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    DERIVATIVES OF UREA AND RELATED DIAMINES, METHODS FOR THEIR MANUFACTURE, AND USES THEREFOR
    1.
    发明公开
    DERIVATIVES OF UREA AND RELATED DIAMINES, METHODS FOR THEIR MANUFACTURE, AND USES THEREFOR 审中-公开
    尿素及相关二胺，制造方法的衍生物及其用途

    公开(公告)号：EP2041103A2

    公开(公告)日：2009-04-01

    申请号：EP07765216.2

    申请日：2007-07-10

    申请人： Galapagos SAS ,  Amgen, Inc

    发明人： DEPREZ, Pierre ,  LIVELY, Sarah ,  TEMAL-LAIB, Taoues

    IPC分类号： C07D277/48 ,  C07D277/82 ,  C07D417/12 ,  A61K31/17 ,  A61K31/426 ,  A61K31/428 ,  C07C275/18 ,  C07C275/28

    CPC分类号： C07D277/48 ,  C07C275/42 ,  C07C2601/14 ,  C07C2603/18 ,  C07D277/82 ,  C07D417/12

    摘要： Compounds of formula (I): Z is >CH-, >C=CH- or >N-, R1 and R2 are optionally substituted and are the same or different, and each represents an aryl group, a heteroaryl group, or Z, R1 and R2 form a fused ring structure of formula: in which A represents a single bond, or linking group, R3 represents hydrogen, a group selected from: -AIkCOOR, -AIkNR7R8, -AIkCONR7R8, -AIkCOR9, -AIkSO2NR10R10', -AIkOR10, and -AIkS(O)nR10, in which AIk is alkyl, R is hydrogen or alkyl, R7 and R8 each represents H, optionally substituted alkyl, alkylaminoalkyl or dialkylaminoalkyl, or CONR7R8 forms an optionally substituted heterocycle, and R10 and R10 are hydrogen atom, optionally substituted alkyl, an alkylaminoalkyl group, an optionally substituted cycle, optionally spaced by an AIk group as defined, Q represents >C=0 or >C=S, R5 is a hydrogen atom or an alkyl, alkoxy, hydroxyalkyl, alkylthio, or thioalkyl group, p is 1, 2 or 3, q is 0, 1 or 2, R6 represents an optionally substituted aryl or heteroaryl group, and salts and esters thereof, are useful as calcimimetics in therapy.

    摘要翻译： 式（I）的化合物：Z是> CH - ，> C = CH-或> N-，R 1和R 2任选地substituiertem并且它们是相同的或不同的，并且每个darstellt芳基，杂芳基，或者 Z，R 1和R 2形成下式的稠环结构：其中A代表单键，或连接基团，R 3 darstellt氢，基团选自：-AlkCOOR，-AlkNR 7 R 8，R 7 -AlkCONR 8，-AlkCOR 9，-AlkSO 2 NR 10 R 10”，-AlkOR1O，和-AlkS（O）N R 10，在其中Alk是烷基，R是氢或烷基，R 7和R 8各自darstellt H，任选 取代的烷基，烷基氨基烷基，或二烷基氨基烷基，或CONR 7 R 8组的形式在任选取代的杂环，且R“°和R 10”是氢原子，任选取代的烷基，在烷基氨基烷基，任选substituiertem循环，任选地被烷基隔开 所定义的，q darstellt> C = O或> C = S，R 5是氢原子或烷基，烷氧基，羟烷基，烷硫基，或硫代烷基，p是1，2或3，q为0，1或2个 中，R 6可选darstellt到 LY substituiertem芳基或杂芳基，和其盐和酯，如在治疗拟钙剂有用。