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1. 发明授权

US08097708B2 10a-Azalide compound 失效
标题翻译： 10a-叠氮化合物
公开(公告)号：US08097708B2
公开(公告)日：2012-01-17
申请号：US12223675
申请日：2007-02-07
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Akira Manaka , Haruhisa Ogita , Jun Kurosaka , Madoka Kawamura , Masato Kashimura , Naoki Sasamoto , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara , Dai Kubota
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Akira Manaka , Haruhisa Ogita , Jun Kurosaka , Madoka Kawamura , Masato Kashimura , Naoki Sasamoto , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara , Dai Kubota
IPC分类号： C07H17/08
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]提供具有抗血友病嗜血杆菌和抗红霉素抗性细菌（例如抗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化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。

2. 发明授权

US08293715B2 10a-Azalide compound crosslinked at 10a- and 12-positions 失效
标题翻译：在10a-和12位交联的10a-氮杂环戊烯化合物
公开(公告)号：US08293715B2
公开(公告)日：2012-10-23
申请号：US12671813
申请日：2008-08-06
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara
IPC分类号： A61K31/70 , C07H17/08
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。

3. 发明申请

US20110237784A1 10A-AZALIDE COMPOUND CROSSLINKED AT 10A- AND 12-POSITIONS 失效
标题翻译： 10A-AZALIDE化合物在10A和12位置交联
公开(公告)号：US20110237784A1
公开(公告)日：2011-09-29
申请号：US12671813
申请日：2008-08-06
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara
IPC分类号： C07H17/08 , C07H17/00
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

US20090281292A1 10a-Azalide Compound 失效
标题翻译： 10a-叠氮化合物
公开(公告)号：US20090281292A1
公开(公告)日：2009-11-12
申请号：US12223675
申请日：2007-02-07
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Akira Manaka , Haruhisa Ogita , Jun Kurosaka , Madoka Kawamura , Masato Kashimura , Naoki Sasamoto , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara , Dai Kubota
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Akira Manaka , Haruhisa Ogita , Jun Kurosaka , Madoka Kawamura , Masato Kashimura , Naoki Sasamoto , Tomoaki Miura , Kenichi Kanemoto , Tomohiro Ozawa , Ken Chikauchi , Eiki Shitara , Dai Kubota
IPC分类号： C07H17/08 , C07H15/04
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]提供具有抗血友病嗜血杆菌和抗红霉素抗性细菌（例如抗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化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。

5. 发明申请

US20140046043A1 C-4" POSITION SUBSTITUTED MACROLIDE DERIVATIVE 有权
标题翻译： C-4“位置取代大理石衍生物
公开(公告)号：US20140046043A1
公开(公告)日：2014-02-13
申请号：US14000556
申请日：2012-02-20
申请人： Tomohiro Sugimoto , Naoki Sasamoto , Jun Kurosaka , Masato Hayashi , Kanako Yamamoto , Masato Kashimura , Yasunobu Ushiki , Haruhisa Ogita , Tomoaki Miura , Kenichi Kanemoto , Kou Kumura , Satoshi Yoshida , Keiji Tamura , Eiki Shitara
发明人： Tomohiro Sugimoto , Naoki Sasamoto , Jun Kurosaka , Masato Hayashi , Kanako Yamamoto , Masato Kashimura , Yasunobu Ushiki , Haruhisa Ogita , Tomoaki Miura , Kenichi Kanemoto , Kou Kumura , Satoshi Yoshida , Keiji Tamura , Eiki Shitara
IPC分类号： C07H17/08
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。

6. 发明授权

US09139609B2 C-4″ position substituted macrolide derivative 有权
标题翻译： C-4“位取代的大环内酯衍生物
公开(公告)号：US09139609B2
公开(公告)日：2015-09-22
申请号：US14000556
申请日：2012-02-20
申请人： Tomohiro Sugimoto , Naoki Sasamoto , Jun Kurosaka , Masato Hayashi , Kanako Yamamoto , Masato Kashimura , Yasunobu Ushiki , Haruhisa Ogita , Tomoaki Miura , Kenichi Kanemoto , Kou Kumura , Satoshi Yoshida , Keiji Tamura , Eiki Shitara
发明人： Tomohiro Sugimoto , Naoki Sasamoto , Jun Kurosaka , Masato Hayashi , Kanako Yamamoto , Masato Kashimura , Yasunobu Ushiki , Haruhisa Ogita , Tomoaki Miura , Kenichi Kanemoto , Kou Kumura , Satoshi Yoshida , Keiji Tamura , Eiki Shitara
IPC分类号： A61K31/70 , C07H17/08
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。

7. 发明申请

US20110152239A1 10A-AZALIDE COMPOUND HAVING 4-MEMBERED RING STRUCTURE 失效
标题翻译：具有4结构环结构的10A-腈化合物
公开(公告)号：US20110152239A1
公开(公告)日：2011-06-23
申请号：US12992335
申请日：2009-05-15
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Satoshi Yoshida , Kou Kumura , Keiichi Ajito
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Satoshi Yoshida , Kou Kumura , Keiichi Ajito
IPC分类号： A61K31/397 , C07D498/08 , A61P31/00
CPC分类号： C07H17/00
摘要： The present invention relates to a process for preparing compositions of high concentrations of omega-3 fatty acids from krill. Furthermore, the invention relates to a composition comprising high concentrations of omega-3 fatty acids, and a lipid fraction from krill comprising high amounts of the fatty acids with chain length C14 and C 16.
摘要翻译：本发明涉及从磷虾制备高浓度ω-3脂肪酸的组合物的方法。此外，本发明涉及包含高浓度的ω-3脂肪酸的组合物和包含大量链长C14和C16的脂肪酸的磷虾的脂质部分。

