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    • 4. 发明申请
    • 2,2-BIS(HYDROXYMETHYL)CYCLOPROPYLIDENEMETHYL - PURINES AND -PYRIMIDINES AS ANTIVIRAL AGENTS
    • 2,2-BIS(羟甲基)环丙基二乙烯基 - 嘌呤和嘧啶类作为抗病毒剂
    • WO2003104440A2
    • 2003-12-18
    • PCT/US2003/007916
    • 2003-03-14
    • WAYNE STATE UNIVERSITYTHE REGENTS OF THE UNIVERSITY OF MICHIGANZEMLICKA, JiriZHOU, ShaomanDRACH,John, C.
    • ZEMLICKA, JiriZHOU, ShaomanDRACH,John, C.
    • C12N
    • C07D239/36C07D239/54C07D473/18C07D473/30C07D473/34C07D473/40
    • Compounds which are active against viruses have the following formulas: Formula (I), Formula (II), wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino­6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-­6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-­6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.
    • 对病毒有活性的化合物具有下式:式(I),式(II),其中B是嘌呤或嘧啶杂环或碱基。 在优选的实施方案中,嘌呤包括6-氨基嘌呤(腺嘌呤),6-羟基嘌呤(次黄嘌呤),2-氨基-6-羟基嘌呤(鸟嘌呤),2,6-二氨基嘌呤,2-氨基-6-叠氮基嘌呤,2 2-氨基-6-氯嘌呤,2-氨基-6-氟嘌呤,2-氨基-6-氟代嘌呤,2-氨基-6-甲氧基嘌呤,2-氨基-6-环丙基氨基嘌呤,2 2-氨基-6-烷基氨基或2-氨基-6-二烷基氨基取代的嘌呤,2-氨基-6-硫嘌呤,2-氨基-6-烷硫基取代的嘌呤,3-脱氮嘌呤,7-脱氮嘌呤和8-氮杂嘌呤。 嘧啶含有胞嘧啶,尿嘧啶和胸腺嘧啶,5-卤素取代的胞嘧啶和尿嘧啶,5-烷基取代的胞嘧啶和尿嘧啶,包括具有饱和或不饱和烷基的衍生物和6-氮杂嘧啶。