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    DIOXOLANE THYMINE AND COMBINATIONS FOR USE AGAINST 3TC/ AZT RESISTANT STRAINS OF HIV
    2.
    发明公开
    DIOXOLANE THYMINE AND COMBINATIONS FOR USE AGAINST 3TC/ AZT RESISTANT STRAINS OF HIV 审中-公开
    二氧THYMINUND组合AGAINST 3TC / AZT耐药的HIV毒株

    公开(公告)号：EP1569659A4

    公开(公告)日：2009-03-25

    申请号：EP03812874

    申请日：2003-12-08

    申请人： UNIV GEORGIA RES FOUND ,  UNIV EMORY

    发明人： CHU CHUNG K ,  SCHINAZI RAYMOND F

    IPC分类号： A61K31/70 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/65 ,  A61K31/675 ,  A61K45/06 ,  A61P31/18

    CPC分类号： A61K45/06 ,  A61K31/505 ,  A61K31/513 ,  A61K31/52 ,  A61K31/65 ,  A61K31/675 ,  A61K31/70 ,  A61K2300/00

    摘要： The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate, diphosphate, triphosphate or phosphodiester group, for use in the treatment of HIV infections which exhibit resistance to 3TC and/or AZT. Preferably, compounds according to the present invention are combined with at least one anti-HIV agent which inhibits HIV by a mechanism other than through the inhibition of thymidine kinase (TK). These agents include those selected from among nucleoside reverse transcriptase inhibitors (NRTI), non-nucloeoside reverse transcriptase inhibitors, protease inhibitors, fusion inhibitors, among others. These agents are generally selected from the group consisting of 3TC (Lamivudine), AZT (Zidovudine), (-)-FTC, ddI (Didanosine), ddC (zalcitabine), abacavir (ABC), tenofovir (PMPA), D-D4FC (Reverset), D4T (Stavudine), Racivir, L-D4FC, NVP (Nevirapine), DLV (Delavirdine), EFV (Efavirenz), SQVM (Saquinavir mesylate), RTV (Ritonavir), IDV (Indinavir), SQV (Saquinavir), NFV (Nelfinavir), APV (Amprenavir), LPV (Lopinavir), fuseon and mixtures thereof. The TK dependent agents, such as AZT and D4T, may be used in combination with one of the dioloxane thymine compounds according to the present invention, but the use of such agents may be less preferred. In preferred compositions according to the present invention, Rl is preferably H or a C2-C18 acyl group or a monophosphate group. Pharmaceutical compositions and methods of reducing the likelihood that a patient at risk for contract an HIV infection will contract the infection are other aspects of the present invention.

    NEUROPROTECTIVE COMPOUNDS AND USES THEREOF
    9.
    发明公开
    NEUROPROTECTIVE COMPOUNDS AND USES THEREOF 失效
    NERVENSCHÜTZENDEVERBINDUNGEN UND IHRE VERWENDUNGEN

    公开(公告)号：EP1005334A4

    公开(公告)日：2001-09-19

    申请号：EP98918620

    申请日：1998-04-23

    申请人： CORNELL RES FOUNDATION INC ,  UNIV GEORGIA RES FOUND

    发明人： JOH TONG H ,  CHO SUNGHEE ,  CHU CHUNG K ,  DU JINFA

    IPC分类号： A61P9/00 ,  A61K31/165 ,  A61P25/00 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07C233/18 ,  C07C233/22

    CPC分类号： C07C233/18

    摘要： The present invention relates to a compound having formula (I) where X = R1O, F, Br, I, C1, or a C1 to C5 alkyl group; R1 = a C1 to C10 alkyl group or a C1 to C10 aryl group, n = 1 or 2, R2 = aC1 to C6 alkyl group, an amino acid, a heterocycle, a secondary or tertiary C3 to C4 hydrocarbon, or (a) where R3 = H or CH3, or pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions which include the compounds, as well as methods of making and using the compounds.

    摘要翻译： 本发明涉及具有下式的化合物：其中X = R1O，F，Br，I，C1或C1至C5烷基，R1 = C1至C10烷基或C1至C10芳基，n = 1或2，R2 = C1至C6烷基，氨基酸，杂环，仲或叔C3至C4烃，或其中R3 = H或CH3，或其药学上可接受的盐。 本发明还涉及包含化合物的药物组合物，以及制备和使用该化合物的方法。