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    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
    1.
    发明授权
    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation 失效
    O-烷基大环内酯和azalide衍生物及其制备方法

    公开(公告)号：US07435805B2

    公开(公告)日：2008-10-14

    申请号：US10851768

    申请日：2004-05-21

    申请人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    发明人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    IPC分类号： C07H17/08

    CPC分类号： C07H17/00 ,  C07H17/08

    摘要： The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.

    摘要翻译： 本公开内容涉及新的11-O-烷基大环内酯和氮杂ides啶及其药学上可接受的盐和溶剂合物，以及其药物组合物。 本公开还涉及通过在过渡金属卤化物或硼酸的存在下使用重氮烷烃在具有邻位二醇体系的大环内酯和氮杂环丙烷的区域选择性11-O-烷基化作用下制备11-O-烷基大环内酯和氮杂环丁烷的方法， 催化剂。 在另一方面，本公开涉及11-O-烷基大环内酯和氮杂环丁烷作为抗细菌剂或中间体用于合成其它抗菌剂的用途。

    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
    2.
    发明申请
    O-alkyl macrolide and azalide derivatives and regioselective process for their preparation 失效
    O-烷基大环内酯和azalide衍生物及其制备方法

    公开(公告)号：US20050164958A1

    公开(公告)日：2005-07-28

    申请号：US10851768

    申请日：2004-05-21

    申请人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    发明人： Davor Kidemet ,  Gorjana Lazarevski ,  Marko Derek ,  Marija Leljak

    IPC分类号： A61K31/7052 ,  C07H17/00 ,  C07H17/08

    CPC分类号： C07H17/00 ,  C07H17/08

    摘要： The present disclsoure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.

    摘要翻译： 本发明涉及新的11-O-烷基大环内酯和氮杂环丁烷及其药学上可接受的盐和溶剂合物，以及其药物组合物。 本公开还涉及通过在过渡金属卤化物或硼酸的存在下使用重氮烷烃在具有邻位二醇体系的大环内酯和氮杂环丙烷的区域选择性11-O-烷基化作用下制备11-O-烷基大环内酯和氮杂环丁烷的方法， 催化剂。 在另一方面，本公开涉及11-O-烷基大环内酯和氮杂环丁烷作为抗细菌剂或中间体用于合成其它抗菌剂的用途。

    New 3-decladinosyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 9a, 11-cyclic carbamates
    5.
    发明申请
    New 3-decladinosyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 9a, 11-cyclic carbamates 失效

    公开(公告)号：US20060154878A1

    公开(公告)日：2006-07-13

    申请号：US10527940

    申请日：2003-09-26

    申请人： Andrea Fajdetic ,  Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Stjepan Mutak

    发明人： Andrea Fajdetic ,  Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Stjepan Mutak

    IPC分类号： A61K31/7048 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl stands for unaromatic, partially or completely saturated 3-10-membered monocyclic or bicyclic ring system, which includes 3-8-membered monocyclic or bicyclic ring, which includes 6-membered aromatic or heteroaromatic ring connected with a unaromatic ring with or without incorporated O, S or N atom, unsubstituted or substituted with 1-4 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.

    3,6-hemiketals from the class of 9A-azalides
    6.
    发明授权
    3,6-hemiketals from the class of 9A-azalides 失效
    来自9A-azalides类的3,6-hemiketals

    公开(公告)号：US06369035B1

    公开(公告)日：2002-04-09

    申请号：US09529642

    申请日：2000-04-17

    申请人： Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Mladen Vinkovic

    发明人： Gabrijela Kobrehel ,  Gorjana Lazarevski ,  Mladen Vinkovic

    IPC分类号： A61K3170

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： The invention relates to novel compounds from the class of macrolide antibiotics. Particularly, the invention relates to novel 3,6-heiketals from the class of 9a-azalides, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.

    摘要翻译： 本发明涉及来自大环内酯类抗生素类的新化合物。 特别地，本发明涉及来自9-氮杂类的新型3,6-尾环，其与无机或有机酸的药学上可接受的加成盐，其制备方法及其作为抗生素或作为其用途的中间体 合成其他大环内酯类抗生素。

    O-methyl derivatives of azithromycin A
    7.
    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.

    Derivatives from the class of oleandomycin
    8.
    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

    申请人： Gordana Burek ,  Gorjana Lazarevski ,  Gabrijela Kobrehel

    发明人： Gordana Burek ,  Gorjana Lazarevski ,  Gabrijela Kobrehel

    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。

    Decladinosyl-macrolides with anti-inflammatory activity
    10.
    发明授权
    Decladinosyl-macrolides with anti-inflammatory activity 失效
    具有抗炎活性的宣称大肠杆菌素

    公开(公告)号：US07910559B2

    公开(公告)日：2011-03-22

    申请号：US11813876

    申请日：2006-01-13

    申请人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

    发明人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

    摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地说，本发明涉及在C-3位上缺少被克拉替糖糖化的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用途 特别是与过量分泌TNF-α，IL-1，IL-6，IL-8，IL-2或IL-5相关的那些疾病的治疗中， 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。