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公开(公告)号：EP0619319B1
公开(公告)日：1997-03-05
申请号：EP93900446.1
申请日：1992-12-25
CPC分类号： C07H17/08
摘要： A 3-carbamoylated 5-O-desosaminyl-6-O-methylerythronolide derivative represented by general formula (I) and a pharmaceutically acceptable acid addition salt thereof, which are novel macrolide antibiotics with a potent antibacterial power, wherein R?1 and R2¿ each represent hydrogen, phenyl optionally substituted by halogen, nitro or amino, alkyl optionally containing nitrogen, oxygen or sulfur, or aralkyl, or alternatively R?1 and R2¿ are combined together with the nitrogen atom to form a nitrogenous ring; Z represents oxo or hydroxyimino; V represents hydroxy; W represents hydrogen or hydroxy, or alternatively V and W are combined together to form a cyclic carbonate group or an oxazoline ring; and R represents hydrogen or acyl.
摘要翻译： 由通式（I）表示的3-氨基甲酰基化5-O-德糖胺基-6-O-甲基赤藓糖酸内酯衍生物及其药学上可接受的酸加成盐，它们是具有强效抗菌力的新型大环内酯类抗生素，其中R 1和R 2' 各自代表氢，任选被卤素，硝基或氨基取代的苯基，任选含有氮，氧或硫的烷基或芳烷基，或者R 1和R 2与氮原子一起形成含氮环; Z代表氧代或羟基亚氨基; V代表羟基; W表示氢或羟基，或者V和W结合在一起形成环状碳酸酯基团或恶唑啉环; 和R代表氢或酰基。
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公开(公告)号：EP0945459A1
公开(公告)日：1999-09-29
申请号：EP97943199.6
申请日：1997-10-14
发明人： ASAKA, Toshifumi , KASHIMURA, Masato , MATSUURA, Akiko , SUGIMOTO, Tomohiro , TANIKAWA, Tetsuya , ISHII, Takaaki
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： An erythromycin A derivative represented by Formula (I):
[wherein n is an integer of from 1 to 4, R 1 is a group represented by the formula:
a group represented by the formula:
a pyridylacetyl group, a cycloalkylmethyl group having 4 to 8 carbon atoms or a 1,2-bis(ethoxycarbonyl)vinyl group, R 2 is the same group as defined for R 1 , a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkanoyl group having 2 to 6 carbon atoms or an alkoxycarbonyl group having 2 to 6 carbon atoms, R 1 and R 2 together form a group of the formula: =CH-R 14 , or R 1 and R 2 together with the nitrogen atom to which they are attached form a group represented by the formula:
R 15 and R 16 are each a hydrogen atom or when W is a carbon atom, R 15 and R 16 together with the carbon atoms to which they are attached form a benzene ring or a naphthalene ring, R 3 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a cinnamyl group, R 4 is a hydrogen atom, an acetyl group, an ethylsuccinyl group or a nicotinoyl group, A is a group represented by the formula:
-OC(=O)-R 17 , -OC(=O)-CH 2 -R 17 , -OC(=O)-NH-R 17 , -O-R 17 or -OC(=O)-O-R 17 , and R 5 and R 6 are each a hydrogen atom or an alkyl group having 1 to 5 carbon atoms] or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only against known erythromycin-sensitive bacteria but also erythromycin-resistant bacteria.摘要翻译： 由式（I）表示的红霉素A衍生物：其中n是1至4的整数，R 1是由下式表示的基团：CHEM>由下式表示的基团：
吡啶基乙酰基，具有4-8个碳原子的环烷基甲基或1,2-双（乙氧基羰基）乙烯基，R 2是与R 1所定义的相同的基团，氢原子，具有 1至5个碳原子，具有2至6个碳原子的烷酰基或具有2至6个碳原子的烷氧基羰基，R 1和R 2一起形成下式的基团：= CH-R 14 或R 1和R 2与它们所连接的氮原子一起形成由下式表示的基团： R 15和R 16各自为氢原子或当W为 碳原子，R 15和R 16与它们所连接的碳原子一起形成苯环或萘环，R 3是氢原子，具有1至5个碳原子的烷基 或肉桂基，R 4是氢 原子，乙酰基，乙基琥珀酰基或烟酰基，A是下式表示的基团：-OC（= O）-R 17，-OC（= O）-CH 2 -R 17， OC（= O）-NH-R 17，-OR 17或-OC（= O）-OR 17，R 5和R 6各自为氢原子或烷基 具有1至5个碳原子或其药学上可接受的盐对抗已知的红霉素敏感细菌而且对红霉素抗性细菌具有很强的抗菌活性。 -
3.发明公开
公开(公告)号：EP0553353A1
公开(公告)日：1993-08-04
申请号：EP91917071.2
申请日：1991-10-08
发明人： ASAKA, Toshifumi , MISAWA, Yoko , KASHIMURA, Masato , MORIMOTO, Shigeo , WATANABE, Yoshiaki , HATAYAMA, Katsuo
CPC分类号： C07H17/08
摘要： Modified erythromycin having remarkably alleviated bitterness and improved bioabsorbability, comprising a compound prepared by introducing a group represented by the formula: -O-CO-O-[(CH₂) m -O] n -R (wherein R represents C₁ to C₁₂ alkyl, m represents an integer of 2 to 4, and n represents an integer of 1 to 7), into the 2'-position of an erythromycin, or its salt.
