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1. 发明授权

US08476429B2 Tri-, tetra-substituted-3-aminopyrrolidine derivative 有权
标题翻译：三取代的3-氨基吡咯烷衍生物
公开(公告)号：US08476429B2
公开(公告)日：2013-07-02
申请号：US13455486
申请日：2012-04-25
申请人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
发明人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
IPC分类号： A61K31/47 , C07D215/00
CPC分类号： C07D207/14 , Y02P20/55
摘要： An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.
摘要翻译：用于生产喹诺酮合成抗菌剂的中间体和用于感染的治疗剂，其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性。

2. 发明授权

US08618094B2 Fused substituted aminopyrrolidine derivative 有权
标题翻译：熔融取代氨基吡咯烷衍生物
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。

3. 发明申请

US20130029977A9 Fused substituted aminopyrrolidine derivative 有权
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.

4. 发明授权

US07563805B2 Tri-, tetra-substituted-3-aminopyrrolidine derivative 有权
标题翻译：三取代的3-氨基吡咯烷衍生物
公开(公告)号：US07563805B2
公开(公告)日：2009-07-21
申请号：US11413153
申请日：2006-04-28
申请人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
发明人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00
CPC分类号： C07D207/14 , Y02P20/55
摘要： A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):
摘要翻译：提供喹诺酮合成抗菌剂和用于感染的治疗剂，其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性，并且也是高度安全的。所提供的化合物由下式（I）表示：其中R1和R2表示氢原子等; R3表示含有1〜6个碳原子的烷基等; R4和R5独立地表示氢原子，含有1至6个碳原子的烷基等，条件是R4和R5不同时表示氢原子; 取代基R 4和R 5一起表示（a）包含由R 4和R 5共有的碳原子与吡咯烷环形成螺环结构的3至6元环状结构; R6和R7独立地表示氢原子，含有1至6个碳原子的烷基等; R8表示含有1〜6个碳原子的卤素取代的烷基等; X1表示氢原子或卤素原子; A表示氮原子或由式（II）表示的部分：

5. 发明授权

US08211910B2 Tri-, tetra-substituted-3-aminopyrrolidine derivative 有权
标题翻译：三取代的3-氨基吡咯烷衍生物
公开(公告)号：US08211910B2
公开(公告)日：2012-07-03
申请号：US12422726
申请日：2009-04-13
申请人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
发明人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
IPC分类号： A01N43/42 , A61K31/47 , C07D215/00
CPC分类号： C07D207/14 , Y02P20/55
摘要： A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by formula (I):
摘要翻译：提供喹诺酮合成抗菌剂和用于感染的治疗剂，其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性，并且也是高度安全的。所提供的化合物由式（I）表示：

6. 发明申请

US20120108582A1 Fused substituted aminopyrrolidine derivative 有权
标题翻译：熔融取代氨基吡咯烷衍生物
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。

7. 发明申请

US20060264428A1 Tri-, tetra-substituted-3-aminopyrrolidine derivative 有权
标题翻译：三取代的3-氨基吡咯烷衍生物
公开(公告)号：US20060264428A1
公开(公告)日：2006-11-23
申请号：US11413153
申请日：2006-04-28
申请人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
发明人： Hisashi Takahashi , Hiroaki Inagaki , Satoshi Komoriya , Makoto Takemura , Rie Miyauchi
IPC分类号： A61K31/538 , A61K31/4745 , A61K31/4709 , C07D491/14 , C07D471/02 , C07D403/02
CPC分类号： C07D207/14 , Y02P20/55
摘要： A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):
摘要翻译：提供喹诺酮合成抗菌剂和用于感染的治疗剂，其对革兰氏阳性和革兰氏阴性细菌都具有广谱和强抗菌活性，并且也是高度安全的。所提供的化合物由下式（I）表示：其中R 1和R 2代表氢原子等; R 3表示含有1至6个碳原子的烷基等; R 4和R 5独立地表示氢原子，含有1至6个碳原子的烷基等，条件是R 4 O >和R 5不同时表示氢原子; 或取代基R 4和R 5一起表示（a）包含由R 4共享的碳原子的3至6元环结构和R 5与吡咯烷环形成螺环结构; R 6和R 7独立地表示氢原子，含有1至6个碳原子的烷基等; R 8表示含有1至6个碳原子的卤素取代的烷基等; X 1表示氢原子或卤素原子; A表示氮原子或由式（II）表示的部分：

8. 发明申请

US20090270637A1 PROCESS FOR PREPARATION OF TETRASUBSTITUTED 5-AZASPIRO[2.4]- HEPTANE DERIVATIVES AND OPTICALLY ACTIVE INTERMEDIATES THEREOF 失效
标题翻译：四唑衍生物的制备方法[2.4] - 丙氨酸衍生物及其光学活性中间体
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。

9. 发明授权

US07842818B2 Process for preparation of tetrasubstituted 5-azaspiro[2.4]- heptane derivatives and optically active intermediates thereof 失效
标题翻译：制备四取代的5-氮杂螺[2.4] - 庚烷衍生物及其光学活性中间体的方法
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。

10. 发明授权

US06573260B1 Cycloalkyl-substituted aminomethylpyrrolidine derivatives 失效
标题翻译：环烷基取代的氨基甲基吡咯烷衍生物
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]}。

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