L-ascorbic acid 2-phosphate zinc salt and process for manufacturing the same
    2.
    发明授权
    L-ascorbic acid 2-phosphate zinc salt and process for manufacturing the same 失效
    L-抗坏血酸2-磷酸锌盐及其制造方法

    公开(公告)号:US06420419B1

    公开(公告)日:2002-07-16

    申请号:US09095895

    申请日:1998-06-11

    IPC分类号: A61K31341

    CPC分类号: A61K31/665 C07D307/62

    摘要: L-Ascorbic acid 2-phosphate zinc salt and a salt hydrate thereof having excellent solubility and exhibiting good stability even under weakly acidic conditions. Also disclosed is a process of manufacturing L-ascorbic acid 2-phosphate zinc salt by displacing a cation of a salt of an L-ascorbic acid 2-phosphate other than a zinc salt with a zinc cation. Further disclosed is a composition containing L-ascorbic acid 2-phosphate zinc salt or a salt hydrate thereof as an active ingredient.

    摘要翻译: L-抗坏血酸2-磷酸锌盐及其盐水合物,即使在弱酸性条件下也具有优异的溶解性和良好的稳定性。 还公开了通过用锌阳离子置换除了锌盐之外的L-抗坏血酸2-磷酸盐的阳离子来制造L-抗坏血酸2-磷酸锌盐的方法。 进一步公开了含有L-抗坏血酸2-磷酸锌盐或其盐水合物作为活性成分的组合物。

    Silicon compounds derived from ascorbic acid
    5.
    发明授权
    Silicon compounds derived from ascorbic acid 失效
    衍生自抗坏血酸的硅化合物

    公开(公告)号:US06780888B1

    公开(公告)日:2004-08-24

    申请号:US10111537

    申请日:2002-05-24

    IPC分类号: A61K31341

    摘要: The invention concerns novel silicon compounds derived from ascorbic acid consisting of a silicon-containing chain or of silanes, comprising at least a radical A of formula (I) wherein: at least one of the radicals L is a divalent radical for fixing A on the silicon chain. The invention further concerns methods for preparing said compounds, compositions, in particular cosmetic or pharmaceutical, containing them, and their use as antioxidant and/or anti-free radical agent, particularly for treating oxidant stress, for treating the effects of exposure to the sun and for preventing ageing.

    摘要翻译: 本发明涉及衍生自由含硅链或硅烷组成的抗坏血酸的新型硅化合物,其至少包含式(I)的基团A,其中:基团L中的至少一个是用于将A固定的二价基团 硅链。 本发明还涉及制备所述化合物,组合物,特别是含有它们的化妆品或药物的方法,以及它们作为抗氧化剂和/或抗自由基剂的用途,特别是用于治疗氧化应激,用于治疗暴露于太阳的作用 并防止老化。

    Method for treating inflammatory diseases by administering a thrombin inhibitor
    7.
    发明授权
    Method for treating inflammatory diseases by administering a thrombin inhibitor 失效
    通过施用凝血酶抑制剂治疗炎性疾病的方法

    公开(公告)号:US06232315B1

    公开(公告)日:2001-05-15

    申请号:US09407821

    申请日:1999-09-28

    IPC分类号: A61K31341

    摘要: The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof. The invention is also a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor and an NSAID, e.g., a COX-2 inhibitor. Such diseases include but are not limited to nephritis, systemic lupus, erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylene-carboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof and the COX-2 inhibitor is 3-phenyl-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明是治疗患者炎性疾病的方法,其包括用包含凝血酶抑制剂的组合物治疗患者。 这些疾病包括但不限于肾炎,系统性红斑狼疮,类风湿性关节炎,肾小球性肾炎和囊状病。 在一类方法中,凝血酶抑制剂选自3-(2-苯乙基氨基)-6-甲基-1-(2-氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基)-2-吡嗪酮,N ' - [[1-(氨基亚氨基甲基)-4-哌啶基]甲基] -N-(3,3-二苯基丙酰基)-L-脯氨酸酰胺和3-(2-苯乙基氨基)-6-甲基-1-(2- 氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基)-2-吡啶酮或其药学上可接受的盐。本发明还是一种治疗患者炎症性疾病的方法,其包括用包含凝血酶抑制剂和NSAID的组合物治疗患者 ,例如COX-2抑制剂。 这些疾病包括但不限于肾炎,系统性红斑狼疮,红斑狼疮,类风湿性关节炎,肾小球性肾炎和囊性疾病。 在一类方法中,凝血酶抑制剂选自3-(2-苯乙基氨基)-6-甲基-1-(2-氨基-6-甲基-5-亚甲基 - 甲酰胺基甲基吡啶基)-2-吡嗪酮 ,N' - [[1-(氨基亚氨基甲基)-4-哌啶基]甲基] -N-(3,3-二苯基丙酰基)-L-脯氨酰胺和3-(2-苯乙基氨基)-6-甲基-1-( 2-氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基)-2-吡啶酮或其药学上可接受的盐,COX-2抑制剂是3-苯基-4-(4-(甲基磺酰基)苯基)-2-(5H) - 呋喃酮或其药学上可接受的盐。

    Prenyl transferase inhibitors
    10.
    发明授权
    Prenyl transferase inhibitors 失效
    丙烯酰转移酶抑制剂

    公开(公告)号:US06586461B1

    公开(公告)日:2003-07-01

    申请号:US09334704

    申请日:1999-06-16

    申请人: Richard A. Gibbs

    发明人: Richard A. Gibbs

    IPC分类号: A61K31341

    摘要: Farnesyl diphosphate analogs, specifically the 3-substituted alcohol precursors of the diphosphate analogs, 3-allylfarnesol and 3-vinylfarnesol, are potent inhibitors of mammalian protein fanesyltransferase (FTase). 3-allylgeranylgeraniol is a highly specific cellular inhibitor of protein geranylgeranylation (GGTase I). Furthermore, these compounds are able to efficiently block the anchorage-dependent growth of ras transformed cells. While 3-allylfarnesol inhibits protein farnesylation in situ, 3-vinylfarnesol instead leads to the abnormal prenylation of proteins with the 3-vinylfarnesyl group. In a similar manner, treatment with 3-allylgeranylgeraniol inhibits protein geranylgeranylation while 3-vinylgeranylgeraniol restores protein geranylgeranylation in cells.

    摘要翻译: 法呢基二磷酸类似物,特别是二磷酸酯类似物的3-取代醇前体,3-烯丙基法呢醇和3-乙烯基法呢醇是哺乳动物蛋白质扇形转移酶(FTase)的有效抑制剂。 3-烯丙基香叶基香叶醇是一种高度特异性的蛋白质香叶基香叶基化细胞抑制剂(GGTase I)。 此外,这些化合物能够有效阻断ras转化细胞的依赖于锚定依赖的生长。 虽然3-烯丙基法呢醇原位抑制蛋白质法呢基,但3-乙烯基法呢醇代替导致3-乙烯基法呢基的蛋白异戊二烯化。 以类似的方式,用3-烯丙基ger牛儿基香叶醇处理抑制蛋白质香叶基香叶基化,而3-乙烯基ger牛儿基甘油还原细胞中的蛋白质香叶基香叶基化。