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    • 3. 发明授权
    • Substituted N′-pyrrolo[1,2-a]quinoxalin-4-yl-hydrazides as anti-cancer agents
    • 取代的N'-吡咯并[1,2-a]喹喔啉-4-基 - 酰肼作为抗癌剂
    • US07947682B2
    • 2011-05-24
    • US11027465
    • 2004-12-29
    • Nouri NeamatiAntonio Garofalo
    • Nouri NeamatiAntonio Garofalo
    • C07D487/04A61K31/519A61P35/04
    • C07D487/04C07D471/14
    • Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Such compounds include a compound of Formula II, wherein R is H, alkyl, or halogen; R′ is H, alkyl, or halogen; X is CH or N; and Y comprises a homocyclic or heterocyclic ring. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression.
    • 用于治疗癌症的新型化合物和与血管生成功能相关的疾病。 这些化合物包括式II化合物,其中R是H,烷基或卤素; R'是H,烷基或卤素; X是CH或N; 并且Y包含一个或多个杂环。 还公开了制备化合物,药物组合物和含有化合物的包装产品的方法,使用这些分子治疗癌症的方法(例如,白血病,非小细胞肺癌,结肠癌,CNS癌,黑素瘤,卵巢癌 ,乳腺癌,肾癌和前列腺癌)和与血管发生功能相关的病症(例如年龄相关性黄斑变性,黄斑营养不良和糖尿病),监测治疗的方法,基因表达谱的方法和方法 调节基因表达。
    • 6. 发明授权
    • Thiazepine inhibitors of HIV-1 integrase
    • HIV-1整合酶的噻吗嗪抑制剂
    • US07015212B1
    • 2006-03-21
    • US10009210
    • 2000-05-10
    • Nouri NeamatiYves PommierAntonio GarofaloVito Nacci
    • Nouri NeamatiYves PommierAntonio GarofaloVito Nacci
    • C07D513/04A61K31/55A61P31/18
    • C07D513/04
    • The present invention discloses non-catechol compounds, such as thiazolothiazepines, and analogs and derivatives thereof, which are anti-integrase inhibitors. The compounds, which are useful as treatments for HIV disease, include compounds (I), (II), (III), or pharmaceutically acceptable salts thereof wherein A is thiazole, benzene, naphthalene, pyridine, pyrimidine, pyrazine, or quinoline; R is one or more of H, halogen, lower alkyl, lower alkoxy, NO2, lower ester or carboxylic acid; X—Y is CH2—S, S—CH2, CH2—O, CH2—S(O). S(O)—CH2, CH2—CH2, CH2—CH2—CH2, or CH2—CH2—CH2—CH2; R4 is H or hydroxy; R5 is H, phenyl, or alkylamine; W is S or O; and R6 is H, substituted or unsubstituted alkyl or amine; and Z is S, O, CH2, CH2CH2, or C═O.
    • 本发明公开了非邻苯二酚化合物,如噻唑并噻嗪类及其类似物及其衍生物,它们是抗整联酶抑制剂。 可用作HIV疾病治疗的化合物包括化合物(I),(II),(III)或其药学上可接受的盐,其中A是噻唑,苯,萘,吡啶,嘧啶,吡嗪或喹啉; R是H,卤素,低级烷基,低级烷氧基,NO 2,低级酯或羧酸中的一种或多种。 XY是CH 2 -S,S-CH 2,CH 2 -O,CH 2 -S( O)。 S(O)-CH 2 CH 2,CH 2 -CH 2,CH 2 -CH 2 CH 2 CH 2或CH 2 -CH 2 -CH 2 CH 2 CH 2, 2 R 4是H或羟基; R 5是H,苯基或烷基胺; W是S或O; R 6是H,取代或未取代的烷基或胺; Z是S,O,CH 2,CH 2 CH 2,或C-O。