9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin a 9a,11-cyclic carbamates
    5.
    发明授权
    9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin a 9a,11-cyclic carbamates 失效
    9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素a 9a,11-环状氨基甲酸酯

    公开(公告)号:US5434140A

    公开(公告)日:1995-07-18

    申请号:US178559

    申请日:1994-01-07

    CPC分类号: C07H17/08 C07H17/00

    摘要: The invention relates to 9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin A 9a,11-cyclic carbamates, novel semisynthetic macrolide antibiotics from the genus of azalides, of the formula (I) ##STR1## whereinR.sup.1 .dbd.R.sup.2 .dbd.CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 .dbd.R.sup.4 .dbd.CH.sub.3, (IA)R.sup.1 .dbd.R.sup.2 .dbd.CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 .dbd.CH.sub.3, R.sup.4 .dbd.H, (IB)R.sup.1 .dbd.R.sup.2 .dbd.CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 .dbd.R.sup.4 .dbd.H, (IC)R.sup.1 .dbd.R.sup.2 .dbd.H, R.sup.3 .dbd.R.sup.4 .dbd.CH.sub.3,(ID)R.sup.1 .dbd.R.sup.2 .dbd.R.sup.4 .dbd.H, R.sup.3 .dbd.CH.sub.3,(IE)R.sup.1 .dbd.R.sup.2 .dbd.R.sup.3 .dbd.R.sup.4 .dbd.H, (IF)R.sup.1 .dbd.H, R.sup.2 .dbd.R.sup.3 .dbd.R.sup.4 .dbd.CH.sub.3,(IG)R.sup.1 .dbd.R.sup.4 .dbd.H, R.sup.2 .dbd.R.sup.3 .dbd.CH.sub.3,(IH)R.sup.1 .dbd.R.sup.3 .dbd.R.sup.4 .dbd.H, R.sup.2 .dbd.CH.sub.3,(IJ)to pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to intermediates and to processes for the preparation thereof, to a process for preparing pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in treatment of bacterial infections.

    摘要翻译: 本发明涉及9-脱氧-9a-氮杂-11-脱氧-9a-高红霉素A 9a,11-环状氨基甲酸酯,由式(I)的化合物制备的新的半合成大环内酯类抗生素,其中R1 = R2 = CO 2 CH 2 C 6 H 5,R 3 = R 4 = CH 3,(IA)R 1 = R 2 = CO 2 CH 2 C 6 H 5,R 3 = CH 3,R 4 = H,(IB)R 1 = R 2 = CO 2 CH 2 C 6 H 5, R3 = R4 = CH3,(ID)R1 = R2 = R4 = H,R3 = CH3,(IE)R1 = R2 = R3 = R4 = H,(IF)R1 = H,R2 = R3 = R4 = CH3,( IG)R1 = R4 = H,R2 = R3 = CH3,(1H)R1 = R3 = R4 = H,R2 = CH3,(IJ)与其与无机或有机酸的药学上可接受的加成盐, 制备药物组合物的方法以及所获得的药物组合物在细菌感染治疗中的用途。

    O-methyl derivatives of azithromycin A
    6.
    发明授权
    O-methyl derivatives of azithromycin A 失效
    阿奇霉素A的O-甲基衍生物

    公开(公告)号:US5250518A

    公开(公告)日:1993-10-05

    申请号:US731781

    申请日:1991-07-18

    CPC分类号: C07H17/08

    摘要: The invention relates to O-methyl derivatives of azithromycin A of the formula (I) ##STR1## wherein Ia R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =CH.sub.3, R.sup.4 =R.sup.5 =HIb R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =R.sup.4 =CH.sub.3, R.sup.5 =HIc R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =R.sup.5 =H, R.sup.4 =C.sub.3Id R.sup.1 =R.sup.2 =CO.sub.2 CH.sub.2 C.sub.6 H.sub.5, R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3Ie R.sup.1 =R.sup.2 =R.sup.4 =R.sup.5 =H, R.sup.3 =CH.sub.3If R.sup.1 =R.sup.2 =R.sup.5 =H, R.sup.3 =R.sup.4 =CH.sub.3Ig R.sup.1 =R.sup.2 =R.sup.3 =R.sup.5 =H, R.sup.4 =CH.sub.3Ih R.sup.1 =R.sup.2 =H, R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3Ii R.sup.1 =R.sup.4 =R.sup.5 =H, R.sup.2 =R.sup.3 =CH.sub.3Ij R.sup.1 =R.sup.5 =H, R.sup.2 =R.sup.3 =R.sup.4 =CH.sub.3Ik R.sup.1 =R.sup.3 =R.sup.5 =H, R.sup.2 =R.sup.4 =CH.sub.3Il R.sup.1 =H, R.sup.2 =R.sup.3 =R.sup.4 =R.sup.5 =CH.sub.3to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to their use in the obtaining of antibacterial pharmaceutical preparations.