8. 发明授权

US08299035B2 10a-azalide compound having 4-membered ring structure 失效
标题翻译：具有4元环结构的10a-氮杂化合物
公开(公告)号：US08299035B2
公开(公告)日：2012-10-30
申请号：US12992335
申请日：2009-05-15
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Satoshi Yoshida , Kou Kumura , Keiichi Ajito
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Satoshi Yoshida , Kou Kumura , Keiichi Ajito
IPC分类号： A61K31/70 , C07H17/08
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 pneunococci 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-氮杂化合物化合物，并且对偶联流感嗜血杆菌或抗红霉素抗性细菌（例如耐药性球芽孢杆菌和链球菌）。

9. 发明授权

US06169168A Erythromycin A derivatives 失效
标题翻译：红霉素A衍生物
公开(公告)号：US06169168A
公开(公告)日：2001-01-02
申请号：US09403877
申请日：1999-10-28
申请人： Toshifumi Asaka , Masato Kashimura , Tomohiro Sugimoto , Tetsuya Tanikawa , Takaaki Ishii , Akiko Matsuura
发明人： Toshifumi Asaka , Masato Kashimura , Tomohiro Sugimoto , Tetsuya Tanikawa , Takaaki Ishii , Akiko Matsuura
IPC分类号： C07H1708
CPC分类号： C07H17/08
摘要： An erythromycin A derivative represented by the formula: wherein n is an integer of from 1 to 8, R1 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R2 is a pyridylmethyl group, a quinolylmethyl group, a pyridylsulfonyl group or quinolylsulfonyl group, R3 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or a cinnamyl group, R4 is a cladinosyloxy group or a group represented by the formula: wherein m is 0 or 1, R5 is a pyridyl group, a quinolyl group, a phenyl group, a phenyl group substituted with one, two or three members selected from alkyl groups having 1 to 6 carbon atoms, a nitro group, alkoxy groups having 1 to 3 carbon atoms and halogen atoms, or a pyridyl or quinolyl group substituted with one or two members selected from alkyl groups having 1 to 6 carbon atoms, a nitro group, alkoxy groups having 1 to 3 carbon atoms and halogen atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：由下式表示的红霉素A衍生物：其中n为1至8的整数，R 1为氢原子或具有1至6个碳原子的烷基，R 2为吡啶基甲基，喹啉甲基，吡啶基磺酰基或喹啉基磺酰基，R3是氢原子，具有1-6个碳原子的烷基或肉桂基，R4是一个分子链烷氧基或由下式表示的基团：其中m是0或1，R5是吡啶基，喹啉基，苯基，被一个，两个或三个选自具有1至6个碳原子的基团取代的苯基，硝基，具有1至3个碳原子的烷氧基和卤素原子，或吡啶基或喹啉基被一个或两个选自具有1至6个碳原子的基团，硝基，具有1至3个碳原子的烷氧基和卤素原子取代的基团; 或其药学上可接受的盐。

10. 发明授权

US06165986A Erythromycin a derivatives 失效
标题翻译：红霉素a衍生物
公开(公告)号：US06165986A
公开(公告)日：2000-12-26
申请号：US355827
申请日：1999-08-05
申请人： Toshifumi Asaka , Masato Kashimura , Akiko Matsuura , Tomohiro Sugimoto , Tetsuya Tanikawa , Takaaki Ishii
发明人： Toshifumi Asaka , Masato Kashimura , Akiko Matsuura , Tomohiro Sugimoto , Tetsuya Tanikawa , Takaaki Ishii
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： An erythromycin A derivative represented by Formula (I): ##STR1## (wherein n is an integer of 2 to 4, R.sup.1 is a pyridylmethyl group, a furylmethyl group, a thienylmethyl group, a quinolylmethyl group or a benzyl group having 1 to 3 substitutents selected from the group consisting of an alkyl group having 1 to 5 carbon atoms, a nitro group, an alkoxy group having 1 to 5 carbon atoms, an amino group and an amino group substituted by 1 or 2 alkyl groups having 1 to 5 carbon atoms, R.sup.2 is the same group as defined for R.sup.1, a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an acetyl group or a pyridylacetyl group, and R.sup.3 is an alkyl group having 1 to 5 carbon atoms or a cinnamyl group) or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only known erythromycin-sensitive bacteria but also erythromycin-resistant bacteria and Haemophilus influenzae.
摘要翻译： PCT No.PCT / JP97 / 03685 Sec。 371日期1999年8月5日 102（e）1999年8月5日PCT PCT 1997年10月14日PCT公布。第WO98 / 40392号公报日期：1998年9月17日由式（I）表示的红霉素A衍生物：其中，n为2〜4的整数，R 1为吡啶基甲基，呋喃基甲基，噻吩基甲基，喹啉甲基或苄基，至3个选自具有1至5个碳原子的烷基，硝基，1至5个碳原子的烷氧基，氨基和被1或2个烷基取代的氨基的3个取代基，其具有1至 5个碳原子，R2为与R1，氢原子，碳原子数1〜5的烷基，乙酰基或吡啶基乙酰基所定义的基团，R3为碳原子数为1〜5的烷基或肉桂基）或其药学上可接受的盐对于不仅已知的红霉素敏感细菌而且对红霉素抗性细菌和流感嗜血杆菌具有强的抗菌活性。

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