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11. 发明授权

US06391889B1 Cis-substituted aminocyclopropane derivatives 有权
公开(公告)号：US06391889B1
公开(公告)日：2002-05-21
申请号：US09214433
申请日：1999-01-06
申请人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Yohhei Ishida
发明人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Yohhei Ishida
IPC分类号： A61K314709
摘要： The present invention is to provide an antimicrobial agent wherein the active ingredient is a compound represented by the following formula, a salt, a hydrate, a hydrate of the salt, or a stereochemically isomeric form thereof: wherein the compound exhibits a potent antimicrobial activity on a broad range of microorganisms.

12. 发明授权

US06184388B2 Substituted aminocycloalkylpyrrolidine derivatives and cis-substituted aminocycloalkylpyrrolidine derivatives 失效
标题翻译：取代的氨基环烷基吡咯烷衍生物和顺式取代的氨基环烷基吡咯烷衍生物
公开(公告)号：US06184388B2
公开(公告)日：2001-02-06
申请号：US09397515
申请日：1999-09-17
申请人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Kenichi Kimura , Satoru Miyauchi , Hitoshi Ohki , Kazuyuki Sugita , Rie Miyauchi
发明人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Kenichi Kimura , Satoru Miyauchi , Hitoshi Ohki , Kazuyuki Sugita , Rie Miyauchi
IPC分类号： C07D20708
CPC分类号： C07D401/04 , C07D207/273 , C07D498/04
摘要： An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof: wherein Q is represented by formula (II) or (IV). Also disclosed is a quinolone derivative where R4 and the substituent on the pyrrolidine ring of the following formula: are located at the cis-configuration; and Q is represented by the formula:
摘要翻译：公开了具有优异的抗微生物活性和高安全性的抗微生物药物，其包含作为活性成分的具有取代的氨基环烷基吡咯烷作为取代基的喹诺酮衍生物，并且还被式（I）表示的各种取代基，其盐和水合物其中Q由式（II）或（IV）表示。还公开了喹诺酮衍生物，其中R4和下式的吡咯烷环上的取代基位于顺式构型; Q由下式表示：

13. 发明授权

US06949662B2 Cis-substituted aminocyclopropane derivative 失效
标题翻译：顺式取代的氨基环丙烷衍生物
公开(公告)号：US06949662B2
公开(公告)日：2005-09-27
申请号：US10107339
申请日：2002-03-28
申请人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Yohhei Ishida
发明人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Yohhei Ishida
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , C07D207/24 , C07D207/26 , C07D401/04 , C07D207/09
CPC分类号： C07D207/26 , A61K31/4375 , A61K31/4709 , C07D207/24 , C07D401/04 , Y02A50/475
摘要： The present invention relates to an antimicrobial compound having high safety as well as potent antimicrobial activity on a broad range of microorganisms represented by the following formula:
摘要翻译：本发明涉及具有高安全性的抗微生物化合物以及对由下列通式表示的广泛的微生物有效的抗微生物活性：

14. 发明授权

US6121285A Substituted aminocycloalkylpyrrolidine derivatives and cis-substituted aminocycloalkylpyrrolidine derivatives 失效
标题翻译：取代的氨基环烷基吡咯烷衍生物和顺式取代的氨基环烷基吡咯烷衍生物
公开(公告)号：US6121285A
公开(公告)日：2000-09-19
申请号：US82155
申请日：1998-05-21
申请人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Kenichi Kimura , Satoru Miyauchi , Hitoshi Ohki , Kazuyuki Sugita , Rie Miyauchi
发明人： Makoto Takemura , Youichi Kimura , Hisashi Takahashi , Kenichi Kimura , Satoru Miyauchi , Hitoshi Ohki , Kazuyuki Sugita , Rie Miyauchi
IPC分类号： C07D207/08 , C07D207/10 , C07D207/46 , C07D215/16 , C07D471/02
CPC分类号： C07D401/04 , C07D207/273 , C07D498/04
摘要： An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone-derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof: ##STR1## wherein Q is represented by formula (II) or (IV). ##STR2## Also disclosed is a quinolone derivative where R.sup.4 and the substituent on the pyrrolidine ring of the following formula: ##STR3## are located at the cis-configuration; and Q is represented by the formula: ##STR4##
摘要翻译：公开了具有优异的抗微生物活性和高安全性的抗微生物药物，其包含作为活性成分的具有取代的氨基环烷基吡咯烷作为取代基的喹诺酮衍生物，并且还被式（I）表示的各种取代基，其盐和其水合物：其中Q由式（II）或（IV）表示。还公开了喹诺酮衍生物，其中R4和下式的吡咯烷环上的取代基位于顺式构型; Q由下式表示：

