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1. 发明申请

WO2006120541A1 ETHER LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS 审中-公开
标题翻译：用于治疗微生物感染的其他连接的微量元素
公开(公告)号：WO2006120541A1
公开(公告)日：2006-11-16
申请号：PCT/IB2006/001194
申请日：2006-05-09
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , GLAXO GROUP LTD. , ALIHODZIC, Sulejman , PAVLOVIC, Drazen , HUNT, Eric , FORREST, Andrew, Keith , PALEJ, Ivana , KAPIC, Samra , STIMAC, Vlado
发明人： ALIHODZIC, Sulejman , PAVLOVIC, Drazen , HUNT, Eric , FORREST, Andrew, Keith , PALEJ, Ivana , KAPIC, Samra , STIMAC, Vlado
IPC分类号： C07H17/08 , A61K31/7048
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) in which R 1 is a ether moiety 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14-或15-元大环内酯，其中R 1是醚部分及其药学上可接受的衍生物，其制备方法和它们用于治疗或预防人或动物体内的全身或局部微生物感染。

2. 发明申请

WO2007054296A1 MACROLONES 审中-公开
公开(公告)号：WO2007054296A1
公开(公告)日：2007-05-18
申请号：PCT/EP2006/010733
申请日：2006-11-07
申请人： GLAXO GROUP LIMITED , GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , ALIHODZIC, Sulejman , BERGE, John, Michael , FRYDRYCH, Catherine, Simone, Victoire , KAPIC, Samra , PALEJ, Ivana
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.
摘要翻译：具有抗微生物活性的式（I）化合物或其药学上可接受的衍生物，其制备方法，含有它们的组合物及其在药物中的用途。

3. 发明申请

WO2005108412A1 ESTER LINKED MACROLIDES USEFUL FOR THE TREATMENT OF MICROBIAL INFECTIONS 审中-公开
标题翻译：用于治疗微生物感染的ESTER链接宏
公开(公告)号：WO2005108412A1
公开(公告)日：2005-11-17
申请号：PCT/IB2005/001186
申请日：2005-05-02
申请人： PLIVA-ISTRAZIVACKI INSTITUT D.O.O. , ALIHODZIC, Sulejman , MUTAK, Stjepan , PAVLOVIC, Drazen , PALEJ, Ivana , STIMAC, Vlado , KAPIC, Samra , ZUPAN, Adrijana , MATANOVIC, Maja
发明人： ALIHODZIC, Sulejman , MUTAK, Stjepan , PAVLOVIC, Drazen , PALEJ, Ivana , STIMAC, Vlado , KAPIC, Samra , ZUPAN, Adrijana , MATANOVIC, Maja
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 infoections 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，用于其制备及其用于治疗或预防人体全身或局部微生物信息的方法或动物体。

4. 发明申请

WO2010086351A1 3'-N-SUBSTITUTED 9-DEOXO-9A-METHYL-9A-AZA-HOMOERYTHROMYCIN HAVING ANTIMALARIAL ACTIVITY 审中-公开
标题翻译：具有抗体活性的3'-取代的9-脱氧-9-甲基-9a-氨基 - 异亮氨酸
公开(公告)号：WO2010086351A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050969
申请日：2010-01-28
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , ALIHODZIC, Sulejman , STARCEVIC, Kristina
发明人： ALIHODZIC, Sulejman , STARCEVIC, Kristina
IPC分类号： C07H17/08 , A61K31/7048 , A61P33/06
CPC分类号： C07H17/08 , A61K31/7048 , Y02A50/411
摘要： The present invention relates to novel 3'- N -substituted 9-deoxo-9a-methyl-9a-aza-9a- homoerythromycin A derivatives having antimalarial activity. More particularly, the invention relates to 3'- N -substituted-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A and 3'- N -substituted-3-O-decladinosyl-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity, to the intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof having antimalarial activity.
摘要翻译：本发明涉及具有抗疟活性的新的3'-N-取代的9-脱氧-9a-甲基-9a-氮杂-9a-高红霉素A衍生物。更具体地，本发明涉及3'-N-取代-9-脱氧-9a-甲基-9a-氮杂-9a-高红霉素A和3'-N-取代-3-O-降乳素-9-脱氧-9a- 具有抗疟活性的甲基-9a-氮杂-9a-高红霉素A衍生物，其制备中间体，其制备方法，作为治疗剂的用途及其具有抗疟活性的盐。

