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1. 发明申请

WO2007125414A3 9A-SUBSTITUTED AZALIDES FOR THE TRATMENT OF MALARIA 审中-公开
标题翻译： 9A替代疟疾治疗药物
公开(公告)号：WO2007125414A3
公开(公告)日：2008-01-17
申请号：PCT/IB2007001216
申请日：2007-05-01
申请人： GLAXOSMITHKLINE ZAGREB , 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
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。

2. 发明申请

WO2002068438A2 9A-N-[N'-(PHENYLSULFONYL)CARBAMOYL] DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHROMYCIN A AND OF 5-O-DESOSAMINYL-9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHRONOLIDE A 审中-公开
标题翻译： 9A-N- [N' - （苯基磺酰基）碳酰胺] 9-脱氧-9-二氢-9a-氮杂-9-羟基肉桂素A和5-O-去甲酰氨基-9-脱氧-9-二氢-9-氮杂的衍生物 -9A-HOMOERYTHRONOLIDE A
公开(公告)号：WO2002068438A2
公开(公告)日：2002-09-06
申请号：PCT/HR2002/000010
申请日：2002-02-27
申请人： PLIVA D.D. , KUJUNDZIC, Nedjeljko , BUKVIC KRAJACIC, Mirjana , DUMIC, Miljenko , HASENOHRL, Andrea
发明人： KUJUNDZIC, Nedjeljko , BUKVIC KRAJACIC, Mirjana , DUMIC, Miljenko , HASENOHRL, Andrea
IPC分类号： C07H17/00
CPC分类号： C07H17/00
摘要： The invention relates to 9a-N[N'-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-homoerythromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A, novel semisynthetic macrolide antibiotics from the class of azalides, of the general formula 1 wherein R 1 denotes H, C 1 -C 4 alkyl or halogen and R denotes H or cladinosyl radical, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to intermediates and methods for their preparation, to a process for the preparation of pharmaceutical compositions as well as to the use of pharmaceutical compositions in the treatment of bacterial infections.
摘要翻译：本发明涉及9-脱氧-9-二氢-9a-氮杂 - 高红霉素A的9a-N [N' - （苯基磺酰基）氨基甲酰基]衍生物和5-O-脱氨基-9-脱氧-9-二氢-9a-氮杂 -9a-同型三聚氰胺A，通式1的新型半合成大环内酯类抗生素，其中R 1表示H，C 1 -C 4烷基或卤素，R表示H或克棱糖基，其药学上可接受的加成盐与无机或有机酸，中间体及其制备方法，制备药物组合物的方法以及药物组合物在治疗细菌感染中的用途。

3. 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。

4. 发明申请

WO2004043985A1 SUBSTITUTED 9A-N-{N'-[4-(SULFONYL)PHENYL]CARBAMOYL} DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERITHROMYCIN A AND 5-0-DESOSAMINYL-9-DEOXO-9-DI-HYDRO-9A-AZA-9A-HOMOERITHRONOLIDE A 审中-公开
标题翻译：取代9-DEOXO-9-二氢-9a-氨基-9a-羟基甲霜灵A和5-0-去甲酰氨基-9-脱氧-9-氨基-9-脱氧-9- {[N' - [4-（磺酰基）苯基]碳酰胺}衍生物 DI-HYDRO-9A-AZA-9A-HOMOERRONOLIDE A
公开(公告)号：WO2004043985A1
公开(公告)日：2004-05-27
申请号：PCT/HR2003/000058
申请日：2003-11-10
申请人： PLIVA d.d. , KUJUNDZIC, Nedjeljko , BUKVIC KRAJACIC, Mirjana , BRAJSA, Karmen
发明人： KUJUNDZIC, Nedjeljko , BUKVIC KRAJACIC, Mirjana , BRAJSA, Karmen
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The invention relates to substituted 9a-N-{N'-[4-(sulfonyl)phenyl]carbamoyl} derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-di-hydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series general formula (1), wherein R represents H or cladinosyl moiety and R1 represents chloro, amino, phenylamino, 2-pyridylamino, 3,4-dimethyl-4-isoxazolylamino and 5-methyl-3-isoxazolylamino group, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to the process for their preparation of pharmaceutical composition as well as the use their compositions for sterilization rooms and medical instruments as well as for protection of wall and wooden coatings.
摘要翻译：本发明涉及9-脱氧-9-二氢-9a-氮杂-9a-高雪霉素A的取代的9a-N- {N' - [4-（磺酰基）苯基]氨基甲酰基}衍生物和5-0-去磺酰基-9- 脱氧-9-二氢-9a-氮杂-9a-高丝氨酸烯醇内酯A，通式（1）的氮杂类化合物的新型半合成大环内酯抗生素，其中R表示H或克拉糖糖基部分，R1表示氯，氨基，苯基氨基，2-吡啶基氨基，3,4-二甲基-4-异恶唑基氨基和5-甲基-3-异恶唑基氨基及其与无机或有机酸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将其组合物用于灭菌房间和医疗仪器以及保护墙壁和木器漆。

