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Method for the Treatment or prophylaxis of a viral infection by Flaviviridae, Orthomyxoviridae, Paramyxoviridae, or abnormal Cell Proliferation and use of modified Nucleosides

机译:治疗或预防黄病毒科,正粘病毒科,副粘病毒科或细胞增殖异常的病毒感染的方法以及使用修饰的核苷

摘要

Method for treating a Flaviviridae infection by a virus (including BVDV and HCV) (including influenza Orthomyxoviridae, paramyxoviridae (A and b) or including RSV), or conditions associated with an abnormal Cell Proliferation, in a host, including Animals, and especially Human Beings, which utilizes a nucleoside of formula (1S, 1b, 1c) - (2S, 2b, 2c)Or its enantiomer BETA L or its acceptable Salt or prodrug for pharmaceutical use: D, where each is Hydrogen, alkyl, acyl, monophosphate, diphosphate and triphosphate guanosine diphosphate Ester, Ester, Ester or amino acid phospholipid triphosphate; each W1 and W2 is CH or independently N; each x1 and x2 is independently Hydrogen, halogen (F, CL, Br or i), NH2, nhr4, nr4r4 ', nhor4,Nr4nr4 'R4', 'Oh, or4, SH or SR4, Y1 is o, s or Z; each is CH2 or NH; each R1 and R1 is independently Hydrogen, Lower alkyl, aryl alquinilo alquenilo Lower, Lower, alkylaryl, halogen (F, CL, Br or i), NH2, NHR5, nr5r5', nhor5, nr5nhr5 R5, nr5nr5 ',' 'Oh, OR5, sh, SR5, NO2, n Or, CH2OH, ch2or5, CO2H, co2r5, CONH2, conhr5,Conr5r5 'cn' Or 'independently; each R2 and R2 is Hydrogen or Halogen (F, CL, Br or i), Oh, sh, OCH3, Sch3, NH2, nhch3 = CH2, CH, CN, ch2nh2, CH2OH CO2H; R3, R3' and each is independently Hydrogen or Halogen (F, CL BR, or i), Oh, sh, Sch3, NH2 OCH3, CH3, C2H5, nhch3, = CH2, CH, CN, ch2nh2, CH2O H, CO2H; each R4, R4, R4, R5, R6, '' 'and' 'regardless R5 is Hydrogen, Lower alkyl,Lower alquenilo, aryl or arylalkyl as insustituido or substituted phenyl or benzyl; so that the General formula for the nucleoside (1S, 1b, 1c) or (2S, 2b, 2c) at least one of R2 and R2 is Hydrogen and at least one of R3 and R3 is Hydrogen, also it provides an effective process for Quantification of viral load and, in particular, The Viral Load of BVDV, HCV and West Nile virus.In a host, using a quantitative polymerase chain reaction (Real Time rt-pcr '' ''). In addition, we describe fluorescence probe molecules that can produce in proportion to the amount of virus in a sample.
机译:在宿主(包括动物,尤其是人类)中治疗病毒(包括BVDV和HCV)(包括流感正粘病毒科,副粘病毒科(A和b)或包括RSV)或与细胞增殖异常有关的疾病的黄病毒科感染的方法利用式(1S,1b,1c)-(2S,2b,2c)核苷或其对映异构体BETA L或其药学上可接受的盐或前药的生物:D,其中每个均为氢,烷基,酰基,一磷酸,二磷酸和三磷酸鸟苷二磷酸酯,酯,酯或氨基酸磷脂三磷酸; W1和W2各自为CH或独立为N; x1和x2各自独立地是氢,卤素(F,CL,Br或i),NH2,nhr4,nr4r4',nhor4,Nr4nr4'R4','Oh或or4,SH或SR4,Y1是o,s或Z;分别是CH2或NH;每个R1和R1独立地是氢,低级烷基,芳基alquinilo alquenilo低级,低级,烷基芳基,卤素(F,CL,Br或i),NH2,NHR5,nr5r5',nhor5,nr5nhr5 R5,nr5nr5',''Oh, OR5,sh,SR5,NO2,n Or,CH2OH,ch2or5,CO2H,co2r5,CONH2,conhr5,Conr5r5'cn'或'独立地;每个R 2和R 2是氢或卤素(F,CL,Br或i),Oh,sh,OCH 3,Sch 3,NH 2,nhch 3 = CH 2,CH,CN,ch 2 nh 2,CH 2 OH CO 2H。 R3,R3'且各自独立地为氢或卤素(F,CL BR或i),Oh,sh,Sch3,NH2 OCH3,CH3,C2H5,nhch3 = CH2,CH,CN,ch2nh2,CH2O H,CO2H;各个R 4,R 4,R 4,R 5,R 6,“′”和“ R 5”均与R 5无关,是氢,低级烷基,低级烷基,芳基或芳基烷基作为取代基或取代的苯基或苄基;因此,R 2和R 2中至少一个为氢,R 3和R 3中至少一个为氢的核苷(1S,1b,1c)或(2S,2b,2c)的通式也提供了一种有效的方法定量病毒载量,尤其是BVDV,HCV和西尼罗河病毒的病毒载量。在宿主中,使用定量聚合酶链反应(实时rt-pcr'''')。另外,我们描述了可以与样品中病毒数量成比例产生的荧光探针分子。

著录项

  • 公开/公告号AR035596A1

    专利类型

  • 公开/公告日2004-06-16

    原文格式PDF

  • 申请/专利权人 PHARMASSET LIMITED;

    申请/专利号AR2001P105106

  • 发明设计人

    申请日2001-10-31

  • 分类号A61K31/7052;A61P31/12;C07H19/00;C07H19/06;C07H19/10;C07H19/16;C07H19/20;

  • 国家 AR

  • 入库时间 2022-08-21 23:12:20

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