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1. 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

2. 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。

3. 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。

4. 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。

5. 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。

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