Thymidine derivatives and therapeutic method of use
    1.
    发明授权
    Thymidine derivatives and therapeutic method of use 失效
    胸苷衍生物及其治疗方法

    公开(公告)号:US5306722A

    公开(公告)日:1994-04-26

    申请号:US939232

    申请日:1992-09-02

    CPC分类号: C07H19/06

    摘要: Thymidine kinase inhibitor of formula I ##STR1## in which R is C.sub.1-6 alkyl or AR(CH.sub.2).sub.n --, wherein Ar represents phenyl optionally substituted with one to five same or different halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; and n equals one to six.A further aspect of the present invention provides a method of inhibiting viral thymidine kinase. Yet another aspect of the invention relates to treating herpes simplex viral infections in mammals. Yet another aspect of the invention provides a pharmaceutical formulation.

    摘要翻译: 式I的胸苷激酶抑制剂(*化学结构*)I其中R是C 1-6烷基或AR(CH 2)n - ,其中Ar表示任选被1至5个相同或不同的卤素,C 1-6烷基或C 1 -C 6烷基取代的苯基, 6烷氧基; n等于1到6。 本发明的另一方面提供了抑制病毒胸苷激酶的方法。 本发明的另一方面涉及治疗哺乳动物中的单纯疱疹病毒感染。 本发明的另一方面提供一种药物制剂。

    Carbapenem antibiotics
    5.
    发明授权

    公开(公告)号:US4665170A

    公开(公告)日:1987-05-12

    申请号:US822576

    申请日:1986-01-27

    CPC分类号: C07D295/088 C07D477/20

    摘要: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

    Carbapenem antibiotics
    6.
    发明授权
    Carbapenem antibiotics 失效
    卡巴布本抗生素

    公开(公告)号:US4640799A

    公开(公告)日:1987-02-03

    申请号:US762735

    申请日:1985-08-05

    CPC分类号: C07D295/088 C07D477/20

    摘要: Disclosed are novel carbapenem derivatives characterized by a 2-substituent of the formula ##STR1## in which A represents cyclopentylene, cyclohexylene or C.sub.2 -C.sub.6 alkylene optionally substituted by one or more C.sub.1 -C.sub.4 alkyl groups; R.sup.5 represents either (a) an optionally substituted aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, aryl, araliphatic, heteroaryl, heteroaraliphatic, heterocyclyl or heterocyclyl-aliphatic radical or (b) a divalent phenylene or C.sub.1 -C.sub.4 alkylene group joined to the ##STR2## ring so as to form a bridged polycyclic group; and ##STR3## represents a quaternized nitrogen-containing non-aromatic heterocycle. Such derivatives are useful as potent antibacterial agents.

    摘要翻译: 公开了新的碳青霉烯衍生物,其特征在于具有式“IMAGE”的2-取代基,其中A表示任选被一个或多个C 1 -C 4烷基取代的亚环戊基,亚环己基或C 2 -C 6亚烷基; R 5表示(a)任选取代的脂族,脂环族,脂环族 - 脂族,芳基,芳脂族,杂芳基,杂脂肪族基,杂环基或杂环基 - 脂族基团或(b)二价亚苯基或C1-C4亚烷基, 环以形成桥连多环基团; 并且表示季铵化的含氮非芳族杂环。 这些衍生物可用作有效的抗菌剂。

    Cephalosporin derivatives
    8.
    发明授权
    Cephalosporin derivatives 失效
    头孢菌素衍生物

    公开(公告)号:US5734047A

    公开(公告)日:1998-03-31

    申请号:US761738

    申请日:1996-12-05

    CPC分类号: C07D501/00

    摘要: Novel cephem derivatives represented by the general formula ##STR1## wherein Ar is an optionally substituted lipophilic phenyl, naphthyl, benzthiazolyl or pyridyl group; R.sup.1 represents a group of the formula ##STR2## in which R.sup.8 and R.sup.9 are each independently hydrogen, C.sub.1 -C.sub.6 alkyl or (C.sub.1 -C.sub.6)alkoxycarbonyl, said C.sub.1 -C.sub.6 alkyl group being optionally substituted by 1-5 hydroxy or C.sub.1 -C.sub.6 alkoxy groups; m is either 0 or 1; A is a C.sub.2 -C.sub.10 alkyl group optionally substituted by 1-5 hydroxy groups; and R.sup.2 and R.sup.3 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.

    摘要翻译: 由通式 + TR 表示的新型头孢烯衍生物,其中Ar是任选取代的亲脂性苯基,萘基,苯并噻唑基或吡啶基; R 1表示式(VIII)的基团,其中R 8和R 9各自独立地为氢,C 1 -C 6烷基或(C 1 -C 6)烷氧基羰基,所述C 1 -C 6烷基任选被1-5个羟基或C 1 -C 6 烷氧基 m为0或1; A是任选被1-5个羟基取代的C 2 -C 10烷基; 且R 2和R 3各自独立地为氢或C 1 -C 6烷基。 衍生物是革兰氏阳性抗菌剂,特别适用于治疗耐甲氧西林金黄色葡萄球菌引起的疾病。