摘要翻译： 改进的红霉素具有显着缓解的苦味和改善的生物吸收性，包括通过引入由下式表示的基团制备的化合物：-O-CO-O - [（CH2）mO] nR（其中R表示C1至C12烷基，m表示整数 2〜4，n表示1〜7的整数），进入红霉素或其盐的2'-位。
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公开(公告)号：EP0559896B1
公开(公告)日：1997-08-27
申请号：EP92902490.9
申请日：1991-11-22
发明人： KASHIMURA, Masato, Raionzugahden , ASAKA, Toshifumi , MORIMOTO, Shigeo , HATAYAMA, Katsuo, Horisakichodanchi 35-3
摘要： A 6-O-methylerythromycin A derivative represented by general formula (I) and pharmaceutically acceptable salts thereof, having a potent antibacterial activity against gram-negative bacteria and a more potent activity against gram-positive bacteria than that of known compounds. In the said formula, R?1 and R2¿ represent each hydrogen or C¿1? to C3 alkyl, and A represents nitrogen or N←O.
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公开(公告)号：EP0682038A1
公开(公告)日：1995-11-15
申请号：EP94904756.7
申请日：1994-01-24
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： A novel macrolide antibiotic having a potent antimicrobial activity, represented by general formula (1), which is produced by introducing a specified aryloxy or alkyloxy group into the 3-position of a 5-O-desosaminylerythronolide derivative, wherein Y represents oxygen-containing C₄-C₆ cycloalkyl, optionally substituted phenyl, glucopyranosyl, ribopyranosyl, benzyl or methyl; U represents hydrogen or acyl; Z represents oxygen or N-OR₁ wherein R₁ represents hydrogen, alkanoyl or optionally substituted benzyl; and A represents a group that forms an erythronolide which may form a cyclic carbonate group between the 11- and the 12-positions or a double bond between the 10- and 11-positions.
摘要翻译： 一种通式（1）所示的具有有效抗微生物活性的新型大环内酯类抗生素，它是通过在5-O-去杂氨基红霉素衍生物的3位引入一个特定的芳氧基或烷氧基得到的，其中Y代表含氧C 4 任选取代的苯基，吡喃葡萄糖基，核糖吡喃糖基，苄基或甲基; U代表氢或酰基; Z代表氧或N-OR 1，其中R 1代表氢，链烷酰基或任意取代的苄基; A表示形成可在11位和12位之间形成环状碳酸酯基或10位和11位之间的双键的乙交酯（erythronolide）的基团。
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公开(公告)号：EP2077271A1
公开(公告)日：2009-07-08
申请号：EP07742762.3
申请日：2007-05-01
IPC分类号： C07H17/08 , A61K31/7048 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/00 , A61P29/00 , A61P35/00 , A61P43/00
CPC分类号： C07H17/08 , A61K31/7048 , A61K31/7052 , C07H17/00
摘要： Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).
摘要翻译： 由式（I）和式（IV）表示的化合物具有MMP-9产生的抑制活性，因此可用作副作用小于传统MMP酶活性抑制剂的药物，作为致癌的预防和治疗药物 血管生成，慢性风湿性关节炎，经皮冠状动脉腔内血管成形术后血管内膜增厚，血管动脉硬化，出血性中风，急性心肌梗塞，慢性心力衰竭，动脉瘤，肺癌转移，成人呼吸窘迫综合征，哮喘，间质性肺纤维化，慢性鼻窦炎， 支气管炎或慢性阻塞性肺病（COPD）。
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公开(公告)号：EP0619319A1
公开(公告)日：1994-10-12
申请号：EP93900446.1
申请日：1992-12-25
CPC分类号： C07H17/08
摘要： A 3-carbamoylated 5-O-desosaminyl-6-O-methylerythronolide derivative represented by general formula (I) and a pharmaceutically acceptable acid addition salt thereof, which are novel macrolide antibiotics with a potent antibacterial power, wherein R¹ and R² each represent hydrogen, phenyl optionally substituted by halogen, nitro or amino, alkyl optionally containing nitrogen, oxygen or sulfur, or aralkyl, or alternatively R¹ and R² are combined together with the nitrogen atom to form a nitrogenous ring; Z represents oxo or hydroxyimino; V represents hydroxy; W represents hydrogen or hydroxy, or alternatively V and W are combined together to form a cyclic carbonate group or an oxazoline ring; and R represents hydrogen or acyl.
摘要翻译： 由通式（I）表示的3-氨基甲酰基化5-O-德糖胺基-6-O-甲基赤藓糖酸内酯衍生物及其药学上可接受的酸加成盐，它们是具有强抗菌力的新型大环内酯类抗生素，其中R 1和R 2各自代表氢 任选被卤素，硝基或氨基取代的苯基，任选含有氮，氧或硫的烷基，或芳烷基，或者R 1和R 2与氮原子结合在一起形成含氮环; Z代表氧代或羟基亚氨基; V代表羟基; W表示氢或羟基，或者V和W结合在一起形成环状碳酸酯基团或恶唑啉环; 和R代表氢或酰基。
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公开(公告)号：EP0559896A1
公开(公告)日：1993-09-15
申请号：EP92902490.9
申请日：1991-11-22
发明人： KASHIMURA, Masato, Raionzugahden , ASAKA, Toshifumi , MORIMOTO, Shigeo , HATAYAMA, Katsuo, Horisakichodanchi 35-3
摘要： A 6-O-methylerythromycin A derivative represented by general formula (I) and pharmaceutically acceptable salts thereof, having a potent antibacterial activity against gram-negative bacteria and a more potent activity against gram-positive bacteria than that of known compounds. In the said formula, R¹ and R² represent each hydrogen or C₁ to C₃ alkyl, and A represents nitrogen or N → O.
摘要翻译： 由通式（I）表示的6-O-甲基红霉素A衍生物及其药学上可接受的盐，其具有对革兰氏阴性菌的有效抗菌活性和比对已知化合物具有更强的抗革兰氏阳性菌活性。 在上式中，R 1和R 2代表氢或C 1 -C 3烷基，A代表氮或N→O.
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