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1. 发明申请

US20110039795A1 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：US20110039795A1
公开(公告)日：2011-02-17
申请号：US12988908
申请日：2009-04-20
申请人： Mirjana Bukvic-Krajacic , Antun Hutinec , Goran Kragol , Nedjeljko Kujundzic , Zorica Marusic-Istuk
发明人： Mirjana Bukvic-Krajacic , Antun Hutinec , Goran Kragol , Nedjeljko Kujundzic , Zorica Marusic-Istuk
IPC分类号： A61K31/7048 , C07H17/00 , A61K31/7052 , C07H17/08 , A61P29/00 , A61P9/10 , A61P11/00 , A61P11/06
CPC分类号： C07H17/08
摘要： Novel 2′-O,3′-N-bridged macrolides useful in treatment of inflammatory diseases. More particularly, the invention relates to 2′-O,3′-N-bridged 14-membered macrolides and to 2′-O,3′-N-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'-N-桥联大环内酯类。更具体地说，本发明涉及可用于治疗由嗜中性粒细胞主导的炎性疾病引起的2'-O，3'-N-桥接的14-元大环内酯和2'-O，3'-N-桥接的15-元氮杂大环内酯嗜中性粒细胞浸润和/或与嗜中性粒细胞改变的细胞功能相关的疾病，其制备中间体，其制备方法，其作为治疗剂的用途及其盐。

2. 发明申请

US20080200404A1 Novel Antimalarial 9A-Carbamoyl-Aminoalkyl and 9A-Thiocarbamoyl-Aminoalkyl Azalides 审中-公开
标题翻译：新型抗疟药9A-氨基甲酰基 - 氨基烷基和9A-硫代氨基甲酰基 - 氨基烷基氮杂环戊烷
公开(公告)号：US20080200404A1
公开(公告)日：2008-08-21
申请号：US11813875
申请日：2006-01-13
申请人： Mirjana Bukvic Krajacic , Nedjeljko Kujundzic , Zrinka Ivezic , Sulejman Alihodzic , Antun Hutinec , Andrea Fajdetic
发明人： Mirjana Bukvic Krajacic , Nedjeljko Kujundzic , Zrinka Ivezic , Sulejman Alihodzic , Antun Hutinec , Andrea Fajdetic
IPC分类号： A61K31/7048 , C07H17/08 , A61P33/02 , A61P33/06
CPC分类号： A61K31/7052 , C07H17/08 , Y02A50/411
摘要： Novel 9a-N′-substituted-carbamoyl- and thiocarbamoyl-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-β-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 - 和硫代氨基甲酰基 - 氨基烷基-9a-氮杂-9-脱氧-9-二氢-9a-高红霉素A和3-O-降解十二烷基-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，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。

3. 发明申请

US20070066544A1 3-Decladinosyl 9a-n-carbamoyl and 9a-n-thiocarbamoyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 审中-公开
标题翻译： 9-去氧-9-二氢-9a-氮杂-9a-高红霉素a的3-突变二糖基-9a-正 - 氨基甲酰基和9a-正 - 硫代氨基甲酰基衍生物
公开(公告)号：US20070066544A1
公开(公告)日：2007-03-22
申请号：US10557025
申请日：2004-05-11
申请人： Zorica Marusic-Istuk , Nedjeljko Kujundzic , Stjepan Mutak
发明人： Zorica Marusic-Istuk , Nedjeljko Kujundzic , Stjepan Mutak
IPC分类号： A61K31/7052 , C07H17/08
CPC分类号： C07H17/08
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9a-N-carbamoyl- and 9a-N-thiocarbamoyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process 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9a-N-氨基甲酰基 - 和9a-N-硫代氨基甲酰基-9-脱氧-9-二氢-9a-氮杂-9a-高红霉素A的新的3-降乳糖苷衍生物，它们的与无机或有机酸及其水合物的药学上可接受的加成盐，用于合成具有抗菌活性的其它大环内酯类化合物的中间体，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与该方法用于制备药物组合物，以及用于治疗细菌感染的药物组合物。