5. 发明申请

WO2007125414A2 9A-SUBSTITUTED AZALIDES 审中-公开
标题翻译： 9A替代的AZALIDES
公开(公告)号：WO2007125414A2
公开(公告)日：2007-11-08
申请号：PCT/IB2007/001216
申请日：2007-05-01
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , ALIHODZIC, Sulejman , FAJDETIC, Andrea , HUTINEC, Antun , IVEZIC, Zrinka , KUJUNDZIC, Nedjeljko , RUPCIC, Renata
发明人： ALIHODZIC, Sulejman , FAJDETIC, Andrea , HUTINEC, Antun , IVEZIC, Zrinka , KUJUNDZIC, Nedjeljko , RUPCIC, Renata
IPC分类号： A61K31/395 , A61K31/7052 , A61P33/06
CPC分类号： A61K31/395 , A61K31/7052 , Y02A50/411
摘要： The present invention relates to novel 9a-substituted azalides having antimalarial activity. More particularly, the invention relates to 9a-substituted 9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A, 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-5-O-dedesosaminyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity, to the method of preparation, to the method of use, and to pharmaceutically acceptable derivatives thereof having antimalarial activity.
摘要翻译：本发明涉及具有抗疟活性的新的9a取代的氮杂。啶。更具体地说，本发明涉及9a-取代的9a-氮杂-9-脱氧-9-二氢-9a-高红霉素A，3-O-降乳腺苷-9a-氮杂-9-脱氧-9-二氢-9a-高红霉素A和 3-O-抗坏血糖基-5-O-二去甲氨基-9a-氮杂-9-脱氧-9-二氢-9a-高红霉素具有抗疟活性的化合物，制备方法及其药学上可接受的衍生物具有抗疟活性。

6. 发明申请

WO2006106440A1 MACROLIDE COMPOUNDS CONTAINING BIOTIN AND PHOTO-AFFINITY GROUP FOR MACROLIDE TARGET IDENTIFICATION 审中-公开
标题翻译：含有生物素和光敏组合物的大分子化合物用于宏观目标鉴定
公开(公告)号：WO2006106440A1
公开(公告)日：2006-10-12
申请号：PCT/IB2006/001484
申请日：2006-01-13
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , CULIC, Ognjen , BOSNAR, Martina , MARJANOVIC, Nikola , MILDNER, Boris , TOMASKOVIC, Linda , ALIHODZIC, Sulejman
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.
摘要翻译：本发明涉及由通式结构I表示的新型大环内酯类化合物，其中M为大环内酯，P为含有亲电子基团的含有生物素的亚单位，L为连接分子，以及其药学上可接受的盐和溶剂合物，其制备方法和中间体以及使用这些化合物用于大环内酯的靶标鉴定。

