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1. 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。

2. 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：

3. 发明授权

US06191129B1 Bicyclic amine derivative 失效
标题翻译：双环胺衍生物
公开(公告)号：US06191129B1
公开(公告)日：2001-02-20
申请号：US09147893
申请日：1999-03-18
申请人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami
发明人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami
IPC分类号： A61K315383
CPC分类号： C07D498/06
摘要： A pyridobenzoxazine derivative having a bicyclic amine derivative as its substituent, represented by the formula (I): exhibiting antimcrobial activity, and useful in treating infectious diseases and preserving food and agricultural products.
摘要翻译：由式（I）表示的具有双环胺衍生物作为取代基的吡啶并苯并恶嗪衍生物：具有抗菌活性，可用于治疗感染性疾病和保存食品和农产品。

4. 发明授权

US07186843B2 Aminomethylpyrrolidine derivatives having aromatic substituents 失效
公开(公告)号：US07186843B2
公开(公告)日：2007-03-06
申请号：US10834079
申请日：2004-04-29
申请人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Toshiyuki Takeda , Rie Miyauchi
发明人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Toshiyuki Takeda , Rie Miyauchi
IPC分类号： C07D207/09 , C07D401/12 , C07D403/12
CPC分类号： C07D401/04 , C07D405/14
摘要： This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atom, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10:hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3:>C═C (—A1═)—N(—R9)—, >N—C (—A1>)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.

5. 发明授权

US07176313B2 Anti acid-fast bacterial agent containing pyridonecarboxylic acids as active ingredient 失效
标题翻译：抗酸抗菌剂含有吡啶酮羧酸作为有效成分
公开(公告)号：US07176313B2
公开(公告)日：2007-02-13
申请号：US10203199
申请日：2001-02-07
申请人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Kenji Namba , Mayumi Tanaka , Rie Miyauchi
发明人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Kenji Namba , Mayumi Tanaka , Rie Miyauchi
IPC分类号： C07D401/04
CPC分类号： A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/4995 , A61K31/5383 , C07D215/56 , C07D401/04 , C07D471/04 , C07D487/08
摘要： An anti acid-fast bacterial agent containing, as an active ingredient, a pyridonecarboxylic acid derivative represented by the following general formula (1), a salt thereof, or a hydrate thereof, which shows excellent antibacterial activity against Mycobacterium tuberculosis and atypical acid-fast bacteria and exhibits good pharmacokinetics and safety
摘要翻译：一种抗酸抗菌剂，其特征在于，含有下列通式（1）表示的吡啶酮羧酸衍生物或其盐或其水合物作为活性成分，其对结核分枝杆菌和非典型抗酸性具有优异的抗菌活性细菌，药代动力学和安全性好

6. 发明授权

US06762181B1 Aminomethylpyrrolidine derivatives having aromatic substituents 失效
标题翻译：具有芳香取代基的氨基甲基吡咯烷衍生物
公开(公告)号：US06762181B1
公开(公告)日：2004-07-13
申请号：US09936050
申请日：2001-09-07
申请人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Toshiyuki Takeda , Rie Miyauchi
发明人： Makoto Takemura , Hisashi Takahashi , Katsuhiro Kawakami , Toshiyuki Takeda , Rie Miyauchi
IPC分类号： A61K314375
CPC分类号： C07D401/04 , C07D405/14
摘要： This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both. In the formula, R2, R3: hydrogen atom, an alkyl group; R4, R5, R6: hydrogen atoms, hydroxyl group, a halogen atom, carbamoyl group, an alkyl group, an alkoxyl group, an alkylthio group; R7, R8: hydrogen atom, an alkyl group; R9: an alkyl group, an alkenyl group, a halogenoalkyl group, a cyclic alkyl group, an aryl group, a heteroaryl group, an alkoxyl group having from 1 to 6 carbon atoms, an alkylamino group; R10: hydrogen atom, an alkylthio group; R11: hydrogen atom, amino group, hydroxyl group, thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; X1: halogen atom, a hydrogen atom; A1: nitrogen atom, C—X2; X2: hydrogen atom, amino group, a halogen atom, cyano group, an halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxyl group; A2, A3: >C═C(—A1═)—N(—R9)—, >N—C(—A1═)═C(—R9)—; R10 and R9 or R9 and X2 may be integrated to form a ring structure; and Y: hydrogen atom, ester forming group.
摘要翻译：本发明提供了一种喹诺酮衍生物，其具有对各种细菌的抗菌活性，包括耐药菌株，其为下式的化合物，其中R 1为任选取代的芳族基团，其两者的盐或两者的水合物。式R 2，R 3：氢原子，烷基; R 4，R 5，R 6：氢原子，羟基，卤素原子，氨基甲酰基，烷基，烷氧基，烷硫基; R 7，R 8：氢原子，烷基; R 9：烷基，烯基，卤代烷基，环状烷基，芳基，杂芳基，碳原子数1〜6的烷氧基，烷基氨基， R 10：氢原子，烷硫基; R 11：氢原子，氨基，羟基，硫醇基，卤代甲基，烷基，烯基，炔基，烷氧基; X 1：卤素原子，氢原子; A 1：氮原子，C-X 2; X 2：氢原子，氨基，卤原子，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基，烷氧基; A 2，A 3：C = C（-A 1 =）-N（-R 9） - ，> NC（-A 1）= C（-R 9） >） - ; R 10和R 9或R 9和X 2可以一体形成环结构; 和Y：氢原子，酯形成基团。

7. 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。

8. 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:

9. 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。

10. 发明授权

US06462040B1 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：US06462040B1
公开(公告)日：2002-10-08
申请号：US09907909
申请日：2001-07-19
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： A61K3153
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：本发明涉及一种具有高安全性的抗微生物化合物，以及对由下式表示的广泛的微生物有效的抗微生物活性：

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