公开(公告)号：US20110166131A1

公开(公告)日：2011-07-07

申请号：US13045567

申请日：2011-03-11

申请人： Hisashi TAKAHASHI ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi TAKAHASHI ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/5383 ,  C07D498/06 ,  A61P31/04

CPC分类号： C07D401/04 ,  C07D498/06

摘要： A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I):

摘要翻译： 用于治疗感染性疾病的喹诺酮类抗菌化合物或化合物的盐或水合物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥 ），其具有更高的安全性，并且具有式（I）的结构：

公开(公告)号：US07977327B2

公开(公告)日：2011-07-12

申请号：US11596318

申请日：2005-05-13

申请人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/54

CPC分类号： C07D401/04 ,  C07D498/06

摘要： A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I):

摘要翻译： 用于治疗感染性疾病的喹诺酮类抗菌化合物或化合物的盐或水合物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥 ），其具有更高的安全性，并且具有式（I）的结构：

公开(公告)号：US20080045520A1

公开(公告)日：2008-02-21

申请号：US11596318

申请日：2005-05-13

申请人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/4709 ,  A61K31/538 ,  A61P31/00 ,  A61P31/04 ,  C07D215/14 ,  C07D498/06

CPC分类号： C07D401/04 ,  C07D498/06

摘要： The present invention contemplates provision of a quinolone antibacterial agent and a drug for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), and which exhibit higher safety. A compound represented by the following formula (I): a salt of the compound, or a hydrate of the compound or the salt; and an antibacterial drug and an infectious disease treating drug containing the compound as an active ingredient.

摘要翻译： 本发明考虑提供喹诺酮抗菌剂和用于治疗感染性疾病的药物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥） ，而且安全性更高。 由下式（I）表示的化合物：化合物的盐或化合物或其盐的水合物; 以及含有该化合物作为活性成分的抗菌药物和感染性疾病治疗药物。

公开(公告)号：US08455482B2

公开(公告)日：2013-06-04

申请号：US13045567

申请日：2011-03-11

申请人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

发明人： Hisashi Takahashi ,  Junichi Kuroyanagi ,  Rie Miyauchi ,  Masatoshi Nagamochi ,  Makoto Takemura ,  Isao Hayakawa

IPC分类号： A61K31/535

CPC分类号： C07D401/04 ,  C07D498/06

摘要： A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g., convulsion), which exhibit higher safety, and which has a structure of formula (I):

摘要翻译： 用于治疗感染性疾病的喹诺酮类抗菌化合物或化合物的盐或水合物，其对革兰氏阳性和革兰氏阴性菌具有强力的抗菌活性和较高的选择性毒性，其不引起副作用（例如惊厥 ），其具有更高的安全性，并且具有式（I）的结构：

公开(公告)号：US08618094B2

公开(公告)日：2013-12-31

申请号：US12459612

申请日：2009-07-02

申请人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

发明人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

IPC分类号： C07D401/10 ,  C07D498/06 ,  A61K31/4709 ,  A61K31/5383

CPC分类号： C07D498/06 ,  C07D209/02 ,  C07D209/56 ,  C07D401/04 ,  C07D401/14 ,  C07D491/048 ,  C07D491/052 ,  Y02P20/55

摘要： A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

摘要翻译： 提供了作为药物具有优异性能的喹诺酮合成抗菌剂，其不仅对革兰氏阴性菌具有很强的抗菌活性，而且对喹诺酮类抗菌剂具有低敏感性的革兰氏阳性球菌具有很强的抗菌活性，并且其表现出高安全性和优异的药代动力学 。 由式（I）表示的化合物或其盐或其水合物。 具体地，其中取代基R6和R7与它们所键合的碳原子一起形成式（I）的喹诺酮衍生物形成可以含有氧原子作为环组成原子的环状结构，所述环状结构形成5- 4,5,5-或5-6稠合双环吡咯烷基取代基，该取代基与含有吡啶并苯并恶嗪结构的喹诺酮母体骨架Q结合。

