Invention Grant
US07605147B2 Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same 失效
无环核苷膦酸衍生物,其盐及其制备方法

Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same
Abstract:
The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1): in which represents single bond or double bond, R1, R2, R3, R7 and R8 are defined herein, Y represents —O—, —S—, —CH(Z)-, ═C(Z)-, —N(Z)-, ═N—, or —SiH(Z)-, wherein Z represents hydrogen, hydroxy or halogen, or represents C1-C7-alkyl, C1-C5-alkoxy, allyl, hydroxy-C1-C7-alkyl, C1-C7-aminoalkyl or phenyl, Q represents a group having the following formula: wherein X1, and X2 independently of one another represent hydrogen, amino, hydroxy or halogen, or represent C1-C7-alkyl, C1-C5-alkoxy, allyl, hydroxy-C1-C7-alkyl, phenyl or phenoxy each of which is optionally substituted by nitro or C1-C5-alkoxy, or represent C6-C10-arylthio which is optionally substituted by nitro, amino, C1-C6-alkyl or C1-C4-alkoxy, or represent C6-C12-arylamino, C1-C7-alkylamino, di(C1-C7-alkyl)amino, C3-C6-cycloalkylamino or a structure of wherein n denotes an integer of 1 or 2 and Y1 represents O, CH2 or N—R (R represents C1-C7-alkyl or C6-C12-aryl), which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.
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