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1. 发明公开

EP0924213A4 PYRIDOBENZOXAZINE DERIVATIVES 失效
标题翻译： PYRIDOBENZOXAZINDERIVATE
公开(公告)号：EP0924213A4
公开(公告)日：2002-10-23
申请号：EP97941258
申请日：1997-09-26
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , TAKAHASHI HISASHI , KAWAKAMI KATSUHIRO
IPC分类号： C07D498/06 , A61K31/535 , C07D498/04
CPC分类号： C07D498/06
摘要： Derivatives having potent antibacterial activities on gram-negative and gram-positive bacteria and, at the same time, favorable dynamics in vivo and a high safety; and excellent drugs. Compounds represented by general formula (I) and salts thereof, hydrates thereof, and antibacterial agents containing the same as the active ingredient. In said formula, R1 represents hydrogen or C¿1-6? alkyl optionally having substituent(s) selected from the group consisting of hydroxy, halogeno, C1-6 alkylthio and C1-6 alkoxy; R?2¿ represents hydrogen or amino optionally having one or two substituents selected from the group consisting of formyl, C¿1-6? alkyl and C2-6 acyl; and R?3¿ represents hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, etoxycarbonyl, cholin, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, C¿1-6? alkyl, C2-7 alkoxymethyl, or phenylalkyl composed of C1-6 alkylene and phenyl.
摘要翻译：对革兰氏阴性和革兰氏阳性细菌具有强效抗菌活性的衍生物，同时具有良好的体内动力学和高安全性; 和优秀的药物。通式（I）表示的化合物及其盐，其水合物和含有它们作为活性成分的抗菌剂。在所述式中，R1代表氢或C1-6- 任选具有选自羟基，卤代，C 1-6烷硫基和C 1-6烷氧基的取代基的烷基; R 2'代表氢或任选具有一个或两个选自甲酰基，C 1-6 - 烷基和C 2-6酰基; 苯基，乙酰氧基甲基，新戊酰氧基甲基，乙酰氧基羰基，胆碱，二甲基氨基乙基，5-茚满基，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，C 1-6 - 烷基，C 2-7烷氧基甲基或由C 1-6亚烷基和苯基组成的苯基烷基。

2. 发明公开

EP1262477A4 ANTI-ACID-FAST BACTERIAL AGENTS CONTAINING PYRIDONECARBOXYLIC ACIDS AS THE ACTIVE INGREDIENT 有权
标题翻译：对酸耐药菌有效的抗菌剂吡啶羧酸作为有效成分CONTAIN
公开(公告)号：EP1262477A4
公开(公告)日：2003-07-02
申请号：EP01904335
申请日：2001-02-07
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , TAKAHASHI HISASHI , KAWAKAMI KATSUHIRO , NAMBA KENJI , TANAKA MAYUMI , MIYAUCHI RIE
IPC分类号： A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/4995 , A61K31/5383 , A61P31/04 , A61P31/08 , C07D215/56 , C07D401/04 , C07D471/04 , C07D487/08 , C07D498/06 , C07D519/00 , A61P31/06 , C07D453/02
CPC分类号： A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/4995 , A61K31/5383 , C07D215/56 , C07D401/04 , C07D471/04 , C07D487/08
摘要： Anti-acid-fast bacterial agents containing as the active ingredient compounds represented by the general formula (1), salts thereof or hydrates of the same. Namely, pyridonecarboxylic acid derivatives having an excellent antibacterial activity on tubercle bacillus and atypical acid-fast bacteria, favorable kinetics in vivo and a high safety.
摘要翻译：抗抗酸细菌剂含有作为活性成分，由以下通式表示的吡啶酮羧酸衍生物（1），其盐，或其水合物，其显示针对结核分枝杆菌和非典型耐酸优异的抗菌活性细菌具有良好的药代动力学和安全性。