5. 发明申请

WO2004052904A3 NOVEL SEMISYNTHETIC MACROLIDE ANTIBIOTICS OF THE AZALIDE SERIES 审中-公开
标题翻译：亚氯酸盐系列的新型半胱氨酸抗体抗体
公开(公告)号：WO2004052904A3
公开(公告)日：2004-09-02
申请号：PCT/HR0300062
申请日：2003-12-10
申请人： PLIVA ISTRAZIVACKI INST D O O , KUJUNDZIC NEDJELJKO , BUKVIC KRAJACIC MIRJANA , BRAJSA KARMEN
发明人： KUJUNDZIC NEDJELJKO , BUKVIC KRAJACIC MIRJANA , BRAJSA KARMEN
IPC分类号： A61K31/70 , A61P31/04 , C07H17/00 , C07H17/08
CPC分类号： C07H17/00
摘要： The invention relates to N"-substituted 9a-N-(N'-carbamoyl-gamma-aminopropyl), 9a--N-(N'-thiocarbamoyl-gamma-aminopropyl), 9a-N-[N'-((beta-cyanoethyl)-N'-carbamoyl-gamma -aminopropyl] and 9a-N-[N'-((beta-cyanoethyl)-N'-thiocarbamoyl-gamma-aminopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R represents H or (beta-cyanoethyl moiety, R represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, beta-phenylethyl, ethoxycarbonylmethyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents 0 and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.
摘要翻译：本发明涉及N“ - 取代的9a-N-（N'-氨基甲酰基-γ-氨基丙基），9a-N-（N'-硫代氨基甲酰基-γ-氨基丙基），9a-N- [N' - （（β - 氰基乙基）-N'-氨基甲酰基-γ-氨基丙基]和9a-N- [N' - （（β-氰基乙基）-N'-硫代氨基甲酰基-γ-氨基丙基]衍生物的9-脱氧-9-二氢-9a- 氮杂-9a-高雪霉素A和5-0-去氨基-9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸新霉素A是通式1的氮杂类化合物的新型半合成大环内酯类抗生素，其中R表示H或（β-氰基乙基部分，R 2表示异丙基，1-萘基，2-萘基，苄基，2-（三氟甲基）苯基，3-苯基丙基，β-苯基乙基，乙氧基羰基甲基， 1-（1-萘基）乙基，3,4,5-三甲氧基苯基和2,4-二氯苯基，X代表0和S，以及它们与无机或有机酸的可接受的加成盐，用于制备它们的药物组合物以及在治疗中使用它们的组合物细菌感染。

