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    NEW 3-DECLADINOSYL DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHROMYCIN A 9A,11-CYCLIC CARBAMATES
    1.
    发明授权
    NEW 3-DECLADINOSYL DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHROMYCIN A 9A,11-CYCLIC CARBAMATES 有权
    9-脱氧 - 9-二氢9A-AZA-9A-HOMOERYTHROMICIN甲9A 3- decladinosyl衍生物，11-环状氨基甲酸酯

    公开(公告)号：EP1543016B1

    公开(公告)日：2009-04-15

    申请号：EP03769705.9

    申请日：2003-09-26

    申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

    发明人： BERDIK, Andrea GlaxoSmithKline istrazivacki centar Zagreb d.o.o. ,  KOBREHEL, Gabrijela ,  LAZAREVSKI, Gorjana GlaxoSmithKline istrazivacki centar Zagreb d.o.o. ,  MUTAK, Stjepan GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

    IPC分类号： C07H17/08 ,  C07H17/00 ,  A61K31/7048 ,  A61P31/04

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-deoxo-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-Cl-C3dialkyl, CN, SO2NH2, C1-C3alkil, -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 proces 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.

    Compounds with anti-inflammatory activity
    8.
    发明公开
    Compounds with anti-inflammatory activity 有权
    具有抗炎活性的化合物

    公开(公告)号：EP2070940A1

    公开(公告)日：2009-06-17

    申请号：EP09075145.4

    申请日：2004-04-23

    申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

    发明人： Mercep, Mladen ,  Mesic, Milan ,  Tomaskovic, Linda ,  Markovic, Stribor ,  Hrvacic, Boska ,  Makaruha, Oresta ,  Poljak, Vionja

    IPC分类号： C07J1/00 ,  C07D413/12 ,  C07D273/00

    CPC分类号： C07D273/00 ,  C07D413/12 ,  C07D473/04 ,  C07H17/08 ,  C07J1/00

    摘要： The present invention relates to new compounds represented by Formula I:

    wherein M represents a macrolide subunit of the substructure II:

    L represents the chain of the substructure III:

             -X 1 -(CH 2 ) m -Q-(CH 2 ) n -X 2 -      III

    D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity;
    The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to processe and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.

    摘要翻译： 本发明涉及由式I表示的新化合物：其中M表示亚结构II的大环内酯亚单位：L表示亚结构III的链：-X1-（CH2）mQ-（CH2）n-X2-III D表示 来自具有抗炎活性的类固醇或非甾体（NSAID）药物的类固醇或非甾体亚单位; 本发明还涉及这样制备的化合物的药学上可接受的盐和溶剂化物，用于其制备的加工和中间体，以及改善的治疗作用和用于治疗人类和动物中的炎性疾病和病症的用途。

    THIADIBENZOAZULENE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES
    9.
    发明授权
    THIADIBENZOAZULENE DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES 有权
    THIADIBENZOAZULENDERIVATE炎症性疾病的治疗

    公开(公告)号：EP1603921B1

    公开(公告)日：2009-06-17

    申请号：EP04717708.4

    申请日：2004-03-05

    申请人： GlaxoSmithKline istrazivacki centar Zagreb d.o.o.

    发明人： MERCEP, Mladen ,  MESIC,Milan ,  PESIC, Dijana ,  BENKO, Iva

    IPC分类号： C07D495/04 ,  A61K31/382 ,  A61P29/00

    CPC分类号： C07D495/04

    摘要： The present invention relates to novel 1-thia-dibenzoazulene derivatives of the formula (I), wherein X individually denotes a hetero atom -O- or -S-; Y and Z independently from each other individually denote a fragment of the formula (II) to their pharmacologically acceptable esters, salts and solvates, to processes and intermediates for the preparation thereof, to a process for preparing pharmaceutical formulations for the treatment of inflammatory diseases and conditions and to the use thereof in the treatment of inflammatory diseases and conditions in humans and animals. These compounds inhibit tumour necrosis factor-α(TNF-(α) production and interleukin-1 (IL-1) production and exhibit an analgetic action.