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1. 发明授权

US5849757A Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials 失效
标题翻译：被双环氨基取代的吡啶酮羧酸衍生物作为抗菌剂
公开(公告)号：US5849757A
公开(公告)日：1998-12-15
申请号：US875678
申请日：1997-08-04
申请人： Makoto Takemura , Youichi Kimura , Katsuhiro Kawakami , Kenichi Kimura , Hitoshi Ohki , Norikazu Matsuhashi , Haruko Kawato
发明人： Makoto Takemura , Youichi Kimura , Katsuhiro Kawakami , Kenichi Kimura , Hitoshi Ohki , Norikazu Matsuhashi , Haruko Kawato
IPC分类号： C07D401/04 , A61K31/435 , A61K31/47 , C07D471/04
CPC分类号： C07D401/04
摘要： This invention relates to a N.sub.1 -(halogenocyclopropyl)-substituted pyridonecarboxylic acid derivative represented by the following formula (I): ##STR1## wherein X.sup.1 is a halogen atom or a hydrogen atom; X.sup.2 is a halogen atom; R.sup.1 is a hydrogen atom, a hydroxyl group, a thiol group, a halogenomethyl group, an amino group, an alkyl group or an alkoxy group which may have a substituent group; R.sup.2 is a group represented by the following formula (II): ##STR2## wherein R.sup.3 and R.sup.4 are independently a hydrogen atom or an alkyl group and n is an integer of 1 or 2; A is a nitrogen atom or a partial structure of the following formula (III): ##STR3## wherein X.sup.3 is a hydrogen atom, a halogen atom, a cyano group, an amino group, an alkyl group, a halogenomethyl group, an alkoxyl group or a halogenomethoxyl group which may have a substituent group; and R is 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 phthalidynyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxymethyl group or a phenylalkyl group, and provides a heterocyclic compound useful as antibacterial drugs.
摘要翻译： PCT No.PCT / JP96 / 00208 Sec。 371日期：1997年8月4日 102（e）日期1997年8月4日PCT PCT 1996年2月1日PCT公布。公开号WO96 / 23782 日本特开2006年8月8日本发明涉及由下式（I）表示的N1-（卤代环丙基） - 取代吡啶酮羧酸衍生物：其中X 1为卤原子或氢原子; X2是卤原子; R1是可以具有取代基的氢原子，羟基，硫醇基，卤代甲基，氨基，烷基或烷氧基; R2是由下式（II）表示的基团：其中R3和R4独立地是氢原子或烷基，n是1或2的整数; A是氮原子或下式（III）的部分结构：可以具有取代基的卤素原子，氰基，氨基，烷基，卤代甲基，烷氧基或卤代甲氧基 ; R为氢原子，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，邻苯二甲酰炔基，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，提供可用作抗菌药物的杂环化合物。

2. 发明授权

US06194434B1 Cycloalkylaminomethylpyrrolidine derivatives 失效
标题翻译：环烷基氨基甲基吡咯烷衍生物
公开(公告)号：US06194434B1
公开(公告)日：2001-02-27
申请号：US09171637
申请日：1998-10-22
申请人： Makoto Takemura , Youichi Kimura , Katsuhiro Kawakami , Hitoshi Ohki
发明人： Makoto Takemura , Youichi Kimura , Katsuhiro Kawakami , Hitoshi Ohki
IPC分类号： A61K3147
CPC分类号： C07D401/04
摘要： A quinolone derivative represented by formula (I): wherein R1 represents a cycloalkyl group; R2 represents a hydrogen atom, an amino group, a hydroxyl group, a thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, or an alkoxyl group; R3 represents an amino group, a halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, or an alkoxyl group; R4 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R5 represents a cycloalkyl group having 3 to 6 carbon atoms; the above R1 to R5 may be substituted; X represents a halogen atom or a hydrogen atom; and Y 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, a 3-acetoxy-2-oxobutyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxymethyl group having 2 to 7 carbon atoms, or a phenylalkyl group having 1 to 6 carbon atoms in the alkyl moiety thereof, or a salt thereof. The compound exhibits high and broad antimicrobial activity against various bacteria including bacteria resistant to drugs and high safety.
摘要翻译：由式（I）表示的喹诺酮衍生物：其中R1表示环烷基; R2表示氢原子，氨基，羟基，硫醇基，卤代甲基，烷基，烯基，炔基或烷氧基; R3表示氨基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; R4表示氢原子或碳原子数1〜6的烷基。 R5表示碳原子数3〜6的环烷基; 上述R 1〜R 5可以被取代; X表示卤素原子或氢原子; Y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，碳原子数1〜6的烷基，碳原子数2〜7的烷氧基甲基或碳原子数1〜6的苯基烷基其烷基部分的原子，或其盐。该化合物对各种细菌（包括对药物有抗性的细菌和高安全性）具有高而广的抗菌活性。

3. 发明授权

US06586604B2 Tricyclic amine derivatives 失效
公开(公告)号：US06586604B2
公开(公告)日：2003-07-01
申请号：US09875852
申请日：2001-06-08
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:

