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

    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
    4.
    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.

    Derivatives from the class of oleandomycin
    7.
    发明授权
    Derivatives from the class of oleandomycin 失效
    来自类胡萝卜霉素的衍生物

    公开(公告)号:US06573367B1

    公开(公告)日:2003-06-03

    申请号:US09869606

    申请日:2001-07-02

    IPC分类号: C07H100

    CPC分类号: C07H13/12 C07H15/26 C07H17/08

    摘要: The invention relates to novel compounds from the class of the macrolide antibiotic oleandomycin of the general formula (I) wherein R1 has the individual meaning of —CH2CH3 group, of a fragment of the formula (II), together with R2 has the meaning of a fragment of the formula (III) or together with R4 has the meaning of a fragment of the formula (IV) or a fragment of the formula (V) R2 together with R3 has the meaning of a ketone or together with R1 has the meaning of a fragment of the formula (III), R3 has the individual meaning of OH group or together with R2 has the meaning of a ketone, R4 has the individual meaning of a methyl group, or together with R1 has the meaning of a fragment of the formula (IV) or of a fragment of the formula (V), R5 has the individual meaning of hydrogen or a benzyloxycarbonyl group, R6 has the individual meaning of hydrogen, a methyl group or a benzyloxycarbonyl group, to intermediates for the preparation thereof, to a process for preparing them as well as to pharmaceutically acceptable addition salts thereof with inorganic or organic acids.

    摘要翻译: 本发明涉及通式(I)的大环内酯类抗生素素多霉素类别的新化合物,其中R 1具有-CH 2 CH 3基团的单独含义,式(II)的片段,以及R2具有片段的含义 式(III)或与R4一起具有式(Ⅳ)的片段或式(Ⅴ)的片段的含义R 2与R 3一起具有酮的含义或与R 1一起具有以下含义: 式(III)的片段,R3具有OH基团的单独含义或与R2一起具有酮的含义,R4具有甲基的单独含义,或与R 1一起具有式 (Ⅳ)或式(Ⅴ)的片段,R5具有氢或苄氧基羰基的独立含义,R 6具有氢,甲基或苄氧基羰基的单个含义,用于制备其中间体, 一个准备它们以及pha的过程 其药学上可接受的加成盐与无机或有机酸。

    8a- and 9a-15-membered lactams
    9.
    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
    10.
    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。