4. 发明授权

US07365056B2 Substituted 9a-N-(N′-(sulfonyl)phenylcarbamoyl)derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithomycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9-a-aza-9a-homoerithronolide A 失效
标题翻译： 9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸霉素A的9-N（N' - （磺酰基）苯基氨基甲酰基）衍生物和5-0-去氨基-9-脱氧-9-二氢-9- -aza-9a-高三烯宁内酯A
公开(公告)号：US07365056B2
公开(公告)日：2008-04-29
申请号：US10534628
申请日：2003-11-10
申请人： Nedjeljko Kujundzic , Mirjana Bukvic Krajacic , Karmen Brajsa
发明人： Nedjeljko Kujundzic , Mirjana Bukvic Krajacic , Karmen Brajsa
IPC分类号： A61K31/70 , 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-isoxalylamino 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-异柠檬酰氨基和5-甲基-3-异恶唑基氨基，以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过程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

5. 发明授权

US07342000B2 Semisynthetic macrolide antibiotics of the azalide series 失效
标题翻译：半合成大环内酯类抗生素的azalide系列
公开(公告)号：US07342000B2
公开(公告)日：2008-03-11
申请号：US10538376
申请日：2003-12-10
申请人： Nedjeljko Kujundzic , Mirjana Bukvic Krajacic , Karmen Brajsa
发明人： Nedjeljko Kujundzic , Mirjana Bukvic Krajacic , Karmen Brajsa
IPC分类号： A61K31/70 , C07H17/08
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-am inopropyl] 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 semi-synthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R1 represents H or β-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, β-phenylethyl, ethoxycarbonyl-methyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents O 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-脱氧-9-二氢-9a-氮杂-9a的9a-N- [N'-β-氰基乙基] -N'-硫代氨基甲酰基-γ-氨基丙基]衍生物高锰霉素A和5-O-脱雄氨基-9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸新一烯内酯A是通式1的氮杂环丁烷系新型半合成大环内酯类抗生素，其中R表示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O和S及其可接受的加成盐与无机或有机酸，制备其药物组合物的方法以及使用它们的组成在治疗细菌感染。

6. 发明授权

US06852702B2 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 失效
标题翻译： 9-脱氧-9-二氢-9a-氮杂-9a-高红霉素A的9α-N- [N' - （苯基磺酰基）氨基甲酰基]衍生物和5-O-去酰氨基-9-脱氧-9-二氢-9a-氮杂 -9a-homoeryronronideide A
公开(公告)号：US06852702B2
公开(公告)日：2005-02-08
申请号：US10469253
申请日：2002-02-27
申请人： Nedjeljko Kujundzic , Mirjana Bukvic Krajacic , Miljenko Dumic , Andrea Hasenohrl
发明人： Nedjeljko Kujundzic , Mirjana Bukvic Krajacic , Miljenko Dumic , Andrea Hasenohrl
IPC分类号： A61P31/04 , C07H17/00 , A61K31/70 , C07H1/00 , C07H17/08
CPC分类号： C07H17/00
摘要： 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 and their pharmaceutically acceptable addition salts with inorganic or organic acids are provided, along with a process for their preparation, pharmaceutical compositons, and use in treating bacterial infections.
摘要翻译： 9-脱氧-9-二氢-9a-氮杂-9a-高红霉素A的9α-N- [N' - （苯基磺酰基）氨基甲酰基]衍生物和5-O-去酰氨基-9-脱氧-9-二氢-9a-氮杂提供了与无机或有机酸的药学上可接受的加成盐以及其制备方法，药物组合物和用于治疗细菌感染的方法。

