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1. 发明公开

EP2287173A1 10A-AZALIDE COMPOUND HAVING 4-MEMBERED RING STRUCTURE 审中-公开
标题翻译： 10A-AZALIDVERBINDUNG MIT 4-GLIEDRIGER RINGSTRUKTUR
公开(公告)号：EP2287173A1
公开(公告)日：2011-02-23
申请号：EP09746388.9
申请日：2009-05-15
申请人： Taisho Pharmaceutical Co., Ltd. , Meiji Seika Kaisha, Ltd.
发明人： SUGIMOTO, Tomohiro , YAMAMOTO, Kanako , KUROSAKA, Jun , SASAMOTO, Naoki , KASHIMURA, Masato , MIURA, Tomoaki , KANEMOTO, Kenichi , YOSHIDA, Satoshi , KUMURA, Kou , AJITO, Keiichi
IPC分类号： C07H17/00 , A61K31/7052 , A61P31/04
CPC分类号： C07H17/00
摘要： A 10a-azalide compound having a 4-membered ring structure crosslinked at the 10a- and 12-positions, which is represented by the formula (I), and is effective on even Haemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
摘要翻译：具有由式（I）表示的在10a-和12位交联的4元环结构的10a-氮杂化合物，并且对均匀流感嗜血杆菌或红霉素抗性细菌（例如耐药性肺炎球菌和链球菌）。

2. 发明公开

EP1985620A1 10a-AZALIDE COMPOUND 审中-公开
标题翻译： 10A-AZALIDVERBINDUNG
公开(公告)号：EP1985620A1
公开(公告)日：2008-10-29
申请号：EP07706316.2
申请日：2007-02-07
申请人： TAISHO PHARMACEUTICAL CO., LTD , Meiji Seika Kaisha Ltd.
发明人： SUGIMOTO, Tomohiro , YAMAMOTO, Kanako , MANAKA, Akira , OGITA, Haruhisa , KUROSAKA, Jun , KAWAMURA, Madoka , KASHIMURA, Masato , SASAMOTO, Naoki , MIURA, Tomoaki , KANEMOTO, Kenichi , OZAWA, Tomohiro , CHIKAUCHI, Ken , SHITARA, Eiki , KUBOTA, Dai
IPC分类号： C07H17/00 , C07H15/12 , A61K31/7052 , A61P31/04
CPC分类号： C07H17/00 , A61K31/7052
摘要： [Object]: To provide a compound having a novel structure effective against Hemophilus influenzae and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria.
[Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against Hemophilus influenzae , erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.
摘要翻译： [目的]提供具有抗血友病流感嗜血杆菌和抗红霉素的细菌（例如耐药性肺炎球菌和链球菌）以及常规红霉素敏感细菌的新型结构的化合物。 [溶液]：由式（I）表示的新型10a-氮杂化合物，其药学上可接受的盐或其溶剂合物或其制备的中间体。本发明的化合物对流感嗜血杆菌，抗红霉素的肺炎球菌等具有优异的抗菌活性，因此可用作感染性疾病的治疗剂。

3. 发明公开

EP2177526A1 10A-AZALIDE COMPOUND CROSSLINKED AT POSITION-10A AND POSITION-12 审中-公开
标题翻译：位置10A位置12 VERNETZTE 10A-AZALIDVERBINDUNG
公开(公告)号：EP2177526A1
公开(公告)日：2010-04-21
申请号：EP08790393.6
申请日：2008-08-06
申请人： Taisho Pharmaceutical Co. Ltd. , Meiji Seika Kaisha Ltd.
发明人： SUGIMOTO, Tomohiro , YAMAMOTO, Kanako , KUROSAKA, Jun , SASAMOTO, Naoki , KASHIMURA, Masato , MIURA, Tomoaki , KANEMOTO, Kenichi , OZAWA, Tomohiro , CHIKAUCHI, Ken , SHITARA, Eiki
IPC分类号： C07H17/08 , A61K31/7056 , A61P31/04
CPC分类号： C07H17/00
摘要： A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even Hemophilus influenzae , or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
摘要翻译：在10a-和12位交联的新的10a-氮杂化合物，其由下式表示，并且对流感嗜血杆菌或红霉素抗性细菌（例如抗性肺炎球菌和链球菌）有效。

