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    PROCESS FOR PRODUCING NEW LIPOPHYL MURAMYL-PEPTIDES
    21.
    发明专利
    PROCESS FOR PRODUCING NEW LIPOPHYL MURAMYL-PEPTIDES 未知

    公开(公告)号：HU188861B

    公开(公告)日：1986-05-28

    申请号：HU185480

    申请日：1980-07-24

    Applicant: CIBA GEIGY AG

    Inventor： TARCSAY LAJOS ,  HARTMANN ALBERT ,  BASCHANG GERHARD ,  STANEK JAROSLAV

    IPC: C07H13/00 ,  A61K38/00 ,  A61K38/14 ,  A61K39/39 ,  A61P37/04 ,  C07K1/06 ,  C07K1/113 ,  C07K9/00 ,  C07K14/52 ,  C07K14/53 ,  C07K14/535 ,  C07K5/02

    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.

    23.
    发明专利
    未知

    公开(公告)号：FI853982A0

    公开(公告)日：1985-10-14

    申请号：FI853982

    申请日：1985-10-14

    Applicant: CIBA GEIGY AG

    Inventor： TARCSAY LAJOS ,  EIBL HANSJOERG ,  FANKHAUSER PETER ,  PEIL ANITA

    IPC: A61K9/127 ,  A61K9/00 ,  A61K9/50 ,  A61K47/24 ,  C07F9/10 ,  A61K

    Abstract: The invention relates to pharmaceutical compositions containing synthetic, substantially pure phosphatidyl serine and phosphatidyl choline and a substance or a mixture of substances having biological activity. The invention also relates to mixtures comprising synthetic, substantially pure phosphatidyl serine and phosphatidyl choline, and also to processes for the manufacture of the pharmaecutical compositions, and the use thereof.

    PROCESSES FOR THE MANUFACTURE OF NOVEL GLUCOSE DERIVATIVES
    24.
    发明专利
    PROCESSES FOR THE MANUFACTURE OF NOVEL GLUCOSE DERIVATIVES 未知

    公开(公告)号：CA1183528A

    公开(公告)日：1985-03-05

    申请号：CA403054

    申请日：1982-05-14

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  DIETRICH FELIX M ,  GISLER ROLAND ,  HARTMANN ALBERT ,  STANEK JAROSLAV ,  TARCSAY LAJOS

    IPC: C07C103/52

    Abstract: The invention relates to processes for the manufacture of muramyl peptide derivatives of the formula I (I) characterised in that at least one of the radicals R7, R9 and R13 represents lower alkyl, whilst the others represent hydrogen. The remaining substituents of the formula I are defined in claim 1. These compounds possess excellent immunomodulatory activity whilst, at the same time, especially when the substituent R7 represents lower alkyl, the pyrogenic side effect is greatly reduced as compared with the corresponding NH-compounds. They can therefore be used in the form of pharmaceutical preparations. In addition, the compounds according to the invention are used for the manufacture of the conjugates with antigens described in European Patent Application No. 79100513.5 and in Canadian Patent Application No. 321 992.

    LIPOPHILIC MURAMYL PEPTIDES AND PROCESSES FOR THEIR MANUFACTURE
    25.
    发明专利
    LIPOPHILIC MURAMYL PEPTIDES AND PROCESSES FOR THEIR MANUFACTURE 未知

    公开(公告)号：CA1183129A

    公开(公告)日：1985-02-26

    申请号：CA356860

    申请日：1980-07-23

    Applicant: CIBA GEIGY AG

    Inventor： TARCSAY LAJOS ,  BASCHANG GERHARD ,  HARTMANN ALBERT ,  STANEK JAROSLAV

    IPC: C07H13/00 ,  A61K38/00 ,  A61K38/14 ,  A61K39/39 ,  A61P37/04 ,  C07K1/06 ,  C07K1/113 ,  C07K9/00 ,  C07K14/52 ,  C07K14/53 ,  C07K14/535 ,  C07C103/52 ,  C07H15/00

