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    PROCESSES FOR THE MANUFACTURE OF NOVEL GLUCOSE DERIVATIVES
    5.
    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.

    9.
    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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