; (c) R2, R3, and R4 are positively charged moieties, or at least one but not all of R2,R3, or R4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X− is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R3 or R4 must have an alkyl moiety of at least 10 carbon atoms. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.

    摘要翻译： 本发明提供了一般结构的新型酰胺类阳离子脂质：或其盐或溶剂合物或其对映体，其中： （a）Y是1至约20个碳原子的直链或亚烷基; （b）R 1为H或亲油部分; （c）R 2，R 3和R 4为带正电荷的部分，或至少一个但不全部为R 2，R 3或R 4为正部分，其余独立地选自H，1至约6个碳原子的烷基部分 原子或约5至约10个碳原子的杂环部分; （d）n和p独立地选自0至8的整数，使得n和o的和为1至16; （e）X-是阴离子或聚阴离子，（f）m是0至等于脂质上存在的正电荷数的整数; 条件是如果Y是直链，n和p的和为1，则R3或R4中的一个必须具有至少10个碳原子的烷基部分。本发明还提供这些脂质与聚阴离子大分子的组合物，方法 用于干扰利用这些组合物的细胞中的蛋白质表达和用于制备其的试剂盒。

    Amide-based cationic lipids
    3.
    发明授权
    Amide-based cationic lipids 失效
    酰胺类阳离子脂质

    公开(公告)号：US6020526A

    公开(公告)日：2000-02-01

    申请号：US681297

    申请日：1996-07-22

    申请人： David Aaron Schwartz ,  William J. Daily ,  Brian Patrick Dwyer ,  Kumar Srinivasan ,  Bob Dale Brown

    发明人： David Aaron Schwartz ,  William J. Daily ,  Brian Patrick Dwyer ,  Kumar Srinivasan ,  Bob Dale Brown

    IPC分类号： C12N15/09 ,  A61K9/127 ,  C07C237/06 ,  C07C237/10 ,  C07C237/22 ,  C07K5/06 ,  C07K5/068 ,  C07K5/09 ,  C07C233/05

    CPC分类号： B82Y5/00 ,  A61K9/1272 ,  C07C237/06 ,  C07C237/10 ,  C07C237/22 ,  C07K5/06086 ,  C07K5/0815

    摘要： The present invention provides novel amide-based cationic lipids of the general structure: ##STR1## or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R.sub.1 is H or a lipophilic moiety; (c) R.sub.2, R.sub.3, and R.sub.4 are positively charged moieties, or at least one but not all of R.sub.2, R.sub.3, or R.sub.4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X.sup.- is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R.sub.3 or R.sub.4 must have an alkyl moiety of at least 10 carbon atoms.The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.

    摘要翻译： 本发明提供了一般结构的新型酰胺类阳离子脂质：或其盐或溶剂合物或其对映体，其中： （a）Y是1至约20个碳原子的直链或亚烷基; （b）R 1为H或亲油部分; （c）R 2，R 3和R 4为带正电荷的部分，或至少一个但不全部为R 2，R 3或R 4为正部分，其余独立地选自H，1至约6个碳原子的烷基部分 原子或约5至约10个碳原子的杂环部分; （d）n和p独立地选自0至8的整数，使得n和o的和为1至16; （e）X-是阴离子或聚阴离子，（f）m是0至等于脂质上存在的正电荷数的整数; 条件是如果Y是直链，并且n和p之和为1，则R3或R4之一必须具有至少10个碳原子的烷基部分。 本发明还提供了这些脂质与聚阴离子大分子的组合物，利用这些组合物干扰细胞中的蛋白质表达的方法和用于制备该组合物的试剂盒。

    Methylphosphonate dimer synthesis
    5.
    发明授权
    Methylphosphonate dimer synthesis 失效
    甲基膦酸二聚体合成

    公开(公告)号：US5789576A

    公开(公告)日：1998-08-04

    申请号：US353530

    申请日：1994-12-09

    申请人： William J. Daily ,  David Aaron Schwartz

    发明人： William J. Daily ,  David Aaron Schwartz

    IPC分类号： C07H19/04 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C07H19/04

    摘要： Processes for the stereospecific synthesis of 2',2"-bis(deoxy)di-nucleosides and for the stereoselective synthesis of 2',2"-bis(substituted) dinucleosides are provided. Also provided are activated 2'-substituted-nucleoside alkylphosphonate active esters useful in the synthesis of these dinucleosides.

