摘要:
The present invention relates to a novel nucleotide analogue having the general formula (I) and pharmaceutically acceptable salts, esters, or salt of such esters: wherein n, X, Q U R1′, R1, Z and R2 are defined here within. The compounds object of the present invention may be a single enantiomers or as mixtures of said enantiomers, the compounds may have a &agr;D, &agr;-L, &bgr;-D, &bgr;-L, R or S configuration at each chiral center or mixtures thereof. This invention also relates to pharmaceutical compositions containing them, alone or in combination with other therapeutic agents, and their use as antiviral agents, particularly against HIV and/or HBV infections in mammals.
摘要翻译:本发明涉及具有通式(I)的新型核苷酸类似物和这些酯的药学上可接受的盐,酯或盐:其中n,X,Q U R1',R1,Z和R2在此定义。 本发明的化合物可以是单一对映异构体或作为所述对映体的混合物,所述化合物可以在每个手性中心具有αD,α-L,β-D,β-L,R或S构型或其混合物。 本发明还涉及含有它们的单独或与其它治疗剂组合的药物组合物,以及它们作为抗病毒剂的用途,特别是用于哺乳动物中的HIV和/或HBV感染。
摘要:
Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.
摘要:
Disclosed are compounds of the formula wherein R1 is hydrogen or an acyl group having 1 to 16 carbon atoms; R2 is a purine or pyrimidine base or an analogue or derivative thereof; Z is O, S, S═O or SO2; and pharmaceutically acceptable derivatives thereof. Also described are processes for and intermediates of use in their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds in the antiviral treatment of mammals.
摘要翻译:公开了下式的化合物其中R 1是氢或具有1至16个碳原子的酰基; R 2是嘌呤或嘧啶碱基或其类似物或衍生物; Z是O,S,S-O或SO 2; 及其药学上可接受的衍生物。 还描述了其制备中使用的方法和中间体,含有这些化合物的药物组合物,以及这些化合物在哺乳动物的抗病毒治疗中的用途。
摘要:
Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH-halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;Q and U are independently selected from: O, S, and CH(R.sub.a) wherein R.sub.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6 alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.
摘要:
The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.
摘要:
Disclosed are compounds of the formula wherein R1 is hydrogen or an acyl group having 1 to 16 carbon atoms; R2 is a purine or pyrimidine base or an analogue or derivative thereof; Z is O, S, S═O or SO2; and pharmaceutically acceptable derivatives thereof. Also, described are process for and intermediates of use in their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds in the antiviral treatment of mammals.
摘要翻译:公开了下式的化合物其中R 1是氢或具有1至16个碳原子的酰基; R 2是嘌呤或嘧啶碱基或其类似物或衍生物; Z是O,S,S-O或SO 2; 及其药学上可接受的衍生物。 还描述了其制备中使用的方法和中间体,含有这些化合物的药物组合物,以及这些化合物在哺乳动物的抗病毒治疗中的用途。
摘要:
Nucleotide analogues having the general formula (I) and pharmaceutically acceptable derivatives: ##STR1## wherein n is 0 or an integer; X is O or S, CH.sub.2, CH-halogen, CH--N.sub.3, or C.dbd.CH.sub.2 ;Q and U are independently selected from: O, S, and CH(R.sub.a) wherein R.sub.a is hydrogen, OH, halogen, N.sub.3, NH.sub.2, SH, carboxyl, C.sub.1-6 alkyl or R.sub.a is CH.sub.2 (R.sub.b) wherein R.sub.b is hydrogen, OH, SH, NH.sub.2, C.sub.1-6 alkyl or carboxyl; or both Q and U are CH when Q and U are linked by a double bond;Z is selected from: O, a C.sub.1-6 alkoxy, a C.sub.1-6 thioalkyl, a C.sub.1-6 aminoalkyl, (CH.sub.2).sub.m wherein m is 0 or an integer, and N(R.sub.c).sub.2 wherein both R.sub.c are independently hydrogen or a C.sub.1-6 alkyl; andR2 is a purine or pyrimidine base or an analogue or derivative thereof. Members of this series of analogues possess anti-viral activity.
摘要:
This invention relates to novel substituted 1,3-oxathiolanes and substituted 1,3-dithiolanes or pharmaceutically acceptable salts and esters thereof, of the formula: ##STR1## wherein X is S, S.dbd.O, or SO.sub.2 ;Y is O, S, S.dbd.O, or SO.sub.2 ;R.sub.1 is hydrogen, trisubstituted silyl, C.sub.1-6 alkyl, aralkyl, or C.sub.1-6 acyl, and R.sub.2 is a pyrimidine base or an analogue or derivative thereof.This invention also relates to processes for preparing these compounds, intermediates useful in their preparation, to pharmaceutical compositions containing them and to the use of these compounds as antiviral agents.
摘要:
Use of a compound of formula (I) or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of hepatitis B is disclosed. ##STR1##
摘要:
Compounds represented by formula: wherein X, Y and Z are as defined herein, pharmaceutically acceptable salts thereof, and related compounds, are suitable for use in treating or preventing a Flaviviridae viral infection in a host.