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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。

3. 发明授权

US07524951B2 Intermediates of 2-substituted carbapenem derivatives and process for production thereof 失效
公开(公告)号：US07524951B2
公开(公告)日：2009-04-28
申请号：US10538466
申请日：2003-12-15
申请人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
发明人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
IPC分类号： C07D519/06 , C07D513/04
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.

4. 发明申请

US20090082571A1 Intermediates of 2-substituted carbapenem derivatives and process for production thereof 审中-公开
标题翻译： 2-取代的碳青霉烯衍生物的中间体及其制备方法
公开(公告)号：US20090082571A1
公开(公告)日：2009-03-26
申请号：US12289750
申请日：2008-11-03
申请人： Toshiro Sasaki , Takashi Ando , Takahiro Imai , Dai Kubota , Eiki Shitara , Kunio Atsumi
发明人： Toshiro Sasaki , Takashi Ando , Takahiro Imai , Dai Kubota , Eiki Shitara , Kunio Atsumi
IPC分类号： C07D513/04
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.
摘要翻译：本发明涉及由式（1）表示的化合物及其制备方法。这些化合物的使用可以以安全和成本有效的方式实现具有有效抗微生物活性和广谱抗菌谱的碳青霉烯衍生物的生产。

5. 发明申请

US20090036685A1 Process for Producing Imidazothiazole Derivatives 审中-公开
标题翻译：生产咪唑噻唑衍生物的方法
公开(公告)号：US20090036685A1
公开(公告)日：2009-02-05
申请号：US11989139
申请日：2006-07-21
申请人： Dai Kubota , Yasuo Yamamoto , Toshiro Sasaki , Takashi Ando , Eiki Shitara , Katsuya Sakata , Kenji Suzuki
发明人： Dai Kubota , Yasuo Yamamoto , Toshiro Sasaki , Takashi Ando , Eiki Shitara , Katsuya Sakata , Kenji Suzuki
IPC分类号： C07D401/14
CPC分类号： C07D519/00 , C07D513/04
摘要： Disclosed is a process for producing an imidazothiazole derivative of formula (I) useful as an intermediate for the production of carbapenem derivatives having potent antimicrobial activity and a broad antimicrobial spectrum, that is, a novel method for nicotinoylating an imidazo[5,1-b]thiazole ring at its 7-position. The process comprises reacting a compound of formula (II) with a compound of formula (III).
摘要翻译：公开了一种制备式（I）的咪唑并噻唑衍生物的方法，其用作制备具有有效抗微生物活性和广谱抗菌谱的碳青霉烯衍生物的中间体，即咪唑并[5,1-b ]噻唑环。该方法包括使式（II）化合物与式（III）化合物反应。

6. 发明授权

US07563901B2 Intermediates of 2-substituted carbapenem derivatives and process for production thereof 失效
公开(公告)号：US07563901B2
公开(公告)日：2009-07-21
申请号：US12071120
申请日：2008-02-15
申请人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
发明人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
IPC分类号： C07D513/02 , A61K31/429
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.

7. 发明申请

US20080076917A1 Intermediates of 2-Substituted Carbapenem Derivatives and Process for Production Thereof 失效
标题翻译： 2-取代的碳青霉烯衍生物的中间体及其制备方法
公开(公告)号：US20080076917A1
公开(公告)日：2008-03-27
申请号：US10538466
申请日：2003-12-15
申请人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
发明人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
IPC分类号： C07D205/00 , C07D487/00
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.
摘要翻译：本发明涉及由式（1）表示的化合物及其制备方法。这些化合物的使用可以以安全和成本有效的方式实现具有有效抗微生物活性和广谱抗菌谱的碳青霉烯衍生物的生产。

