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    ACYL DERIVATIVES
    43.
    发明专利
    ACYL DERIVATIVES 未知

    公开(公告)号：CA1240314A

    公开(公告)日：1988-08-09

    申请号：CA387618

    申请日：1981-10-08

    Applicant: HOFFMANN LA ROCHE

    Inventor： MONTAVON MARC ,  REINER ROLAND

    IPC: C07D501/18

    Abstract: Novel cephalosporin derivatives are disclosed of the formula: I wherein R1 represents a hydrogen atom or a methoxy group and Y represents a 6-membered, optionally substituted heterocyclic group which contains 1,2 or 3 nitrogen atoms but which is not aromatic and is not enolisable to an aromatic group; at least one of said nitrogen atoms being substituted and at least one of said nitrogen atoms forming an amide group with an adjacent carbonyl group, and wherein the carboxyl group in the 4-position can be protected by salt formation with an inorganic or tertiary organic base. The derivatives I are useful as in-termediates in preparing cephalosporins having antibiotic activity.

    CEPHALOSPORINS
    45.
    发明专利
    CEPHALOSPORINS 未知

    公开(公告)号：AU554552B2

    公开(公告)日：1986-08-28

    申请号：AU7574181

    申请日：1981-09-29

    Applicant: HOFFMANN LA ROCHE

    Inventor： REINER ROLAND

    IPC: C07D253/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D253/075 ,  C07D501/00 ,  C07D501/18 ,  C07D501/36

    Abstract: There is presented compounds of the formula I wherein X represents the 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.

    ACYL DERIVATIVES
    48.
    发明专利
    ACYL DERIVATIVES 未知

    公开(公告)号：CA1177824A

    公开(公告)日：1984-11-13

    申请号：CA387723

    申请日：1981-10-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： REINER ROLAND ,  WEISS URS

    IPC: C07D293/06 ,  C07D501/20 ,  C07D501/24 ,  C07D505/00

    Abstract: RAN 4410/147 Acyl derivatives of the general formula I in which Rl represents one of the 3-substituents usable in cephalosporin chemistry, R2 represents hydrogen, lower alkyl or COOR3-lower alkyl, wherein R3 signifies hydrogen, a cation of a base or a readily hydrolyzable ester group, and X represents sulphur, oxygen or one of the groups -SO- and -SO2-, as well as readily hydrolyzable esters, readily hydrolyzable ethers and salts of these compounds and hydrates of the compounds of formula I or of their esters, ethers and salts, pharmaceutical preparations containing such compounds, their use in the treatment or prophylaxis of infectious diseases, their manufacture as well as novel starting materials used in their manufacture.

    49.
    发明专利
    未知

    公开(公告)号：FI842614A0

    公开(公告)日：1984-06-28

    申请号：FI842614

    申请日：1984-06-28

    Applicant: HOFFMANN LA ROCHE

    Inventor： MONTAVON MARC ,  REINER ROLAND

    IPC: C07D501/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/16 ,  C07D501/36 ,  C07D501/46 ,  C07D

    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.

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