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    83.
    发明专利
    未知

    公开(公告)号：FI83524B

    公开(公告)日：1991-04-15

    申请号：FI840259

    申请日：1984-01-23

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  HARTMANN ALBERT ,  WACKER OSKAR

    IPC: A61K38/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/04 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/103 ,  C07K7/02 ,  C07K7/06 ,  C07K9/00

    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.

    ACYLATED HEXOSE DERIVATIVES OF DI AND TRIPEPTIDES
    84.
    发明专利
    ACYLATED HEXOSE DERIVATIVES OF DI AND TRIPEPTIDES 未知

    公开(公告)号：AU597571B2

    公开(公告)日：1990-06-07

    申请号：AU5376886

    申请日：1986-02-19

    Applicant: CIBA GEIGY AG

    Inventor： WACKER OSKAR ,  HARTMANN ALBERT ,  STANEK JAROSLAV ,  FECHTIG BRUNO ,  BASCHANG GERHARD

    IPC: C07K9/00 ,  A61K31/70 ,  A61K37/02

    Abstract: The derivatives have the formula I in which the hexose moiety is derived from D-glucose, D-mannose or D-galactose, n is 0 or 1, and R , R and R are, independently of one another, lower alkanoyl or benzoyl, R is lower alkyl or phenyl, R , R and R are, independently of one another, hydrogen or lower alkyl, or R and R together are trimethylene and R is hydrogen, R is hydrogen or unsubstituted or phenyl-, hydroxyl-, mercapto- or lower alkylthio-substituted lower alkyl, R and R are, independently of one another, hydroxyl, amino, C1-10-alkoxy, aryl-lower alkoxy, alkanoyloxy-lower alkoxy with up to 16 C atoms, aroyloxy-lower alkoxy, 3-cholesteryloxy or 2-trimethylammonioethyloxy, R is hydrogen, carboxyl, lower alkoxycarbonyl or aryl-lower alkoxycarbonyl and R is hydrogen or unsubstituted or amino-, hydroxyl-, lower alkanoylamino-, lower alkanoyloxy-, 2-benzyloxycarbonylaminoethylsulphinyl-, 2-benzyloxycarbonylaminoethylsulphonyl-, 2-lower-alkoxycarbonyl- aminoethylsulphinyl-, 2-lower-alkoxycarbonylaminoethylsulphonyl- or guanidino-substituted lower alkyl, with the proviso that at least one of the radicals R and R is different from hydroxyl, amino and C1-7-alkoxy or R is different from hydrogen, carboxyl and alkoxycarbonyl with up to 7 C atoms in the alkoxy moiety, and these compounds and salts thereof where appropriate can be used for the prophylaxis and therapy of viral infections.

    ACYLATED SUGAR DERIVATIVES, PROCESSES FOR THEIR MANUFACTURE, AND THEIR USE
    85.
    发明专利
    ACYLATED SUGAR DERIVATIVES, PROCESSES FOR THEIR MANUFACTURE, AND THEIR USE 未知

    公开(公告)号：CA1262015A

    公开(公告)日：1989-09-26

    申请号：CA482399

    申请日：1985-05-27

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  HARTMANN ALBERT ,  WACKER OSKAR

    IPC: A61K38/00 ,  A61K39/39 ,  A61P37/04 ,  C07K1/113 ,  C07K9/00 ,  A61K37/02

    Abstract: Acylated sugar derivatives, processes for their manufacture, and their use 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 di als 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 orthoor 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.

    88.
    发明专利
    未知

    公开(公告)号：FI78300B

    公开(公告)日：1989-03-31

    申请号：FI852841

    申请日：1985-07-22

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  FECHTIG BRUNO ,  HARTMANN ALBERT ,  LUKAS BOHUMIR ,  WACKER OSKAR

    IPC: A61K31/66 ,  A61P31/12 ,  C07F9/09 ,  C07F9/10

    Abstract: Described are phosphatidyl compounds of the formula I (I) in which R1 represents C3-14-alkanoyl, benzoyl, the acyl radical of an alpha -aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the alpha -amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a beta -aminocarboxylic acid or an alpha - or beta -hydroxycarboxylic acid, T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen, Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy, W represents hydrogen, and Z represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C8-30-carboxylic acid or is etherified by an aliphatic C8-30-alcohol, or each of W and Z represents a hydroxymethyl group that is esterified by an aliphatic C8-30-carboxylic acid or is etherified by an aliphatic C8-30-alcohol, and their salts, and processes for their manufacture. The mentioned novel compounds, and structurally related compounds that are likewise described and that belong to the state of the art, are used for the propylaxis and treatment of viral infections.