6. 发明申请

WO2004043984A1 SUBSTITUTED 9a-N-[N'-(BENZENESULFONYL)CARBAMOYL-Y-AMINOPROPYL]AND 9a-N-[N'-(B-CYANEOTHYL)-N'-(BENZENESULFONYL)CARBAMOYL-Y-AMINOPROPYL]DERIVATIVES OF 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERITHROMYCIN A AND 5-0-DESOSAMINYL-9-DEOXO-9-DIHYDRO-9A-AZA-HOMOERITHRONOLIDE A 审中-公开
标题翻译：取代的9-N- [N' - （苯并呋喃基）羰基亚氨基亚氨基]和9a-N- [N' - （B-氰基乙基）-N' - （苯并呋喃基）羰基-Y-亚氨基]衍生物 -9-二氢-9a-AZA-9A-羟基甲霜灵A和5-0-去甲酰氨基-9-脱氧-9-二氢-9a-氮杂 - 二氢吲哚
公开(公告)号：WO2004043984A1
公开(公告)日：2004-05-27
申请号：PCT/HR2003/000057
申请日：2003-11-10
申请人： PLIVA D.D. , KUJUNDZIC, Nedjeljko , BUKVIC KRAJACIC, Mirjana , BRAJSA, Karmen
发明人： PLIVA D.D. , KUJUNDZIC, Nedjeljko , BUKVIC KRAJACIC, Mirjana , BRAJSA, Karmen
IPC分类号： C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： The invention relates to substituted 9a-N-[N’-(benzenesulfonyl)carbamoyl-γ-aminopropyl] and 9a-N-[N’-(β-cyanoethyl)-N’-(benzenesulfonyl)carbamoyl-γ-aminopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the formula (I) wherein R represents H or cladinosyl moiety, R 1 represents H or β-cyanoethyl group an R 2 represents H or fluoro, chloro and methyl group, and pharmaceutically acceptable salts thereof with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions as well as to the use their compositions for sterilization rooms and medical instruments as well as for protection of wall and wooden coatings.
摘要翻译：本发明涉及取代的9a-N- [N' - （苯磺酰基）氨基甲酰基-γ-氨基丙基]和9a-N- [N' - （β-氰乙基）-N' - （苯磺酰基）氨基甲酰基-γ-氨基丙基]衍生物的9-脱氧-9-二氢-9a-氮杂-9a-高雪霉素A和5-O-脱氨基-9-脱氧-9-二氢-9a-氮杂-9a-高氯三烯内酰脲A，该氮化物系列的新型半合成大环内酯类抗生素，式（I）的化合物，其中R表示H或克拉糖苷基部分，R 1表示H或β-氰基乙基，R 2表示H或氟，氯和甲基，以及其与无机或有机酸的药学上可接受的盐，用于制备药物组合物的方法以及将其组合物用于灭菌室和医疗仪器以及用于保护墙壁和木器漆。

7. 发明申请

WO2009130189A1 2'-O,3'-N-BRIDGED MACROLIDES 审中-公开
标题翻译： 2'-O，3'-N-BRIDGED MACROLIDES
公开(公告)号：WO2009130189A1
公开(公告)日：2009-10-29
申请号：PCT/EP2009/054685
申请日：2009-04-20
申请人： GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. , BUKVIC-KRAJACIC, Mirjana , HUTINEC, Antun , KRAGOL, Goran , KUJUNDZIC, Nedjeljko , MARUSIC-ISTUK, Zorica
发明人： BUKVIC-KRAJACIC, Mirjana , HUTINEC, Antun , KRAGOL, Goran , KUJUNDZIC, Nedjeljko , MARUSIC-ISTUK, Zorica
IPC分类号： C07H17/08 , A61K31/7048
CPC分类号： C07H17/08
摘要： Novel 2 ' -O, 3 ' -/V-bridged macrolides useful in treatment of inflammatory diseases. More particularly, the invention relates to 2 ' -O, 3 ' -/V-bridged 14- membered macrolides and to 2 ' - O, 3 ' -/V-bridged 15-membered azalide macrolides useful in treatment of neutrophil dominated inflammatory diseases resulting from neutrophilic infiltration and/or diseases associated with altered cellular functionality of neutrophils, to intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof.
摘要翻译：用于治疗炎性疾病的新型2'-O，3' - / V桥联大环内酯类。更具体地说，本发明涉及用于治疗嗜中性粒细胞主导的炎性疾病的2'-O，3' - / - V-桥接的14-元大环内酯和2' - O，3' - / - 桥接的15-元氮杂环丁二烯大环内酯由嗜中性粒细胞浸润和/或与嗜中性粒细胞的细胞功能改变相关的疾病，其制备中间体，其制备方法，作为治疗剂及其盐的用途引起的。