3. 发明公开

EP0900793A4 CYCLOALKYLAMINOMETHYLPYRROLIDINE DERIVATIVES 失效
标题翻译： CYCLOALKYLAMINOMETHYLPYRROLIDINEDERIVATE
公开(公告)号：EP0900793A4
公开(公告)日：1999-07-07
申请号：EP97919690
申请日：1997-04-24
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , KIMURA YOUICHI , KAWAKAMI KATSUHIRO , OHKI HITOSHI
IPC分类号： A61K31/47 , C07D401/04
CPC分类号： C07D401/04
摘要： Compounds of general formula (I) and salts thereof, giving quinolone derivatives which exhibit high antibacterial activity against various bacteria including resistant ones and high safety, wherein R1 is cycloalkyl; R2 is hydrogen, amino, hydroxyl, mercapto, halogenomethyl, alkyl, alkenyl, alkynyl or alkoxy; R3 is amino, halogenomethyl, halogenomethoxy, alkyl, alkenyl, alkynyl or alkoxy; R4 is hydrogen or C¿1?-C6 alkyl; R?5 is C¿3-C6 cycloalkyl; and X is halogeno or hydrogen, with the proviso that these substituents may be further substituted; and Y is hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, choline, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, C1-C6 alkyl, C2-C7 alkoxymethyl or phenylalkyl composed of C1-C6 alkylene and phenyl.
摘要翻译：通式（I）的化合物及其盐，给出对各种细菌（包括抗性细菌和高安全性）表现出高抗菌活性的喹诺酮衍生物，其中R1是环烷基; R2是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; R3是氨基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; R4是氢或C1-C6烷基; R 5是C 3 -C 6环烷基; X是卤代或氢，条件是这些取代基可被进一步取代; Y为氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆碱，二甲基氨基乙基，5-茚满基，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， -C6烷基，C2-C7烷氧基甲基或由C1-C6亚烷基和苯基组成的苯基烷基。

4. 发明公开

EP1298131A4 QUINOLONECARBOXYLIC ACID DERIVATIVE 审中-公开
标题翻译：喹诺酮导数的
公开(公告)号：EP1298131A4
公开(公告)日：2004-09-08
申请号：EP01917706
申请日：2001-03-30
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , TAKAHASHI HISASHI , KAWAKAMI KATSUHIRO , ITOH MASAO , SUZUKI TETSUYA , OHTANI TSUYOSHI , SEKIGUCHI MASAYASU , MIYAUCHI RIE , HAYAKAWA ISAO
IPC分类号： A61K31/4709 , A61P31/04 , C07D401/04 , C07M7/00
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 monohydrochloride monohydrate and antibacterial agents containing the same. This compound is excellent in antibacterial activity and safety and highly stable to light and humidity, which makes it useful as an antibacterial agent.

5. 发明公开

EP0947513A4 TRICYCLIC AMINE DERIVATIVES 失效
标题翻译： DREIRINGIGE氨基衍生物
公开(公告)号：EP0947513A4
公开(公告)日：2002-10-02
申请号：EP97909605
申请日：1997-10-23
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , TAKAHASHI HISASHI , KIMURA KENICHI , MIYAUCHI RIE , OHKI HITOSHI , KAWAKAMI KATSUHIRO
IPC分类号： C07D401/04 , C07D455/02 , C07D471/04 , C07D491/16 , C07D498/04 , C07D498/06 , C07D513/04 , A61K31/47 , C07D209/94 , C07D455/06
CPC分类号： C07D401/04 , C07D455/02 , C07D471/04 , C07D513/04
摘要： Compounds represented by general formula (I) carrying a tricylic amine substituent optionally having various substituents, their salts, hydrates thereof or drugs containing these compounds as the active ingredient. Because of having favorable antibacterial activities on gram-negative and gram-positive bacteria and being excellent both in the dynamics in vivo and safety, these compounds are useful in treating infectious diseases. In said formula (I), Q represents a partial structure which is preferably represented by formula (a); or (b) and may have various substituents.
摘要翻译：由通式（I）表示的带有任选具有各种取代基的三取代胺取代基的化合物，其盐，其水合物或含有这些化合物的药物作为活性成分。由于对革兰氏阴性菌和革兰氏阳性菌具有良好的抗菌活性，并且在体内动力学和安全性方面均优异，所以这些化合物可用于治疗感染性疾病。在所述式（I）中，Q表示优选由式（a）表示的部分结构; 或（b）并可具有各种取代基。

