3-arylquinazoline derivatives as selective estrogen receptor beta modulators
    8.
    发明授权
    3-arylquinazoline derivatives as selective estrogen receptor beta modulators 有权
    3-芳基喹唑啉衍生物作为选择性雌激素受体β调节剂

    公开(公告)号:US07381730B2

    公开(公告)日:2008-06-03

    申请号:US10387666

    申请日:2003-03-13

    摘要: Novel quinazoline derivatives possessing activity as estrogen receptor beta (ERβ) modulators are provided which have the general formula I wherein X is O or S; A and B are each independently CR′″ or N; R, R′ and R″ are each independently hydrogen, alkyl, benzyl, p-methoxybenzyl, allyl, or Si(R4)3, wherein at least one of R, R′ and R″ is hydrogen; R′″ is hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R1, R2 and R3 are each independently hydrogen, halogen, CF3, OR5, S(O)nR6, NR7R8, cycloalkyl or alkyl; R4 is a alkyl; R5, R6, R7 and R8 in each functional group are each independently hydrogen, cycloalkyl or alkyl; and n is an integer from 0 to 2. In addition, a method is provided for preventing, inhibiting or treating the progression or onset of pathological conditions associated with the estrogen receptor and to pharmaceutical compositions containing such compounds.

    摘要翻译: 提供具有雌激素受体β(ERbeta)调节剂活性的新型喹唑啉衍生物,其具有通式I,其中X为O或S; A和B各自独立地为CR“或N; R,R'和R“各自独立地为氢,烷基,苄基,对甲氧基苄基,烯丙基或Si(R 4 N 3)3,其中至少一个 R,R'和R“是氢; R“'是氢,卤素,CF 3或OR 5,S(O)n R 6 R 6, NR 7 R 8,环烷基或烷基; R 1,R 2和R 3各自独立地为氢,卤素,CF 3或OR 3, 5,S(O)n R 6,NR 7 R 8,环烷基或烷基 ; R 4是烷基; 各官能团中的R 5,R 6,R 7和R 8分别独立地为氢,环烷基或 烷基; n为0-2的整数。此外,提供了用于预防,抑制或治疗与雌激素受体相关的病理状况的进展或发作的方法以及含有这些化合物的药物组合物。