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    Erythromycin derivatives
    1.
    发明授权
    Erythromycin derivatives 失效
    红霉素衍生物

    公开(公告)号：US3736313A

    公开(公告)日：1973-05-29

    申请号：US3736313D

    申请日：1971-02-26

    Applicant: ABBOTT LAB

    Inventor： JONES P ,  PERUN T

    IPC: C07H17/08 ,  C07C129/18

    CPC classification number: C07H17/08

    Abstract: THE 2'',4"-DI-O-ALKANOYL AND THE 2'',4",11-TRI-O-ALKANOYL DERIVATIVES OR ERYTHROMYCIN ARE PREPARED BY ESTERFICATION OF ERYTHROMYCIN WITH AN APPROPRIATE ACID ANHYDRIDE. THESE RESULTING ESTER DERIVATIVES ARE INITIALLY DE-ESTERFIED IN THE 2''-POSITION TO PROPARE THE 4"-O-ALKANOYL OR THE 4",11-DI-O-ALKANOYL ERYTHORMYCIN, AND THEN, IF DESIRED, THESE DE-ESTERFICATION PRODUCTS ARE REACTED WITH ANOTHER ACID ANHYDRIDE TO PREPARE A DISSIMILARLY DI-SUBSTITUTED OR TRI-SUBSTITUTED ESTER. THROUGH REPETITIVE ESTERFICATION AND DE-ESTERFICATION, COMBINATIONS OF THE MONO SUBSTITUTED AND THE SIMILARLY OR DISSIMILARLY MULTIPLE SUBSTITUTED ERYTHROMYCIN ESTERS ARE PREPARED. THESE COMPOUNDS HAVE ANTIBIOTIC ACTIVITY.

    SELDOMYCIN FACTOR 5 DERIVATIVES
    4.
    发明专利
    SELDOMYCIN FACTOR 5 DERIVATIVES 未知

    公开(公告)号：ZA774580B

    公开(公告)日：1978-06-28

    申请号：ZA774580

    申请日：1977-07-28

    Applicant: ABBOTT LAB

    Inventor： PERUN T ,  CARNEY R ,  MCALPINE J

    IPC: C07H15/236 ,  A61K

    Abstract: Described are novel derivatives of seldomycin factor 5 (XK-88-5) and particularly 3'-deoxyseldomycin factor 5, which exhibit improved activity against gram-positive and gram-negative bacteria resistant to aminoglycoside antibiotics, and a method of preparing them.

    ERYTHROMYCIN DERIVATIVES
    6.
    发明专利
    ERYTHROMYCIN DERIVATIVES 未知

    公开(公告)号：GB1270771A

    公开(公告)日：1972-04-12

    申请号：GB1804970

    申请日：1970-04-15

    Applicant: ABBOTT LAB

    Inventor： PERUN T ,  JONES P

    IPC: C07H17/08

    Abstract: 1,270,771. Erythromycin derivatives. ABBOTT LABORATORIES. 15 April, 1970 [1 May, 1969], No. 18049/70. Heading C2A. Erythromycin derivatives having antibiotic activity of the general formula in which R 1 is H or OH and R 2 is H or an O-C 1-4 alkanoyl provided that when R 2 is H R 3 is also H and R 4 is an O-C 1-4 alkanoyl and when R 2 is O-alkanoyl, R 3 and R 4 are independently selected from H and O-C 1-4 alkanoyl groups, and salts thereof with acids may be prepared from erythromycin as shown in the accompanying flow chart wherein reaction type (1) indicates the reaction of erythromycin or an ester derivative thereof to introduce an ester group only into the unsubltituted 2 position without effecting the 11 or 4 11 positions; (2) indicates the reaction of erythromycin to introduce an ester group into the 2 1 and 4 11 positions without affecting the unsubstituted 11 position; (3) indicates the reaction of erythromycin or an ester derivative thereof to introduce an ester group into the unsubstituted 11 position; and also into the 2 1 or 4 11 positions if they also are unsubstituted; and (4) indicates the hydrolysis of a 2 1 or a 4 11 ester. Examples of erythromycin derivatives prepared include 11-acetyl erythromycins A and B, and 11-formyl erythromycins A and B. Antibiotic compositions for oral administration in the form of tablets or capsules comprise the above erythromycin derivatives and a carrier or filler.

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