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1. 发明申请

US20090048221A1 Conjugates with Anti-Inflammatory Activity 审中-公开
标题翻译：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。

2. 发明授权

US07091187B2 Compounds, compositions and methods for treatment of inflammatory diseases and conditions 失效
标题翻译：用于治疗炎性疾病和病症的化合物，组合物和方法
公开(公告)号：US07091187B2
公开(公告)日：2006-08-15
申请号：US10615716
申请日：2003-07-08
申请人： Mladen Mercep , Milan Mesic , Linda Tomaskovic , Stribor Markovic , Oresta Makaruha , Visnja Poljak
发明人： Mladen Mercep , Milan Mesic , Linda Tomaskovic , Stribor Markovic , Oresta Makaruha , Visnja Poljak
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, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (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. Such compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-α. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.
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），S代表衍生自类固醇药物的类固醇亚单位（类固醇部分）具有抗炎活性，L表示连接M和S的连接分子，（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，以及（d）其在治疗中的用途的炎症疾病和病症在人类和动物。这些化合物抑制许多引起炎症，过敏或同种异体免疫的免疫应答的细胞因子和免疫介质，包括但不限于IL-1,2,4,5,6,10,12，GMCSF，ICAM和TNF-α。重要的是，抗炎类固醇通过结合糖皮质激素受体发挥直接的抗炎作用。

3. 发明申请

US20050080003A1 Compounds with anti-inflammatory activity 失效
标题翻译：具有抗炎活性的化合物
公开(公告)号：US20050080003A1
公开(公告)日：2005-04-14
申请号：US10830858
申请日：2004-04-22
申请人： Mladen Mercep , Milan Mesic , Linda Tomaskovic , Stribor Markovic , Boska Hrvacic , Oresta Makaruha , Visnja Poljak
发明人： Mladen Mercep , Milan Mesic , Linda Tomaskovic , Stribor Markovic , Boska Hrvacic , Oresta Makaruha , Visnja Poljak
IPC分类号： C07D273/00 , C07D413/12 , C07D473/04 , C07H17/08 , C07J1/00 , A61K38/16 , C07K9/00
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 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表示下结构III的链：-X 1 - （CH 2）mQ-（CH 2）n X 2 - III D代表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; 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，以及改进的治疗作用以及用于治疗人和动物的炎性疾病和病症的用途。

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