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    Multi-mechanistic chemical cleavage using certain metal complexes
    4.
    发明授权
    Multi-mechanistic chemical cleavage using certain metal complexes 失效
    使用某些金属络合物进行多机械化学裂解

    公开(公告)号：US5798491A

    公开(公告)日：1998-08-25

    申请号：US458347

    申请日：1995-06-02

    申请人： Darren Magda ,  Jonathan L. Sessler

    发明人： Darren Magda ,  Jonathan L. Sessler

    IPC分类号： C12N15/09 ,  A61K31/40 ,  A61K31/70 ,  A61K41/00 ,  A61K47/48 ,  A61K48/00 ,  A61K49/00 ,  A61P31/12 ,  A61P35/00 ,  B01J31/18 ,  C07D487/22 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C12N15/113 ,  C07B61/00

    CPC分类号： C12N15/113 ,  A61K41/0038 ,  A61K41/0042 ,  A61K41/0076 ,  A61K47/48069 ,  A61K49/0021 ,  B01J31/1815 ,  C07D487/22 ,  C07H21/00 ,  B01J2531/025 ,  B01J2531/36 ,  C12N2310/15 ,  C12N2310/321 ,  C12N2310/3511

    摘要： The invention is directed to a particular class of metal complexes, specifically certain texaphyrin metal complexes, which both hydrolyze and photocleave RNA, and which also both hydrolyze RNA and photocleave DNA. In one embodiment, the present invention is directed to a method for both hydrolyzing and photocleaving a polymer of ribonucleic acid, the method comprising the steps of contacting the polymer of ribonucleic acid with a texaphyrin metal complex exhibiting catalytic activity for both hydrolysis and photocleavage of ribonucleic acid polymers, incubating the polymer and the metal complex under conditions and for a time sufficient to hydrolyze the phosphate ester bond of the polymer, and exposing the texaphyrin metal complex to light for a time sufficient to photocleave the polymer. In another embodiment of the present invention, the invention is directed to a method for both hydrolyzing a polymer of ribonucleic acid and photocleaving a polymer of deoxyribonucleic acid, the method comprising the steps of contacting a mixture of the ribonucleic acid polymer and the deoxyribonucleic acid polymer with a texaphyrin metal complex exhibiting catalytic activity for both hydrolysis of ribonucleic acid polymers and photocleavage of deoxyribonucleic acid polymers, incubating the polymer mixture and the metal complex under conditions and for a time sufficient to hydrolyze the phosphate ester bond of the ribonucleic acid polymer, and exposing the texaphyrin metal complex to light for a time sufficient to photocleave the deoxyribonucleic acid polymer.

    摘要翻译： 本发明涉及特定类别的金属络合物，特别是某些泰克萨菲瑞金属络合物，它们水解和脱色RNA，并且还水解RNA和光切割DNA。 在一个实施方案中，本发明涉及水解和光切割核糖核酸聚合物的方法，所述方法包括以下步骤：使核糖核酸的聚合物与表现出用于核糖核酸的水解和光切割的催化活性的泰克萨菲瑞金属络合物 酸性聚合物，在足以水解聚合物的磷酸酯键的条件和时间下孵育聚合物和金属络合物，并将泰克萨菲瑞金属络合物暴露于光下足以使聚合物光滑的时间。 在本发明的另一个实施方案中，本发明涉及水解核糖核酸聚合物和光切割脱氧核糖核酸聚合物的方法，该方法包括以下步骤：使核糖核酸聚合物和脱氧核糖核酸聚合物 具有表现出对核糖核酸聚合物的水解和脱氧核糖核酸聚合物的光切割的催化活性的特沙弗林金属络合物，在足以水解核糖核酸聚合物的磷酸酯键的条件和时间下孵育聚合物混合物和金属络合物，以及 将泰克萨菲芬金属络合物曝光一段足以使脱氧核糖核酸聚合物光滑的时间。

    Phosphoramidite derivatives of texaphyrins
    7.
    发明授权
    Phosphoramidite derivatives of texaphyrins 失效
    泰克萨菲瑞的亚磷酰胺衍生物

    公开(公告)号：US5633354A

    公开(公告)日：1997-05-27

    申请号：US614638

    申请日：1996-03-13

    申请人： Darren Magda ,  Jonathan L. Sessler ,  Brent L. Iverson ,  Petra I. Sansom ,  Shaun P. Crofts

    发明人： Darren Magda ,  Jonathan L. Sessler ,  Brent L. Iverson ,  Petra I. Sansom ,  Shaun P. Crofts

    IPC分类号： C07H21/00 ,  C07F7/00 ,  C07F9/6524 ,  C07D187/22

    CPC分类号： C07H21/00 ,  A61K47/48069

    摘要： The invention is directed to a method of incorporating expanded porphyrins, and particularly of incorporating a sapphyrin or a texaphyrin, before, during, or after chemical synthesis of an oligomer to form an expanded porphyrin-oligonucleotide conjugate, and particularly a sapphyrin- or texaphyrin-oligonucleotide conjugate. This method includes reacting derivatized nucleotides and a sapphyrin or a texaphyrin in a desired order in an automated or manual DNA synthesizer having a solid support to form a sapphyrin- or a texaphyrin-oligonucleotide conjugate.

