Antiviral phosphoramidates
    4.
    发明申请
    Antiviral phosphoramidates 有权
    抗病毒氨基磷酸

    公开(公告)号:US20070042988A1

    公开(公告)日:2007-02-22

    申请号:US11503558

    申请日:2006-08-11

    CPC分类号: C07H19/10 C07H19/04

    摘要: The invention provides novel nucleoside compounds of formula I wherein R1, R2a, R2b, R3, R4, R5, R6, R8a, R9 and R10 are as defined herein which are useful for the treatment of Hepatitis C Virus (HCV) mediated diseases. The invention further provides methods for treatment or prophylaxis of HCV mediated diseases with compounds of formula I and pharmaceutical compositions comprising these compounds,

    摘要翻译: 本发明提供了式I的新型核苷化合物,其中R 1,R 2,R 2,R 2b,R 3, R 4,R 5,R 6,R 8a,R 9和R 9,和 R 10如本文所定义,其可用于治疗丙型肝炎病毒(HCV)介导的疾病。 本发明还提供了用式I化合物治疗或预防HCV介导的疾病的方法和包含这些化合物的药物组合物,

    Nucleoside aryl phosphoramidates and their use as anti-viral agents for the treatment of hepatitis C virus
    5.
    发明授权
    Nucleoside aryl phosphoramidates and their use as anti-viral agents for the treatment of hepatitis C virus 失效
    核苷芳基氨基磷酸酯及其作为抗病毒药物用于治疗丙型肝炎病毒的用途

    公开(公告)号:US08658616B2

    公开(公告)日:2014-02-25

    申请号:US12516253

    申请日:2007-11-23

    CPC分类号: C07H19/20

    摘要: Compounds having the general formula (I): are provided which have enhanced inhibitory potency and are thus useful in methods of prophylaxis or treatment of a viral infection such as hepatitis C virus. The compounds are phosphoramidate derivatives of nucleoside compounds derived from bases such as adenine and guanine. The glycoside moiety of the nucleoside compound can be substituted at the ss-2′ position with methyl and the phosphoramidate group can be 1-naphthyl linked by —O— to the P atom. These compounds can be administered as pharmaceutical compositions, and methods for their preparation are also provided.

    摘要翻译: 提供具有通式(I)的化合物,其具有增强的抑制效力,因此可用于预防或治疗病毒感染如丙型肝炎病毒的方法。 这些化合物是衍生自诸如腺嘌呤和鸟嘌呤的碱的核苷化合物的氨基磷酸衍生物。 核苷化合物的糖苷部分可以在β-2'位被甲基取代,氨基磷酸酯基可以通过-O-连接到P原子上的1-萘基。 这些化合物可以作为药物组合物施用,并且还提供了它们的制备方法。

    Phosphoramidate compounds and methods of use
    7.
    发明授权
    Phosphoramidate compounds and methods of use 有权
    氨基磷酸酯化合物及其使用方法

    公开(公告)号:US07951787B2

    公开(公告)日:2011-05-31

    申请号:US10560887

    申请日:2004-07-20

    CPC分类号: C07H19/10

    摘要: Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an α-amino acid moiety. The α-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.

    摘要翻译: 描述了核苷酸的氨基磷酸衍生物及其在治疗癌症中的用途。 例如,脱氧尿苷,阿糖胞苷,吉西他滨和西酞胺中的每一个的碱基部分可以在5-位被取代。 氨基磷酸酯部分已经连接到P原子上的芳基-O部分和α-氨基酸部分。 α-氨基酸部分可以对应于或衍生自天然存在的或非天然存在的氨基酸。

    Anti-Viral Pyrimidine Nucleoside Derivatives
    8.
    发明申请
    Anti-Viral Pyrimidine Nucleoside Derivatives 有权
    抗病毒嘧啶核苷衍生物

    公开(公告)号:US20100222295A1

    公开(公告)日:2010-09-02

    申请号:US12226044

    申请日:2007-05-09

    摘要: A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.

    摘要翻译: 用于治疗或预防病毒感染的化合物,例如由水痘带状疱疹病毒引起的水痘或带状疱疹,所述具有通式(II)的化合物:其中X是O,S,NH或CH 2,Y 是O,S或NH,Z是O,S或CH 2,R 1是C 1-6烷基,优选正烷基,例如正戊基或正己基,R 2和R 3之一是OH,另一个是 R3和R2是中性的,非极性的氨基酸部分,或其药学上可接受的盐或水合物。 所述中性,非极性氨基酸部分R 2或R 3可以是(Ⅳ):其中R 4,R 5,R 6和R 7各自独立地为H或C 1-2烷基。 在优选的实施方案中,R2或R3之一是缬氨酸,亮氨酸,异亮氨酸或丙氨酸,特别是缬氨酸。

    Phosphoramidate derivatives of nucleoside compounds for use in the treatment of cancer
    9.
    发明申请
    Phosphoramidate derivatives of nucleoside compounds for use in the treatment of cancer 有权
    用于治疗癌症的核苷化合物的氨基磷酸衍生物

    公开(公告)号:US20090215715A1

    公开(公告)日:2009-08-27

    申请号:US11886931

    申请日:2006-03-16

    CPC分类号: C07H19/20

    摘要: Phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludaribine and clofarabine have enhanced therapeutic potency in homo sapiens, in particular, enhanced potency with respect to a cancer such as leukaemia. Suitably the phosphoramidate is substituted at the P atom by Ar—O, where Ar is aryl or heteroaryl, either of which may be optionally substituted. Formula (I).

    摘要翻译: 核苷化合物如克拉屈滨,异克立哌啶,氟达拉滨和氯法拉滨的氨基磷酸衍生物具有增强的智力治疗效力,特别是增强白血病等癌症的效力。 适当地,氨基磷酸酯在P原子被Ar-O取代,其中Ar是芳基或杂芳基,其中任一个可以是任选取代的。 式(I)。