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    • 3. 发明授权
    • Process for synthesizing 4-substituted azetidinone derivatives
    • 合成4-取代的氮杂环丁酮衍生物的方法
    • US06867297B1
    • 2005-03-15
    • US09178594
    • 1998-10-26
    • Masaji IshiguroTakashi NakatsukaRie TanakaTetsuo ShimamotoTakuro Yoshida
    • Masaji IshiguroTakashi NakatsukaRie TanakaTetsuo ShimamotoTakuro Yoshida
    • C07D205/08
    • C07D205/08
    • An azetidinone derivative represented by the general formula (1) (wherein OR1 is a protected hydroxyl group; R2 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group or a substituted or unsubstituted aromatic group) is reacted with an ester compound represented by the formula (2) (wherein CO2R3 is an esterified carboxyl group; X and Y are the same or different and represent individually a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted alkyloxy group, a substituted or unsubstituted alkenyloxy group, a substituted or unsubstituted aralkyloxy group, a substituted or unsubstituted aryloxy group, a substituted or unsubstituted silyloxy group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic-thio group, a substituted or unsubstituted heterocyclic-oxy group, a substituted or unsubstituted acyl group, a substituted or unsubstituted ester group, a substituted or unsubstituted thio ester group, a substituted or unsubstituted amide group, a substituted or unsubstituted amino group, a hydrogen atom or halogen atom, or are taken together with each other to form a substituted or unsubstituted cycloalkan-2-on-1-yl group) in the presence of zinc and copper compounds to synthesis a 4-substituted azetidinone derivative represented by the formula (3) (wherein OR1, CO2R3, X and Y are as defined above).
    • 由通式(1)表示的氮杂环丁酮衍生物(其中OR 1为保护的羟基; R2为取代或未取代的烷基,取代或未取代的烯基或取代或未取代的芳族基团)与表示的酯化合物 通式(2)(其中CO 2 R 3是酯化的羧基; X和Y相同或不同,分别代表取代或未取代的烷基,取代或未取代的烯基,取代或未取代的芳烷基,取代或未取代的芳烷基, 未取代的芳基,取代或未取代的烷硫基,取代或未取代的链烯硫基,取代或未取代的芳烷硫基,取代或未取代的芳硫基,取代或未取代的烷氧基,取代或未取代的烯氧基,取代或未取代的 芳烷氧基,取代或未取代的芳氧基,取代基 取代或未取代的杂环基,取代或未取代的杂环硫基,取代或未取代的杂环氧基,取代或未取代的酰基,取代或未取代的酯基,取代或未取代的硫代 酯基,取代或未取代的酰胺基,取代或未取代的氨基,氢原子或卤素原子,或彼此一起形成取代或未取代的环烷烃-2-基-1-基) 存在锌和铜化合物以合成由式(3)表示的4-取代的氮杂环丁酮衍生物(其中OR1,CO2R3,X和Y如上定义)。
    • 6. 发明申请
    • Penem derivatives and antimicrobial agent containing the same
    • Penem衍生物和含有相同的抗微生物剂
    • US20050004092A1
    • 2005-01-06
    • US10831694
    • 2004-04-26
    • Masaji IshiguroTakashi NakatsukaRie TanakaKoshi NamikawaShinsuke Matsuki
    • Masaji IshiguroTakashi NakatsukaRie TanakaKoshi NamikawaShinsuke Matsuki
    • C07D499/74C07D499/88A61K31/43
    • C07D499/88Y02P20/55
    • A penem derivative represented by the following formula (I): wherein R1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof. The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA. It is therefore useful not only as a general antibacterial agent but also as an antibacterial agent for MRSA against which no general antibacterial agents are recognized to be-effective.
    • 由下式(I)表示的pen嗪衍生物:其中R1表示取代或未取代的烷基,取代或未取代的烯基,取代或未取代的芳烷基,取代或未取代的芳基,取代或未取代的烷硫基, 取代或未取代的链烯硫基,取代或未取代的芳烷硫基,取代或未取代的芳硫基,取代或未取代的杂环基,取代或未取代的杂环硫基,取代或未取代的酰硫基,巯基或氢原子 R 2表示氢原子或羧基保护基; 或其药理学上可接受的盐。 化合物(I)表现出强烈的抗菌活性,特别是对MRSA具有较强的活性。 因此,不仅可以作为一般的抗菌剂,而且作为MRSA的抗菌剂也是有用的,其中没有一般的抗菌剂被认为是有效的。