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    • 1. 发明公开
    • 세팔로스포린 유도체의 신규한 제조 방법
    • 制造CEPHOROSPORIN衍生物的新工艺
    • KR1020010049719A
    • 2001-06-15
    • KR1020000038364
    • 2000-07-05
    • 에프. 호프만-라 로슈 아게
    • 스푸르파울트릭케스게오르크
    • C07D501/48
    • C07D501/00Y02P20/55
    • PURPOSE: Provided is a novel process for the manufacture of cephalosporin derivatives to offer easier access to pharmacologically useful cephalosporins. CONSTITUTION: Cephalosporin derivatives are represented by the formula(I), wherein R1 is an amino protecting group, R2 is a carboxy protecting group and R is hydrogen, lower alkyl, lower alkoxy, cycloalkyl, cycloalkenyl, cycloalkyl-lower alkyl, lower alkenyl, lower alkynyl, aryl, aryl-lower alkyl, heterocyclyl or heterocyclyl-lower alkyl; the lower alkyl, cycloalkyl, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl and the heterocyclyl moieties being unsubstituted or substituted with at least one group selected from carboxy, amino, aminoethyl, carbamoyl, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen and trifluoromethyl. The manufacturing method comprises the steps of: converting a phosphonium salt of the formula(II) into the corresponding ylide of the formula(III); reacting it with aldehyde of the formula(IV).
    • 目的:提供一种用于制造头孢菌素衍生物以提供更容易获得药理学上有用的头孢菌素的新方法。 构成:头孢菌素衍生物由式(I)表示,其中R1是氨基保护基,R2是羧基保护基,R是氢,低级烷基,低级烷氧基,环烷基,环烯基,环烷基 - 低级烷基,低级烯基, 低级炔基,芳基,芳基 - 低级烷基,杂环基或杂环基 - 低级烷基; 低级烷基,环烷基,低级烯基,环烯基,低级炔基,芳基 - 低级烷基,芳基和杂环基部分是未取代的或被至少一个选自羧基,氨基,氨基乙基,氨基甲酰基,硝基,氰基,低级烷基, 低级烷氧基,羟基,卤素和三氟甲基。 制造方法包括以下步骤:将式(II)的鏻盐转化成式(III)的相应的叶立德; 使其与式(IV)的醛反应。
    • 7. 发明公开
    • 3-피리디늄 메틸세펨 화합물
    • 3-PYRIDINIUM METHYLCEPHEM化合物
    • KR1020060135796A
    • 2006-12-29
    • KR1020067017921
    • 2005-03-03
    • 시오노기세이야쿠가부시키가이샤
    • 니시타니야스히로야스카타다츠로야마와키겐지
    • C07D501/56A61K31/397C07D501/48
    • C07D501/00
    • A compound represented by the formula [Chemical formula 1] (I) {wherein A is optionally substituted lower alkylene [substituent: mono- or di(lower alkyl), lower alkylidene, or C2 or higher (lower alkylene)]; and Z+ is either of the following groups: [Chemical formula 2] (Z-1) (Z-2) [wherein R 1 and R2 each independently is hydrogen, optionally substituted amino(lower alkyl), optionally substituted aminocycloalkyl, optionally substituted cyclic amino, or optionally substituted (cyclic amino)lower alkyl; R9 is hydrogen or lower alkyl, provided that R1 and R9 may form an optionally substituted cyclic amino in cooperation with the adjacent nitrogen atom; R3 is hydrogen or amino; and X is nitrogen or CR4 (R4 is hydrogen or optionally substituted lower alkyl)]}, a pharmaceutically acceptable salt of the compound, or a solvate of either.
    • 由式[化学式1](I)表示的化合物{其中A是任选取代的低级亚烷基[取代基:一或二(低级烷基),低级亚烷基,或者C 2或更高(低级亚烷基)]; 和Z +是以下基团:[化学式2](Z-1)(Z-2)[其中R 1和R 2各自独立地为氢,任选取代的氨基(低级烷基),任选取代的氨基环烷基,任选取代的环状 氨基或任选取代的(环状氨基)低级烷基; R 9是氢或低级烷基,条件是R 1和R 9可以与相邻的氮原子一起形成任选取代的环状氨基; R3是氢或氨基; 并且X是氮或CR 4(R 4是氢或任选取代的低级烷基)],化合物的药学上可接受的盐或其中任何一种的溶剂合物。