7. 发明申请

WO2006085228A2 NOVEL ANTIMALARIAL 9A-CARBAMOYL-AMINOALKYL AND 9A-THIOCARBAMOYL-AMINOALKYL AZALIDES 审中-公开
标题翻译：新型抗氨基-9-氨基 - 氨基亚氨基和9A-三氨基甲酰胺基亚氨基
公开(公告)号：WO2006085228A2
公开(公告)日：2006-08-17
申请号：PCT/IB2006/001227
申请日：2006-01-13
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , BUKVIC KRAJACIC, Mirjana , KUJUNDZIC, Nedjeljko , IVEZIC, Zrinka , ALIHODZIC, Sulejman , HUTINEC, Antun , FAJDETIC, Andrea
发明人： BUKVIC KRAJACIC, Mirjana , KUJUNDZIC, Nedjeljko , IVEZIC, Zrinka , ALIHODZIC, Sulejman , HUTINEC, Antun , FAJDETIC, Andrea
CPC分类号： A61K31/7052 , C07H17/08 , Y02A50/411
摘要： Novel 9a-N'-substituted-carbamoyl- and tMocarbamoyl-aminoalkyl-9a-aza-9-deoxo- 9-dihydro-9a-homoerythromycin A and 3- O -decladinosyl-9a-aza-9-deoxo-9-dihydro- 9a-homoerythromycin A compounds having antimalarial activity are claimed. More particularly, the invention relates to 9a-N'-substituted-carbamoyl- and thiocarbamoyl- ß-aminoethyl- or -γ-aminopropyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds and to pharmaceutically acceptable derivatives thereof having antimalarial activity.
摘要翻译：新的9a-N'-取代的氨基甲酰基 - 和叔氨基甲酰基 - 氨基烷基-9a-氮杂-9-脱氧-9-二氢-9a-高红霉素A和3-O-降解腺苷-9a-氮杂-9-脱氧-9-二氢 - 要求具有抗疟活性的9a-同色红霉素A化合物。更具体地说，本发明涉及9a-N'-取代的氨基甲酰基 - 和硫代氨基甲酰基-β-氨基乙基或-γ-氨基丙基-9a-氮杂-9-脱氧-9-二氢-9a-高红霉素A和3-O- 抗坏血酸基-9a-氮杂-9-脱氧-9-二氢-9a-高红霉素A化合物及其具有抗疟活性的药学上可接受的衍生物。

