Fluorescent dyes
    7.
    发明授权
    Fluorescent dyes 有权
    荧光染料

    公开(公告)号:US08604204B2

    公开(公告)日:2013-12-10

    申请号:US13733324

    申请日:2013-01-03

    IPC分类号: C07D417/02 C12Q1/00

    摘要: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified to provide beneficial properties.

    摘要翻译: 本发明提供可用于检测或定量所需靶分子(例如蛋白质,核酸和细胞器器)的染料,活性染料和标记试剂。 提供可以在染料与靶分子的结合提供信号产生的溶液中游离的染料。 还提供了包含可用于将染料连接到将与所需靶分子结合的探针的反应性基团的染料。 已经对本发明的新型染料进行了改进以提供有益的性质。

    Dual-use peptidase inhibitors as prodrugs for a therapy of inflammatory and other diseases
    10.
    发明授权
    Dual-use peptidase inhibitors as prodrugs for a therapy of inflammatory and other diseases 失效
    双用肽酶抑制剂作为治疗炎症和其他疾病的前药

    公开(公告)号:US08470855B2

    公开(公告)日:2013-06-25

    申请号:US12085096

    申请日:2006-11-10

    摘要: Compounds of the general formulae (1) and (2) A-B-D-B′-A′  (1) and A-B-D-E  (2) in which A and A′ may be identical or different and are the residue in which X is S, O, CH2, CH2CH2, CH2O or CH2NH, and Y is H or CN, and * designates a chiral carbon atom preferably in S- or L-configuration; B and B′ may be identical or different and are an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkylene residue, cycloalkylene residue, aralkylene residue, heterocycloalkylene residue, heteroarylalkylene residue, arylamidoalkylene residue, heteroarylamidoalkylene residue, unsubstituted or mono- or poly-substituted arylene residue or heteroarylene residue having one or more five-, six- or seven-membered ring(s); D is —S—S— or —Se—Se—; and E is the group —CH2—CH(NH2)—R9 or —CH2—*CH(NH2)—R9 respectively in which R9 is an O, N or S containing or non-containing, unsubstituted or substituted, unbranched or branched alkyl residue, cycloalkyl residue, aralkyl residue, heterocycloalkyl residue, heteroarylalkyl residue, arylamidoalkyl residue, heteroarylamidoalkyl residue, unsubstituted or mono- or poly-substituted aryl residue or heteroaryl residue having one or more five-, six- or seven-membered ring(s) and * designates a chiral carbon atom preferably in the S- or L-configuration; or the acid addition salts thereof with organic and/or inorganic acids; as well as to the use of the compounds of the general formulae (1) and (2) in medicine.

    摘要翻译: 通式(1)和(2)ABD-B'-A'(1)和ABDE(2)的化合物,其中A和A'可以相同或不同,并且是其中X是S,O, CH2,CH2CH2,CH2O或CH2NH,Y是H或CN,*表示手性碳原子,优选为S-或L-构型; B和B'可以相同或不同,是含有或不含,未取代或未取代的未支化或支链的亚烷基,亚环烷基,亚芳基残基,杂环亚烷基残基,杂芳基亚烷基残基,芳基酰氨基亚烷基残基,杂芳基酰氨基亚烷基残基 未取代的或单取代或多取代的亚芳基或具有一个或多个五元,六元或七元环的杂芳基残基; D是-S-S-或-Se-Se-; 并且E分别是基团-CH 2 -CH(NH 2)-R 9或-CH 2 - * CH(NH 2)-R 9,其中R 9是含有或不含有,未取代或取代的未支化或支链烷基的O,N或S 残基,环烷基残基,芳烷基残基,杂环烷基残基,杂芳基烷基残基,芳基酰氨基烷基残基,杂芳基氨基烷基残基,未取代的或单取代或多取代的芳基残基或具有一个或多个五元,六元或七元环的杂芳基残基, 和*表示优选为S-或L-构型的手性碳原子; 或其与有机和/或无机酸的酸加成盐; 以及在药物中使用通式(1)和(2)的化合物。