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1. 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。

2. 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。

3. 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。

4. 发明申请

WO2005021567A1 O-ALKYL MACROLIDE AND AZALIDE DERIVATIVES AND REGIOSELECTIVE PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： O-ALKYL MACROLIDE和AZALIDE衍生物及其制备方法
公开(公告)号：WO2005021567A1
公开(公告)日：2005-03-10
申请号：PCT/HR2003/000047
申请日：2003-09-04
申请人： PLIVA - ISTRAZIVACKI INSTITUT D.O.O. , KIDEMET, Davor , LAZAREVSKI, Gorjana , DEREK, Marko , LELJAK, Marija
发明人： KIDEMET, Davor , LAZAREVSKI, Gorjana , DEREK, Marko , LELJAK, Marija
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to a process for regioselective O-alkylation of macrolide and azalide derivatives, specifically 11-0-alkyl derivatives represented by formula (I) (1) R 1 wherein A is 14-membered macrolide derivative and 15-membered azalide derivative, and R 1 is C1-C4 alkyl group comprising reacting an macrolide or azalide derivative with vicinal hydroxyl system with diazoalkane of the formula R 2 - CH N2 wherein R 2 is a hydrogen or C1-C3 alkyl group in the presence of transition-metal halides and of boric acid as catalysts, respectively, preferably H3B03, TiC14 and SnC12 in suitable inert organic solvent and to new compounds represented by the formula (I). C
摘要翻译：本发明涉及大环内酯和氮杂环丁烷衍生物，特别是式（I）（1）R 1表示的11-0-烷基衍生物的区域选择性O-烷基化方法，其中A是14-元大环内酯衍生物和15-元氮杂衍生物，R 1是C 1 -C 4烷基，包括使大环内酯或氮杂衍生物与邻位羟基系与式R 2 -CH 2的重氮烷反应，其中R 2是氢或C 1 -C 3烷基在过渡金属卤化物和硼酸作为催化剂存在下，分别在合适的惰性有机溶剂中，优选H3B03，TiC14和SnC12，以及由式（I）表示的新化合物。 C

5. 发明申请

WO2004106354A1 Q-ALKYL MACROLIDE AND AZALIDE DERIVATIVES AND REGIOSELECTIVE PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译： Q-ALKYL MACROLIDE和AZALIDE衍生物及其制备方法
公开(公告)号：WO2004106354A1
公开(公告)日：2004-12-09
申请号：PCT/IB2004/001749
申请日：2004-05-27
申请人： PLIVA-ISTRAZIVACKI INSTITUT D.O.O. , KIDEMET, Davor , LAZAREVSKI, Gorjana , DEREK, Marko , LELJAK, Marija
发明人： KIDEMET, Davor , LAZAREVSKI, Gorjana , DEREK, Marko , LELJAK, Marija
IPC分类号： C07H17/00
CPC分类号： C07H17/00 , C07H17/08
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.
摘要翻译：本发明涉及新的11-O-烷基大环内酯和氮杂ides啶及其药学上可接受的盐和溶剂合物，以及其药物组合物。本公开还涉及通过在过渡金属卤化物或硼酸的存在下使用重氮烷烃在具有邻位二醇体系的大环内酯和氮杂环丙烷的区域选择性11-O-烷基化作用下制备11-O-烷基大环内酯和氮杂环丁烷的方法，催化剂。在另一方面，本公开内容涉及11-O-烷基大环内酯和氮杂氧化物作为抗细菌剂或中间体用于合成其它抗菌剂的用途。

