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    Dual-use peptidase inhibitors as prodrugs for a therapy of inflammatory and other diseases
    8.
    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

    申请人： Siegfried Ansorge ,  Klaus Neubert ,  Ute Bank ,  Irene Reichstein ,  Jürgen Faust ,  Michael Täger ,  Petra Fuchs ,  Bianca Senns

    发明人： Siegfried Ansorge ,  Klaus Neubert ,  Ute Bank ,  Irene Reichstein ,  Jürgen Faust ,  Michael Täger ,  Petra Fuchs ,  Bianca Senns

    IPC分类号： A61K31/4439 ,  A61K31/444 ,  A61K31/427 ,  A61K31/4025 ,  C07D277/04 ,  C07D207/04 ,  C07D401/02 ,  C07D401/14 ,  C07D417/02 ,  C07D417/14

    CPC分类号： C07D277/04 ,  C07D295/185 ,  C07D417/12 ,  C07D417/14

    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。