8a- and 9a-15-membered lactams
    24.
    发明授权
    8a- and 9a-15-membered lactams 失效
    8a-和9α-15-元内酰胺

    公开(公告)号:US06593360B1

    公开(公告)日:2003-07-15

    申请号:US09959204

    申请日:2002-01-22

    IPC分类号: C07H1708

    CPC分类号: C07H17/08

    摘要: The invention relates to novel 15-membered 8a- and 9a-lactams from the class of 6-O-methyl-erythromycin A of general formula (I) their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates for their preparation, to a process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to their hydrates, to a process for the preparation of pharmaceutical compositions as well as to a use of pharmaceutical compositions for the treatment of bacterial infections.

    摘要翻译: 本发明涉及由通式(I)的6-O-甲基 - 红霉素A类别的与无机或有机酸及其水合物的药学上可接受的加成盐与其中间体的新型15-元8a-和9-内酰胺, 制备,其制备方法,其与无机或有机酸的药学上可接受的加成盐,其水合物,制备药物组合物的方法以及药物组合物用于治疗细菌感染的用途。

    .beta.,.beta.-distributed derivatives of
9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A
    25.
    发明授权
    .beta.,.beta.-distributed derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A 失效
    9-脱氧-9a-N-乙烯基-9a-氮杂-9a-高红霉素A的β,β分布衍生物

    公开(公告)号:US6071886A

    公开(公告)日:2000-06-06

    申请号:US223978

    申请日:1998-12-31

    CPC分类号: C07H17/08

    摘要: The present invention relates to .beta.,.beta.-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A, new semisynthetic antibiotics of macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are mutually the same or different and represent nitrile, carboxy group of the formula COOR.sup.3, wherein R.sup.3 represents C.sub.1 -C.sub.4 alkyl group, or keto group of the formula COR.sup.4, wherein R.sup.4 represents C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for the preparation thereof, to a process for the preparation of pharmaceutical compositions, as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.

    摘要翻译: 本发明涉及9-脱氧-9a-N-乙烯基-9a-氮杂-9a-高红霉素A的β,β-二取代衍生物,通式(I)的大环内酯类的新的半合成抗生素,其中R1和R2相互 表示腈,式COOR 3的羧基,其中R 3表示C 1 -C 4烷基,或式COR 4的酮基(其中R 4表示C 1 -C 4烷基)与其药学上可接受的加成盐与无机或 有机酸,其制备方法,制备药物组合物的方法,以及所用药物组合物在细菌感染治疗中的用途。

    9-deoxo-9a-aza-11-deoxy-9a-homoerythromycin a 9a,11-cyclic carbamates
    26.
    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。