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1. 发明申请

US20080090773A1 Macrolones - Amino Substituted Quinolones 失效
标题翻译：羟考酮 - 氨基取代喹诺酮类
公开(公告)号：US20080090773A1
公开(公告)日：2008-04-17
申请号：US11719004
申请日：2005-11-09
申请人： Desmond Best , John Elder , Andrew Forrest , Robert Sheppard , Andrea Fajdetic
发明人： Desmond Best , John Elder , Andrew Forrest , Robert Sheppard , Andrea Fajdetic
IPC分类号： A61K31/7048 , A61P31/00 , C07H17/08
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医药中的用途。

2. 发明申请

US20060154878A1 New 3-decladinosyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 9a, 11-cyclic carbamates 失效
公开(公告)号：US20060154878A1
公开(公告)日：2006-07-13
申请号：US10527940
申请日：2003-09-26
申请人： Andrea Fajdetic , Gabrijela Kobrehel , Gorjana Lazarevski , Stjepan Mutak
发明人： Andrea Fajdetic , Gabrijela Kobrehel , Gorjana Lazarevski , Stjepan Mutak
IPC分类号： A61K31/7048 , C07H17/08
CPC分类号： C07H17/08 , C07H17/00
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-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 R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)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, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, 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, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, 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.

3. 发明授权

US07718621B2 Macrolones—amino substituted quinolones 失效
标题翻译：羟考酮 - 氨基取代的喹诺酮类
公开(公告)号：US07718621B2
公开(公告)日：2010-05-18
申请号：US11719004
申请日：2005-11-09
申请人： Desmond John Best , John Stephen Elder , Andrew Keith Forrest , Robert John Sheppard , Andrea Fajdetic
发明人： Desmond John Best , John Stephen Elder , Andrew Keith Forrest , Robert John Sheppard , Andrea Fajdetic
IPC分类号： A61K31/70 , C07H17/08
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医药中的用途。

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。

6. 发明授权

US07358367B2 Present invention relates to the new 3-decladinosyl derivatives of 9-deoxo-9a-aza9a-homoerythromycin a 9a, 11-cyclic carbamates 失效
公开(公告)号：US07358367B2
公开(公告)日：2008-04-15
申请号：US10527940
申请日：2003-09-26
申请人： Andrea Fajdetic , Gabrijela Kobrehel , Gorjana Lazarevski , Stjepan Mutak
发明人： Andrea Fajdetic , Gabrijela Kobrehel , Gorjana Lazarevski , Stjepan Mutak
IPC分类号： C07D498/08
CPC分类号： C07H17/08 , C07H17/00
摘要： The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-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 R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)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, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, 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, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1C3alkil, —C(O)—, COOH or R1 together with R2 stands for ketone, R2 individually stands for hydrogen or together with R1 stands for ketone or together with R3 stands for ether, R3 individually stands for hydroxyl, a group of the formula —OX or together with R2 stands for ether, R4 individually stands for hydrogen, C1-C4alkyl group or C2-C4alkenyl group, and R5 individually stands for hydrogen or hydroxyl protected group, 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

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