Carbo-acyclic nucleoside derivatives as antiviral and antineoplastic
agents
    1.
    发明授权
    Carbo-acyclic nucleoside derivatives as antiviral and antineoplastic agents 失效
    无环核苷衍生物作为抗病毒和抗肿瘤药物

    公开(公告)号:US6017923A

    公开(公告)日:2000-01-25

    申请号:US564296

    申请日:1996-05-31

    摘要: ##STR1## The present invention is directed to a class of novel carbocyclic derivatives having formulas (I) and (II) and their use as anti-viral and anti-neoplastic agents, wherein X
    1 and X
    2 are each independently hydrogen, fluorine, or chlorine, R is hydrogen or hydroxymethyl, J is a radical of formulas (a), (b) and (c). Y
    1 is a CH group, a CCl group, a CBr group or a CNH
    2 group, Y
    2 and Y
    3 are each independently nitrogen or a CH group, Y
    1 is a CH group, a CCl group, a CBr group or a CNH
    2 group, Y
    2 and Y
    3 are each independently nitrogen or a CH group, Y
    4 is hydrogen, C
    1 -C
    4 alkyl, C
    1 -C
    4 alkoxy or halogen, Y
    5 is NH
    2 or C
    1 -C
    4 alkoxy, Q is NH
    2 , NHOH, NHCH
    3 , OH, or hydrogen, and V is hydrogen, halogen or NH
    2 ; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 本发明涉及一类具有式(I)和(II)的新型碳环衍生物及其作为抗病毒和抗肿瘤剂的用途,其中X1和X2各自独立地为氢,氟或氯,R为 氢或羟甲基,J为式(a),(b)和(c)的基团。 Y1是CH基,CCl基,CBr基或CNH2基,Y2和Y3各自独立地是氮或CH基,Y1是CH基,CCl基,CBr基或CNH2基,Y2和 Y3各自独立地为氮或CH基,Y4为氢,C1-C4烷基,C1-C4烷氧基或卤素,Y5为NH2或C1-C4烷氧基,Q为NH2,NHOH,NHCH3,OH或氢,V 是氢,卤素或NH 2; 或其药学上可接受的盐。

    Prevention of glycoprotein enveloped virus infectivity by
pyridinyloxazole-2-ones
    3.
    发明授权
    Prevention of glycoprotein enveloped virus infectivity by pyridinyloxazole-2-ones 失效
    通过吡啶基恶唑-2-酮预防糖蛋白包膜病毒感染

    公开(公告)号:US5063238A

    公开(公告)日:1991-11-05

    申请号:US590522

    申请日:1990-10-03

    IPC分类号: A61K31/44

    CPC分类号: A61K31/44

    摘要: This invention relates to pyridinyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.

    摘要翻译: 本发明涉及作为蛋白激酶C抑制剂的能力的有用的抗包膜病毒剂的吡啶基恶唑-2-酮。 这些衍生物被公开以有效地治疗包括HIV感染的包膜病毒感染,因此可用于治疗AIDS和ARC。

    Anti-herpes castanospermine esters
    6.
    发明授权
    Anti-herpes castanospermine esters 失效
    抗疱睾丸素酯

    公开(公告)号:US5385911A

    公开(公告)日:1995-01-31

    申请号:US41532

    申请日:1993-04-01

    摘要: Certain Castanospermine ester derivatives of the formula: ##STR1## wherein R, R.sub.1 and R.sub.2 are each independently hydrogen, C.sub.1-14 alkanoyl, C.sub.1-14 alkenoyl, cyclohexanecarbonyl, C.sub.1-8 alkoxyacetyl, ##STR2## naphthalenecarbonyl optionally substituted by methyl or halogen; phenyl (C.sub.2-6 alkanoyl) wherein the phenyl is optionally substituted by methyl or halogen; cinnamoyl; pyridinecarbonyl optionally substituted by methyl or halogen; dihydropyridine carbonyl optionally substituted by C.sub.1 -C.sub.10 alkyl; thiophenecarbonyl optionally substituted by methyl or halogen; or furancarbonyl optionally substituted by methyl or halogen; Y is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, trifluoromethyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylmercapto, cyano or dimethylamino; Y' is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or it is combined with Y to give 3,4-methylenedioxy; Y" is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or halogen; with R, R.sub.1 and R.sub.2 being selected in such a way that at least one of them, but not more than two of them, is hydrogen; are disclosed to be effective in treating diseases caused by Herpes Simplex Virus (HSV) Types 1 and 2.

