发明授权
EP1159271B1 ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
有权
ANIVIRALE 2.4嘧啶二酮衍生物及其生产工艺
- 专利标题: ANTIVIRAL 2,4-PYRIMIDINEDIONE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
- 专利标题(中): ANIVIRALE 2.4嘧啶二酮衍生物及其生产工艺
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申请号: EP00908087.0申请日: 2000-03-03
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公开(公告)号: EP1159271B1公开(公告)日: 2004-08-25
- 发明人: SON, Jong, Chan , SHIN, Seun, Shil , KIM, Shin, Keol , LEE, Chong, Kyo , KIM, Hae, Soo
- 申请人: Korea Research Institute of Chemical Technology
- 申请人地址: 100, Jang-dong, Yuseong-gu Daejeon 305-343 KR
- 专利权人: Korea Research Institute of Chemical Technology
- 当前专利权人: Korea Research Institute of Chemical Technology
- 当前专利权人地址: 100, Jang-dong, Yuseong-gu Daejeon 305-343 KR
- 代理机构: Lorenz, Werner, Dr.-Ing.
- 优先权: KR9907165 19990304
- 国际公布: WO2000051990 20000908
- 主分类号: C07D239/04
- IPC分类号: C07D239/04 ; A61K31/495 ; A61P31/18
摘要:
2,4-pyrimidinedione derivatives of formula (I) having high antiviral activity against wild-type and mutant HIV-1 and low toxicity are useful for treating AIDS (I) wherein: R1 is a C¿6-10? aryl or C3-10 heteroaryl group optionally having one or more substituents selected from the group consisting of halogen, C1-6 alkyl, C1-6 alkyl substituted with one or more halogen atoms, C3-6 cycloalkyl, cyano, nitro, hydroxy, thiohydroxy, azido, C1-6 alkoxy, oximino, C1-3 alkyloximino, O-(C1-6 alkyl)-substituted oximino, C-1-6 alkylcarbonyl, C3-6 cycloalkylcarbonyl, hydroxymethyl, azidomethyl, C1-6 alkoxymethyl, C1-6 acyloxymethyl, carbamoyloxymethyl, aminomethyl, N-(C1-3 alkyl) aminomethyl, N,N-di(C1-3 alkyl) aminomethyl, carboxy, C1-6 alkoxycarbonyl, aziridine, amino, hydroxyethylamino, cyclopropylamino, C1-6 alkylamino, di(C1-6 alkyl) amino, trifluoroacetamido, C1-6 acylamido, carbamoyl, hydroxyethylcarbamoyl, cyclopropylcarbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl) carbamoyl, aminocarbamoyl, dimethylaminocarbamoyl, hydrazino, 1,1-dimethylhydrazino, imidazolyl, triazolyl and tetrazolyl; a tetrahydropyridyl or piperidyl group optionally substituted with a C1-6 alkyl or C1-6 alkoxycarbonyl group; a tetrahydropyranyl group; or a tetrahydrofuryl group; R?2¿ is hydrogen, halogen, nitro, cyano, C¿1-3? alkoxycarbonyl, C1-3 alkylamino, di(C1-3 alkyl) amino, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl, C1-6 alkyl, C3-6 cycloalkyl or benzyl; R?3 and R4¿ are each independently hydrogen, halogen, hydroxy, cyano, nitro, amino, acetamido, trifluoroacetamido, azido, C¿1-3? alkyl, C1-3 alkyl substituted with one or more halogen atoms, C1-3 alkoxycarbonyl, carbamoyl, C1-3 alkylcarbamoyl, di(C1-3 alkyl) carbamoyl or C1-3 alkoxy; A is O or S; and Z is O, S, C=O, NH or CH2.
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