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    9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin a 9a,11-cyclic carbamates
    3.
    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

    申请人： Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Slobodan Djokic

    发明人： Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Slobodan Djokic

    IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    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。

    Metal complexes of N-methyl-11-aza-10-deoxo-10-dihydro-erythromycin A or 11-aza-10-deoxo-10-dihydro-erythromycin A, method for the manufacture thereof and their use in the manufacture of pharmaceuticals
    4.
    发明授权
    Metal complexes of N-methyl-11-aza-10-deoxo-10-dihydro-erythromycin A or 11-aza-10-deoxo-10-dihydro-erythromycin A, method for the manufacture thereof and their use in the manufacture of pharmaceuticals 失效
    N-甲基-11-氮杂-10-脱氧-10-二氢 - 红霉素A或11-氮杂-10-脱氧-10-二氢 - 红霉素A的金属络合物，其制造方法及其在药物制造中的应用

    公开(公告)号：US4963528A

    公开(公告)日：1990-10-16

    申请号：US94555

    申请日：1987-09-09

    申请人： Zlatko Vajtner ,  Nevenka Lopotar ,  Slobodan Djokic

    发明人： Zlatko Vajtner ,  Nevenka Lopotar ,  Slobodan Djokic

    IPC分类号： C07F1/08 ,  A61K31/295 ,  A61K31/315 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/00

    摘要： New 2:1 complexes of N-methyl-11-aza-10-deoxo-10-dihydroerythromycin A or 11-aza-10-deoxo-10-dihydroerythromycin A with bivalent metals chosen form the group comprising Cu.sup.+2, Zn.sup.+2, Co.sup.+2, Ni.sup.+2 and Ca.sup.+2, a process for their manufacture and their use in the manufacture of antibiotically active pharmaceuticals.New 2:1 complexes of N-methyl-11-aza-10-deoxo-10-dihydroerythromycin A or 11-aza-10-deoxo-10-dihydroerythromycin A with bivalent metals chosen from the group comprising Cu.sup.+2, Zn.sup.+2, Co.sup.+2, Ni.sup.+2 and Ca.sup.+2 are made by reacting N-methyl-11-aza-10-deoxo-10-dihydroerythromycin A or 11-aza-10-deoxo-10-dihydroerythromycin A in its free base form or in its water-soluble salt form with salts of said bivalent metals. The compounds possess antibiotic activity.

    摘要翻译： 新型的2:1配合物的N-甲基-11-氮杂-10-脱氧-10-二氢红霉素A或11-氮杂-10-脱氧-10-二氢红霉素A与二价金属组成，选自Cu +2，Zn + 2 ，Co + 2，Ni + 2和Ca + 2，其制造方法及其在制备抗生物活性药物中的应用。 新的2:1络合物的N-甲基-11-氮杂-10-脱氧-10-二氢红霉素A或11-氮杂-10-脱氧-10-二氢红霉素A与选自Cu +2，Zn + 2的二价金属 通过N-甲基-11-氮杂-10-脱氧-10-二氢红霉素A或11-氮杂-10-脱氧-10-二氢红霉素A以游离碱形式反应制备Co + 2，Ni + 2和Ca + 或以其所述二价金属的盐的水溶性盐形式。 该化合物具有抗生素活性。

    O-methyl derivatives of azithromycin A
    8.
    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

    申请人： Gabrijela Kobrehel ,  Slobodan Djokic ,  Gorjana Lazarevski

    发明人： Gabrijela Kobrehel ,  Slobodan Djokic ,  Gorjana Lazarevski

    IPC分类号： C07H17/00 ,  A61K31/00 ,  A61K31/70 ,  A61K31/7042 ,  A61P31/04 ,  C07D413/14 ,  C07H17/02 ,  C07H17/08

    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.