    摘要翻译： 本发明涉及在低聚物的化学合成之前，期间或之后掺入膨胀的卟啉，特别是引入卟啉或特沙弗林的方法，以形成发泡的卟啉 - 寡核苷酸缀合物，特别是卟啉 - 或泰克萨菲瑞 - 寡核苷酸缀合物。 该方法包括在具有固体支持物的自动或手动DNA合成仪中以期望的顺序使衍生化的核苷酸与泰夫沙弗反应形成卟啉或泰克萨菲瑞 - 寡核苷酸缀合物。

    Reduced sp.sup.3 texaphyrins
    8.
    发明授权
    Reduced sp.sup.3 texaphyrins 失效
    减少sp3泰克萨菲

    公开(公告)号：US5504205A

    公开(公告)日：1996-04-02

    申请号：US280351

    申请日：1994-07-26

    申请人： Jonathan L. Sessler ,  Gregory W. Hemmi ,  Tarak D. Mody

    发明人： Jonathan L. Sessler ,  Gregory W. Hemmi ,  Tarak D. Mody

    IPC分类号： A61K31/40 ,  A61K41/00 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/04 ,  A61L2/00 ,  A61P35/00 ,  A61P43/00 ,  C07D487/22 ,  C07H17/02 ,  C07H21/00

    CPC分类号： A61K51/0485 ,  A61K41/0009 ,  A61K41/0038 ,  A61K41/0076 ,  A61K47/48069 ,  A61K49/0021 ,  A61K49/0036 ,  A61K49/0058 ,  A61K49/04 ,  A61K49/106 ,  A61K51/1093 ,  A61L2/0011 ,  C07D487/22 ,  C07H17/02 ,  C07H21/00

    摘要： The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.

    摘要翻译： 本发明涉及保持亲油性的水溶性羟基取代的泰克萨菲瑞，合成这些化合物及其用途。 这些膨胀的卟啉大环是二价和三价金属离子的有效螯合剂。 本发明的羟基取代的泰克萨菲瑞衍生物的各种金属（例如，转变，主要和镧系元素）络合物具有不寻常的水溶性和稳定性。 它们在生理上重要的区域（即690-880nm）中强烈吸收光。 它们具有增强的放松性，因此在磁共振成像中是有用的。 它们以高产率形成长寿命的三重态，并且作为产生单线态氧的光敏剂。 因此，它们可用于灭活或破坏感染了这种病毒以及肿瘤细胞的人类免疫缺陷病毒（HIV-1），单核细胞或其他细胞。 它们是水溶性的，但它们保持足够的亲脂性，以便对富含脂质的区域如动脉粥样化和肿瘤具有更大的亲和力。 它们可用于磁共振成像，随后光动力学肿瘤治疗治疗动脉粥样化和肿瘤。 这些性质加上其高的化学稳定性和在水中的明显的溶解度，增加了它们的用途。

    Sapphyrins, derivatives and syntheses
    10.
    发明授权
    Sapphyrins, derivatives and syntheses 失效
    SAPPHYRINS，衍生物和合成物

    公开(公告)号：US5159065A

    公开(公告)日：1992-10-27

    申请号：US454298

    申请日：1989-12-21

    申请人： Jonathan L. Sessler ,  Michael J. Cyr

    发明人： Jonathan L. Sessler ,  Michael J. Cyr

    IPC分类号： A61K41/00 ,  A61K47/48 ,  C07D487/22 ,  C07H15/26 ,  C07H21/00 ,  C12N15/10

    CPC分类号： C07D487/22 ,  A61K41/0076 ,  A61K47/48023 ,  A61K47/48069 ,  A61K47/48153 ,  C07H15/26 ,  C07H21/00 ,  C12N15/101

    摘要： The present invention involves, in addition to many unique substituted sapphyrins, a novel method for synthesizing sapphyrins with good efficiency and high yield. An improved 9-step synthesis of substituted sapphyrins, e.g., the two C.sub.2 symmetric sapphyrins, compounds 2 and 4 of FIG. 1C, is described herein. This synthesis involves as an important step the condensation between a tripyrrane diacid and a diformyl bipyrrole. The key tripyrrane component is prepared in three high-yield steps from readily available pyrrolic precursors and the bipyrrole portion is prepared in four steps from ethyl 3-methyl-4-methylpyrrole-2-carboxylate in roughly 33% yield overall.

    摘要翻译： 本发明除了许多独特的取代的莽草酮之外，还涉及以高效率和高收率合成卟啉的新方法。 取代的莽草酮的改进的9步合成，例如两个C2对称卟啉，图2的化合物2和4。 在此描述1C。 该合成涉及三氯二萜与二酰基双吡咯之间的缩合的重要步骤。 从容易获得的吡咯前体的三个高产率步骤中制备关键的三卤组分，并且从4-甲基-4-甲基吡咯-2-甲酸乙酯中分三步制备双吡咯部分，总产率为33％。