ACYLATED SUGAR DERIVATIVES
    51.
    发明专利

    公开(公告)号:AU4312785A

    公开(公告)日:1985-12-05

    申请号:AU4312785

    申请日:1985-05-29

    Applicant: CIBA GEIGY AG

    Abstract: There are described sugar derivatives of the formula I (I) that have immuno-stimulating action and that contain as inventive element at least one radical A1 or A2. These radicals A1 and A2, which may be constituents of the radicals R1, R2, R4, R6, R9, R10 or R12 according to formula I, are defined as follows: A1 represents lower alkanoyl that is substituted by aryl, heteroaryl or heteroarylthio and that may be additionally substituted by an ethylene radical which, with the above-mentioned aryl or heteroaryl substituent, forms a five-membered ring or represents ortho- or ortho/meta-substituted aroyl. A2 represents lower alkoxy substituted by aryl, heteroaryl or heteroarylthio. Also described are processes for the manufacture of the compounds of the formula I and novel intermediates.

    ANTIBIOTIC PREPARATIONS HAVING INCREASED EFFECTIVENESS, PROCESSES FOR THEIR MANUFACTURE AND METHOD FOR INCREASING THE ANTIBIOTIC ACTION OF ANTIBIOTICS

    公开(公告)号:CA1175748A

    公开(公告)日:1984-10-09

    申请号:CA369055

    申请日:1981-01-22

    Applicant: CIBA GEIGY AG

    Abstract: The invention relates to pharmaceutical preparations that contain an antibiotic and a muramylpeptide of the formula I or a salt thereof, to processes for their manufacture and to a method for increasing the antibiotic effectiveness of antibiotics. (I) In the formula I, X represents carbonyl or carbonyloxy, R1 represents optionally substituted alkyl or aryl, R2, R3, R4 and R6 represent hydrogen or lower alkyl, R5 represents hydrogen, optionally substituted lower alkyl, cycloalkyl, aryl or nitrogen-containing heterocyclyl, or R4 and R5 together represent also C3-C4 alkylene, R7 represents hydrogen or free, esterified or amidated carboxyl, one of the radicals A1 and A2 represents a radical of the formula II and the other of the radicals A1 and A2 represents optionally substituted or functionally modified hydroxy or amino. (II) In the formula II, T represents NH or O, Y represents an optionally substituted alkylene group that can also be interrupted by oxycarbonyl or iminocarbonyl, W represents hydrogen and Z represents an optionally esterified or etherified 1,2-dihydroxyethyl or 2-hydroxyethyl group, or W and Z represent an optionally esterified or etherified hydroxymethyl group.

    58.
    发明专利
    未知

    公开(公告)号:FI840259A0

    公开(公告)日:1984-01-23

    申请号:FI840259

    申请日:1984-01-23

    Applicant: CIBA GEIGY AG

    Abstract: The invention relates to lipopeptides of the formula I, (I) * = -R** = -R or -S*** = -R in which each of Ra1 and Rb1, independently of the other, represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 7 to 21 carbon atoms that is optionally substituted by oxygen functions, or one of the radicals Ra1-CO- and Rb1-CO- represents hydrogen and the other of the radicals Ra1-CO- and Rb1-CO- represents an acyl radical, wherein Ra1 and Rb1 have the meanings given above, R2 represents an aliphatic or cycloaliphatic-aliphatic hydrocarbon radical having from 1 to 21 carbon atoms that is optionally substituted by oxygen functions, n=0 or 1, As DEG represents a radical of the formula -O-Kw-CO- or -NH-Kw-CO- wherein Kw represents an aliphatic hydrocarbon radical having a maximum of 12 carbon atoms, As1 represents a D- or L- alpha -amino acid, each of Z1 and Z2, independently of the other, represents hydroxy or the N-terminal radical of a D- or L- alpha -aminocarboxylic acid, of an amino-lower alkanesulphonic acid or of a peptide having a maximum of 6 amino acids from the group consisting of D- or L- alpha -aminocarboxylic acids and amino-lower alkanesulphonic acids, and Z3 represents hydrogen or -CO-Z4 wherein Z4 represents hydroxy or the N-terminal radical of a D- or L- alpha -amino acid, of an amino-lower alkanesulphonic acid or of a peptide having a maximum of 6 amino acids from the group consisting of D- or L- alpha -aminocarboxylic acids and amino-lower alkanesulphonic acids, and the amides and esters of such compounds that contain carboxy groups. The novel lipopeptides have an immunity-stimulating action.

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