    Abstract: Novel lipophilic muramyl peptides and processes for their manufacture The invention relates muramyl peptide compounds, especially of the formula (D) (L) (D) in which R1 represents, for example, alkyl or phenyl, R3 represents, for example ) hydrogen or methyl. and R5 represents, for exampie, hydrogen or lower alkyl optionally substituted, for example, by hydroxy, mercapto, or methylthio, and in which one of the radicals A1 and A2 represents a group of the formula in which T represents the group of the formula -NH or -O, and Y represents an alkylene radical optionally interrupted by a radical of the formula -CO-O- or -CO-NH-, and in which W represents hydrogen and Z represents a hydroxy-substituted ethyl group, wherein at least one hydroxy group is esterified by a long-chained acyl radical or W and Z represent hydroxymethyl, wherein hydroxy is esterified by a long-chained acyl radical, and the other of the radicals A1 and A2 represents optionally etherified hydroxy ox optionally substituted amino. The novel compounds have immunopotentiating properties.

    30.
    发明专利
    未知

    公开(公告)号：NO793993A

    公开(公告)日：1979-08-27

    申请号：NO793993

    申请日：1979-12-07

    Applicant: CIBA GEIGY AG

    Inventor： BASCHANG GERHARD ,  DIETRICH FELIX M ,  GISLER ROLAND ,  STANEK JAROSLAV ,  HARTMANN ALBERT ,  TARCSAY LAJOS

    IPC: G01N33/531 ,  A61K38/14 ,  A61K39/00 ,  A61K39/385 ,  A61K39/39 ,  C07H9/04 ,  C07H15/04 ,  C07H23/00 ,  C07K1/113 ,  C07K9/00 ,  C07K14/76 ,  C07K16/00 ,  C07K19/00 ,  C07H

    CPC classification number: C07H9/04 ,  A61K39/385 ,  A61K2039/55583 ,  A61K2039/6062 ,  C07H23/00 ,  C07K9/005 ,  Y02A50/41 ,  Y02A50/412 ,  Y02A50/414 ,  Y02A50/416 ,  Y02A50/423

    Abstract: (A) Novel antigen derivs. (I) consist of an antigen to which at least one muramyl peptide is covalently bonded, opt. via a bridging gp. Prefd. cpds. are of formula (Ia): A-[(Z)m-MP]n (Ia) (A is an antigen residue; Z is a bridging gp.; MP is a muramyl peptide residue; m = 0 or 1; n >=1). The muramyl peptides are pref. of formula (III) (or the corresp. oligomers). (X is CO, COO or SO2; R1 is H, alkyl, opt. substd. benzyl or acyl; R2 is opt. substd. alkyl or carbocyclic aryl; R4 and R6 are each H, alkyl, opt. substd. benzyl or acyl; R3 is H or alkyl; R7, R9 and R13 are each H or lower alkyl; R8 is H, lower alkyl, opt. etherified or esterified lower hydroxyalkyl or mercaptoalkyl, opt. acylated aminoalkyl, 5 or 6C cycloalkyl, (5 or 6C cycloalkyl)-lower alkyl, opt. substd. aryl or aralkyl, or N-contg. heterocyclyl or heterocyclyl-lower alkyl; R7 and R8 can also together form 3 or 4C alkylene; R10, R11 and R12 are each opt. esterified or amidated carboxy, and R11 can also be H; or R1, R4 and R6 are tri-(lower alkyl)-silyl, pref. SiMe3). (B) Cpds. (II) are new provided that (i) X is CO and (ii) at least one of R7, R9 and R13 is lower alkyl unless R1, R4 and R6 are trialkylsilyl or R7 and R8 form a ring. (I) are used in a wide variety of vaccines against bacteria, viruses, tumour cells, parasites, allergens etc.

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