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    [4,5]-fused-3,6-disubstituted-pyridazines with sulfur-containing substituents in position three for the treatment of neoplasia
    5.
    发明授权
    [4,5]-fused-3,6-disubstituted-pyridazines with sulfur-containing substituents in position three for the treatment of neoplasia 失效
    [4,5] - 三位含硫取代基的3,6-二取代哒嗪用于治疗瘤形成

    公开(公告)号：US06486158B1

    公开(公告)日：2002-11-26

    申请号：US09875107

    申请日：2001-06-06

    申请人： Xiaojing Wang ,  Gerhard Sperl ,  Paul Gross ,  Rifat Pamukcu ,  Gary A. Piazza

    发明人： Xiaojing Wang ,  Gerhard Sperl ,  Paul Gross ,  Rifat Pamukcu ,  Gary A. Piazza

    IPC分类号： C07D47104

    CPC分类号： C07D237/30 ,  C07D237/32

    摘要： [4,5]-Fused-3,6 disubstituted-pydidazines of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia: wherein Y1 and Y2 are independently selected from the group consisting of (CH2)n,—C(X)—NH—,—(CH2)n—C(X)—O—, and X is O or S; R1 is selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, and substituted or unsubstituted phenyl, pyridinyl, and the like; R2 is selected from the group consisting of substituted or unsubstituted phenyl, benzyl, pyridinyl, and the like; “A” is a benzene ring fused with the pyridazine ring; and R3 is independently selected in each instance form the group consisting of halogen, lower alkyl, and the like.

    摘要翻译： [4,5] - 式I的3,6-二取代哒嗪可用于诱导或促进凋亡和阻止不受控制的肿瘤细胞增殖，并且特别可用于阻滞和治疗瘤形成：其中Y 1和Y 2被独立地选择 由（CH 2）n，-C（X）-NH - ， - （CH 2）n C（X）-O-，X为O或S组成的组; R 1选自低级烷基，低级 烯基，低级炔基和取代或未取代的苯基，吡啶基等; R2选自取代或未取代的苯基，苄基，吡啶基等;“A”是与哒嗪环稠合的苯环 ; R 3各自独立地选自卤素，低级烷基等。

    Methods for using a phosphodiesterase in pharmaceutical screening to identify compounds for treatment of neoplasia
    6.
    发明授权
    Methods for using a phosphodiesterase in pharmaceutical screening to identify compounds for treatment of neoplasia 失效
    在药物筛选中使用磷酸二酯酶鉴定用于治疗瘤形成的化合物的方法

    公开(公告)号：US6156528A

    公开(公告)日：2000-12-05

    申请号：US216070

    申请日：1998-12-19

    申请人： Rifat Pamukcu ,  Gary A. Piazza

    发明人： Rifat Pamukcu ,  Gary A. Piazza

    IPC分类号： C12Q1/26 ,  C12Q1/44 ,  C12Q1/533 ,  G01N33/50

    CPC分类号： C12Q1/44 ,  C12Q1/26 ,  C12Q1/533 ,  G01N33/5011

    摘要： This invention provides a method to identify compounds potentially useful for the treatment of neoplasia in mammals. The phosphodiesterase inhibitory activity of a compound is determined along with COX inhibitory activity. Growth inhibitory and apoptosis inducing effects on cultured tumor cells are also determined. Compounds that exhibit phosphodiesterase inhibiton, growth inhibition and apoptosis induction, but not substantial prostaglandin inhibitory activity, are desirable for the treatment of neoplasia.

    摘要翻译： 本发明提供了鉴定潜在地可用于治疗哺乳动物瘤形成的化合物的方法。 确定化合物的磷酸二酯酶抑制活性与COX抑制活性。 还测定了对培养的肿瘤细胞的生长抑制和凋亡诱导作用。 表现出磷酸二酯酶抑制，生长抑制和细胞凋亡诱导但不是实质性前列腺素抑制活性的化合物对于治疗瘤形成是理想的。