Antiviral helioxanthin analogs
    3.
    发明授权
    Antiviral helioxanthin analogs 有权
    抗病毒螺甲黄素类似物

    公开(公告)号:US07754718B2

    公开(公告)日:2010-07-13

    申请号:US11579284

    申请日:2005-05-02

    IPC分类号: A61K31/502 C07D237/26

    摘要: The present invention relates to novel antiviral helioxanthin analogs. These compounds may particularly be used alone or in combination with other drugs for the treatment of the following: hepadnaviruses, flaviviruses, herpesviruses and human immunodeficiency virus. In addition, compounds according to the present invention can be used to prevent or reduce the likelihood of the occurrence of tumors secondary to virus infection as well as other infections or disease states that are secondary to the virus infection.

    摘要翻译: 本发明涉及新的抗病毒螺甲黄素类似物。 这些化合物可以单独使用或与其他药物组合使用,用于治疗以下物质:肝素病毒,黄病毒,疱疹病毒和人类免疫缺陷病毒。 此外,根据本发明的化合物可用于预防或减少继发于病毒感染的肿瘤以及其它感染或继发于病毒感染的疾病状态的可能性。

    Method of treating cancer and other conditions or disease states using L-cytosine nucleoside analogs
    5.
    发明授权
    Method of treating cancer and other conditions or disease states using L-cytosine nucleoside analogs 有权
    使用L-胞嘧啶核苷类似物治疗癌症和其他病症或疾病状态的方法

    公开(公告)号:US07951788B2

    公开(公告)日:2011-05-31

    申请号:US11992044

    申请日:2006-11-22

    申请人: Yung-chi Cheng

    发明人: Yung-chi Cheng

    IPC分类号: A01N43/04 A61K31/70

    摘要: The present invention relates to the use of the compound according to formula (I) Where S is (A) or (B); X is H or F; R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or a phosphodiester group, a (C) or (D) group; Where Nu is a radical of a biologically active compound such as an anticancer, antihyperproliferative or antiviral compound such that an amino group or hydroxyl group from said biologically active agent forms a phosphate, phosphoramidate, carbonate or urethane group with the adjacent moiety; Each R8 is independently H, or a C1-C20 alkyl or ether group, preferably H or a C1-C2 alkyl group; k is 0-12, preferably, 0-2; R2 is H, an acyl group or a C1-C20 alkyl or ether group; and pharmaceutically acceptable salts, solvates or polymorphs thereof for the treatment of tumors, cancer and hyperproliferative diseases, among other conditions or disease states.

    摘要翻译: 本发明涉及式(I)化合物的用途,其中S为(A)或(B); X为H或F; R1是H,酰基,C1-C20烷基或醚基,磷酸酯,二磷酸酯,三磷酸酯或磷酸二酯基,(C)或(D)基团; 其中Nu是生物活性化合物如抗癌,抗增白或抗病毒化合物的基团,使得所述生物活性剂的氨基或羟基与相邻部分形成磷酸酯,氨基磷酸酯,碳酸酯或氨基甲酸酯基团; 每个R 8独立地是H或C 1 -C 20烷基或醚基,优选H或C 1 -C 2烷基; k为0-12,优选为0-2; R2是H,酰基或C1-C20烷基或醚基; 和其药学上可接受的盐,溶剂合物或多晶型物,用于治疗肿瘤,癌症和过度增殖性疾病等疾病状态。

    Process for inhibiting herpes simplex virus-specified thymidine kinase
    6.
    发明授权
    Process for inhibiting herpes simplex virus-specified thymidine kinase 失效
    抑制单纯疱疹病毒特异性胸苷激酶的方法

    公开(公告)号:US5008252A

    公开(公告)日:1991-04-16

    申请号:US28507

    申请日:1987-03-20

    IPC分类号: A61K31/045

    摘要: The invention relates to a method of selectively inhibiting herpes simplex virus-specified thymidine kinase. The method comprises exposing mammalian cells infected with the virus to an effective amount of 5'-ethynylthymidine. The invention further relates to a pharmaceutical composition comprising 5'-ethynylthymidine as the active ingredient together with a pharmaceutically acceptable carrier.

    摘要翻译: 本发明涉及一种选择性抑制单纯疱疹病毒特异性胸苷激酶的方法。 该方法包括将感染病毒的哺乳动物细胞暴露于有效量的5'-乙炔基胸苷。 本发明还涉及包含5'-乙炔基胸苷作为活性成分以及药学上可接受的载体的药物组合物。

    Compounds and methods to increase anti-p-glycoprotein activity of baicalein by alkylation on the a ring
    9.
    发明申请
    Compounds and methods to increase anti-p-glycoprotein activity of baicalein by alkylation on the a ring 有权
    通过在环上烷基化增加黄芩素的抗β-糖蛋白活性的化合物和方法

    公开(公告)号:US20070161605A1

    公开(公告)日:2007-07-12

    申请号:US10586822

    申请日:2005-01-31

    CPC分类号: C07D311/32 C07D311/30

    摘要: The present invention is directed to analogs of baicalein according to formula (I): where R5 is H, (C1-C12)alkyl, (C2-C13)acyl, or an optionally substituted phenyl or benzyl group, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group; R6 and R7 are each independently H, (C1-C12)alkyl, (C2-C13)acyl, or an optionally substituted phenyl or benzyl or together form a —OCR1R2O— group wherein each of R1 and R2 is independently H, a C1-C3 alkyl group or an optionally substituted phenyl or benzyl group; and R8 is H, OH, an O-acyl group, a C1,-C4 alkyl or alkoxy group, F, Cl, Br or I, or a pharmaceutically acceptable salt thereof, which exhibit anti-P-glycoprotein activity and methods of enhancing the bioavailability of active compounds, especially orally administered compounds, by inhibition of P-glycoprotein 170 (P-gp 170) and/or CYP450 enzyme, especially CYP450 3A4 enzyme. Pharmaceutical compositions based upon these novel derivatives according to the present invention are also described herein.

    摘要翻译: 本发明涉及式(I)的黄芩素类似物:其中R 5是H,(C 1 -C 12) 烷基,(C 2 -C 13)酰基或任选取代的苯基或苄基,酰基,C 1 -C 3烷基 烷基或醚基,磷酸酯,二磷酸酯,三磷酸酯或磷酸二酯基; R 6和R 7各自独立地为H,(C 1 -C 12 - )烷基,(C 1 -C 12) 酰基或任选取代的苯基或苄基,或一起形成-OCR 1 R 12, O-基团,其中R 1和R 2各自独立地为H,C 1 -C 3 - 基团或任选取代的苯基或苄基; R 8是H,OH,O-酰基,C 1〜C 4烷基或烷氧基,F,Cl ,Br或I,或其药学上可接受的盐,其通过抑制P-糖蛋白170(P-gp 170)和/或其衍生物来显示抗P-糖蛋白活性和增强活性化合物,特别是口服给药化合物的生物利用度的方法, 或CYP450酶,特别是CYP450 3A4酶。 基于本发明的这些新型衍生物的药物组合物也在本文中描述。