    摘要翻译： 提供了2'，2“ - 双（脱氧）二核苷的立体有择合成方法和2'，2” - 双（取代）二核苷的立体选择性合成方法。 还提供了用于合成这些二核苷的活化的2'-取代 - 核苷烷基膦酸酯活性酯。

    Amide-based cationic lipids
    6.
    发明授权
    Amide-based cationic lipids 失效
    酰胺类阳离子脂质

    公开(公告)号：US06638529B2

    公开(公告)日：2003-10-28

    申请号：US10046332

    申请日：2002-01-14

    申请人： David Aaron Schwartz ,  William J. Daily ,  Brian Patrick Dwyer ,  Kumar Srinivasan ,  Bob Dale Brown

    发明人： David Aaron Schwartz ,  William J. Daily ,  Brian Patrick Dwyer ,  Kumar Srinivasan ,  Bob Dale Brown

    IPC分类号： A61K9127

    CPC分类号： B82Y5/00 ,  A61K9/1272 ,  C07C237/06 ,  C07C237/10 ,  C07C237/22 ,  C07K5/0215 ,  C07K5/06086 ,  C07K5/0815

    摘要： The present invention provides novel amide-based cationic lipids of the general structure: or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R1 is H or a lipophilic moiety; (c) R2, R3, and R4 are positively charged moieties, or at least one but not all of R2, R3, or R4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X− is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R3 or R4 must have an alkyl moiety of at least 10 carbon atoms. The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.

    摘要翻译： 本发明提供了一般结构的新型酰胺类阳离子脂质：或其盐或溶剂合物或其对映体，其中： （a）Y是1至约20个碳原子的直链或亚烷基; （b）R 1为H或亲油部分; （c）R 2，R 3和R 4为带正电荷的部分，或至少一个但不全部为R 2，R 3或R 4为正部分，其余为独立选自H，1至约6个碳原子的烷基部分 原子或约5至约10个碳原子的杂环部分; （d）n和p独立地选自0至8的整数，使得n和o的和为1至16; （e）X 1是阴离子或聚阴离子，（f）m是0至等于脂质上存在的正电荷数的整数; 条件是如果Y是直链，n和p的和为1，则R3或R4中的一个必须具有至少10个碳原子的烷基部分。本发明还提供这些脂质与聚阴离子大分子的组合物，方法 用于干扰利用这些组合物的细胞中的蛋白质表达和用于制备其的试剂盒。

    Oligonucleoside cleavage compounds and therapies
    7.
    发明授权
    Oligonucleoside cleavage compounds and therapies 失效
    寡核苷切割化合物和疗法

    公开(公告)号：US5854410A

    公开(公告)日：1998-12-29

    申请号：US223355

    申请日：1994-03-31

    申请人： Lyle J. Arnold, Jr. ,  Mark A. Reynolds ,  David A. Schwartz ,  William J. Daily

    发明人： Lyle J. Arnold, Jr. ,  Mark A. Reynolds ,  David A. Schwartz ,  William J. Daily

    IPC分类号： C07H21/00 ,  C12N15/113 ,  C07H21/04 ,  C12Q1/68

    CPC分类号： C12N15/113 ,  C07H21/00 ,  C12N2310/3125 ,  C12N2310/334 ,  C12N2310/3511 ,  C12N2310/3515 ,  C12N2310/53

    摘要： Methods and compounds for selective cleavage of nucleic acid are described. The compounds generally contain three functionalities: (1) an oligonucleoside portion which is substantially complementary to at least a portion of the target nucleic acid, thereby providing selectivity to the compound; (2) a non-complementary portion which replaces one of the otherwise-complementary nucleoside bases in the oligonucleoside and which serves to place the target nucleic acid strand into a conformation that favors the cleavage of a phosphodiester linkage opposite the non-complementary portion; and (3) a cleavage moiety which possesses one or more and preferably two or more of the features of (a) proton donation, (b) proton acceptance, (c) hydrogen bonding, (d) charge neutralization and (e) Lewis acidity. These compounds may be used for the study and treatment of diseases involving foreign genetic materials or alterations to or inappropriate expression of genomic DNA.

    摘要翻译： 描述了用于选择性切割核酸的方法和化合物。 化合物通常含有三个官能团：（1）寡核苷酸部分，其与目标核酸的至少一部分基本上互补，从而为化合物提供选择性; （2）替代寡核苷酸之一的其它互补核苷碱基的非互补部分，其用于将靶核酸链置于有利于与非互补部分相对的磷酸二酯键的切割的构象; （3）具有（a）质子供体，（b）质子接受，（c）氢键，（d）电荷中和和（e）路易斯酸度的一个或多个，优选两个或多个特征的切割部分 。 这些化合物可用于研究和治疗涉及外来遗传物质的疾病或基因组DNA的改变或不恰当的表达。