7. 发明申请

US20070270356A1 Substituted 9A-N-[N'-(Benzenesulfonyl)Carbamoyl-Y-Aminopropyl] and 9A-N-[N'(B-Cyanoethyl)-N'-(Benzenesulfonyl)Carbamoyl-Y-Aminopropyl]Derivatives of 9-Deoxo-9-Dihydro-9A-Aza-9A-Homoerithomycin A 审中-公开
标题翻译： 9-Deoxo-取代的9A-N- [N' - （苯磺酰基）氨基甲酰基-N-氨基丙基]和9A-N- [N'（B-氰基乙基）-N' - （苯磺酰基）氨基甲酰基-Y-氨基丙基] 9-二氢-9A-Aza-9A-同源霉素A
公开(公告)号：US20070270356A1
公开(公告)日：2007-11-22
申请号：US10534261
申请日：2003-11-10
申请人： Nedjeljko Kujundzic , Mirjana Krajacic , Karmen Brajsa
发明人： Nedjeljko Kujundzic , Mirjana Krajacic , Karmen Brajsa
IPC分类号： A61K31/7048 , A61P31/04 , 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-( )-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, R1 represents H or β-cyanoethyl group an R2 represents II 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-（（S） - 氨基甲酰基-9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸内酯A），这种新的半合成大环内酯类抗生素，其中R表示H或克拉糖苷基部分的式（I），R 1表示H或β-氰基乙基，R 2表示II或氟，氯和甲基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。

8. 发明申请

US20090105301A1 9A-SUBSTITUTED AZALIDES FOR THE TREATMENT OF MALARIA 审中-公开
标题翻译： 9A替代疟疾治疗药物
公开(公告)号：US20090105301A1
公开(公告)日：2009-04-23
申请号：US12299042
申请日：2007-05-01
申请人： Sulejman Alihodzic , Andrea Fajdetic , Anton Hutinec , Zrinka Ivezic , Nedjeljko Kujundzic , Renata Rupcic
发明人： Sulejman Alihodzic , Andrea Fajdetic , Anton Hutinec , Zrinka Ivezic , Nedjeljko Kujundzic , Renata Rupcic
IPC分类号： A61K31/4709 , C07D267/00 , A61K31/395
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。

9. 发明授权

US5854219A 9-N-ethenyl derivatives of 9(S)-erythromycylamine 失效
标题翻译： 9（S） - 红霉素胺的9-N-乙烯基衍生物
公开(公告)号：US5854219A
公开(公告)日：1998-12-29
申请号：US956352
申请日：1997-10-23
申请人： Nedjeljko Kujundzic , Dina Pavlovic , Gabrijela Kobrehel , Gorjana Lazarevski , Zeljko Kelneric
发明人： Nedjeljko Kujundzic , Dina Pavlovic , Gabrijela Kobrehel , Gorjana Lazarevski , Zeljko Kelneric
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C07D315/00 , C07G11/00
CPC分类号： A61K31/7048 , C07H17/08
摘要： The invention relates to 9-N-ethenyl derivatives of 9 (S)-erythromycylamine, new semisynthetic antibiotics of the macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent nitryl, a carboxyl group of the formula COOR.sup.3, wherein R.sup.3 represents a C.sub.1 -C.sub.4 alkyl group, or a keto group of the formula COR.sup.4, wherein R.sup.4 represents a C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation, to a process for the preparation of the pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.
摘要翻译：本发明涉及9（S） - 红霉素胺的9-N-乙烯基衍生物，通式（I）的大环内酯类的新的半合成抗生素：其中R1和R2相同或不同，代表硝基，式COOR 3的羧基，其中R 3表示C 1 -C 4烷基，或式COR 4的酮基（其中R 4表示C 1 -C 4烷基）与其与无机或有机酸的药学上可接受的加成盐，制备方法，制备药物组合物的方法以及所获得的药物组合物在细菌感染治疗中的用途。

10. 发明申请

US20060252709A1 Novel semisynthetic macrolide antibiotics of the azalide series 失效
标题翻译：新型半合成大环内酯类抗生素的阿扎那肽系列
公开(公告)号：US20060252709A1
公开(公告)日：2006-11-09
申请号：US10538376
申请日：2003-12-10
申请人： Nedjeljko Kujundzic , Mirjana Krajacic , Karmen Brajsa
发明人： Nedjeljko Kujundzic , Mirjana Krajacic , Karmen Brajsa
IPC分类号： A61K31/7052 , C07H17/08
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-amino-propyl), 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, R1 represents H or (β-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluommethyl)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-N-氧代-9-二氢 - 9a-aza-9a-高雪霉素A和5-0-脱氨基-9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸新一烯内酯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或克拉糖苷基部分，R 1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表示0和S，以及它们可接受的加成盐与无机或有机酸，制备其药物组合物的方法以及使用它们的组合物治疗细菌感染。

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