    摘要翻译: 其中R,R 1和R 2各自独立地为氢,C 1-14烷酰基,C 1-14链烯酰基,环己烷羰基,C 1-8烷氧基乙酰基,任选被甲基或卤素取代的萘甲酰基的某些蓖麻精酯衍生物。 苯基(C 2-6烷酰基),其中苯基任选被甲基或卤素取代; 肉桂酰; 任选被甲基或卤素取代的吡啶羰基; 任选被C 1 -C 10烷基取代的二氢吡啶羰基; 任选被甲基或卤素取代的噻吩羰基; 或任选被甲基或卤素取代的呋喃羰基; Y是氢,C 1-4烷基,C 1-4烷氧基,卤素,三氟甲基,C 1-4烷基磺酰基,C 1-4烷基巯基,氰基或二甲基氨基; Y'是氢,C 1-4烷基,C 1-4烷氧基,卤素,或与Y结合,得到3,4-亚甲二氧基; Y“是氢,C 1-4烷基,C 1-4烷氧基或卤素; 其中R,R 1和R 2以这样的方式进行选择,使得它们中的至少一个,但不超过其中之一为氢; 被公开以有效治疗由1型和2型单纯疱疹病毒(HSV)引起的疾病。

    Prevention of glycoprotein enveloped virus infectivity by quinolyl- and
isoquinolyloxazole-2-zones
    8.
    发明授权
    Prevention of glycoprotein enveloped virus infectivity by quinolyl- and isoquinolyloxazole-2-zones 失效
    通过喹啉基和异喹唑啉-2-区预防糖蛋白包膜病毒感染

    公开(公告)号:US5061715A

    公开(公告)日:1991-10-29

    申请号:US590523

    申请日:1990-10-03

    IPC分类号: A61K31/47

    CPC分类号: A61K31/47

    摘要: This invention relates to quinolyloxazole-2-ones which are useful anti-enveloped virus agents by virtue of their ability to act as protein kinase C inhibitors. These derivatives are disclosed to be effective in treating enveloped virus infections including HIV infections and are thus useful in the treatment of AIDS and ARC.

    摘要翻译: 本发明涉及由于其作为蛋白激酶C抑制剂的能力而是有用的抗包膜病毒剂的喹喔啉-2-酮。 这些衍生物被公开以有效地治疗包括HIV感染的包膜病毒感染,因此可用于治疗AIDS和ARC。

    Methods of treating gout with chalcone derivatives
    9.
    发明授权
    Methods of treating gout with chalcone derivatives 失效
    用查耳酮衍生物治疗痛风的方法

    公开(公告)号:US4863968A

    公开(公告)日:1989-09-05

    申请号:US285331

    申请日:1988-12-14

    IPC分类号: A61K31/165

    CPC分类号: A61K31/165

    摘要: Certain chalcone derivatives are reported to inhibit the polymerization of tubulin to form microtubules and are therefore antimitotic agents which can be used as antigout agents. The chalcone derivatives are also reported to inhibit the destruction of the myelin sheath in the central nervous system of multiple sclerosis patients and are thus useful in controlling the progressive nature of the disease.

    摘要翻译: 据报道某些查耳酮衍生物抑制微管蛋白的聚合形成微管,因此可以用作抗突变剂的抗有丝分裂剂。 据报道,查耳酮衍生物可抑制多发性硬化患者的中枢神经系统中的髓鞘的破坏,因此可用于控制疾病的进行性质。