6. 发明公开

EP1182202A4 AMINOMETHYLPYRROLIDINE DERIVATIVES HAVING AROMATIC SUBSTITUENTS 有权
标题翻译： WITH族取代基氨基甲基吡咯衍生物
公开(公告)号：EP1182202A4
公开(公告)日：2002-03-27
申请号：EP00907973
申请日：2000-03-09
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , TAKAHASHI HISASHI , KAWAKAMI KATSUHIRO , TAKEDA TOSHIYUKI , MIYAUCHI RIE
IPC分类号： C07D401/14 , A61K31/4709 , A61P31/04 , C07D401/04 , C07D405/14 , C07D417/14 , C07D498/06 , A61K31/435 , A61K31/4375 , A61K31/44 , A61K31/519 , A61K31/5383 , C07D455/02 , C07D471/04
CPC分类号： C07D401/04 , C07D405/14
摘要： Quinolone derivatives having potent antibacterial effects on various bacteria including insensible bacilli, which are compounds represented by general formula (1), salts of the same, or hydrates of both: wherein R1 is an optionally substituted aromatic group; R?2 and R3¿ are each hydrogen or alkyl; R?4, R5 and R6¿ are each hydrogen, hydroxyl, halogeno, or the like; R?7 and R8¿ are each hydrogen or alkyl; R9 is alkyl, alkenyl, halogenoalkyl, or the like; R10 is hydrogen or alkylthio; R11 is hydrogen, amino, hydroxyl, or the like; X1 is halogeno or hydrogen; A1 is nitrogen or C-X2; X2 is hydrogen, amino, halogeno, or the like; A?2 and A3¿ are each ⊃C=C(-A?1=)-N(-R9¿)- or ⊃N-C(-A?1=)=C(-R9)-; R10 and R9 or R9 and X2¿ may be united to form a ring structure; and Y is hydrogen or an ester-forming group.

7. 发明公开

EP0807630A4 HETEROCYCLIC COMPOUNDS 失效
标题翻译：杂环化合物
公开(公告)号：EP0807630A4
公开(公告)日：1998-05-13
申请号：EP96901518
申请日：1996-02-01
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , KIMURA YOUICHI , KAWAKAMI KATSUHIRO , KIMURA KENICHI , OHKI HITOSHI , MATSUHASHI NORIKAZU , KAWATO HARUKO
IPC分类号： C07D401/04 , A61K31/435 , A61K31/47 , C07D471/04
CPC分类号： C07D401/04
摘要： N1-(Halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by general formula (I), heterocyclic compounds useful as antibacterial agents, wherein X1 represents halo or hydrogen; X2 represents halo; R1 represents hydrogen, hydroxy, thiol, halomethyl, amino, alkyl or alkoxy; R2 represents a group of general formula (II) (wherein R?3 and R4¿ represent each hydrogen or alkyl; and n represents an integer of 1 or 2); A represents nitrogen or a group of general formula (III), (wherein X3 represents halo, cyano, amino, alkyl, halomethyl, alkoxy or halomethoxy); and R represents 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.

8. 发明公开

EP1479681A4 IMIDAZO(1,2-a)PYRIDINE DERIVATIVE 审中-公开
标题翻译：咪唑并（1,2-a）的PYRIDINDERIVAT
公开(公告)号：EP1479681A4
公开(公告)日：2006-05-10
申请号：EP03734891
申请日：2003-01-30
申请人： DAIICHI SEIYAKU CO
发明人： TAKEMURA MAKOTO , TAKAHASHI HISASHI , KAWAKAMI KATSUHIRO , TAKESHITA HIROSHI , KIMURA YOUICHI , WATANABE JUN , SUGIMOTO YUICHI , KITAMURA AKIHIRO , NAKAJIMA RYOHEI , KANAI KAZUO , FUJISAWA TETSUNORI
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
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4375 , A61K31/496 , A61K31/5377 , A61K31/541 , C07D471/14 , C07D491/14
摘要： A compound represented by the following formula (I), which has antifungal activity in a wide spectrum by a novel mechanism, i.e., 1,6-ß-glucan synthesis inhibition, and can specifically or selectively exhibit such activity, a salt thereof, or a solvate of either; and an antifungal agent containing any of these.

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