Compositions and methods for combination antiviral therapy
    3.
    发明申请
    Compositions and methods for combination antiviral therapy 审中-公开
    用于组合抗病毒治疗的组合物和方法

    公开(公告)号:US20060246130A1

    公开(公告)日:2006-11-02

    申请号:US10540794

    申请日:2004-01-13

    摘要: The present invention relates to therapeutic combinations of [2-(6-amino-purin-9 yl)-1-methyl-ethoxymethyl]-phosphonic acid diisopropoxycarbonyloxymethyl ester (tenofovir disoproxil fumarate, Viread®) and (2R,5S,cis)-4-amino-5-fluoro-1-(2 hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, Emtriva™, (−)-cis FTC) and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of tenofovir disoproxil fumarate and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

    摘要翻译: 本发明涉及[2-(6-氨基 - 嘌呤-9基)-1-甲基 - 乙氧基甲基] - 膦酸二异丙氧基羰基氧基甲基酯(替诺福韦来氟米尔富马酸盐,和)(2R,5S,顺式 )-4-氨基-5-氟-1-(2-羟甲基-1,3-氧硫杂环戊烷-5-基) - (1H) - 嘧啶-2-酮(恩曲他滨,Emtriva TM,( - ) - 顺式 FTC)及其生理功能衍生物。 这些组合可用于治疗HIV感染,包括具有对核苷和/或非核苷抑制剂的抗性的HIV突变体的感染。 本发明还涉及替诺福韦地索普西富马酸和恩曲他滨的组合的药物组合物和制剂及其生理功能衍生物,以及这些组合物和制剂的使用的治疗方法。

    Compositions and methods for combination antiviral therapy
    4.
    发明申请
    Compositions and methods for combination antiviral therapy 审中-公开
    用于组合抗病毒治疗的组合物和方法

    公开(公告)号:US20060234982A1

    公开(公告)日:2006-10-19

    申请号:US10540782

    申请日:2004-01-13

    IPC分类号: A61K31/675 A61K31/513

    摘要: The present invention relates to therapeutic combinations of [9-[R-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]-phenoxyphosphinyl]methoxy]propyl]adenine (GS-7340) and (2R, 5S, cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (emtricitabine, (−)-cis FTC, Emtriva™ and their physiologically functional derivatives. The combinations may be useful in the treatment of HIV infections, including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors. The present invention is also concerned with pharmaceutical compositions and formulations of said combinations of GS-7340 and emtricitabine, and their physiologically functional derivatives, as well as therapeutic methods of use of those compositions and formulations.

    摘要翻译: 本发明涉及[9- [R-2 - [[(S) - [[(S)-1-(异丙氧基羰基)乙基]氨基] - 苯氧基氧膦基]甲氧基]丙基]腺嘌呤(GS-7340) 和(2R,5S,顺式)-4-氨基-5-氟-1-(2-羟甲基-1,3-氧硫杂环戊烷-5-基) - (1H) - 嘧啶-2-酮(恩曲他滨,( - ) -cis FTC,Emtriva TM及其生理功能衍生物,这些组合可用于治疗HIV感染,包括具有对核苷和/或非核苷抑制剂具有抗性的HIV突变体的感染,本发明还涉及 所述GS-7340和恩曲他滨组合的药物组合物和制剂及其生理功能衍生物,以及这些组合物和制剂的使用的治疗方法。

    Antiviral phosphonomethoxy nucleotide analogs having increased oral
bioavailability
    10.
    发明授权
    Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability 有权
    具有增加的口服生物利用度的抗病毒膦酰基甲氧基核苷酸类似物

    公开(公告)号:US6069249A

    公开(公告)日:2000-05-30

    申请号:US314607

    申请日:1999-05-19

    IPC分类号: C07F9/6512 C07F9/6561

    CPC分类号: C07F9/65616 C07F9/65121

    摘要: Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure --OC(R.sup.2).sub.2 OC(O)X(R).sub.a, wherein R.sup.2 independently is H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR.sup.3 in which R.sup.3 is C.sub.1 -C.sub.12 alkyl; X is N or O; R is independently H, C.sub.1 -C.sub.12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, --O--, --N.dbd., --NR.sup.4 --, --N(R.sup.4).sub.2 -- or OR.sup.3, R.sup.4 independently is --H or C.sub.1 -C.sub.8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR.sup.3. The compounds are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy of prophylaxis. Embodiments are particularly useful when administered orally.

    摘要翻译: 提供新的化合物,其包含抗病毒膦基甲氧基核苷酸类似物与具有结构-OC(R 2)2 OC(O)X(R)a的碳酸酯和/或氨基甲酸酯的酯,其中R2独立地为H,C1-C12烷基,芳基,烯基 炔基,烷基芳基,炔基芳基,烷芳基,芳基炔基,芳基烯基或芳烷基,其未被取代或被卤素,叠氮基,硝基或OR 3取代,其中R 3是C 1 -C 12烷基; X为N或O; R是独立的H,C 1 -C 12烷基,芳基,烯基,炔基,链烯基芳基,炔基芳基,烷芳基,芳基炔基,芳基烯基或芳烷基,其未被取代或被卤素,叠氮基,硝基,-O - , - N = - , - N(R4)2-或OR3,R4独立地是-H或C1-C8烷基,条件是至少一个R不是H; 和a为1或2,条件是当a为2且X为N时,(a)两个R基团可以一起形成碳环或含氧杂环,或(b)一个R另外可以是OR 3 。 该化合物可用作制备抗病毒化合物或寡核苷酸的中间体,或者可用于直接给患者预防用于抗病毒治疗的患者。 当口服给药时,实施方案特别有用。