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    ACYL DERIVATIVES AND THEIR PREPARATION
    1.
    发明授权
    ACYL DERIVATIVES AND THEIR PREPARATION 失效

    公开(公告)号：KR790001023B1

    公开(公告)日：1979-08-20

    申请号：KR750001368

    申请日：1975-06-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： MONTAVON M ,  REINER R

    Abstract: Acyl cephalosporin derivs. (I, X = acetoxycephalosporinyl; Y = N-substituted 6-membered heterocyclic group) were manufd. by reacting II (X' = deactoxy-cephalosporinyl group contg. protected 4-carboxyl group; W' = free atom or group) with III, or by reacting IV (X'' = deacetoxy-cephalosporinyl group contg. protected 4-carboxyl group) with acids or their reactive derivs. of V (Z = acyl group being thought as substituent of amino acid in cephalosporin), and followed by isolating the protecting group to give I.

    PROCESS FOR PREPARING CEPHALOSPORIN DERIVATIVES
    2.
    发明授权
    PROCESS FOR PREPARING CEPHALOSPORIN DERIVATIVES 失效

    公开(公告)号：KR810000807B1

    公开(公告)日：1981-07-08

    申请号：KR780001679

    申请日：1978-06-02

    Applicant: HOFFMANN LA ROCHE

    Inventor： REINER R ,  MONTAVON M

    IPC: C07D501/36

    Abstract: Title compds. (I; R = furyl, thienyl, Ph; R' = lower alkyl, aminocarbonylmethyl; X = (a), (b), (c); R2, R3, R4 and R5 are H, lower alkyl, carboxymethyl or sulfomethyl), useful as bactericides, were prepd. by the reaction of II and III, or IV(Y = leaving group) and V. Thus, 5.06 g 2-methoxyimino-2-furyl-acetic acid reacted with oxalic chloride in the presence of DMF and Et3N, followed by the addn. of (7R)-7-amino-3-desacetoxy-3-[(1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl)thio cephalosporanic acid in NaOH soln. to give I.

    PROCESS FOR THE MANUFACTURIN OF ACYL DERIVATIVES
    6.
    发明专利
    PROCESS FOR THE MANUFACTURIN OF ACYL DERIVATIVES 未知

    公开(公告)号：YU295280A

    公开(公告)日：1983-06-30

    申请号：YU295280

    申请日：1980-11-20

    Applicant: HOFFMANN LA ROCHE

    Inventor： MONTAVON M ,  REINER R

    IPC: C07D501/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/16 ,  C07D501/36 ,  C07D501/46

    Abstract: For the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 1. A process for the manufacture of acyl derivatives of general formula I see diagramm : EP0030294,P12,F1 in which R represents hydrogen or a readily hydrolyzable ester group, as well as of salts of these compounds and hydrates of these compounds or of their salts by reating a halide of general formula II see diagramm : EP0030294,P12,F2 in which R has the significance given above and Y represents a halogen atom, or a salt of this compound with thiourea and, if desired, converting a compound of formula I obtained into a salt or hydrate or into a hydrate of this salt, characterized in that X signifies one of the groups see diagramm : EP0030294,P13,F3 in which R' represents hydrogen or a readily hydrolysable ether group.

    ACYL DERIVATIVES
    10.
    发明专利
    ACYL DERIVATIVES 未知

    公开(公告)号：ZA783030B

    公开(公告)日：1979-06-27

    申请号：ZA783030

    申请日：1978-05-26

    Applicant: HOFFMANN LA ROCHE

    Inventor： REINER R ,  MONTAVON M

    IPC: A61K31/545 ,  C07C59/00 ,  C07D501/36 ,  C07D501/60

    Abstract: The acyl derivatives provided by the present invention are compounds of the general formula (I) wherein R represents furyl, thienyl or phenyl optionally substituted by halogen, hydroxy, lower alkoxy or lower alkyl, R1 represents alkyl or aminocarbonylmethyl and X represents a group of the formula in which one of the two symbols R2 and R3 or R4 and R5 represents hydrogen and the other represents lower alkyl, carboxymethyl or sulphomethyl, and the pharmaceutically acceptable salts of said compounds and hydrates of said salts. Also disclosed are a process for the manufacture of the compounds and pharmaceutical preparations therefor. The compounds of the present invention have antibiotic activity, especially bactericidal activity.

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