8. 发明申请

US20080167475A1 Intermediates of 2-substituted carbapenem derivatives and process for production thereof 失效
标题翻译： 2-取代的碳青霉烯衍生物的中间体及其制备方法
公开(公告)号：US20080167475A1
公开(公告)日：2008-07-10
申请号：US12071120
申请日：2008-02-15
申请人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
发明人： Toshiro Sasaki , Takashi Ando , Yasuo Yamamoto , Takahiro Imai , Dai Kubota , Katsuhiko Noguchi , Nobuyuki Hori , Eiki Shitara , Kunio Atsumi , Shohei Yasuda
IPC分类号： C07D513/04
CPC分类号： C07D513/04 , C07F9/6561 , Y02P20/55
摘要： The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner.
摘要翻译：本发明涉及由式（1）表示的化合物及其制备方法。这些化合物的使用可以以安全和成本有效的方式实现具有有效抗微生物活性和广谱抗菌谱的碳青霉烯衍生物的生产。

9. 发明授权

US06420558B1 Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists 有权
标题翻译：氨基哌啶衍生物作为整联蛋白α2β拮抗剂
公开(公告)号：US06420558B1
公开(公告)日：2002-07-16
申请号：US09673017
申请日：2000-10-10
申请人： Minoru Ishikawa , Shoichi Murakami , Mikio Yamamoto , Dai Kubota , Mitsugu Hachisu , Kiyoaki Katano , Keiichi Ajito
发明人： Minoru Ishikawa , Shoichi Murakami , Mikio Yamamoto , Dai Kubota , Mitsugu Hachisu , Kiyoaki Katano , Keiichi Ajito
IPC分类号： C07D23902
CPC分类号： C07D235/14 , C07D401/12
摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic group containing two nitrogen atoms or the like; D represents >NH2, >CH2 or the like; X and Z represent CH or a nitrogen atom; R7 and R8 represent alkyl, halogen or the like; Q represents >C═O, >CH2 or the like; R9 represents H, alkyl, aralkyl or the like; R10 represents H, alkynyl or the like; R11 represents H, substituted amino or the like; R12 represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.
摘要翻译：本发明的目的是提供具有整合素α噬菌体拮抗活性，细胞粘附抑制活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗心血管疾病，血管发生相关疾病脑血管疾病等，并用于抑制血小板聚集。根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂合物：其中A表示含有两个氮原子等的5-至7-元杂环基; D表示> NH 2，> CH 2等; X和Z表示CH或氮原子; R 7和R 8表示烷基，卤素等; Q表示> C = O，> CH2等; R 9表示H，烷基，芳烷基等; R 10表示H，炔基等; R11表示H，取代的氨基等; R 12表示H或烷基; m为0〜5; n为0〜4; p和q各自为1至3; r为0或1。

10. 发明申请

US20050059669A1 M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity 审中-公开
标题翻译：具有整合素αvβ3拮抗活性的M取代苯甲酸衍生物
公开(公告)号：US20050059669A1
公开(公告)日：2005-03-17
申请号：US10944712
申请日：2004-09-21
申请人： Keiichi Ajito , Minoru Ishikawa , Dai Kubota , Shoichi Murakami , Mikio Yamamoto , Naokazu Yahata , Kazuyuki Fujishima , Makoto Oyama
发明人： Keiichi Ajito , Minoru Ishikawa , Dai Kubota , Shoichi Murakami , Mikio Yamamoto , Naokazu Yahata , Kazuyuki Fujishima , Makoto Oyama
IPC分类号： C07C229/54 , C07C229/60 , C07D239/14 , C07D239/42 , C07D401/12 , A61K31/496 , A61K31/454 , C07D43/02
CPC分类号： C04B35/632 , C07C229/54 , C07C229/60 , C07D239/14 , C07D239/42 , C07D401/12
摘要： An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.
摘要翻译：本发明的目的是提供具有整合素α噬菌体拮抗活性的m取代苯甲酸衍生物。根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物，其可用于治疗或预防心血管疾病，血管生成相关疾病，脑血管疾病，癌症及其转移，免疫疾病，骨病和其他疾病：其中A表示任选取代的含有两个氮原子的杂环基团，二等基团等; D表示键，NR 4，CR 5 R 6，O，S或-NR 4 -CR 5 R 6 - 。 X表示CH或N; R 7和R 8代表羟基，烷基等; Q表示> C = O等; R 9表示氢，烷基等; J表示键或亚烷基; R 10表示任选取代的羟基，氨基等; R 11表示氢，烷基等; m为0〜5; n为0〜4; p和q各自为0〜3。

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