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    De(n-methyl)-n-substituted derivatives of erythromycin
    2.
    发明授权
    De(n-methyl)-n-substituted derivatives of erythromycin 失效
    DE（N-甲基）-N-取代的嘌呤霉素衍生物

    公开(公告)号：US3681325A

    公开(公告)日：1972-08-01

    申请号：US3681325D

    申请日：1970-09-30

    Applicant: ABBOTT LAB

    Inventor： FREIBERG LESLIE ALAN

    IPC: C07H17/08 ,  C07C47/18

    CPC classification number: C07H17/08

    Abstract: NEW DERIVATIVES OF ERTHROMYCIN A AND B, HAVING ANTIMICROBIAL ACTIVITY OF THE FORMULA

    2-(ERY-O-),3-HO,4-(CH3-N(-Z)-),6-CH3-PERHYDROPYRAN

    WHEREIN Z IS BENZYL; HALO, NITRO, AMINO, LOWERALKYL, LOWERALKOXY, CARBOXYBENZYL, HALOLOWERALKYL, DILOWERALKYLAMINOMETHYL, CARBOXY, LOWERALKOXYMETHYL, CYANO AND HYDROCARBYLENE SUBSTITUTED BENZYL; ALLYL, LOWERALKYL AND PHENYLSUBSTITUTED B AND Y ALLYL, E.G., CROTYL; CYANO; AND CYANOLOWERALKYL; AND ERY IS THE CLADINOSE AND ERYTHRONOLIDE MOIETIES OF ERYTHROMYCIN.

    3-AMINO-3-DEMETHOXYFORTIMICINS
    4.
    发明专利
    3-AMINO-3-DEMETHOXYFORTIMICINS 未知

    公开(公告)号：GB2118180A

    公开(公告)日：1983-10-26

    申请号：GB8308762

    申请日：1983-03-30

    Applicant: ABBOTT LAB

    Inventor： TADANIER JOHN SOLOMAN ,  HALLAS ROBERT ,  FREIBERG LESLIE ALAN ,  BACINO DAVID JAMES

    IPC: A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  C07H15/22 ,  A61K31/71

    Abstract: Disclosed herein are fortimicin derivatives represented by the formula: wherein R is hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, loweracyl, aminoloweracyl, diaminoloweracyl, hydroxyloweracyl, N-loweralkylaminoloweracyl, N,N-diloweralkylaminoloweracyl, or aminohydroxyloweracyl, and the pharmaceutically acceptable salts thereof. Also disclosed are intermediates useful in the preparation of these compounds and compositions of these compounds together with a pharmaceutically acceptable carrier and/or diluent.

    DEMETHYLATION OF 3-AMINO MACROLIDES
    5.
    发明专利
    DEMETHYLATION OF 3-AMINO MACROLIDES 未知

    公开(公告)号：AU3385571A

    公开(公告)日：1973-03-29

    申请号：AU3385571

    申请日：1971-09-23

    Applicant: ABBOTT LAB

    Inventor： FREIBERG LESLIE ALAN

    IPC: C07H17/08 ,  C07D7/04

    Abstract: The 3-dimethyl amino substituent of the desosamine and mycaminose moieties of macrolide antibiotics are mono- and didemethylated by reaction with halogen, preferably iodine, in the presence of base at a controlled pH. The resulting compounds have antibiotic activity, and furthermore are useful as intermediates for alkylation and the like.

    6.
    发明专利
    未知

    公开(公告)号：IT1164161B

    公开(公告)日：1987-04-08

    申请号：IT2050983

    申请日：1983-04-08

    Applicant: ABBOTT LAB

    Inventor： TADANIER JOHN SOLOMAN ,  HALLAS ROBERT ,  FREIBERG LESLIE ALAN ,  BACINO DAVID JAMES

    IPC: A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P31/04 ,  C07H15/224 ,  A61K

    Abstract: Disclosed herein are fortimicin derivatives represented by the formula: wherein R is hydrogen, loweralkyl, aminoloweralkyl, diaminoloweralkyl, N-loweralkylaminoloweralkyl, N,N-diloweralkylaminoloweralkyl, hydroxyloweralkyl, aminohydroxyloweralkyl, N-loweralkylaminohydroxyloweralkyl, N,N-diloweralkylaminohydroxyloweralkyl, loweracyl, aminoloweracyl, diaminoloweracyl, hydroxyloweracyl, N-loweralkylaminoloweracyl, N,N-diloweralkylaminoloweracyl, or aminohydroxyloweracyl, and the pharmaceutically acceptable salts thereof. Also disclosed are intermediates useful in the preparation of these compounds and compositions of these compounds together with a pharmaceutically acceptable carrier and/or diluent.

    7.
    发明专利
    未知

    公开(公告)号：GR73848B

    公开(公告)日：1984-05-07

    申请号：GR810164112

    申请日：1981-02-12

    Applicant: ABBOTT LAB

    Inventor： BODOR NICHOLAS S ,  FREIBERG LESLIE ALAN

    IPC: A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

    Abstract: High water-soluble erythromycin A derivatives wherein the desosamine moiety is quaternized with an acyloxy-, benzoyloxy- or alkoxycarbonyl-(or carboxy)-acylmethyl iodide, bromine or chloride and esterified in the 2-position with loweralkyl or -(CH2)nCO2R sec , wherein R sec is H, loweralkyl or substituted loweralkyl and n is an integer from 1-5. These new esters readily convert to erythromycin A upon administration to warm-blooded animals.

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