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1. 发明申请

US20100197909A1 MUTILIN DERIVATIVE HAVING HETEROCYCLIC AROMATIC RING CARBOXYLIC ACID STRUCTURE IN SUBTITUENT AT 14-POSITION 失效
标题翻译：具有14位位置杂环芳烃环羧基结构的MUTILIN衍生物
公开(公告)号：US20100197909A1
公开(公告)日：2010-08-05
申请号：US12451656
申请日：2008-05-23
申请人： Yasumichi Fukuda , Masanori Takadoi , Yoshikazu Asahina , Taro Sato , Haruaki Kurasaki , Hiroyuki Ebisu , Masaya Takei , Hideyuki Fukuda
发明人： Yasumichi Fukuda , Masanori Takadoi , Yoshikazu Asahina , Taro Sato , Haruaki Kurasaki , Hiroyuki Ebisu , Masaya Takei , Hideyuki Fukuda
IPC分类号： C07D498/04 , C07D413/14 , C07D471/04 , C07D401/10
CPC分类号： C07D401/04 , C07D451/04 , C07D471/04 , C07D498/06
摘要： To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.
摘要翻译：为了提供一种在14位具有取代的新颖的mutilin衍生物，其是对革兰氏阳性菌和革兰氏阴性菌（包括各种耐药性细菌）展现出有力和广泛的抗微生物作用的新型突变体类似物，可用作治疗感染性疾病的药剂。由以下通式（1）表示的mutilin衍生物：或其药学上可接受的加成盐。

2. 发明申请

US20060281779A1 7-(4-Substituted-3-cyclopropylaminomethyl-1 pyrrolidinyl) quinolonecarboxylic acid derivative 有权
标题翻译： 7-（4-取代-3-环丙基氨基甲基-1-吡咯烷基）喹啉酮羧酸衍生物
公开(公告)号：US20060281779A1
公开(公告)日：2006-12-14
申请号：US10569062
申请日：2004-09-08
申请人： Yoshikazu Asahina , Masaya Takei
发明人： Yoshikazu Asahina , Masaya Takei
IPC分类号： A61K31/4745 , A61K31/4709 , C07D471/02 , C07D403/02
CPC分类号： C07D471/04 , C07D401/04
摘要： OBJECT To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. SOLVING MEANS There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe. The compounds are shown by the following general formula (I):
摘要翻译：目的提供新的喹诺酮羧酸化合物，其作为对抗常规抗菌剂较不敏感的耐药性细菌有效的安全，强力的抗菌剂。解决办法提供7-（4-取代-3-环丙基氨基甲基吡咯烷基）喹啉酮羧酸衍生物（如1-环丙基-7 - [（3S，4S）-3-环丙基氨基甲基-4-氟-1-吡咯烷基] -6- 氟代-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸），其在安全的情况下对革兰氏阳性菌如MRSA，PRSP和VRE具有强的抗菌活性。该化合物由以下通式（I）表示：

3. 发明授权

US08106072B2 7- (4-substituted-3-cyclopropylaminomethyl-1-pyrrolidinyl) quinolonecarboxylic acid derivative 有权
标题翻译： 7-（4-取代-3-环丙基氨基甲基-1-吡咯烷基）喹啉酮羧酸衍生物
公开(公告)号：US08106072B2
公开(公告)日：2012-01-31
申请号：US12379699
申请日：2009-02-26
申请人： Yoshikazu Asahina , Masaya Takei
发明人： Yoshikazu Asahina , Masaya Takei
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D471/04 , C07D401/04
摘要： ObjectTo provide novel quinolinecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents.Solving MeansThere are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe. The compounds are shown by the following general formula (I):
摘要翻译：目的提供新颖的喹啉羧酸化合物，其作为对抗常规抗菌剂较不敏感的耐药细菌有效的安全，强力的抗菌剂。解决方法提供7-（4-取代-3-环丙基氨基甲基吡咯烷基）喹啉酮羧酸衍生物（如1-环丙基-7 - [（3S，4S）-3-环丙基氨基甲基-4-氟-1-吡咯烷基] -6- 氟代-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸），其在安全的情况下对革兰氏阳性菌如MRSA，PRSP和VRE具有强的抗菌活性。该化合物由以下通式（I）表示：

