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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。

4. 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。

5. 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。

6. 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：

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

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。

9. 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.

10. 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。

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