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    Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders
    7.
    发明公开
    Quinazoline derivatives as histamine H4-receptor inhibitors for use in the treatment of inflammatory disorders 审中-公开
    Chinazolin-Derivate als Histamin H4-Rezeptor Inhibitor zur Behandlung vonentzündlichenErkrankungen

    公开(公告)号：EP2270002A1

    公开(公告)日：2011-01-05

    申请号：EP09251594.9

    申请日：2009-06-18

    申请人： Vereniging voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek en Patiëntenzorg

    发明人： The designation of the inventor has not yet been filed

    IPC分类号： C07D405/04 ,  C07D409/04 ,  C07D295/033 ,  A61K31/517 ,  A61P29/00

    CPC分类号： C07D405/04 ,  C07D239/95 ,  C07D409/04

    摘要： Compounds that modulate the histamine H 4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H 4 receptor, e.g. inflammation, are of formula (I)

    Wherein
    R2 is H or NRxRy, where Rx and Ry are each independently selected from H, C 1-6 alkyl and (CH 2 ) 1-3 C 3-7 cycloalkyl; or Rx and Ry, together with the nitrogen atom to which they are bound form a 4, 5 or 6 membered heterocyclic group;
    NR'R" is one of the following moieties, wherein R' and R" are taken together or separately as defined by each of one said moieties:

    q is 0 or 1;
    p is 0 or 1;
    r is 0 or 1;
    s is 0 or 1;
    Ra is H or OH or F;
    Rb and Rc are each independently H or C 1-3 alkyl;
    Rd is H or OH or NH 2 ;
    Re and Rf are each methyl, or Re and Rf taken together form a methylene or ethylene bridge; and
    R 7 and R 8 are independently selected form H, F, Cl, Br, I, C 1-4 alkyl, C 2-5 alkenyl, C 2-5 alkynyl, C 1-4 alkoxy, C 1-4 alkylthio, (CH 2 ) 0-3 C 3-7 cycloalkyl, O-C 3-6 cycloalkyl, phenyl, benzyl, O-phenyl, NH-phenyl, S-phenyl, O-C 1-4 alkyl-phenyl, C 1-4 alkyl-phenyl, CF 3 , O-CF 3 , S-CF 3 , hydroxy, nitro, cyano, O-C 1-4 alkyl-N(CH 3 ) 2 , and NRmRn, wherein Rm and Rn are independently selected from H, C 1-4 alkyl, phenyl, benzyl and phenethyl, and wherein any phenyl, alkyl or cycloalkyl moiety is optionally substituted with 1 to 3 substituents selected from C 1-3 alkyl, halogen, hydroxy, amino and C 1-3 alkoxy;
    or pharmaceutically acceptable salt, ester, or solvate thereof.

    摘要翻译： 调节组胺H 4受体并可用于治疗或预防组胺H 4受体介导的病症和病症的化合物，例如， 炎症，具有式（I）其中R2是H或NRxRy，其中Rx和Ry各自独立地选自H，C 1-6烷基和（CH 2）1-3 C 3-7环烷基; 或Rx和Ry与它们所连接的氮原子一起形成4,5或6元杂环基; NR'R“是以下部分之一，其中R'和R”一起或分开，如所述部分中的每一个所定义：q为0或1; p为0或1; r为0或1; s为0或1; Ra为H或OH或F; Rb和Rc各自独立地为H或C 1-3烷基; Rd为H或OH或NH 2; Re和Rf各自为甲基，或者Re和Rf一起形成亚甲基或乙烯桥; R 7和R 8独立地选自H，F，Cl，Br，I，C 1-4烷基，C 2-5烯基，C 2-5炔基，C 1-4烷氧基，C 1-4烷硫基， （CH 2）0-3 C 3-7环烷基，OC 3-6环烷基，苯基，苄基，O-苯基，NH-苯基，S-苯基，OC 1-4烷基 - 苯基，C 1-4烷基 - 苯基 ，CF 3，O-CF 3，S-CF 3，羟基，硝基，氰基，OC 1-4烷基-N（CH 3）2和NR m R n，其中R m和R n独立地选自H，C 1-4 烷基，苯基，苄基和苯乙基，其中任何苯基，烷基或环烷基部分任选被1至3个选自C 1-3烷基，卤素，羟基，氨基和C 1-3烷氧基的取代基取代; 或其药学上可接受的盐，酯或溶剂化物。