6. 发明申请

WO2006077501A2 DECLADINOSYL-MACROLIDES WITH ANTI-INFLAMMATORY ACTIVITY 审中-公开
标题翻译：具有抗炎活性的DECLADINOSYL-MACROLIDES
公开(公告)号：WO2006077501A2
公开(公告)日：2006-07-27
申请号：PCT/IB2006/001097
申请日：2006-01-13
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , CULIC, Ognjen , BOSNAR, Martina , ALIHODZIC, Sulejman , LAZAREVSKI, Gorjana , ISTUK MARUSIC, Zorica , HUTINEC, Antun , VELA, Vanja , KRAGOL, Goran
发明人： CULIC, Ognjen , BOSNAR, Martina , ALIHODZIC, Sulejman , LAZAREVSKI, Gorjana , ISTUK MARUSIC, Zorica , HUTINEC, Antun , VELA, Vanja , KRAGOL, Goran
CPC分类号： C07H17/08
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 lacking cladinose sugar substituted at the C-3 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-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
摘要翻译：本发明涉及具有抗炎活性的新型半合成大环内酯类。更具体地说，本发明涉及在C-3位上缺少被克拉替糖糖化的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用途特别是与过量分泌TNF-α，IL-1，IL-6，IL-8，IL-2或IL-5相关的那些疾病; 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

7. 发明申请

WO2004029067A1 THE PRESENT INVENTION RELATES TO THE NEW 3-DECLADINOSYL DERIVATIVES OF 9-DEOXO-9A-AZA9A-HOMOERYTHROMYCIN A 9A,11-CYCLIC CARBAMATES 审中-公开
标题翻译：本发明涉及9-DEOXA-9A-AZA9A-HOMOERYZROMYCIN A 9A，11-环状碳酸酯的新型3-十二烷基衍生物
公开(公告)号：WO2004029067A1
公开(公告)日：2004-04-08
申请号：PCT/HR2003/000051
申请日：2003-09-26
申请人： PLIVA d.d. , KOBREHEL, Gabrijela , LAZAREVSKI, Gorjana , MUTAK, Stjepan
发明人： KOBREHEL, Gabrijela , LAZAREVSKI, Gorjana , MUTAK, Stjepan , BERDIK, Andrea
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-deoxo-9a-aza9a-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 R 1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C 1 -C 6 alkyl group, C 2 -C 6 alkenyl group or X individually stands for C 1 -C 6 alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH 2 ) n -Ar or X individually stands for (CH 2 ) n -heterocycloalkyl, wherein (CH 2 ) 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, NO 2 , NH 2 , amino-C 1 -C 3 alkyl or amino-C 1 -C 3 dialkyl, CN, SO 2 NH 2 , C 1 -C 3 alkyl, 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, NO 2 , NH 2 , amino-C 1 -C 3 alkyl or amino-C l -C 3 dialkyl, CN, SO 2 NH 2 , C 1 -C 3 alkil, -C(O)-, COOH or R 1 together with R 2 stands for ketone, R 2 individually stands for hydrogen or together with R 1 stands for ketone or together with R 3 stands for ether, R 3 individually stands for hydroxyl, a group of the formula -OX or together with R 2 stands for ether, R 4 individually stands for hydrogen, C 1 -C 4 alkyl group or C 2 -C 4 alkenyl group, and R 5 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.
摘要翻译：本发明涉及通式（I）的9-脱氧-9a-氮杂-9a-高红霉素A 9a,11-环状氨基甲酸酯的新型3-降解衍生物，其与无机或有机酸及其水合物的药学上可接受的加成盐，其中R 1各自表示氢，羟基或式（II）的基团，其中X各自表示C 1 -C 6烷基，C 2 -C 6烯基或X各自代表C 1 -C 6烷基，其中至少一个包含O，S或 N原子或X独立地表示（CH 2）n -Ar或X分别代表（CH 2）n - 杂环烷基，其中（CH 2）n各自表示烷基，其中n为1-10，有或无引入原子O，S 或N，其中Ar各自独立地选自0至3个未被取代或被1-3个基团取代的0-3个原子的O，S或N的5-10元单环或环状芳环，其独立地选自卤素，OH，OMe，NO 2 ，NH 2，氨基-C 1 -C 3烷基或氨基-C 1 -C 3二烷基，CN，SO 2 NH 2，C 1 -C 3烷基，和杂环烷基代表不饱和的，部分或完全饱和的3-10元单环或双环环系，其包括3-8元单环或双环，其包括与具有或不具有或不同的芳环连接的6元芳族或杂芳环 OH，OMe，NO 2，NH 2，氨基-C 1 -C 3烷基或氨基-C 1 -C 3二烷基，CN，SO 2 NH 2，C 1 -C 3烷基， C3烷基，-C（O） - ，COOH或R1与R2一起代表酮，R2分别代表氢或与R1一起代表酮或与R3一起代表醚，R3单独代表羟基，一组式 -OX或与R2一起代表醚，R4单独代表氢，C1-C4烷基或C2-C4链烯基，R5分别表示氢或羟基保护基团，用于合成具有抗菌活性的其他大环内酯类化合物的中间体 y，其制备方法，其与无机或有机酸及其水合物的药学上可接受的加成盐，用于制备药物组合物的方法，以及使用药物组合物治疗细菌感染。

