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    Cyclopeptides derived from polymyxins and their preparation
    1.
    发明授权
    Cyclopeptides derived from polymyxins and their preparation 失效
    从多聚氰胺衍生的环状物及其制备

    公开(公告)号：US3753970A

    公开(公告)日：1973-08-21

    申请号：US3753970D

    申请日：1970-08-04

    Applicant: RHONE POULENC SA

    Inventor： BOUCHAUDON J ,  JOLLES G

    IPC: C07K7/62 ,  C07C103/52 ,  C07G7/00 ,  C08H1/00

    CPC classification number: C07K7/62 ,  Y10S930/19 ,  Y10S930/27

    Abstract: THE NEW CYCLOPEPTIDES OF THE FORMULA:

    DAB
    IN WHICH Y-Z REPRESENTS AN AMINO ACID CHAIN SELECTED FROM D-LEU-THR,D-PHE-LEU, D-LEU-LEU AND D-LEU-ILEU, G REPRESENTS AN AMINO-PROTECTING RADICAL OF THE FORMULA:

    PY-CH(-R)-OOC-

    IN WHICH PY REPRESENTS PYRIDYL, PYRIDYL-N-OXIDE, OR PYRIDYL OR PYRIDYL-N-OXIDE CARRYING A METHYL SUBSTITUENT, R REPRESENTS HYDROGEN, ALKYL OF 1 TO THROUGH 5 CARBON ATOMS, OR PHENYL, AND DAB REPRESENTS A,Y-DIAMINOBUTYRIC AID, THE AMINO ACIDS HAVING THE L-CONFFIGURATION UNLESS OTHERWISE INDICATED, SAID CYCLOPEPTIDES CONTAINING ONLY A SINGLE FREE AMINO GROUP, ARE USEFUL INTERMEDIATES FOR THE SYNTHESIS OF SEMI-SYNTHETIC PRODUCTS DERIVED FROM POLYMYXINS.

    Process for the preparation of cyclopeptides derived from polymyxins
    2.
    发明授权
    Process for the preparation of cyclopeptides derived from polymyxins 失效
    用于制备衍生自多聚霉素的环孢菌素的方法

    公开(公告)号：US3817973A

    公开(公告)日：1974-06-18

    申请号：US22229672

    申请日：1972-01-31

    Applicant: RHONE POULENC SA

    Inventor： BOUCHAUDON J ,  JOLLES G

    IPC: A61K38/00 ,  C07K7/62 ,  C07C103/52 ,  C07G7/00

    CPC classification number: C07K7/62 ,  A61K38/00 ,  Y02P20/55 ,  Y10S930/19 ,  Y10S930/27

    Abstract: D R A W I N G
    WHEREIN A is alkyl of three through 18 carbon atoms optionally substituted by hydroxy, amino or cyano; or alkyl of one through four carbon atoms substituted by a monocyclic or polycyclic alkyl radical or phenyl optionally substituted by halogen or alkoxy; or phenyl optionally substituted by halogen or alkoxy, X is -CO- or -SO2-, and Y-Z is one of the chains D-Phe-Leu, D-Leu-Leu and DLeu-Ileu, are prepared by introducing the grouping A-X-Dab-ThrDab- onto the appropriate cyclopeptide having its amino functions protected. New polymyxins of the said formula have antibiotic properties.
    Polymyxins of the formula

    Abstract translation: 式AD的多粘菌素是任选被羟基，氨基或氰基取代的三至十八个碳原子的烷基; 或被单环或多环烷基取代的一至四个碳原子的烷基或任选被卤素或烷氧基取代的苯基; 或任选被卤素或烷氧基取代的苯基，X是-CO-或-SO 2 - ，Y Z是链D-Phe-Leu，D-Leu-Leu和D-Leu-Ileu之一，通过引入分组 AX-Dab-Thr-Dab-保护其具有氨基功能的适当的环肽。 所述配方的新型多粘菌素具有抗生素特性。

    New cyclopeptides
    3.
    发明授权
    New cyclopeptides 失效
    新循环

    公开(公告)号：US3719656A

    公开(公告)日：1973-03-06

    申请号：US3719656D

    申请日：1969-12-24

    Applicant: RHONE POULENC SA

    Inventor： JOLLES G

    IPC: A61K38/00 ,  C07K7/64 ,  C07C103/52

    CPC classification number: C07K7/64 ,  A61K38/00 ,  Y10S930/19 ,  Y10S930/27

    Abstract: Cyclopeptides having antitubercular activity derived from antibiotics of the formula: R-cyclopeptide A wherein cyclopeptide A designates a nonapeptide residue of the formula: IN WHICH MePro signifies L-trans-4-methyl-proline; MeThr signified L-N-methylthreonine; MeVal signifies L-N-methylvaline; MeLeu signifies D-N-methylleucine; Pro signifies L-proline; Gly signifies glycine, and Leu signifies L-leucine, and R represents hydrogen or an alkanoyl, alkenoyl, alkadienoyl, alkoxycarbonyl, aroyl, aralkanoyl, arylsulphenyl, arylsulphinyl, aryl sulphonyl, cycloalkylcarbonyl, heterocyclyclcarbonyl or heterocyclylakanoyl radical, or a residue of a linear or cyclic peptide radical attached through a carbonyl group to the nitrogen atom of the Ltrans-4-methyl-proline grouping the the side chain of the cyclopeptide A, and non-toxic acid addition and quaternary ammonium salts thereof, possess antitubercular activity and activity against gram-positive and gram-negative microorganisms.

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