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1. 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]}。

2. 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：

3. 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：

4. 发明授权

US07977327B2 Substituted pyrrolidine derivative 失效
标题翻译：取代的吡咯烷衍生物
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：

5. 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。

6. 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。

7. 发明申请

US20080045520A1 Substituted Pyrrolidine Derivative 失效
标题翻译：取代的吡咯烷衍生物
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。

8. 发明申请

US20070123560A1 Dehalogeno-compounds 有权
标题翻译：脱卤素化合物
公开(公告)号：US20070123560A1
公开(公告)日：2007-05-31
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： A61K31/4745 , A61K31/4709 , C07D471/02 , C07D403/02
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。

9. 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

10. 发明申请

US20090111358A1 Polishing apparatus and polishing method 有权
标题翻译：抛光设备和抛光方法
公开(公告)号：US20090111358A1
公开(公告)日：2009-04-30
申请号：US12289507
申请日：2008-10-29
申请人： Hidetaka Nakao , Eisaku Hayashi , Kunio Oishi , Isao Hayakawa , Yoshiaki Miyake , Yoshikuni Tateyama , Takeshi Ashihara
发明人： Hidetaka Nakao , Eisaku Hayashi , Kunio Oishi , Isao Hayakawa , Yoshiaki Miyake , Yoshikuni Tateyama , Takeshi Ashihara
IPC分类号： B24B49/00 , B24B49/16 , B24B7/20
CPC分类号： B24B37/013 , B24B49/16
摘要： The present invention provides a apparatus for polishing an object material such as a film on a substrate. This apparatus includes a polishing table for holding a polishing pad having a polishing surface, a motor configured to drive the polishing table, a holding mechanism configured to hold a substrate having an object material to be polished and to press the substrate against the polishing surface, a dresser configured to dress the polishing surface, and a monitoring unit configured to monitor a removal amount of the object material. The monitoring unit is operable to calculate the removal amount of the object material using a model equation containing a variable representing an integrated value of a torque current of the motor when polishing the object material and a variable representing a cumulative operating time of the dresser.
摘要翻译：本发明提供一种用于在基板上研磨诸如膜的物体材料的装置。该设备包括：用于保持具有抛光表面的抛光垫的抛光台，构造成驱动抛光台的电机;保持机构，其构造成保持具有待抛光物体的基板，并将基板压靠在抛光表面上; 修整器，其被配置为修整抛光表面;以及监视单元，被配置为监视对象材料的移除量。监视单元可操作以使用包含表示电机的转矩电流的积分值的变量的模型方程来计算物体材料的去除量，以及表示修整器的累积操作时间的变量。

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