8. 发明申请

WO2006120545A1 4" AMINO LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS 审中-公开
标题翻译： 4“用于治疗微生物感染的氨基酸连接的有效途径
公开(公告)号：WO2006120545A1
公开(公告)日：2006-11-16
申请号：PCT/IB2006/001213
申请日：2006-05-09
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , ALIHODZIC, Suleijam , LAZAREVSKI, Gorjana
发明人： ALIHODZIC, Suleijam , LAZAREVSKI, Gorjana
IPC分类号： C07H17/08 , C07D413/14 , C07D498/04 , A61K31/7042
CPC分类号： C07D413/14 , 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“位被取代的15元大环内酯及其药学上可接受的衍生物，其制备方法及其在治疗或预防人或动物体内的全身或局部微生物感染中的用途。

9. 发明申请

WO2004009608A3 NOVEL AMORPHOUS 9-DEOXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCIN A, PROCESS FOR PREPARING THE SAME, AND USE THEREOF 审中-公开
公开(公告)号：WO2004009608A3
公开(公告)日：2004-01-29
申请号：PCT/HR2003/000040
申请日：2003-07-21
申请人： PLIVA, d.d. , DUMIC, Miljenko , VINKOVIC, Mladen , ORESIC, Marina , MESTROVIC, Ernest , DANILOVSKI, Aleksandar , DUMBOVIC, Alojz , KNEZEVIC, Zdravka , LAZAREVSKI, Gorjana , FILIC, Darko , CINCIC, Dominik , LAZARIC, Katica , BUCAR, Dejan-Kresimir
发明人： DUMIC, Miljenko , VINKOVIC, Mladen , ORESIC, Marina , MESTROVIC, Ernest , DANILOVSKI, Aleksandar , DUMBOVIC, Alojz , KNEZEVIC, Zdravka , LAZAREVSKI, Gorjana , FILIC, Darko , CINCIC, Dominik , LAZARIC, Katica , BUCAR, Dejan-Kresimir
IPC分类号： C07H17/08
摘要： Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A. In addition, this disclosure is directed to a process for the preparation thereof from crude 9-deoxo-9a-aza-9amethyl-9a-homoerythromycin A via orthorhombic isostructural pseudopolymorphs of 9-deoxo9a-aza-9a-methyl-9a-homoerythromycin A, of the general formula I x H 2 O x S I wherein S represents a water-miscible or water-immiscible organic solvent, characterized by the orthorhombic space group P2 1 2 1 2 1 , with average unit cell parameters a = 8.2 to 9.7 Å, b = 11.5 to 13.5 Å, c = 44.5 to 47.0 Å, α =β = γ = 90°, wherein a, b and c represent the crystal axes lengths and α, β and γ represent the angles between the crystal axes. In addition, pharmaceutical compositions containing the substantially pure amorphous 9-deoxo9a-aza-9a-methyl-9a-homoerythromycin A are disclosed, as well as a method for the treatment of bacterial and protozoal infections, and inflammation related diseases in humans and animals by administration of a pharmaceutical composition containing same.

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