4. 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：

5. 发明授权

US06469023B1 Heterocyclic spiro-derivative 失效
标题翻译：杂环螺衍生物
公开(公告)号：US06469023B1
公开(公告)日：2002-10-22
申请号：US08875863
申请日：1997-08-07
申请人： Makoto Takemura , Youichi Kimura , Hitoshi Ohki
发明人： Makoto Takemura , Youichi Kimura , Hitoshi Ohki
IPC分类号： A61K3144
CPC分类号： C07D401/04
摘要： The present invention provides an antibacterial compound useful as medicines, animal drugs, fisheries drugs or antibacterial preservatives and to an antibacterial agent or preparation which contains the same, more particularly a compound which possesses high safety and excellent activity against a broad range of bacterial species including quinolone-resistant strains. A quinolone derivative of the following formula (I) which has a group derived from the heterocyclic spiro-compound at the 7-positioned R2 and the halogenocyclopropyl group at the N1-position, prefereably a compound of pure isomer, and an antibacterial agent containing the derivative compound.
摘要翻译：本发明提供了可用作药物，动物药物，渔业药物或抗菌防腐剂的抗菌化合物，以及含有该抗菌剂或抗菌剂的抗菌剂或制剂，更具体地，涉及对广泛的细菌种类具有高安全性和优异活性的化合物，包括喹诺酮耐药株。下述式（I）的喹啉酮衍生物，其具有衍生自7-位R2上的杂环螺环化合物和N1位上的卤代环丙基的基团，优选纯异构体的化合物和含有衍生化合物。

6. 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：

7. 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：

8. 发明申请

US20050113397A1 Imidazo[1,2-a]pyridine derivative 审中-公开
标题翻译：咪唑并[1,2-a]吡啶衍生物
公开(公告)号：US20050113397A1
公开(公告)日：2005-05-26
申请号：US10502971
申请日：2003-01-30
申请人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Hiroshi Takeshita , Youichi Kimura , Jun Watanabe , Yuichi Sugimoto , Akihiro Kitamura , Ryohei Nakajima , Kazuo Kanai , Tetsunori Fujisawa
发明人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Hiroshi Takeshita , Youichi Kimura , Jun Watanabe , Yuichi Sugimoto , Akihiro Kitamura , Ryohei Nakajima , Kazuo Kanai , Tetsunori Fujisawa
IPC分类号： A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/541 , A61P31/00 , A61P31/10 , C07D471/04 , C07D471/14 , C07D491/14 , C07D519/00 , A61K31/4745 , A61K31/519 , C07D487/14
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D471/14 , C07D491/14
摘要： A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.
摘要翻译：基于其1,6-β-葡聚糖合成抑制的新机理，通过下式（I）表示的化合物，其能够在宽谱中特异性或选择性表达抗真菌活性的盐或其溶剂化物，以及抗真菌剂包含它们中的任何一个。

9. 发明申请

US20070191356A1 Pyridobenzoxazine derivative 审中-公开
标题翻译：吡啶并苯并恶嗪衍生物
公开(公告)号：US20070191356A1
公开(公告)日：2007-08-16
申请号：US10587946
申请日：2005-02-01
申请人： Makoto Takemura , Hitoshi Ohki
发明人： Makoto Takemura , Hitoshi Ohki
IPC分类号： A61K31/535 , C07D265/38
CPC分类号： C07D498/06 , A23K20/111 , A23K20/195 , A23K50/80 , A23L3/3544 , A61K31/5383
摘要： A quinolone antimicrobial agent having potent antimicrobial activity against gram positive and gram negative bacteria and having high safety is provided. A compound represented by the following formula (1): [Chemical formula 1] [wherein, R1: hydrogen, alkyl, cycloalkyl, or substituted carbonyl derived from amino acid, peptide or tripeptide; R2: hydrogen, alkyl, or cycloalkyl; R3: hydrogen, amino, halogen, or alkyl; R4: hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, choline, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl, or phenylalkyl; X, X1, X2: hydrogen or halogen] or salt thereof, or a hydrate thereof; and antimicrobial agent and therapeutic agent for infections, each containing the compound, salt thereof or a hydrate thereof.
摘要翻译：提供了对革兰氏阳性和革兰氏阴性细菌具有强抗微生物活性并具有高安全性的喹诺酮类抗微生物剂。由下式（1）表示的化合物：[化学式1] [其中，R 1，H 2，氢，烷基，环烷基或衍生自氨基酸，肽或三肽的取代的羰基; R 2：氢，烷基或环烷基; 氢，氨基，卤素或烷基; 吡啶，二甲基氨基乙基，5-茚满基，邻苯二甲酰基，5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，3-甲氧基羰基，乙酰氧基-2-氧代丁基，烷基，烷氧基甲基或苯基烷基; X，X 1，X 2：氢或卤素]或其盐或其水合物; 和抗微生物剂和感染治疗剂，各自含有化合物，其盐或其水合物。

10. 发明授权

US06900225B2 Quinolonecarboxylic acid derivative 失效
标题翻译：喹诺酮羧酸衍生物
公开(公告)号：US06900225B2
公开(公告)日：2005-05-31
申请号：US10275972
申请日：2001-03-30
申请人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Masao Itoh , Tetsuya Suzuki , Tsuyoshi Ohtani , Masayasu Sekiguchi , Rie Miyauchi , Isao Hayakawa
发明人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Masao Itoh , Tetsuya Suzuki , Tsuyoshi Ohtani , Masayasu Sekiguchi , Rie Miyauchi , Isao Hayakawa
IPC分类号： A61K31/4709 , A61P31/04 , C07D401/04 , C07D401/02
CPC分类号： C07D401/04 , A61K31/4709
摘要： (−)-7-[(7S)-7-Amino-5-azaspiro[2.4]heptan-5-yl]-6-fluoro-1-[(1R, 2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid.1HCl.1H2O and antibacterial compositions containing this compound. The compound of the present invention exhibits not only excellent antibacterial activity and safety, but also remarkable stability against light and humidity, and is thus useful as an antibacterial agent.
摘要翻译：（ - ） - 7 - [（7S）-7-氨基-5-氮杂螺[2.4]庚-5-基] -6-氟-1 - [（1R，2S）-2-氟-1-环丙基] 1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸1 HCl.1H 2 O和含有该化合物的抗菌组合物。本发明的化合物不仅表现出优异的抗菌活性和安全性，而且对光和湿度具有显着的稳定性，因此可用作抗菌剂。

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