公开(公告)号：AU5376786A

公开(公告)日：1986-08-28

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 ,  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 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.

公开(公告)号：NO860624A

公开(公告)日：1986-08-21

申请号：NO860624

申请日：1986-02-19

Applicant: CIBA GEIGY AG

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

IPC: C07K9/00 ,  C07K

CPC classification number: C07K9/005

公开(公告)号：DK77286A

公开(公告)日：1986-08-21

申请号：DK77286

申请日：1986-02-19

Applicant: CIBA GEIGY AG

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

IPC: C07K9/00 ,  C07H

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.

公开(公告)号：DD232921A5

公开(公告)日：1986-02-12

申请号：DD27672585

申请日：1985-05-28

Applicant: CIBA GEIGY AG

Inventor： BASCHANG GERHARD ,  HARTMANN ALBERT ,  WACKER OSKAR

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

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.

公开(公告)号：DK236585A

公开(公告)日：1985-11-30

申请号：DK236585

申请日：1985-05-28

Applicant: CIBA GEIGY AG

Inventor： BASCHANG GERHARD ,  HARTMANN ALBERT ,  WACKER OSKAR

IPC: A61K38/00 ,  A61K39/39 ,  A61P37/04 ,  C07K1/113 ,  C07K9/00 ,  C07K

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.

公开(公告)号：NO840263L

公开(公告)日：1984-07-26

申请号：NO840263

申请日：1984-01-24

Applicant: CIBA GEIGY AG

Inventor： BASCHANG GERHARD ,  WACKER OSKAR ,  HARTMANN ALBERT

IPC: C07C20060101 ,  C07K5/08 ,  C07K5/10 ,  C07K7/06 ,  C07C

公开(公告)号：FI840259A

公开(公告)日：1984-07-26

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 ,  C07C91/26

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.

公开(公告)号：AU2374584A

公开(公告)日：1984-07-26

申请号：AU2374584

申请日：1984-01-24

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 ,  C07C103/52

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.

公开(公告)号：ZA8305357B

公开(公告)日：1984-03-28

申请号：ZA8305357

申请日：1983-07-22

Applicant: CIBA GEIGY AG

Inventor： HARTMANN ALBERT ,  WACKER OSKAR ,  BASCHANG GERHARD ,  TARCSAY LAJOS

IPC: A61K38/00 ,  A61K38/14 ,  A61K38/17 ,  A61P31/12 ,  A61P35/00 ,  C07K1/113 ,  C07K9/00 ,  C07K14/52 ,  C07K14/53 ,  C07K14/535 ,  C07H ,  A61K

CPC classification number: C07K9/005

公开(公告)号：NO832691L

公开(公告)日：1984-01-24

申请号：NO832691

申请日：1983-07-22

Applicant: CIBA GEIGY AG

Inventor： HARTMANN ALBERT ,  TARCSAY LAJOS ,  WACKER OSKAR ,  BASCHANG GERHARD

IPC: A61K31/70 ,  A61K38/00 ,  A61K38/14 ,  A61K38/17 ,  A61P31/12 ,  A61P35/00 ,  C07H15/00 ,  C07K1/113 ,  C07K9/00 ,  C07K14/52 ,  C07K14/53 ,  C07K14/535 ,  C07H

Abstract: The compounds of the formula I (I) in which each of R1, R4 and R6, independently of the others, represents hydrogen or lower alkanoyl, R2 represents C1-4-alkyl, hydroxymethyl or phenyl, R3 represents hydrogen or methyl, R5 represents hydrogen or C1-3-alkyl, R7 represents C1-3-alkyl that is unsubstituted or substituted by hydroxy, mercapto or methylthio, R8 represents hydrogen or lower alkyl, X represents oxygen or the group NH, Y represents C1-4-alkylidene, and each of R9 and R10, independently of the other, represents C11-17-alkyl or C11-17-alkenyl, and their salts, have an immunostimulating activeity.