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    Process for labeling nucleic acids and hybridization probes
    4.
    发明授权
    Process for labeling nucleic acids and hybridization probes 失效
    标记核酸和杂交探针的方法

    公开(公告)号：US4617261A

    公开(公告)日：1986-10-14

    申请号：US791332

    申请日：1985-10-25

    申请人： Edward L. Sheldon, III ,  Corey H. Levenson ,  Kary B. Mullis ,  Henry Rapoport ,  Robert M. Watson

    发明人： Edward L. Sheldon, III ,  Corey H. Levenson ,  Kary B. Mullis ,  Henry Rapoport ,  Robert M. Watson

    IPC分类号： C07D493/04 ,  C07D513/04 ,  C07D519/00 ,  C07H21/00 ,  C12Q1/68 ,  G01N33/48

    CPC分类号： C07D493/04 ,  C07D513/04 ,  C07H21/00 ,  C12Q1/68 ,  Y10T436/143333

    摘要： Nucleic acids may be labeled by intercalating the alkylating intercalation moiety of a labeling reagent into a partially double-stranded nucleic acid to form a complex and activating the complex to cause covalent bonding between the reagent and the nucleic acid. Preferably, the labeled nucleic acid is a hybridization probe for detecting nucleic acid sequences capable of hybridizing with a hybridizing region of the nucleic acid. Also preferably the label moiety is non-radioactive. The labeling reagent is of the formula:[A--[B--Lwhere A is an alkylating intercalation moiety, B is a divalent organic moiety of the formula: ##STR1## where Y is O, NH or N--CHO, x is a number from 1 to 4, y is a number from 2 to 4, and L is a monovalent label moiety, wherein B is exclusive of any portion of the intercalation and label moieties.Preferably A is a 4-methylene-substituted psoralen moiety, and most preferably A is a 4'-methylene-substituted-4,5',8-trimethylpsoralen moeity and L is biotin.

    摘要翻译： 可以通过将标记试剂的烷基化插层部分嵌入部分双链核酸中以形成复合物并激活复合物以引起试剂和核酸之间的共价键来标记核酸。 优选地，标记的核酸是用于检测能够与核酸的杂交区域杂交的核酸序列的杂交探针。 还优选地，标记部分是非放射性的。 标记试剂具有下式：[A- [BL，其中A是烷基化插层部分，B是下式的二价有机部分：其中Y是O，NH或N-CHO，x是从 1至4，y为2至4的数，L为单价标记部分，其中B不包括插层和标记部分的任何部分。 优选A是4-亚甲基取代的补骨脂素部分，最优选A是4'-亚甲基取代的-4,5'，8-三甲基肉桂酸酯，L是生物素。

    Process for labeling nucleic acids using psoralen derivatives
    5.
    发明授权
    Process for labeling nucleic acids using psoralen derivatives 失效
    使用补骨脂素衍生物标记核酸的方法

    公开(公告)号：US4582789A

    公开(公告)日：1986-04-15

    申请号：US683263

    申请日：1984-12-18

    申请人： Edward L. Sheldon, III ,  Corey H. Levenson ,  Kary B. Mullis ,  Henry Rapoport

    发明人： Edward L. Sheldon, III ,  Corey H. Levenson ,  Kary B. Mullis ,  Henry Rapoport

    IPC分类号： C07D493/04 ,  C07D513/04 ,  C07D519/00 ,  C07H21/00 ,  C12Q1/68 ,  G01N33/566

    CPC分类号： C07D493/04 ,  C07D513/04 ,  C07H21/00

    摘要： A labeling reagent of the formula:[A][B]Lis prepared where A is an alkylating intercalation moiety, B is a divalent organic spacer arm moiety with a straight chain of at least two carbon atoms, and L is a monovalent label moiety capable of producing a detectable signal, e.g., a signal detectable by spectroscopic, photochemical, chemical, immunochemical or biochemical means. Preferably A is a 4'-methylene-substituted psoralen moiety, and most preferably A is a 4'-methylene-substituted 4,5',8-trimethylpsoralen moiety.This reagent may be used to label nucleic acids, preferably DNA, by intercalating the alkylating intercalation moiety of the reagent into an at least partially double-stranded nucleic acid to form a complex and activating the complex to cause covalent bonding between the reagent and the nucleic acid. Preferably, the labeled nucleic acid is a hybridization probe for detecting nucleic acid sequences capable of hybridizing with a hydridizing region of the nucleic acid. Also preferably the label moiety is non-radioactive.This reagent may also be used in chromosome banding to label specific regions of chromosomes and thereby differentiate them.

    Psoralen compounds
    7.
    发明授权
    Psoralen compounds 失效
    补骨脂素化合物

    公开(公告)号：US06420570B1

    公开(公告)日：2002-07-16

    申请号：US09767611

    申请日：2001-01-22

    申请人： Susan Wollowitz ,  Stephen T. Isaacs ,  Henry Rapoport ,  Hans Peter Spielmann

    发明人： Susan Wollowitz ,  Stephen T. Isaacs ,  Henry Rapoport ,  Hans Peter Spielmann

    IPC分类号： C07D49300

    CPC分类号： C07D493/04 ,  A01N1/0215 ,  A01N43/90 ,  A61K31/365 ,  A61K31/37 ,  A61K41/0019 ,  A61K41/0066 ,  A61L2/0011

    摘要： Psoralen compound compositions are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which yet permit their binding to nucleic acid of pathogens. Reaction conditions that photoactivate these bound psoralens result in covalent crosslinking to nucleic acid, thereby inactivating the pathogen. Higher psoralen binding levels and lower mutagenicity results in safer, more efficient, and reliable inactivation of pathogens. In addition to the psoralen compositions, the invention contemplates inactivating methods using the new psoralens.

    摘要翻译： 合成补骨脂素化合物组合物，其在补骨脂素的4,4'，5'和8位上具有取代，其仍然允许它们与病原体的核酸结合。 激活这些结合的补骨脂素的反应条件导致与核酸的共价交联，从而使病原体灭活。 更高的补骨脂素结合水平和较低的致突变性导致更安全，更有效和可靠的病原体失活。 除了补骨脂素组合物之外，本发明考虑使用新的补骨脂素的灭活方法。