公开(公告)号：US20130029977A9

公开(公告)日：2013-01-31

申请号：US12459612

申请日：2009-07-02

申请人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

发明人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

IPC分类号： A61K31/4709 ,  C07D498/06 ,  A61K31/5383 ,  A61P1/12 ,  A61P29/00 ,  A61P31/04 ,  A61P31/00 ,  A61P33/00 ,  A61P17/00 ,  A61P15/00 ,  A61P17/10 ,  A61P11/08 ,  A61P11/00 ,  A61P13/08 ,  A61P13/02 ,  A61P27/02 ,  A61P1/02 ,  A61P37/00 ,  A61P31/06 ,  A61P31/08 ,  C07D401/10

CPC分类号： C07D498/06 ,  C07D209/02 ,  C07D209/56 ,  C07D401/04 ,  C07D401/14 ,  C07D491/048 ,  C07D491/052 ,  Y02P20/55

摘要： A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

公开(公告)号：US20120108582A1

公开(公告)日：2012-05-03

申请号：US12459612

申请日：2009-07-02

申请人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

发明人： Hisashi Takahashi ,  Satoshi Komoriya ,  Takahiro Kitamura ,  Takashi Odagiri ,  Hiroaki Inagaki ,  Toshifumi Tsuda ,  Kiyoshi Nakayama ,  Makoto Takemura ,  Kenichi Yoshida ,  Rie Miyauchi ,  Masatoshi Nagamochi

IPC分类号： A61K31/4709 ,  C07D498/06 ,  A61K31/5383 ,  A61P1/12 ,  A61P29/00 ,  A61P31/04 ,  A61P31/00 ,  A61P33/00 ,  A61P17/00 ,  A61P15/00 ,  A61P17/10 ,  A61P11/08 ,  A61P11/00 ,  A61P13/08 ,  A61P13/02 ,  A61P27/02 ,  A61P1/02 ,  A61P37/00 ,  A61P31/06 ,  A61P31/08 ,  C07D401/10

CPC分类号： C07D498/06 ,  C07D209/02 ,  C07D209/56 ,  C07D401/04 ,  C07D401/14 ,  C07D491/048 ,  C07D491/052 ,  Y02P20/55

摘要： A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.

摘要翻译： 提供了作为药物具有优异性能的喹诺酮合成抗菌剂，其不仅对革兰氏阴性菌具有很强的抗菌活性，而且对喹诺酮类抗菌剂具有低敏感性的革兰氏阳性球菌具有很强的抗菌活性，并且其表现出高安全性和优异的药代动力学 。 由式（I）表示的化合物或其盐或其水合物。 具体地，其中取代基R6和R7与它们所键合的碳原子一起形成式（I）的喹诺酮衍生物形成可以含有氧原子作为环组成原子的环状结构，所述环状结构形成5- 4,5,5-或5-6稠合双环吡咯烷基取代基，该取代基与含有吡啶并苯并恶嗪结构的喹诺酮母体骨架Q结合。

公开(公告)号：US20090270637A1

公开(公告)日：2009-10-29

申请号：US12067737

申请日：2006-09-28

申请人： Hisashi Takahashi ,  Rie Miyauchi ,  Yasuyuki Takeda ,  Kazuo Kanai ,  Junichi Kuroyanagi ,  Satoshi Komoriya ,  Makoto Takemura

发明人： Hisashi Takahashi ,  Rie Miyauchi ,  Yasuyuki Takeda ,  Kazuo Kanai ,  Junichi Kuroyanagi ,  Satoshi Komoriya ,  Makoto Takemura

IPC分类号： C07D209/54

CPC分类号： C07D209/54 ,  C07D207/14 ,  C07D207/273 ,  C07D207/277 ,  C07D471/04

摘要： The present invention provides a method for effectively producing an optically active form of tetrasubstituted-5-azaspiro[2.4]heptane derivative, which serves as a useful production intermediate for quinolonecarboxylic acid antibacterial agents, and intermediates for the derivative. The present invention is directed to a method for producing a compound (VII) according to the following scheme.

