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    Compounds with anti-inflammatory activity
    3.
    发明授权
    Compounds with anti-inflammatory activity 失效
    具有抗炎活性的化合物

    公开(公告)号：US07579334B2

    公开(公告)日：2009-08-25

    申请号：US10830858

    申请日：2004-04-22

    申请人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic

    发明人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic

    IPC分类号： A61K31/585 ,  A61K31/395 ,  C07J17/00

    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: —X1—(CH2)m-Q-(CH2)n—X2—  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 process 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表示下结构III的链：<？在线公式描述=“在线公式”end =“ 铅“→X1-（CH2）mQ-（CH2）n-X2-III <？in-line-formula description =”In-line Formulas“end =”tail“？> D表示衍生的类固醇或非甾体亚基 来自类固醇或非甾体（NSAID）药物具有抗炎活性; 本发明还涉及这种制备的化合物的药学上可接受的盐和溶剂化物，其制备方法和中间体，以及改善的治疗作用以及在治疗人和动物中的炎性疾病和病症中的用途。

    Nonsteroidal anti-inflammatory substances, compositions and methods for their use
    4.
    发明授权
    Nonsteroidal anti-inflammatory substances, compositions and methods for their use 失效
    非甾体抗炎物质，其使用的组合物和方法

    公开(公告)号：US07109176B2

    公开(公告)日：2006-09-19

    申请号：US10615010

    申请日：2003-07-07

    申请人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic

    发明人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/00

    摘要： The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, D represents a nonsteroidal subunit (nonsteroidal moiety) derived from nonsteroid drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linking group covalently linking M and D; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory diseases and conditions in humans and animals.

    摘要翻译： 本发明涉及（a）由式I表示的新化合物：其中M表示衍生自具有在炎性细胞中积累性质的大环内酯的大环内酯亚单位（大环内酯部分），D表示衍生自非类固醇药物的非甾体亚基（非甾体化合物） 具有抗炎，镇痛和/或解热活性（NSAID），L代表共价连接M和D的连接基团; （b）其药理学上可接受的盐，前药和溶剂化物，（c）其制备方法和中间体，和（d）其用于治疗人和动物的炎性疾病和病症。

    Compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules
    5.
    发明授权
    Compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules 失效
    化合物，组合物作为类固醇/非类固醇抗炎剂的载体，抗肿瘤和抗病毒活性分子

    公开(公告)号：US07157433B2

    公开(公告)日：2007-01-02

    申请号：US10616046

    申请日：2003-07-08

    申请人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic

    发明人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07J17/00 ,  C07J43/003

    摘要： The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents an anti-inflammatory steroid or nonsteroid subunit, or an antineoplastic or antiviral subunit and L represents a linking group covalently linking M and V; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory/neoplastic/viral diseases and conditions in humans and animals.

    摘要翻译： 本发明涉及（a）由式I表示的新化合物：其中M表示衍生自具有炎症细胞积累性质的大环内酯的大环内酯亚单位（大环内酯部分），V表示抗炎类固醇或非类固醇亚基，或 抗肿瘤或抗病毒亚基，L代表共价连接M和V的连接基团; （b）其药理学上可接受的盐，前药和溶剂合物，（c）其制备方法和中间体，和（d）其用于治疗人和动物中的炎性/肿瘤/病毒性疾病和病症。

    Conjugates with Anti-Inflammatory Activity
    6.
    发明申请
    Conjugates with Anti-Inflammatory Activity 审中-公开
    具有抗炎活性的结合物

    公开(公告)号：US20090048221A1

    公开(公告)日：2009-02-19

    申请号：US11718505

    申请日：2005-10-27

    申请人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic ,  Visnja Poljak ,  Gordana Sijan ,  Selvira Selmani

    发明人： Mladen Mercep ,  Milan Mesic ,  Linda Tomaskovic ,  Stribor Markovic ,  Visnja Poljak ,  Gordana Sijan ,  Selvira Selmani

    IPC分类号： A61K31/58 ,  C07J43/00 ,  A61K31/4155 ,  A61P29/00 ,  A61K31/4427 ,  C07D267/00

    CPC分类号： C07J43/003 ,  C07D267/00 ,  C07D413/12

    摘要： Compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure VIII: L represents the chain of the substructure IX or XIII: —X1—(CH2)m-Q-(CH2)n—X2—  IX —X1—(CH2)m—V—(CH2)p-Q-(CH2)n—X2—  XIII and Z represents a steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity are disclosed. Pharmaceutically acceptable salts and solvates of such compounds, processes 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 are also disclosed.

    摘要翻译： 由式I表示的化合物：其中M表示亚结构VIII的大环内酯亚单位：L表示亚结构IX或XIII的链：<？在线公式描述=“在线公式”end =“lead”→> -X1-（CH2）mQ-（CH2）n-X2-IX <？in-line-formula description =“In-line Formulas”end =“tail”？> <？in-line-formula description =“In- - 线性公式“end =”lead“→X1-（CH2）mV-（CH2）pQ-（CH2）n-X2-XIII <？in-line-formula description =”In-line Formulas“end =”tail 并且Z表示衍生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基。 还公开了这些化合物的药学上可接受的盐和溶剂合物，其制备方法和中间体，以及改进的治疗作用以及用于治疗人和动物中的炎性疾病和病症的用途。