4. 发明申请

US20090176824A1 7- (4-substituted-3-cyclopropylaminomethyl-1-pyrrolidinyl) quinolonecarboxylic acid derivative technical field 有权
标题翻译： 7-（4-取代-3-环丙基氨基甲基-1-吡咯烷基）喹啉酮羧酸衍生物技术领域
公开(公告)号：US20090176824A1
公开(公告)日：2009-07-09
申请号：US12379699
申请日：2009-02-26
申请人： Yoshikazu Asahina , Masaya Takei
发明人： Yoshikazu Asahina , Masaya Takei
IPC分类号： A61K31/4375 , A61K31/4709 , C07D471/02 , C07D401/02
CPC分类号： C07D471/04 , C07D401/04
摘要： Object To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents. Solving Means There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe. The compounds are shown by the following general formula (I):
摘要翻译：目的提供新的喹诺酮羧酸化合物，其作为对抗常规抗菌剂较不敏感的耐药细菌有效的安全，强力的抗菌剂。解决方法提供7-（4-取代-3-环丙基氨基甲基吡咯烷基）喹啉酮羧酸衍生物（如1-环丙基-7 - [（3S，4S）-3-环丙基氨基甲基-4-氟-1-吡咯烷基] -6- 氟代-1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸），其在安全的情况下对革兰氏阳性菌如MRSA，PRSP和VRE具有强的抗菌活性。该化合物由以下通式（I）表示：

5. 发明申请

US20050182052A1 10-(3-cyclopropylaminomethyl-1-pyrrolidinyl)pyridobenzoxazinecarboxylic acid derivative effective against resistant bacterium 有权
标题翻译：对抗细菌有效的10-（3-环丙基氨基甲基-1-吡咯烷基）吡啶并苯并恶嗪甲酸衍生物
公开(公告)号：US20050182052A1
公开(公告)日：2005-08-18
申请号：US10508154
申请日：2003-03-13
申请人： Yoshikazu Asahina , Masaya Takei
发明人： Yoshikazu Asahina , Masaya Takei
IPC分类号： A61P31/04 , C07D498/06 , A61K31/538 , C07D491/14
CPC分类号： C07D498/06
摘要： A compound as represented by the general formula (I) shown below exhibits high antibacterial activity against gram-positive bacteria, in particular, such drug-resistant bacteria as mRNA, PRSP and VRE: wherein R1 is a methyl group, a fluoromethyl group, a methoxymethyl group, an acetoxymethyl group, a hydroxymethyl group or a methylene; R2 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable cation and an ester of a prodrug; R3 is a hydrogen atom or a halogen atom; R4 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, a fluoromethyl group, a trifluoromethyl group or a fluorine atom; and R5 is a hydrogen atom or a fluorine atom, with exceptions where R1 is a methyl group, R4 and R5 are at the same time a hydrogen atom, and R3 is a fluorine atom.
摘要翻译：由下述通式（I）表示的化合物对革兰氏阳性细菌，特别是耐药细菌如mRNA，PRSP和VRE具有高抗菌活性：其中R1是甲基，氟甲基，甲氧基甲基，乙酰氧基甲基，羟甲基或亚甲基; R2是氢原子，具有1至3个碳原子的低级烷基，或药学上可接受的阳离子和前药的酯; R3是氢原子或卤素原子; R4是氢原子，碳原子数1〜3的低级烷基，氟甲基，三氟甲基或氟原子。并且R 5为氢原子或氟原子，除了R 1为甲基外，R 4和R 5同时为氢原子，且R 3为氟原子。

6. 发明授权

US07153851B2 10-(3-cyclopropylaminomethyl-1-pyrrolidinyl)pyridobenzoxazinecarboxylic acid derivative effective against resistant bacterium 有权
标题翻译：对抗细菌有效的10-（3-环丙基氨基甲基-1-吡咯烷基）吡啶并苯并恶嗪甲酸衍生物
公开(公告)号：US07153851B2
公开(公告)日：2006-12-26
申请号：US10508154
申请日：2003-03-13
申请人： Yoshikazu Asahina , Masaya Takei
发明人： Yoshikazu Asahina , Masaya Takei
IPC分类号： C07D498/06 , A61K31/5383 , A61P31/04
CPC分类号： C07D498/06
摘要： A compound as represented by the general formula (I) shown below exhibits high antibacterial activity against gram-positive bacteria, in particular, such drug-resistant bacteria as mRNA, PRSP and VRE: wherein R1 is a methyl group, a fluoromethyl group, a methoxymethyl group, an acetoxymethyl group, a hydroxymethyl group or a methylene; R2 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, or a pharmaceutically acceptable cation and an ester of a prodrug; R3 is a hydrogen atom or a halogen atom; R4 is a hydrogen atom, a lower alkyl group having 1 to 3 carbon atoms, a fluoromethyl group, a trifluoromethyl group or a fluorine atom; and R5 is a hydrogen atom or a fluorine atom, with exceptions where R1 is a methyl group, R4 and R5 are at the same time a hydrogen atom, and R3 is a fluorine atom.
摘要翻译：由下述通式（I）表示的化合物对革兰氏阳性细菌，特别是耐药细菌如mRNA，PRSP和VRE具有高抗菌活性：其中R1是甲基，氟甲基，甲氧基甲基，乙酰氧基甲基，羟甲基或亚甲基; R2是氢原子，具有1至3个碳原子的低级烷基，或药学上可接受的阳离子和前药的酯; R3是氢原子或卤素原子; R4是氢原子，碳原子数1〜3的低级烷基，氟甲基，三氟甲基或氟原子。并且R 5为氢原子或氟原子，除了R 1为甲基外，R 4和R 5同时为氢原子，且R 3为氟原子。

