Pyrazolopyrimidine derivatives which are angiotensin II receptor
antagonists
    8.
    发明授权
    Pyrazolopyrimidine derivatives which are angiotensin II receptor antagonists 失效
    作为血管紧张素II受体拮抗剂的吡唑并嘧啶衍生物

    公开(公告)号:US5389632A

    公开(公告)日:1995-02-14

    申请号:US21897

    申请日:1993-02-24

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: The present invention relates to the derivatives of the formula ##STR1## and their tautomeric forms, as well as their addition salts, and to their use in therapeutics, especially for the treatment and prevention of cardiovascular diseases and in particular for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall, especially atherosclerosis.

    摘要翻译: 本发明涉及式(I)的衍生物及其互变异构形式及其加成盐,以及它们在治疗学中的用途,特别是用于治疗和预防心血管疾病,特别是针对 治疗高血压,心功能不全和动脉壁疾病,特别是动脉粥样硬化。

    3-arylquinazoline derivatives as selective estrogen receptor beta modulators
    10.
    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。