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1. 发明公开

EP1453846A1 MACROLIDES 有权
标题翻译：具有抗菌活性的14至15肢体大环内酯类
公开(公告)号：EP1453846A1
公开(公告)日：2004-09-08
申请号：EP02779670.5
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , Pliva - Istrazivacki Institutd.o.o.
发明人： ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , STIMAC, Vlado , TIBASCO, Jessica , SCHOENFELD, Wolfgang
IPC分类号： C07H17/08 , A61K31/70 , A61P31/04
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substitued at the 4' position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

2. 发明公开

EP1485393A2 9-DEXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCIN A DERIVATIVES 有权
标题翻译： 9- DEXO-9A氮杂-9a-甲基-9a-高红霉素A衍生物
公开(公告)号：EP1485393A2
公开(公告)日：2004-12-15
申请号：EP03744475.9
申请日：2003-03-18
申请人： Pliva - Istrazivacki Institutd.o.o.
发明人： DUMIC, Miljenko , VINKOVIC, Mladen , ORESIC, Marina , MESTROVIC, Ernest , DANILOVSKI, Aleksandar , DUMBOVIC, Alojz , KNEZEVIC, Zdravka , LAZAREVSKI, Gorjana , CINCIC, Dominik , FILIC, Darko , LAZARIC, Katica , BUCAR, Dejan-Kresimir
IPC分类号： C07H17/00 , A61K31/70 , A61P33/02 , A61P31/04 , C07H17/08
CPC分类号： C07H17/00 , C07H17/08
摘要： Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a- homo erythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a = 15.5 - 17.0 Å, b = 15.5 - 17.0 Å, and c = 17.5 - 19.5 A, and angles between the crystal axes of α. = Ϝ = 90° and β = 106° - 112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.

3. 发明公开

EP1543016A1 THE PRESENT INVENTION RELATES TO THE NEW 3-DECLADINOSYL DERIVATIVES OF 9-DEOXO-9A-AZA-9A-HOMOERYTHROMYCIN A 9A,11-CYCLIC CARBAMATES 有权
标题翻译： 3-十二烷基-9-脱氧-9-二氢-9a-氨基-9-羟基肉豆素A 9A，11-氯代卡巴酸
公开(公告)号：EP1543016A1
公开(公告)日：2005-06-22
申请号：EP03769705.9
申请日：2003-09-26
申请人： Pliva - Istrazivacki Institutd.o.o.
发明人： BERDIK, Andrea , KOBREHEL, Gabrijela , LAZAREVSKI, Gorjana , MUTAK, Stjepan
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-aza-9a-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.

4. 发明申请

WO2004101590A1 NOVEL 14 AND 15 MEMBERED-RING COMPOUNDS 审中-公开
标题翻译： 14号和15号会议化合物
公开(公告)号：WO2004101590A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/005086
申请日：2004-05-11
申请人： GLAXO GROUP LIMITED , PLIVA - ISTRAZIVACKI INSTITUT D.O.O. , ALIHODZIC, Sulejman , BERDIK, Andrea , JARVEST, Richard, Lewis , LAZAREVSKI, Gorjana
发明人： ALIHODZIC, Sulejman , BERDIK, Andrea , JARVEST, Richard, Lewis , LAZAREVSKI, Gorjana
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to 15-membered macrolides substituted at the 4" position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.
摘要翻译：本发明涉及在式（I）的4“位取代的15元大环内酯及其药学上可接受的衍生物，用于其制备及其用于治疗或预防人或动物体内全身或局部微生物感染的用途。

5. 发明申请

WO2004101586A1 NOVEL 14 AND 15 MEMBERED-RING COMPOUNDS 审中-公开
标题翻译： 14号和15号会议化合物
公开(公告)号：WO2004101586A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/005082
申请日：2004-05-11
申请人： GLAXO GROUP LIMITED , PLIVA - ISTRAZIVACKI INSTITUT D.O.O. , ALIHODZIC, Sulejman , FORREST, Andrew, Keith , JARVEST, Richard, Lewis , LAZAREVSKI, Gorjana , PAVLOVIC, Drazen
发明人： ALIHODZIC, Sulejman , FORREST, Andrew, Keith , JARVEST, Richard, Lewis , LAZAREVSKI, Gorjana , PAVLOVIC, Drazen
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to 14- or 15-membered macrolides substituted at the 4" position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.
摘要翻译：本发明涉及在式（I）的4“位取代的14-或15-元大环内酯及其药学上可接受的衍生物，用于其制备及其在治疗或预防人体全身或局部微生物感染中的用途或动物体。

6. 发明申请

WO2003042228A1 MACROLIDES 审中-公开
标题翻译：大环内酯类
公开(公告)号：WO2003042228A1
公开(公告)日：2003-05-22
申请号：PCT/GB2002/005101
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , PLIVA D.D. , ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , SCHOENFELD, Wolfgang , STIMAC, Vlado , TIBASCO, Jessica
发明人： ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , SCHOENFELD, Wolfgang , STIMAC, Vlado , TIBASCO, Jessica
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substitued at the 4" position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.
摘要翻译：本发明涉及在式（I）的4“位取代的14或15元大环内酯及其药学上可接受的盐和溶剂化物，其制备方法及其在治疗或预防人体全身或局部细菌感染中的用途或动物体。

7. 发明授权

EP1453846B1 14 OR 15 MEMBERED MACROLIDES WITH ANTIBACTERIAL ACTIVITY 有权
标题翻译：具有抗菌活性的14至15肢体大环内酯类
公开(公告)号：EP1453846B1
公开(公告)日：2007-05-16
申请号：EP02779670.5
申请日：2002-11-13
申请人： GLAXO GROUP LIMITED , GlaxoSmithKline istrazivacki centar Zagreb d.o.o.
发明人： ALIHODZIC, Sulejman , ANDREOTTI, Daniele , BERDIK, Andrea , BIENTINESI, Ilaria , BIONDI, Stefano , CIRACO, Manuela , DAMIANI, Federica , DJEREK, Marko , DUMIC, Miljenko , ERAKOVIC, Vesna , HUTINEC, Antun , LAZAREVSKI, Gorjana , LOCIURO, Sergio , MARSIC, Natasa , MARUSIC-ISTUK, Zorica , MUTAK, Stjepan , PAIO, Alfredo , PAVLOVIC, Drazen , QUAGLIA, Anna , STIMAC, Vlado , TIBASCO, Jessica , SCHOENFELD, Wolfgang
IPC分类号： C07H17/08 , A61K31/70 , A61P31/04
CPC分类号： C07H17/08
摘要： The present invention relates to 14 or 15 membered macrolides substitued at the 4" position of formula (I) and pharmaceutically acceptable salts and solvates thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.

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