PROCESS FOR PREPARING CEPHEM DERIVATIVES

    公开(公告)号:KR860002184B1

    公开(公告)日:1986-12-24

    申请号:KR780000888

    申请日:1978-03-30

    Applicant: HOECHST AG

    Abstract: Title compds. I[R1=H, protected amino; R2=H, alkyl, alkenyl, Ph, benzyl; R3=H, ester, anion; R4=H, alkoxy; A=-CH2SR5, -CH2Y; R5=hetero cyclic group; Y=pyridinium, quinolinium group! were prepd. Thus, 2.6 g mixt. of H2O, ethanol, and 7-beta-[alpha-sinmethoximino-alpha-(2- amino-thiazol-4-yl)-acetamido!-cephalosporanic acid were dissolved in 50ml H2O with 1.5 g 2-mercapto-3-oxy-4phenyl-1,3-thiazole and incubated for 2 h at 64≦̸C at pH 6.0-7.0 to give 0.9 g 7-beta-[alpha- sin-methoximino-alpha-(2-amino-thiazol-4yl)-acetamido!-3-(3-oxy-4- phenyl-1,3-thiazol-2-yl-thiomethyl)-3cephem-4-carboxylic acid.

    PROCESS FOR PREPARING CEPHEM DERIVATIVES

    公开(公告)号:KR830000733A

    公开(公告)日:1983-04-18

    申请号:KR780001066

    申请日:1978-04-13

    Applicant: HOECHST AG

    Abstract: Cephems I(R1=H, (un) substituted alkyl, acyl, arylsulfonyl, alkylsulfonyl, amino-protective group; R2=H, (un)substituted alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl, acyl, aryl, arylsulfonyl, alkylsulfonyl, heterocycle; R3=H, esterforming group, cation; R4=H, alkoxy; A=H, (un) substituted alkoxy or alkenoxy, halo, alkyl; X=S, O, CH2, NH), useful as antimicrobial agents were prepd. I(R=R3=R4=H; R1=Me, Et; R2=H, Na; X=S) are esp. effective against Pseudomonas. E.g., dicyclohexylcarbodiimide-midiated coupling of 2-synmethoxyimino-2-(2tritylamino-4-thiazolyl) acetic acid with 7-aminoceph-3-em-4-carboxylic acid, followed by purifn. via the (H2NCH2)2 salt, gave I(R, R2-R4=H, R1=Me)

    Substituted p-hydroxyphenyl-hydrazones and process for their manufacture
    3.
    发明授权
    Substituted p-hydroxyphenyl-hydrazones and process for their manufacture 失效
    取代的对羟基苯酚和水解产物及其制备方法

    公开(公告)号:US3573287A

    公开(公告)日:1971-03-30

    申请号:US3573287D

    申请日:1968-08-07

    Applicant: HOECHST AG

    CPC classification number: A61K31/44 C09B26/04

    Abstract: SUBSTITUTED P-HYDROXYPHENYL-HYDRAZONES OF THE FORMULA

    1-R4,3-((4-(HO-),R1,R2-PHENYL)-NH-N=C(-R3)-)PYRIDINIUM

    X(-)

    IN WHICH R1 AND R2 REPRESENT HYDROGEN, HALOGEN, LOWER ALKYL OR ALKOXY, CARBOXY, CARBAMOYL, LOWER CARBALKOXY, CARBOBENZOXY, SULFOXY OR SULFAMOUL; R3 REPRESNETS HYDROGEN OR LOWER ALKYL HAVING 1 TO 3 CARBON ATOMS, R4 REPRESENTS AN ALKYL RADICAL HAVING 1 TO 12 CARBON ATOMS, WHICH MAY CARRY ONE OR SEVERAL HYDROXY, LOWER ALKOXY, CARBOXY, LOWER CARBALKOXY, CARBAMOYL, NITRILE, SULFO, LOWER SULFALKOXY AND/OR SULFAMOYL GROUPS, AND X REPRESENTS THE ANION OF A NON-TOXIC ACID, WHICH COMPOUNDS HAVE BACTERIOSTATIC PROPERTIES.

