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    • 3. 发明公开
    • 신규 세팔로스포린계 항생제 및 이의 제조 방법
    • 新CEPHALOSPORIN抗生素及其制备方法
    • KR1020020085180A
    • 2002-11-16
    • KR1020010024547
    • 2001-05-07
    • 주식회사 엘지생명과학
    • 김근태이창석유은정장용진황상열조양래
    • C07D501/44
    • PURPOSE: Provided is a novel cephalosporin compound which is represented by the formula(1) and has strong antibiotic effect on MRSA. Also, provided are its preparation process and a composition of antibiotics containing the compound of the formula(1). CONSTITUTION: The cephalosporin compound of the formula(1), wherein the formula is as described in the description, its pharmaceutically acceptable nontoxic salts, its physiologically hydrolyzable ester, hydrate, solvate and its isomer display antibiotic effect on gram positive bacteria and have broad antibiotic spectrum. Thus, they are very useful for the prevention and treatment of diseases associated with infection of bacteria in a human and an animal.
    • 目的:提供由式(1)表示的新型头孢菌素化合物,对MRSA具有很强的抗生素作用。 还提供其制备方法和含有式(1)化合物的抗生素的组合物。 构型:式(1)的头孢菌素化合物,其中式如描述中所述,其药学上可接受的无毒盐,其生理上可水解的酯,水合物,溶剂合物及其异构体对革兰氏阳性细菌显示出抗生素效应并具有广泛的抗生素 光谱。 因此,它们对于预防和治疗与人和动物中的细菌感染相关的疾病非常有用。
    • 6. 发明公开
    • 신규 세팔로스포린계 유도체합성
    • 生产CEPHOROSPORIN衍生物的方法
    • KR1020010054717A
    • 2001-07-02
    • KR1019990055645
    • 1999-12-07
    • 영진약품 주식회사
    • 김성규백장훈박성훈
    • C07D501/44
    • PURPOSE: Provided is a method for producing cephalosporin derivatives which is useful as antibacterial agents having a strong antibacterial activity for various bacteria. CONSTITUTION: The cephalosporin derivatives having a strong antibacterial activity for various bacteria are represented by formula (I), in which R is aminothiazole, aminothiodiazole, alkylophenylthio; R1 is hydrogen, Na, K, diphenylmethyl; and R2 is phenyl and piperidylthiocarbonyl. The method for producing cephalosporin derivatives of formula (I) comprises the steps of: reacting thiol compounds represented by formula (III) with diphenylphosphoryloxy compounds represented by formula (II) to produce 3-cephem compounds represented by formula (IV); deacylating 3-cephem compounds of formula (IV) to produce 7-amino-3-cephem derivatives represented by formula (V); and acylating compounds of formula (VI) with compounds of formula (V) to produce the cephalosporin derivatives of formula (I).
    • 目的:提供头孢菌素衍生物的制造方法,其可用作对各种细菌具有强抗菌活性的抗菌剂。 构成:对各种细菌具有强抗菌活性的头孢菌素衍生物由式(I)表示,其中R是氨基噻唑,氨基噻二唑,烷基苯硫基; R1是氢,Na,K,二苯基甲基; 并且R 2是苯基和哌啶基硫代羰基。 制备式(I)头孢菌素衍生物的方法包括以下步骤:使由式(III)表示的硫醇化合物与由式(II)表示的二苯基磷酰氧基化合物反应以制备由式(IV)表示的3-头孢烯化合物; 使式(Ⅳ)的3-头孢烯化合物脱酰基来制备由式(Ⅴ)表示的7-氨基-3-头孢烯衍生物; 和式(Ⅵ)化合物与式(Ⅴ)化合物酰化生成式(I)的头孢菌素衍生物。