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公开(公告)号：EP1844053A2
公开(公告)日：2007-10-17
申请号：EP06727557.8
申请日：2006-01-13
发明人： MERCEP, Mladen , MESIC, Milan , MARKOVIC, Stribor , PESIC, Dijana , OZIMEC LANDEK, Ivana , KOMAC, Marijana , MAKARUHA STEGIC, Oresta , SELMANI, Selvira , BANJANAC, Mihailo , TOMASKOVIC, Linda
IPC分类号： C07D495/04 , C07H17/08 , C07D498/04 , A61K31/7048 , A61K31/7052 , A61K31/55 , A61P29/00
CPC分类号： C07D495/04
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 dibenzo[e,/z]azulene subunit with anti-inflammatory, analgesic and/or antipyretic activity 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表示衍生自大环内酯的大环内酯亚基（大环内酯部分），其具有在炎性细胞中的累积性质，D表示二苯并[e，l] az亚基，其中 抗炎，镇痛和/或解热活性，并且L代表共价连接M和D的连接基团; （b）它们的药理学上可接受的盐，前药和溶剂化物，（c）它们的制备方法和中间体，和（d）它们在治疗人类和动物的炎性疾病和病症中的用途。
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2.发明授权CONJUGATES OF IMMUNE CELL SPECIFIC MACROLIDE COMPOUNDS WITH ANTI-INFLAMMATORY COMPOUNDS FOR IMPROVED CELLULAR TARGETING OF ANTI-INFLAMMATORY THERAPY 有权免疫细胞特异性大环内酯类了有助于提升细胞抗衰炎化合物偶联物靶向抗炎治疗
公开(公告)号：EP1351973B1
公开(公告)日：2010-03-31
申请号：EP02729470.1
申请日：2002-01-03
发明人： MERCEP, Mladen , MESIC, Milan , TOMASKOVIC, Linda , KOMAC, Marijana , HRVACIC, Boska , MARKOVIC, Stribor
CPC分类号： C07J43/003
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公开(公告)号：EP1633771B1
公开(公告)日：2009-07-15
申请号：EP04729157.0
申请日：2004-04-23
发明人： MERCEP, Mladen , MESIC, Milan , TOMASKOVIC, Linda , MARKOVIC, Stribor , HRVACIC, Boska , MAKARUHA, Oresta , POLJAK, Visnja
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, Formula (II); L represents the chain of the substructure III, Formula (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.
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4.发明公开MACROLIDE COMPOUNDS CONTAINING BIOTIN AND PHOTO-AFFINITY GROUP FOR MACROLIDE TARGET IDENTIFICATION 有权与生物素和照片相似组大环内酯类用于标识的大环内酯类靶区
公开(公告)号：EP1836212A1
公开(公告)日：2007-09-26
申请号：EP06755941.9
申请日：2006-01-13
发明人： CULIC, Ognjen , BOSNAR, Martina , MARJANOVIC, Nikola , MILDNER, Boris , TOMASKOVIC, Linda , ALIHODZIC, Sulejman
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to their pharmaceutically acceptable salts and solvates, to processes and intermediates for their preparation and to the use of these compounds for Hie macrolide target identification.
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5.发明公开USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT 审中-公开细胞特异性结合物为胃肠道炎症疾病的治疗
公开(公告)号：EP1778292A2
公开(公告)日：2007-05-02
申请号：EP05786822.6
申请日：2005-08-10
CPC分类号： A61K31/7048 , A61K31/7052 , A61K47/545
摘要： The present invention is directed to methods for the prevention and treatment of inflammatory diseases, disorders, and conditions of gastrointestinal tract by administering to a patient in need of such treatment, conjugate compounds of Formula (VII) having low oralbioavailability, or pharmaceutically acceptable salts, prodrugs, or solvate thereof: wherein M represents a macrolide subunit possessing the property of accumulation in inflammatory cells, T represents an anti-inflammatory subunit that can be a steroid or nonsteroid (nonsteroidal moiety) derived from a non-steroid drug with antiinflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linker covalently linking M and T. The present disclosure is also directed to pharmaceutical compositions containing conjugate compounds of Formula (VII) having low oral-bioavailability.
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