8. 发明申请

WO2006085228A3 9A-CARBAMOYL-Y-AMINOPROPYL AND 9A-THIOCARBAMOYL-Y-AMINOPROPYL-AZALIDES WITH ANTIMALARIAL ACTIVITY 审中-公开
标题翻译：具有抗微生物活性的9A-卡巴铵Y-氨基丙酸和9A-硫代氨基甲酰胺
公开(公告)号：WO2006085228A3
公开(公告)日：2007-01-04
申请号：PCT/IB2006001227
申请日：2006-01-13
申请人： GLAXOSMITHKLINE ZAGREB , 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
IPC分类号： A61K31/7052 , A61P33/06 , C07H17/08
CPC分类号： A61K31/7052 , C07H17/08
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 -?-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。

9. 发明申请

WO2004052904A2 N"-Substituted 9a-N-(N'-carbamoyl-γ-aminopropyl), 9a-N-(N' -thiocarbamoyl-γ-aminopropyl), 9a-N-[N'-((β-cyanoethyl)-N'-carbamoyl-γ -aminopropyl] and 9a-N-[N'-(β-cyanoethyl)-N'-thiocarbamoyl-γ -aminopropyl] derivatives of 9-de 审中-公开
标题翻译： N' - 取代的9a-N-（N'-氨基甲酰基-γ-氨基丙基），9a-N-（N' - 硫代氨基甲酰基-γ-氨基丙基），9a-N- [N' - （（β-氰基乙基） ' - 氨基甲酰基-γ-氨基丙基]和9-de的9a-N- [N' - （β-氰基乙基）-N'-硫代氨基甲酰基-γ-氨基丙基]衍生物
公开(公告)号：WO2004052904A2
公开(公告)日：2004-06-24
申请号：PCT/HR2003/000062
申请日：2003-12-10
申请人： PLIVA D.D. , KUJUNDZIC, Nedjeljko , BUKVIC, Krajacic, Mirjana , BRAJSA, Karmen
发明人： KUJUNDZIC, Nedjeljko , BUKVIC, Krajacic, Mirjana , BRAJSA, Karmen
IPC分类号： C07H17/00
CPC分类号： C07H17/00
摘要： The invention relates to N"-substituted 9a-N-(N'-carbamoyl-γ-aminopropyl), 9a-N-(N'-thiocarbamoyl-γ-aminopropyl), 9a-N-[N'-((β-cyanoethyl)-N'-carbamoyl-γ-aminopropyl] and 9a-N-[N'-((β-cyanoethyl)-N'-thiocarbamoyl-γ-aminopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R 1 represents H or (β-cyanoethyl moiety, R 2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, β-phenylethyl, ethoxycarbonylmethyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents 0 and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.
摘要翻译：本发明涉及N“ - 取代的9a-N-（N'-氨基甲酰基-γ-氨基丙基），9a-N-（N'-硫代氨基甲酰基-γ-氨基丙基），9a-N- [N' - （（β- 氰基乙基）-N'-氨基甲酰基-γ-氨基丙基]和9-9-氧代-9-二氢-9a-氮杂-9α-〔N' - （（β-氰乙基）-N'-硫代氨基甲酰基-γ-氨丙基] -9a-高雪霉素A和5-0-去氨基-9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸内酯A是通式1的氮杂类化合物的新型半合成大环内酯类抗生素，其中R代表H或克棱糖基部分，R 1表示H或（β-氰乙基部分，R 2表示异丙基，1-萘基，2-萘基，苄基，2-（三氟甲基）苯基，3-苯基丙基，β-苯基乙基，乙氧基羰基甲基，1 - （1-萘基）乙基，3,4,5-三甲氧基苯基和2,4-二氯苯基，X表示0和S，以及它们与无机或有机酸的可接受的加成盐，用于制备其药物组合物以及其组成治疗细菌感染。

10. 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。

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