ANTIBACTERIAL MUTILINS
    1.
    发明授权
    ANTIBACTERIAL MUTILINS 有权
    抗菌MUTILINE

    公开(公告)号:EP1320525B1

    公开(公告)日:2004-04-21

    申请号:EP01972046.5

    申请日:2001-09-11

    CPC分类号: C07D211/54 C07D207/12

    摘要: A compound of formula (I) wherein R and R2 together with the nitrogen atom to which they are attached form pyrrolidinyl or piperidinyl, R1 is a group of formula (II) R3 and R'3 are hydrogen, deuterium or halogen, R4, R5 and R10 are independently of each other hydrogen or alkyl, R6, R7 and R8 are hydrogen or deuterium; R9 is amino, alkyl, aryl, heterocyclyl or mercapto; and, if X is oxygen, R9 is additionally hydrogen; R'10 is alkyl, X is sulphur, oxygen, NR10, or N+(R'10)2; Y is sulphur or oxygen, and m is 0, 1 or 2; with the proviso that, when R and R2 together with the nitrogen atom to which they are attached form piperidinyl, m is O, Y is S and Y is attached in position 3 of said piperidine ring, that group of formula (I) which is attached to the piperidine ring via the residue Y is either in the (S)-configuration or in the (R)-configuration, preferably in the (S) -configuration which is e.g. useful as antimicrobial, antibacterial.

    PURIFICATION PROCESS
    2.
    发明授权
    PURIFICATION PROCESS 失效
    净化过程

    公开(公告)号:EP0968214B1

    公开(公告)日:2004-04-07

    申请号:EP98907945.4

    申请日:1998-01-14

    IPC分类号: C07D501/00 C12P17/18

    CPC分类号: C07D501/00

    摘要: Crystalline 2-(aminothiazol-4-yl)-2-(tert.butoxycarbonylmethoxyimino)acetic acid-S-mercapto-benzo-thiazolylester in form of an N,N-dimethylacetamide solvate; a crystalline salt of a 7-[2-(aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid with an amine of formula N(R1)(R2)(R3), wherein R1, R2, and R3 have various meanings, a crystalline sulphuric acid addition salt of a 7-[2-(2-aminothiazol-4-yl)-2-carboxymethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid; and the use of these salts in the production of cefixime, e.g. in form of a trihydrate.

    摘要翻译: N,N-二甲基乙酰胺溶剂化物形式的结晶2-(氨基噻唑-4-基)-2-(叔丁氧基羰基甲氧基亚氨基)乙酸-S-巯基 - 苯并噻唑基酯; 7-(2-(氨基噻唑-4-基)-2-(羧甲氧基亚氨基)乙酰胺基] -3-乙烯基-3-头孢烯-4-羧酸与式N(R 1)(R 2) (R3)(其中R1,R2和R3具有各种含义),7- [2-(2-氨基噻唑-4-基)-2-羧甲氧基亚氨基)乙酰氨基] -3-乙烯基-3 - 头孢烯-4-羧酸; 以及这些盐在头孢克肟生产中的用途,例如 以三水合物的形式。

    Agglomerates of beta-lactam antibiotics
    6.
    发明公开
    Agglomerates of beta-lactam antibiotics 失效
    聚集体β-内酰胺抗生素

    公开(公告)号:EP1283034A2

    公开(公告)日:2003-02-12

    申请号:EP02020921.9

    申请日:1997-03-13

    摘要: Auxiliary-free agglomerates of a β-lactam antibiotic; a mixture of agglomerates of an active β-lactam antibiotic and a second pharmaceutically active agent, with or without auxiliaries; a tablet comprising compressed agglomerates of a β-lactam antibiotic optionally in mixture with pharmaceutically acceptable auxiliaries; and a tablet comprising compressed agglomerates of a β-lactam antibiotic in mixture with a second pharmaceutically active agent and with or without pharmaceutically acceptable auxiliaries.

    摘要翻译: β-内酰胺抗生素的无辅助附聚物; 活性β-内酰胺抗生素和第二药物活性剂的附聚物的混合物,具有或不具有助剂; 包含任选与药学上可接受的助剂混合的β-内酰胺抗生素的压缩附聚物的片剂; 和包含与第二种药物活性剂混合的β-内酰胺抗生素的压缩附聚物和含或不含药学上可接受的助剂的片剂。

    Process for the production of a 3-cephem-4-carboxylic acid derivative
    8.
    发明公开
    Process for the production of a 3-cephem-4-carboxylic acid derivative 失效
    Verfahren zur Herstellung von einem 3-Cephem-4-Carbonsäurederivat

    公开(公告)号:EP1103555A1

    公开(公告)日:2001-05-30

    申请号:EP01104309.8

    申请日:1992-12-21

    IPC分类号: C07D501/18 C07D501/12

    CPC分类号: C07D501/00

    摘要: The invention relates to a new process for the production of pharmaceutically active cephalosporines by depletion of 7-amino-3-[(E)-1-propen-1-yl]-3- cephem-4-carboxylic acid in mixtures of 7-amino-3-[(Z)-1-propen-1-yl]-3- cephem-4-carboxylic acid and 7-amino-3-[(E)-1-propen-1-yl]-3-cephem-4-carboxylic acid, by means of a metal or amine salt of 7-amino-3-[(Z/E)-1-propen-1-yl]-3-cephem-4-carboxylic acid.

    摘要翻译: 本发明涉及通过将7-氨基-3-Ä(E)-1-丙烯-1-基-3-头孢烯-4-羧酸在7-氨基的混合物中的消耗来生产药用活性头孢菌素的新方法 -3-Ä(Z)-1-丙烯-1-基-3-头孢烯-4-羧酸和7-氨基-3-Ä(E)-1-丙烯-1-基-3-头孢烯-4-羧酸 羧酸,通过7-氨基-3-Ä(Z / E)-1-丙烯-1-基-3-头孢烯-4-羧酸的金属或胺盐。