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    • 4. 发明授权
    • Cephalosporin derivatives
    • 头孢菌素衍生物
    • US5734047A
    • 1998-03-31
    • US761738
    • 1996-12-05
    • Choung U. KimMuzammil M. MansuriPeter F. MiscoJohn A. Wichtowski
    • Choung U. KimMuzammil M. MansuriPeter F. MiscoJohn A. Wichtowski
    • C07D501/00C07D501/36A61K31/545
    • C07D501/00
    • 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.
    • 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。
    • 6. 发明授权
    • Carbapenem antibiotics
    • 卡巴布本抗生素
    • US4640799A
    • 1987-02-03
    • US762735
    • 1985-08-05
    • Choung U. KimPeter F. Misco, Jr.
    • Choung U. KimPeter F. Misco, Jr.
    • C07D295/088C07D477/20C07D487/04A61K31/40
    • C07D295/088C07D477/20
    • 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.
    • 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。