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    • 10. 发明申请
    • HETEROCYCLIC COMPOUNDS THAT BLOCK THE EFFECTS OF ADVANCED GLYCATION END PRODUCTS (AGE)
    • 阻止高级糖果终产物(年龄)的影响的杂环化合物
    • WO2005040163A1
    • 2005-05-06
    • PCT/IB2004/003430
    • 2004-10-20
    • DR. REDDY'S LABORATORIES LTDYELESWARAPU, Koteswar, RaoMANOJIT, PalVEDULA MANOHAR, SharmaAKELLA, VenkateswarluPILLARISETTI, SivaramPADAKANTI, SrinivasKALLEDA, Srinivasa, Rao
    • YELESWARAPU, Koteswar, RaoMANOJIT, PalVEDULA MANOHAR, SharmaAKELLA, VenkateswarluPILLARISETTI, SivaramPADAKANTI, SrinivasKALLEDA, Srinivasa, Rao
    • C07D417/12
    • C04B35/632A61K31/427C07D215/56C07D239/88C07D239/90C07D311/30C07D401/12C07D417/12C07D417/14C07D487/04
    • The present invention relates to novel compounds of Formula (Ia) or (Ib), their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. Formula (Ia), or Formula (Ib) in the above formulae L represents Formula (I), Formula (II) or -(CH 2 ) 1 - Q represents Formula (III), or Formula (IV). The present invention also relates to a process for the preparation of the above said novel compounds, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to methods and compositions comprising compounds that treat pathophysiological conditions arising from inflammatory responses. In particular, the present invention is directed to compounds that inhibit or block glycated protein produced induction of the signaling-associated inflammatory responses in tissues, including endothelial cells. The present invention relates to compounds that inhibit smooth muscle proliferation. The present invention also relates to compounds that act as modulators of Perlecan activity and expression. In particular, the present invention is directed to compounds that inhibit smooth muscle cell proliferation by modulating heparan sulfate proteoglycans (HSPG) such as Perlecan. The present invention further relates to the use of compounds to treat vascular occlusive conditions characterized by smooth muscle proliferation such as stenosis, restenosis, neointimal hyperplasia, and atherosclerosis. The compounds of Formula (I) are also useful for the treatment and/or prevention of cancer. The types of cancers include melanoma, prostate, leukemia, lymphoma, non-small lung cancers, cancer of the central nervous system, breast, colon, ovarian or renal cancer.
    • 本发明涉及式(Ia)或(Ib)的新化合物,其药学上可接受的盐和含有它们的药学上可接受的组合物。 上式L中的式(Ia)或式(Ib)表示式(I),式(II)或 - (CH 2)1 -Q表示式(III)或式(IV)。 本发明还涉及制备上述新化合物,其药学上可接受的盐和含有它们的药物组合物的方法。 本发明还涉及包含治疗由炎性反应引起的病理生理状况的化合物的方法和组合物。 特别地,本发明涉及抑制或阻断糖化蛋白质在组织(包括内皮细胞)中产生信号传导相关炎症反应的诱导的化合物。 本发明涉及抑制平滑肌增殖的化合物。 本发明还涉及作为Perlecan活性和表达调节剂的化合物。 特别地,本发明涉及通过调节硫酸乙酰肝素蛋白聚糖(HSPG)如Perlecan来抑制平滑肌细胞增殖的化合物。 本发明还涉及化合物用于治疗以平滑肌增生为特征的血管闭塞状态,例如狭窄,再狭窄,新内膜增生和动脉粥样硬化。 式(I)的化合物也可用于治疗和/或预防癌症。 癌症的类型包括黑素瘤,前列腺癌,白血病,淋巴瘤,非小细胞肺癌,中枢神经系统癌症,乳腺癌,结肠癌,卵巢癌或肾癌。