    Acylamino-cephalosporanic acids
    5.
    发明授权
    Acylamino-cephalosporanic acids 失效
    酰氨基 - 头孢菌酸

    公开(公告)号:US3865820A

    公开(公告)日:1975-02-11

    申请号:US24428772

    申请日:1972-04-14

    Applicant: HOECHST AG

    CPC classification number: C07D499/00

    Abstract: Acylaminocephalosporanic acids of the formula I

    wherein R1, R2 and R3 each represents hydrogen or lower alkyl radicals in which case R1 and R2 may also form together an optionally substituted alkylene radical, A represents an optionally substituted phenylene or thienyl radical, and X represents an oxygen atom or a single bond, the physiologically tolerable salts thereof, pharmaceutical preparations effective against bacterial infections containing these compounds, and a process for the manufacture.

    Abstract translation: 式I的酰氨基头孢烷酸其中R 1,R 2和R 3各自表示氢或低级烷基,其中R 1和R 2也可以一起形成任选取代的亚烷基,A表示任选取代的亚苯基或噻吩基,X表示氧 原子或单键,其生理上可耐受的盐,对含有这些化合物的细菌感染有效的药物制剂及其制备方法。

    Acylamino-cephem-carboxylic acids and process for preparing them
    6.
    发明授权
    Acylamino-cephem-carboxylic acids and process for preparing them 失效
    酰氨基 - 头孢烯羧酸及其制备方法

    公开(公告)号:US3920640A

    公开(公告)日:1975-11-18

    申请号:US35646673

    申请日:1973-05-02

    Applicant: HOECHST AG

    CPC classification number: C07D239/06 C07D233/22 C07D233/26 C07D333/38

    Abstract: IN WHICH R1, R2 and R3 represent hydrogen or lower alkyl groups and R1 and R2 may form together an alkylene group which may be substituted, R4 represents a linear or branched alkyl radical of 1 to 5 carbon atoms, a cyclo-alkyl radical of 3 to 7 carbon atoms which may be interrupted by heteroatoms, X represents a single bond or NH, A represents a phenylene or thienylene group which may be substituted and Y represents a single bond or oxygen, and their physiologically tolerated salts; the novel compounds have very good anti-bacterial properties.

    Acylamino-cephem-carboxylic acids of the general formula

    Abstract translation: 酰基氨基 - 头孢烯羧酸,其通式为R 1,R 2和R 3表示氢或低级烷基,R 1和R 2可以一起形成可被取代的亚烷基,R 4表示1至5的直链或支链烷基 碳原子,可被杂原子中断的3-7个碳原子的环烷基,X表示单键或NH,A表示可被取代的亚苯基或亚噻吩基,Y表示单键或氧,以及 他们的生理耐受盐; 新型化合物具有非常好的抗菌性能。

    Quinoxaline-1,4-dioxides
    7.
    发明授权
    Quinoxaline-1,4-dioxides 失效
    喹喔啉-1,4-二氧化物

    公开(公告)号:US3600388A

    公开(公告)日:1971-08-17

    申请号:US3600388D

    申请日:1969-07-07

    Applicant: HOECHST AG

    CPC classification number: C07D241/52

    Abstract: NEW CARBOXYLIC ACID HYDRAZIDES OF THE GENERAL FOMULA

    1,4-DI-O
    IN WHICH R1 IS LOWER ALKYL, PREFERABLY METHYL, AND R2 AND R3 REPRESENT HYDROGEN, LOWER ALKYL OR ALKOXY, ARE PREPARED BY REACTING A COMPOUND OF THE FORMULA

    1,4-DI-O
    IN WHICH R IS ALKYL, WITH HYDRAZINE HYDRATE UNDER MILD REACTION CONDITIONS. THE PRODUCTS OF THE INVENTION HAVE AN ANTIBACTERIAL ACTIVITY.

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