7. 发明授权

US08222407B2 Mutilin derivative having heterocyclic aromatic ring carboxylic acid structure in substituent at 14-position 失效
标题翻译：在14位的取代基中具有杂环芳环羧酸结构的Mutilin衍生物
公开(公告)号：US08222407B2
公开(公告)日：2012-07-17
申请号：US12451656
申请日：2008-05-23
申请人： Yasumichi Fukuda , Masanori Takadoi , Yoshikazu Asahina , Taro Sato , Haruaki Kurasaki , Hiroyuki Ebisu , Masaya Takei , Hideyuki Fukuda
发明人： Yasumichi Fukuda , Masanori Takadoi , Yoshikazu Asahina , Taro Sato , Haruaki Kurasaki , Hiroyuki Ebisu , Masaya Takei , Hideyuki Fukuda
IPC分类号： C07D498/04 , C07D401/10 , C07D413/14 , C07D471/04
CPC分类号： C07D401/04 , C07D451/04 , C07D471/04 , C07D498/06
摘要： To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.
摘要翻译：为了提供一种在14位具有取代的新颖的mutilin衍生物，其是对革兰氏阳性菌和革兰氏阴性菌（包括各种耐药性细菌）展现出有力和广泛的抗微生物作用的新型突变体类似物，可用作治疗感染性疾病的药剂。由以下通式（1）表示的mutilin衍生物：或其药学上可接受的加成盐。

8. 发明授权

US07514451B2 7-(4-Substituted-3-cyclopropylaminomethyl-1 pyrrolidinyl) quinolonecarboxylic acid derivative 有权
标题翻译： 7-（4-取代-3-环丙基氨基甲基-1-吡咯烷基）喹啉酮羧酸衍生物
公开(公告)号：US07514451B2
公开(公告)日：2009-04-07
申请号：US10569062
申请日：2004-09-08
申请人： Yoshikazu Asahina , Masaya Takei
发明人： Yoshikazu Asahina , Masaya Takei
IPC分类号： C07D471/02 , C07D215/38 , A61K31/44 , A61K31/47
CPC分类号： C07D471/04 , C07D401/04
摘要： To provide novel quinolonecarboxylic acid compounds serving as safe, strong antibacterial agents that are effective against drug-resistant bacteria that are less susceptible to conventional antibacterial agents.There are provided 7-(4-substituted-3-cyclopropylaminomethylpyrrolidinyl)quinolonecarboxylic acid derivatives (such as 1-cyclopropyl-7-[(3S,4S)-3-cyclopropylaminomethyl-4-fluoro-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid) that exhibit strong antibacterial activity against gram-positive bacteria, such as MRSA, PRSP and VRE, while being safe. The compounds are shown by the following general formula (I):
摘要翻译：提供新的喹诺酮羧酸化合物，其作为对抗常规抗菌剂较不敏感的耐药细菌有效的安全，强力的抗菌剂。提供7-（4-取代-3-环丙基氨基甲基吡咯烷基）喹啉酮羧酸衍生物（如1-环丙基-7 - [（3S，4S）-3-环丙基氨基甲基-4-氟-1-吡咯烷基] -6-氟 - 1,4-二氢-8-甲氧基-4-氧代-3-喹啉羧酸），其对于革兰氏阳性菌如MRSA，PRSP和VRE具有强的抗菌活性，同时安全。该化合物由以下通式（I）表示：

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