Substituted pyrazin-2-yl-sulphonamide (-3-pyridyl) compounds and uses thereof
    21.
    发明授权
    Substituted pyrazin-2-yl-sulphonamide (-3-pyridyl) compounds and uses thereof 有权
    取代的吡嗪-2-基 - 磺酰胺(-3-吡啶基)化合物及其用途

    公开(公告)号:US06258817B1

    公开(公告)日:2001-07-10

    申请号:US09504364

    申请日:2000-02-15

    IPC分类号: A01N4360

    摘要: The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

    摘要翻译: 本发明涉及药学上有用的式I化合物,其中A1,A2,A3,A4,B1,m,Ar,W,X,Y,Z和R1具有本文定义的任何含义及其药学上可接受的盐, 和含有它们的药物组合物。 新型化合物具有内皮素受体拮抗剂活性,并且可用于例如治疗疾病或医学病症,其中升高或异常水平的内皮素起重要作用。 本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。

    Pyridine compounds which have useful pharmaceutical activity
    24.
    发明授权
    Pyridine compounds which have useful pharmaceutical activity 失效
    具有有用药物活性的吡啶化合物

    公开(公告)号:US5641793A

    公开(公告)日:1997-06-24

    申请号:US440133

    申请日:1995-05-12

    CPC分类号: C07D213/76

    摘要: The invention concerns pharmaceuticaly useful compounds of the formula I, in which Q, A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutically compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

    摘要翻译: 本发明涉及式I的药用有用化合物,其中Q,A 1,A 2,A 3,R 1,R 2,R 3和R 4具有本文定义的任何含义及其药学上可接受的盐和含有它们的药物组合物。 新化合物具有内皮素受体拮抗剂活性,可用于治疗高血糖或异常水平的内皮素起重要作用的疾病或医学病症。 本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。

    QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS
    26.
    发明申请
    QUINAZOLINE DERIVATIVES AS ANTICANCER AGENTS 审中-公开
    喹诺酮衍生物作为反应剂

    公开(公告)号:US20090239861A1

    公开(公告)日:2009-09-24

    申请号:US12067415

    申请日:2006-09-14

    摘要: A quinazoline derivative of the Formula I: wherein the substituents are as defined in the text for use in the production of an anti-proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm-blooded animal such as man.

    摘要翻译: 式I的喹唑啉衍生物:其中取代基如用于产生抗增殖作用的文本中所定义,其作用单独或部分通过在温血动物中抑制erbB2受体酪氨酸激酶产生,例如 人。

    Pyrimidine compounds
    29.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号:US06710052B2

    公开(公告)日:2004-03-23

    申请号:US10203549

    申请日:2002-08-08

    IPC分类号: C07D23948

    CPC分类号: C07D239/47 C07D417/12

    摘要: Pyrimidine derivatives of the formula (I) wherein: one of Q1 and Q2 or both of Q1 and Q2 is substituted on a ring carbon by one substituent of the formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH— link]; wherein Q1, Q2, G, R1, X, Y1, Y2, Z, n and m are as described within; and pharmaceutically acceptable salts and in vivo hydrolyzable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.

    摘要翻译: 式(I)的嘧啶衍生物其中:Q1和Q2中的一个或Q1和Q2两者在环碳上被式(Ia)的一个取代基取代[条件是当在Q1中存在式(Ia)的取代基时, 不与-NH-链接相邻]; 其中Q 1,Q 2,G,R 1,X,Y 1,Y 2,Z,n和m如上所述; 和其药学上可接受的盐和体内可水解的酯。 还描述了其制备方法,药物组合物及其作为细胞周期蛋白依赖性丝氨酸/苏氨酸激酶(CDK)和粘着斑激酶(FAK)抑制剂的用途。