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31.发明授权REGIOSELECTIVE PROCESS FOR THE PREPARATION OF O-ALKYL MACROLIDE AND AZALIDE DERIVATIVES 有权REGIO选择性工艺用于生产O-烷基大环内酯类阿扎利衍生物
公开(公告)号：EP1633764B1
公开(公告)日：2009-09-09
申请号：EP04735055.8
申请日：2004-05-27
发明人： KIDEMET, Davor (Glaxo Smith Kline) , LAZAREVSKI, Gorjana (Glaxo Smith Kline) , DEREK, Marko (Glaxo Smith Kline) , LELJAK, Marija (Glaxo Smith Kline)
摘要： The present disclooure 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 -0-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.
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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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33.发明授权USE OF 1-OXADIBENZO [E,H] AZULENES FOR THE MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS 有权1- OXADIBENZO [E，H]薁USE药物制剂用于治疗和预防疾病和病症中枢神经系统的制造
公开(公告)号：EP1684742B1
公开(公告)日：2009-01-14
申请号：EP04798731.8
申请日：2004-11-19
发明人： MERCEP, Mladen , MESIC, Milan , PESIC, Dijana
IPC分类号： A61K31/343 , A61K31/34 , A61K31/38 , A61K31/55 , A61P25/00
CPC分类号： A61K31/34 , A61K31/343 , A61K31/38 , A61K31/55
摘要： The present invention relates to the use of compounds from the group of 1-oxadibenzo[e, h]azulenes and of their pharmacologically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.
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公开(公告)号：EP1945652A1
公开(公告)日：2008-07-23
申请号：EP06818432.4
申请日：2006-11-07
发明人： ALIHODZIC, Sulejman , BERGE, John, Michael , FRYDRYCH, Catherine, Simone, Victoire , KAPIC, Samra , PALEJ, Ivana
IPC分类号： C07H17/08 , A61P31/04 , A61K31/706
CPC分类号： C07H17/08
摘要： A compound of formula (I) or a pharmaceutically acceptable derivative thereof, having antimicrobial activity, processes for their preparation, compositions containing them and to their use in medicine.
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35.发明授权1,2-DIAZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF 有权1,2-二氮杂 - 二苯并如肿瘤坏死因子为他们的生产制作和中间产品的抑制剂
公开(公告)号：EP1587807B1
公开(公告)日：2008-06-18
申请号：EP03755234.6
申请日：2003-05-20
发明人： MERCEP, Mladen , MESIC, Milan , PESIC, Dijana
IPC分类号： C07D491/00
CPC分类号： C07D495/04 , C07D491/04
摘要： The present invention relates to derivatives of 1,2-diaza-dibenzoazulene, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-(x (TNF-(x) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.
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公开(公告)号：EP1851236A2
公开(公告)日：2007-11-07
申请号：EP06727595.8
申请日：2006-01-13
发明人： CULIC, Ognjen , BOSNAR, Martina , MARJANOVIC, Nikola , JELIC, Dubravko , ALIHODZIC, Sulejman , VELA, Vanja , MARUSIC-ISTUK, Zorica , ERAKOVIC, Vesna , BOSNJAK, Berislav , HRVACIC, Boska , TOMASKOVIC, Marija , MUNIC, Vesna , IVETIC, Vanesa , HUTINEC, Antun , KRAGOL, Goran , LELJAK, Marija
IPC分类号： C07H17/00 , A61K31/7048 , C07H17/08 , A61P29/00 , A61K31/7052
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 substituted at the 4' 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-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
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37.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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38.发明授权USE OF 1,3-DIAZA-DIBENZO[e,h] AZULENES FOR THE MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS 有权1,3-二氮杂 - 二苯并[E，H]薁USE药物制剂用于治疗和预防疾病和病症中枢神经系统的制造
公开(公告)号：EP1684749B1
公开(公告)日：2007-09-05
申请号：EP04798735.9
申请日：2004-11-19
发明人： MERCEP, Mladen , MESIC, Milan , RUPCIC, Renata , PESIC, Dijana
IPC分类号： A61K31/4184 , A61K31/4188 , A61K31/55 , A61K31/695 , A61P25/00
CPC分类号： A61K31/4184 , A61K31/4188 , A61K31/55 , A61K31/695
摘要： The present invention relates to the use of compounds from the group of 1,3-diazadibenzo[e,h]azulenes and of their pharmaceutically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.
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公开(公告)号：EP1328535B1
公开(公告)日：2007-08-15
申请号：EP01982656.9
申请日：2001-10-19
发明人： ALIHODZIC, Suleman Pliva d.d. , BERDIK, Andrea Pliva d.d. , CARDULLO, Francesca GlaxoSmithKline SpA , HUTINEC, Antun Pliva d.d. , LAZAREVSKI, Gorjana Pliva d.d. , LOCIURO, Sergio GlaxoSmithKline SpA , MARUSIC-ISTUK, Zorica Pliva d.d. , MUTAK, Stjepan Pliva d.d. , POZZAN, Alfonso GlaxoSmithKline SpA , DEREK, Marko Pliva d.d.
摘要： The present invention relates to a compound of formula (I) wherein R1 is hydrogen or together with R2 is oxo; R2 represents hydroxy, OC(O)XR7, OC(O)NHXR7 or R2 together with R1 is an oxo group; R3 is hydrogen or a hydroxyl protecting group; R4 is hydrogen or XR7; R5 is hydrogen, XR7 or C(O)NHXR7; R6 is hydrogen or R5 and R6 taken together with the intervening atoms form a cyclic carbonate having the following structure and pharmaceutically acceptable salts and solvates thereof and solvates thereof; to processes for their preparation and their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译： 本发明涉及式（I）的化合物，其中R 1为氢或与R 2一起为氧代; R2代表羟基，OC（O）XR7，OC（O）NHXR7或R2与R1一起为氧代基; R3是氢或羟基保护基; R4是氢或XR7; R5是氢，XR7或C（O）NHXR7; R6是氢或R5和R6与插入的原子一起形成具有以下结构的环状碳酸酯及其药学上可接受的盐和溶剂合物及其溶剂合物; 其制备方法及其在治疗或预防人体或动物体内全身或局部细菌感染中的用途。
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40.发明授权USE OF 3-AZA-1-OXA-DIBENZO i e,h /i AZULENES FOR THE MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEAS AND DISORDERS 有权作者-3-氮杂 - Aoxa二苯并（E，H）USE薁FOR PRODUCING药物制剂用于治疗和预防疾病和病症中枢神经系统的
公开(公告)号：EP1684766B1
公开(公告)日：2007-06-27
申请号：EP04798733.4
申请日：2004-11-19
发明人： MERCEP, Mladen , MESIC, Milan , PESIC, Dijana , DZAPO, Iva
CPC分类号： A61K31/55 , A61K31/424
摘要： The present invention relates to the use of compounds from the group of 3-aza-l-oxadibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates for the manufacture of a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.
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