Dual-use peptidase inhibitors as prodrugs for a therapy of inflammatory and other diseases
    1.
    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。