    PEPTIDE DERIVATIVES
    89.
    发明专利
    PEPTIDE DERIVATIVES 未知

    公开(公告)号：CA1247089A

    公开(公告)日：1988-12-20

    申请号：CA445858

    申请日：1984-01-23

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  HARTMANN ALBERT ,  WACKER OSKAR

    IPC: A61K38/00 ,  A61P31/04 ,  A61P31/12 ,  A61P37/04 ,  C07K1/02 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/103 ,  C07K7/02 ,  C07K7/06 ,  C07K9/00 ,  A61K37/02

    Abstract: Novel peptide derivatives The invention relates to lipopeptides of the formula I, (I) * = R ** = R or S *** = R in which each of R?a and R?, independently of the other, represents an aliphatic or aliphatic-cycloaliphatic hydrocarbon radical having from 7 to 21 carbon atoms that is optionally substituted by oxygen functions, or one of the radicals R?-CO- and R?-CO- represents hydrogen and the other of the radicals R?-Co- and R?-Co- represents an acyl radical, wherein R? and R? have the meanings given above, R2 represents an aliphatic or aliphatic-cyclo-aliphatic hydrocarbon radical having from 1 to 21 carbon atoms that is optionally substituted by oxygen functions, n = O or 1, As.degree. 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 aminolower 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 immunitystimulating action.

    ACYLATED HEXOSE DERIVATIVES OF DI AND TRIPEPTIDES
    90.
    发明专利
    ACYLATED HEXOSE DERIVATIVES OF DI AND TRIPEPTIDES 未知

    公开(公告)号：AU579448B2

    公开(公告)日：1988-11-24

    申请号：AU5376786

    申请日：1986-02-19

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  HARTMANN ALBERT ,  STANEK JAROSLAV ,  WACKER OSKAR

    IPC: C07K9/00 ,  C07K5/06 ,  C07K5/02 ,  A61K37/02

    Abstract: The derivatives have the formula I in which the hexose moiety is derived from D-glucose, D-mannose or D-galactose, n is 0 or 1, and R is lower alkanoyl or benzoyl, R is lower alkyl or phenyl, R , R and R are, independently of one another, hydrogen or lower alkyl, or R and R together are trimethylene and R is hydrogen, R and R are, independently of one another, hydrogen, lower alkanoyl or benzoyl, R is hydrogen or unsubstituted or phenyl-, hydroxyl-, mercapto- or lower alkylthio-substituted lower alkyl, R and R are, independently of one another, hydroxyl, amino or lower alkoxy, R is hydrogen, carboxyl or lower alkoxycarbonyl and R is hydrogen or unsubstituted or amino-, lower alkanoylamino-, hydroxyl-, guanidino-, lower alkanoyloxy-, 2-benzyloxycarbonylamino- ethylsulphinyl-, 2-benzyloxycarbonylaminoethylsulphonyl-, 2-lower- alkoxycarbonylaminoethylsulphinyl- or 2-lower-alkoxycarbonylamino- ethylsulphonyl-substituted lower alkyl, with the proviso that in the compounds in which the pyranose moiety is derived from D-glucose and, at the same time, n is 0, R , R and R are hydrogen, R is methyl, R is amino and R is hydroxyl, and in which the radicals R , R and R all have the same meaning, R , R and R are different from acetyl and butyryl when R is phenyl and, at the same time, R is hydrogen, and that R , R and R are different from acetyl when R and R are both methyl, and these compounds and salts thereof where appropriate have an antiviral action in vivo.

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