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1. 发明申请

US20110166131A1 SUBSTITUTED PYRROLIDINE DERIVATIVE 失效
标题翻译：取代吡咯烷衍生物
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：

2. 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。

3. 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]}。

4. 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。

5. 发明授权

US08455482B2 Substituted pyrrolidine derivative 失效
标题翻译：取代的吡咯烷衍生物
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：

6. 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。

7. 发明申请

US20090253726A1 TRI-, TETRA-SUBSTITUTED-3-AMINOPYRROLIDINE DERIVATIVE 有权
标题翻译：三取代，三取代的3-氨基吡啶衍生物
公开(公告)号：US20090253726A1
公开(公告)日：2009-10-08
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： A61K31/47 , C07D215/00 , A61P31/04
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：

8. 发明申请

US20090012119A1 FLUOROALKYLPYRROLIDINE DERIVATIVE 审中-公开
标题翻译：氟代甲基吡咯烷衍生物
公开(公告)号：US20090012119A1
公开(公告)日：2009-01-08
申请号：US11813950
申请日：2006-01-20
申请人： Hisashi Takahasi , Rie Miyauchi , Makoto Takemura
发明人： Hisashi Takahasi , Rie Miyauchi , Makoto Takemura
IPC分类号： A61K31/4709 , C07D401/02 , A61P3/04
CPC分类号： C07D401/04
摘要： This invention relates to a compound represented by the following formula (1):[F.1] its salt or a hydrate thereof. R1 represents hydrogen atom, an optionally substituted alkyl group containing 1 to 6 carbon atoms, a cycloalkyl group containing 3 to 6 carbon atoms, or a substituted carbonyl group derived from an amino acid, a dipeptide, or a tripeptide; R2 represents hydrogen atom, an optionally substituted alkyl group containing 1 to 6 carbon atoms, or a cycloalkyl group containing 3 to 6 carbon atoms; R3 represents an alkyl group containing 1 to 6 carbon atoms or a halogen-substituted alkyl group containing 1 to 6 carbon atoms; R4 represents a cycloalkyl group containing 3 to 6 carbon atoms or a halogen-substituted cycloalkyl group containing 3 to 6 carbon atoms; R5 represents hydrogen atom, phenyl group, acetoxymethyl group, pivaloyloxymethyl group, ethoxycarbonyl group, choline group, dimethylaminoethyl group, 5-indanyl group, phthalidyl group, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, 3-acetoxy-2-oxobutyl group, or a phenylalkyl group comprising an alkylene group containing 1 to 6 carbon atoms and phenyl group; X1 and X2 independently represent hydrogen atom or a halogen atom; and X represents hydrogen atom or a halogen atom. This compound exhibits broad and strong antibacterial activity to both Gram positive and Gram negative bacteria as well as high safety, and therefore, this compound is useful as a quinolone antibacterial drug, and a prophylactic and/or therapeutic drug for an infectious disease.
摘要翻译：本发明涉及由下式（1）表示的化合物：[F.1]其盐或其水合物。 R1表示氢原子，含有1-6个碳原子的任意取代的烷基，含有3-6个碳原子的环烷基或衍生自氨基酸，二肽或三肽的取代的羰基; R2表示氢原子，可以具有取代基的碳原子数为1〜6的烷基或碳原子数为3〜6的环烷基。 R3表示含有1至6个碳原子的烷基或含有1至6个碳原子的卤素取代的烷基; R 4表示碳原子数3〜6的环烷基或碳原子数3〜6的卤素取代环烷基。 R5表示氢原子，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆碱基，二甲基氨基乙基，5-二氢化茚基，苯酞基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基， 3-乙酰氧基-2-氧代丁基或含有1〜6个碳原子的亚烷基的苯基烷基和苯基; X1和X2独立地表示氢原子或卤原子; X表示氢原子或卤原子。该化合物对革兰氏阳性和革兰氏阴性细菌具有广泛和强的抗菌活性以及高安全性，因此该化合物可用作喹诺酮抗菌药物，以及用于感染性疾病的预防和/或治疗药物。

9. 发明授权

US06656952B2 Cis-substituted fluoromethylpyrrolidine derivative 失效
标题翻译：顺式取代的氟甲基吡咯烷衍生物
公开(公告)号：US06656952B2
公开(公告)日：2003-12-02
申请号：US09446696
申请日：1999-12-23
申请人： Makoto Takemura , Hisashi Takahashi , Hitoshi Ohki , Kenichi Kimura , Rie Miyauchi , Toshiyuki Takeda
发明人： Makoto Takemura , Hisashi Takahashi , Hitoshi Ohki , Kenichi Kimura , Rie Miyauchi , Toshiyuki Takeda
IPC分类号： A61K3147
CPC分类号： C07D401/04
摘要： An antibacterial drug having potent antibacterial activities upon various bacteria including resistant strains and high safety is disclosed, which comprises as an active ingredient, quinolone derivatives represented by the following formula (I), its salts or hydrates thereof: wherein R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R2 represents a halogenomethoxyl group or an alkoxyl group, R3 represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, a heteroaryl group, an alkoxyl group or an alkylamino group, and R4 represents a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxylmethyl group or a phenylalkyl group. These substituents may further have additional substituents.
摘要翻译：本发明公开了一种对各种细菌（包括耐药菌株）和高度安全性具有有效抗菌活性的抗菌药物，其包含作为活性成分的由下式（I）表示的喹诺酮衍生物，其盐或水合物：其中R 1表示氢原子或碳原子数1〜6的烷基，R 2表示卤代甲氧基或烷氧基，R 3表示烷基，链烯基，卤代烷基，环状烷基，杂芳基基团，烷氧基或烷基氨基，R 4表示氢原子，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆碱基，二甲基氨基乙基，5-二氢化茚基， 5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，3-乙酰氧基-2-氧代丁基，烷基，烷氧基甲基或苯基烷基。这些取代基还可以具有另外的取代基。

10. 发明授权

US06384050B1 Tricyclic amine derivatives 失效
标题翻译：三环胺衍生物
公开(公告)号：US06384050B1
公开(公告)日：2002-05-07
申请号：US09284871
申请日：1999-04-22
申请人： Makoto Takemura , Hisashi Takahashi , Kenichi Kimura , Rie Miyauchi , Hitoshi Ohki , Katsuhiro Kawakami
发明人： Makoto Takemura , Hisashi Takahashi , Kenichi Kimura , Rie Miyauchi , Hitoshi Ohki , Katsuhiro Kawakami
IPC分类号： C07D40104
CPC分类号： C07D401/04 , C07D455/02 , C07D471/04 , C07D513/04
摘要： The present invention relates to a compound having a tricyclic amine substituent which may have various substituents, the compound being represented by formula (I), a salt or hydrate thereof, and a hydrate of the salt and a drug containing them as an active ingredient. They exhibit excellent antimicrobial activity against Gram negative bacteria and Gram positive bacteria with a satisfactory fate and safety and are useful in the treatment of infectious diseases. wherein Q preferably represents the following partial structure which may have various substituents:
摘要翻译：本发明涉及可具有各种取代基的三环胺取代基的化合物，该化合物由式（I）表示，其盐或水合物，以及该盐的水合物和含有它们作为有效成分的药物。它们对革兰氏阴性细菌和革兰氏阳性菌表现出优异的抗微生物活性，具有令人满意的命运和安全性，可用于治疗感染性疾病。其中Q优选表示以下可能具有各种取代基的部分结构：

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