8. 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。

9. 发明申请

WO2010086350A1 9-DEOXO- 9A-METHYL- 9A- AZA- 9A-H0M0ERYTHR0MYCIN A DERIVATIVES FOR THE TREATMENT OF NEUTROPHIL DOMINATED INFLAMMATORY DISEASES 审中-公开
标题翻译： 9-去氧-9-9A-METHYL-9A-AZA-9A-H0MOERYTHROMYCIN用于治疗中性粒细胞性炎症性疾病的衍生物
公开(公告)号：WO2010086350A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/050968
申请日：2010-01-28
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , ALIHODZIC, Sulejman , HUTINEC, Antun , KOSTRUN, Sanja , MATANOVIC SKUGOR, Maja , PALEJ JAKPOVIC, Ivana
发明人： ALIHODZIC, Sulejman , HUTINEC, Antun , KOSTRUN, Sanja , MATANOVIC SKUGOR, Maja , PALEJ JAKPOVIC, Ivana
IPC分类号： C07H17/00 , A61K31/7042 , A61P29/00
CPC分类号： C07H17/00
摘要： 2'-0-substituted 14- or 15-membered azalide macrolides of Formula (I) wherein R 6 represents (i) -C 1-8 alkyl, unsubstituted or substituted at the terminal carbon atom by a group selected from hydroxy, -C 1-3 alkoxy and -C(O)OC 1-3 alkyl, or when -C 1-8 alkyl is branched, substitution can alternatively be by a hydroxyl group at each of two terminal carbon atoms, (ii) -CH(NH 2 )C 1-4 alkyl, wherein the -C 1-4 alkyl group may be optionally interrupted by a heteroatom selected from O, S and N, (iii) -CH 2 N(R 7 )(R 8 ), wherein R 7 and R 8 each independently represent H or -C 1-3 alkyl provided that R 7 and R 8 cannot both simultaneously represent H, (iv) a 4-6-membered heterocyclic ring containing up to 2 heteroatoms independently selected from O, S and N, wherein the heterocyclic ring is unsubstituted or substituted by -C 1-3 alkyl, (v) 5-6 membered heteroaromatic ring, unsubstituted or substituted by one to three groups independently selected from halo, hydroxyl, -C 1-3 alkyl, -C 1-3 alkoxy, -CF 3 , -OCF 3 and -NH 2 , (vi) -CH(NH 2 )CH 2 -aryl wherein the aryl group may be unsubstituted or substituted by one or two substituents independently selected from -C 1-3 alkyl, -C 1-3 alkoxy and hydroxyl, (vii) -C 3-7 cycloalkyl, or (viii) phenyl unsubstituted or substituted by one or two groups independently selected from halo, hydroxyl, -C 1-3 alkyl, -C 1-3 alkoxy, -CF 3 , -OCF 3 and -NH 2 , or salts thereof, useful in the treatment of neutrophil dominated inflammatory diseases, especially in the treatment of neutrophil dominated inflammatory diseases resulting from neutrophilic infiltration and/or diseases associated with altered cellular functionality of neutrophils, to methods for their preparation, to their use as therapeutic agents, and to salts thereof.
摘要翻译：（I）的2'-取代的14-或15-元氮杂大环内酯，其中R 6表示（i）-C 1〜C 8烷基，未被取代或在末端碳原子被选自羟基，-C 1-3烷氧基和 -C（O）OC 1-3烷基，或者当-C 1-8烷基支链时，取代可以是两个末端碳原子上的羟基，（ⅱ）-CH（NH 2）C 1-4烷基，其中-C 1 可以任选地被选自O，S和N的杂原子，（ⅲ）-CH 2 N（R 7）（R 8）中断，其中R 7和R 8各自独立地表示H或-C 1-3烷基，条件是R 7和R 8不能同时同时表示H，（iv）含有至多2个独立地选自O，S和N的杂原子的4-6元杂环，其中杂环是未取代的或被-C 1-3烷基取代，（v）5-6元未被取代或被一至三个独立地选自卤素，羟基，-C 1-3烷基，-C 1-3烷氧基，-CF 3，-OCF 3和-NH 2的基团取代的杂芳环，（vi） -CH（NH 2）CH 2 - 芳基，其中芳基可以是未取代的或被一个或两个独立地选自-C 1-3烷基，-C 1-3烷氧基和羟基的取代基取代，（vii）-C 3-7环烷基或（viii）未被取代或被一个或两个独立地选自卤素，羟基，-C 1-3烷基，-C 1-3烷氧基，-CF 3，-OCF 3和-NH 2的基团或其盐，可用于治疗嗜中性粒细胞主导的炎性疾病，特别是治疗由嗜中性粒细胞浸润引起的嗜中性粒细胞主导的炎性疾病和/或与嗜中性粒细胞的改变的细胞功能相关的疾病，其制备方法，其作为治疗剂的用途及其盐。

10. 发明申请

WO2009016142A1 9-DEOXO-9A-METHYL-9A-AZA-9A-HOMOERYTHROMYCIN A DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MALARIA 审中-公开
标题翻译： 9-DEOXO-9A-甲基-9A-AZA-9A-异亮氨酸衍生物及其用于治疗疟疾的用途
公开(公告)号：WO2009016142A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059848
申请日：2008-07-28
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , ALIHODZIC, Sulejman , PERIC, Mihaela , PESIC, Dijana
发明人： ALIHODZIC, Sulejman , PERIC, Mihaela , PESIC, Dijana
IPC分类号： C07H17/00 , A61K31/7052 , A61P33/06
CPC分类号： C07H17/00
摘要： The present invention relates to novel 2'-O-substituted 9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity. More particularly, the invention relates to 2'-O-substituted-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A and 2'-O-substituted-3-O-decladinosyl-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity, to the intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof having antimalarial activity.
摘要翻译：本发明涉及具有抗疟活性的新的2'-O-取代的9-脱氧-9a-甲基-9a-氮杂-9a-高红霉素A衍生物。更具体地说，本发明涉及2'-O-取代-9-脱氧-9a-甲基-9a-氮杂-9a-高红霉素A和2'-O-取代-3-O-降乳素-9-脱氧-9a- 具有抗疟活性的甲基-9a-氮杂-9a-高红霉素A衍生物，其制备中间体，其制备方法，其作为治疗剂的用途及其具有抗疟活性的盐。

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