摘要翻译： 本发明提供了有效地制备作为喹诺酮羧酸抗菌剂的有用的生产中间体的四取代-5-氮杂螺[2.4]庚烷衍生物的光学活性形式的方法和该衍生物的中间体。 本发明涉及根据下列方案制备化合物（Ⅶ）的方法。

公开(公告)号：US07842818B2

公开(公告)日：2010-11-30

申请号：US12067737

申请日：2006-09-28

申请人： Hisashi Takahashi ,  Rie Miyauchi ,  Yasuyuki Takeda ,  Kazuo Kanai ,  Junichi Kuroyanagi ,  Satoshi Komoriya ,  Makoto Takemura

发明人： Hisashi Takahashi ,  Rie Miyauchi ,  Yasuyuki Takeda ,  Kazuo Kanai ,  Junichi Kuroyanagi ,  Satoshi Komoriya ,  Makoto Takemura

IPC分类号： C07D209/54

CPC分类号： C07D209/54 ,  C07D207/14 ,  C07D207/273 ,  C07D207/277 ,  C07D471/04

摘要： The present invention provides a method for effectively producing an optically active form of tetrasubstituted-5-azaspiro[2.4]heptane derivative, which serves as a useful production intermediate for quinolonecarboxylic acid antibacterial agents, and intermediates for the derivative. The present invention is directed to a method for producing a compound (VII) according to the following scheme.

摘要翻译： 本发明提供了有效地制备作为喹诺酮羧酸抗菌剂的有用的生产中间体的四取代-5-氮杂螺[2.4]庚烷衍生物的光学活性形式的方法和该衍生物的中间体。 本发明涉及根据下列方案制备化合物（Ⅶ）的方法。

公开(公告)号：US06573260B1

公开(公告)日：2003-06-03

申请号：US09856631

申请日：2001-05-24

申请人： Makoto Takemura ,  Hisashi Takahashi ,  Rie Miyauchi ,  Toshiyuki Takeda ,  Isao Hayakawa

发明人： Makoto Takemura ,  Hisashi Takahashi ,  Rie Miyauchi ,  Toshiyuki Takeda ,  Isao Hayakawa

IPC分类号： A61K314709

CPC分类号： C07D401/04

摘要： This invention provides a quinolone derivative which exerts strong antibacterial action upon various bacteria and has high safety, and it relates to a compound having a structure of formula (I), its salts and hydrates thereof: {R1 and R2: hydrogen, alkyl; n: 1 to 4; Q: following structure (Ia): [R3: alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl, alkylamino; R4: hydrogen, alkylthio; R5: hydrogen, amino, hydroxyl, thiol, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; X1: halogen, hydrogen, A1: nitrogen, structure of formula (II): (X2: hydrogen, amino, halogen, cyano, halogenomethyl, halogenomethyl, alkyl, alkenyl, alkynyl, alkoxyl; R4 and R3 or X2 and R3 may together form a cyclic structure; Y: hydrogen, various ester forming groups]}.

摘要翻译： 本发明提供了一种喹诺酮衍生物，其对各种细菌具有强烈的抗菌作用并具有高度的安全性，它涉及具有式（I）结构的化合物及其盐和水合物：{R1和R2：氢，烷基; n：1到4; Q：以下结构（Ia）：[R3：烷基，烯基，卤代烷基，环烷基，芳基，杂芳基，烷氧基，烷基氨基; R4：氢，烷硫基; R5：氢，氨基，羟基，硫醇，卤代甲基，烷基，烯基，炔基，烷氧基; X1：卤素，氢，A1：氮，式（II）的结构：（X2：氢，氨基，卤素，氰基，卤代甲基，卤代甲基，烷基，烯基，炔基，烷氧基; R4和R3或X2和R3可以一起形成 环状结构; Y：氢，各种酯形成基团]}。