15. 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。

16. 发明授权

US5696132A Pyridonecarboxylic acid derivatives 失效
标题翻译：吡啶酮羧酸衍生物
公开(公告)号：US5696132A
公开(公告)日：1997-12-09
申请号：US142444
申请日：1994-01-26
申请人： Isao Hayakawa , Youichi Kimura , Hisashi Takahashi
发明人： Isao Hayakawa , Youichi Kimura , Hisashi Takahashi
IPC分类号： A61K31/435 , A61K31/4375 , A61K31/47 , A61K31/4709 , A61K31/4995 , A61K31/55 , A61P31/00 , A61P31/04 , C07D215/56 , C07D401/04 , C07D471/04 , C07D487/04 , C07D487/08 , C07D519/00 , A61K31/50 , C07D215/233 , C07D241/04
CPC分类号： C07D487/04 , C07D215/56 , C07D401/04 , C07D471/04 , Y02P20/55
摘要： Quinolone derivatives are known as synthetic antimicrobial agents having a condensed pyridonecarboxylic acid skeleton, and those having substituents on various replaceable positions of said skeleton are known. In particular, if diastereomers exist, there are 4 or more kinds of stereoisomers. A mixture of diastereomers is a mixture of isomers having different physical properties and is difficult to apply as a drug as such. The present invention provides an antimicrobial 1-(1,2-cis-2-fluorocyclopropyl)-substituted quinolone derivative represented by formula I shown below which, although involving diastereomers, consists of a single stereoisomer. ##STR1## wherein R.sup.1 represents a methyl group, a difluoromethyl group, etc.; R.sup.2 represents a saturated nitrogen-containing heterocyclic group; A represents C--X.sup.3 or a nitrogen atom; X.sup.1 and X.sup.2 each represents a halogen atom; and X.sup.3 and Z represent a hydrogen atom, etc.
摘要翻译： PCT No.PCT / JP92 / 00687 Sec。 371日期1994年1月26日 102（e）日期1994年1月26日PCT提交1992年5月27日PCT公布。第WO92 / 21659号公报日期：1992年10月12日喹诺酮衍生物被称为具有缩合吡啶酮羧酸骨架的合成抗微生物剂，并且在所述骨架的各种可替换位置具有取代基的那些是已知的。特别是，如果存在非对映异构体，则有4种以上的立体异构体。非对映体的混合物是具有不同物理性质的异构体的混合物，并且难以作为药物应用。本发明提供了下述式I表示的抗微生物1-（1,2-顺式-2-氟环丙基） - 取代喹诺酮衍生物，尽管涉及非对映异构体，但由单一立体异构体组成。（I）其中R1表示甲基，二氟甲基等; R2表示饱和含氮杂环基; A表示C-X3或氮原子; X1和X2各自表示卤素原子; X3和Z表示氢原子等

17. 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]}。

18. 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。

19. 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.

20. 发明授权

US07902226B2 Dehalogeno-compounds 有权
标题翻译：脱卤素化合物
公开(公告)号：US07902226B2
公开(公告)日：2011-03-08
申请号：US11644901
申请日：2006-12-26
申请人： Hisashi Takahashi , Rie Miyauchi , Masao Itoh , Makoto Takemura , Isao Hayakawa
发明人： Hisashi Takahashi , Rie Miyauchi , Masao Itoh , Makoto Takemura , Isao Hayakawa
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D401/04 , C07D471/04
摘要： 3-(1-Aminocycloalkyl)pyrrolidinyl-substituted-6-dehalodeno(hydrogen-substituted)quinolon carboxylic acid derivatives having specific substituents as represented by the following formula (I), its salts, and hydrates thereof exhibit a broad and potent antibacterial activity on gram-negative and gram-positive bacteria, in particular, resistant bacteria typified by gram-positive cocci, including MRSA, PRSP and VRE. Thus these compounds are usable as drugs.
摘要翻译：由下式（I）表示的具有特定取代基的3-（1-氨基环烷基）吡咯烷基 - 取代-6-脱卤素（氢取代）喹诺酮羧酸衍生物，其盐和水合物，表现出广泛有效的抗菌活性革兰氏阴性和革兰氏阳性菌，特别是以革兰氏阳性球菌为代表的抗性细菌，包括MRSA，PRSP和VRE。因此，这些化合物可用作药物。

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