4. 发明申请

WO2012115256A1 C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE 审中-公开
标题翻译： C-4“位置取代大理石衍生物
公开(公告)号：WO2012115256A1
公开(公告)日：2012-08-30
申请号：PCT/JP2012/054677
申请日：2012-02-20
申请人： TAISHO PHARMACEUTICAL CO., LTD. , MEIJI SEIKA PHARMA CO., LTD. , SUGIMOTO, Tomohiro , SASAMOTO, Naoki , KUROSAKA, Jun , HAYASHI, Masato , YAMAMOTO, Kanako , KASHIMURA, Masato , USHIKI, Yasunobu , OGITA, Haruhisa , MIURA, Tomoaki , KANEMOTO, Kenichi , KUMURA, Kou , YOSHIDA, Satoshi , TAMURA, Keiji , SHITARA, Eiki
发明人： SUGIMOTO, Tomohiro , SASAMOTO, Naoki , KUROSAKA, Jun , HAYASHI, Masato , YAMAMOTO, Kanako , KASHIMURA, Masato , USHIKI, Yasunobu , OGITA, Haruhisa , MIURA, Tomoaki , KANEMOTO, Kenichi , KUMURA, Kou , YOSHIDA, Satoshi , TAMURA, Keiji , SHITARA, Eiki
IPC分类号： C07H17/08 , A61K31/7048 , A61P31/04
CPC分类号： C07H17/08
摘要： A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).
摘要翻译：由式（I）表示的大环内酯化合物对抗红霉素抗性细菌（例如抗性肺炎球菌，链球菌和支原体）有效。

5. 发明授权

EP2678349B1 C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE 有权
标题翻译：上的位置C4 - 取代大环内酯衍生物
公开(公告)号：EP2678349B1
公开(公告)日：2016-01-13
申请号：EP12749570.3
申请日：2012-02-20
申请人： Taisho Pharmaceutical Co., Ltd. , Meiji Seika Pharma Co., Ltd.
发明人： SUGIMOTO, Tomohiro , SASAMOTO, Naoki , KUROSAKA, Jun , HAYASHI, Masato , YAMAMOTO, Kanako , KASHIMURA, Masato , USHIKI, Yasunobu , OGITA, Haruhisa , MIURA, Tomoaki , KANEMOTO, Kenichi , KUMURA, Kou , YOSHIDA, Satoshi , TAMURA, Keiji , SHITARA, Eiki
IPC分类号： C07H17/08 , A61K31/7048 , A61P31/04
CPC分类号： C07H17/08

6. 发明公开

EP2678349A1 C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE 有权
标题翻译：上的位置C4 - 取代大环内酯衍生物
公开(公告)号：EP2678349A1
公开(公告)日：2014-01-01
申请号：EP12749570.3
申请日：2012-02-20
申请人： Taisho Pharmaceutical Co., Ltd. , Meiji Seika Pharma Co., Ltd.
发明人： SUGIMOTO, Tomohiro , SASAMOTO, Naoki , KUROSAKA, Jun , HAYASHI, Masato , YAMAMOTO, Kanako , KASHIMURA, Masato , USHIKI, Yasunobu , OGITA, Haruhisa , MIURA, Tomoaki , KANEMOTO, Kenichi , KUMURA, Kou , YOSHIDA, Satoshi , TAMURA, Keiji , SHITARA, Eiki
IPC分类号： C07H17/08 , A61K31/7048 , A61P31/04
CPC分类号： C07H17/08
摘要： A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).

7. 发明公开

EP0945459A1 ERYTHROMYCIN A DERIVATIVES 失效
标题翻译： DORIVATE VON ERYTHROMYCIN-A
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
申请人： TAISHO PHARMACEUTICAL CO. LTD
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。

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