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1. 发明申请

WO1998018783A1 TRICYCLIC AMINE DERIVATIVES 审中-公开
标题翻译：三元胺衍生物
公开(公告)号：WO1998018783A1
公开(公告)日：1998-05-07
申请号：PCT/JP1997003842
申请日：1997-10-23
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , TAKAHASHI, Hisashi , KIMURA, Kenichi , MIYAUCHI, Rie , OHKI, Hitoshi , KAWAKAMI, Katsuhiro
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
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）表示的化合物，其携带任选具有各种取代基的三取代胺取代基，其盐，水合物或含有这些化合物作为活性成分的药物。由于对革兰氏阴性和革兰氏阳性细菌具有良好的抗菌活性，并且在体内和安全性方面都具有优异的作用，因此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），并且可以具有各种取代基。

2. 发明申请

WO1998013370A1 PYRIDOBENZOXAZINE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO1998013370A1
公开(公告)日：1998-04-02
申请号：PCT/JP1997003440
申请日：1997-09-26
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , TAKAHASHI, Hisashi , KAWAKAMI, Katsuhiro
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D498/06
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, R represents hydrogen or C1-6 alkyl optionally having substituent(s) selected from the group consisting of hydroxy, halogeno, C1-6 alkylthio and C1-6 alkoxy; R represents hydrogen or amino optionally having one or two substituents selected from the group consisting of formyl, C1-6 alkyl and C2-6 acyl; and R represents hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, etoxycarbonyl, cholin, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, C1-6 alkyl, C2-7 alkoxymethyl, or phenylalkyl composed of C1-6 alkylene and phenyl.
摘要翻译：衍生物对革兰阴性和革兰氏阳性细菌具有强力的抗菌活性，同时体内有利的动力学和高安全性; 和优良的药物。由通式（I）表示的化合物及其盐，其水合物和含有该活性成分的抗菌剂。在所述式中，R 1表示氢或任选具有选自羟基，卤代C 1-6烷硫基和C 1-6烷氧基的取代基的C 1-6烷基; R 2表示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酰基的取代基的氨基; 并且R 3表示氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，丁氧基羰基，胆碱，二甲基氨基乙基，5-二氢化茚基，邻苯二基苯基，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。

3. 发明申请

WO1998024781A1 SUBSTITUTED AMINOMETHYLPYRROLIDINE DERIVATIVES 审中-公开
标题翻译：取代的氨基甲基吡咯烷衍生物
公开(公告)号：WO1998024781A1
公开(公告)日：1998-06-11
申请号：PCT/JP1996003552
申请日：1996-12-04
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , KAWAKAMI, Katsuhiro , SUGITA, Kazuyuki , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Antibacterial drugs excellent in antibacterial activity and safety, comprising quinolone derivatives having various substituents including a substituted aminomethylpyrrolidine and represented by general formula (I) or salts thereof, or hydrates of both. In said formula, Q is (II) or (IV).
摘要翻译：包含抗菌活性和安全性优异的抗菌药物，包括具有各种取代基的喹诺酮衍生物，包括取代的氨基甲基吡咯烷，并且由通式（I）表示的盐或其盐，或两者的水合物。在所述式中，Q为（II）或（IV）。

4. 发明申请

WO1997040037A1 CYCLOALKYLAMINOMETHYLPYRROLIDINE DERIVATIVES 审中-公开
标题翻译：环丙基氨基甲基吡咯烷衍生物
公开(公告)号：WO1997040037A1
公开(公告)日：1997-10-30
申请号：PCT/JP1997001446
申请日：1997-04-24
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , KAWAKAMI, Katsuhiro , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： 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 R is cycloalkyl; R is hydrogen, amino, hydroxyl, mercapto, halogenomethyl, alkyl, alkenyl, alkynyl or alkoxy; R is amino, halogenomethyl, halogenomethoxy, alkyl, alkenyl, alkynyl or alkoxy; R is hydrogen or C1-C6 alkyl; R is C3-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：给出通式（I）的化合物及其盐，得到喹诺酮衍生物，其对包括耐药性的各种细菌具有高抗菌活性，高安全性，其中R 1为环烷基; R 2是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; R 3是氨基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; R 4是氢或C 1 -C 6烷基; R 5是C 3 -C 6环烷基; 且X为卤素或氢，条件是这些取代基可进一步被取代; 并且Y是氢，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，5-二氢化茚基，邻苯二基苯基，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，C1 -C 1-6烷基，C 2 -C 7烷氧基甲基或由C 1 -C 6亚烷基和苯基组成的苯基烷基。

5. 发明申请

WO1996023782A1 HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译：杂环化合物
公开(公告)号：WO1996023782A1
公开(公告)日：1996-08-08
申请号：PCT/JP1996000208
申请日：1996-02-01
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , KAWAKAMI, Katsuhiro , KIMURA, Kenichi , OHKI, Hitoshi , MATSUHASHI, Norikazu , KAWATO, Haruko
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
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 X represents halo or hydrogen; X represents halo; R represents hydrogen, hydroxy, thiol, halomethyl, amino, alkyl or alkoxy; R represents a group of general formula (II) (wherein R and R 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 X 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.
摘要翻译：由通式（I）表示的N1-（卤代环丙基）取代的吡啶酮羧酸衍生物，可用作抗菌剂的杂环化合物，其中X 1表示卤素或氢; X 2表示卤素; R 1表示氢，羟基，硫醇，卤代甲基，氨基，烷基或烷氧基; R 2表示通式（II）的基团（其中R 3和R 4各自代表氢或烷基; n表示1或2的整数）; A表示氮或通式（III）的基团（其中X 3表示卤素，氰基，氨基，烷基，卤代甲基，烷氧基或卤代甲氧基）; 并且R表示氢，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，5-二氢化茚基，邻苯二基苯基，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，，烷氧基甲基或苯基烷基。

6. 发明申请

WO1998002431A1 cis-SUBSTITUTED AMINOCYCLOPROPANE DERIVATIVES 审中-公开
标题翻译：顺式取代的氨基羰基衍生物
公开(公告)号：WO1998002431A1
公开(公告)日：1998-01-22
申请号：PCT/JP1997002411
申请日：1997-07-11
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , TAKAHASHI, Hisashi , ISHIDA, Yohhei
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D207/26 , A61K31/4375 , A61K31/4709 , C07D207/24 , C07D401/04 , Y02A50/475
摘要： Antibacterial drugs exhibiting potent antibacterial effects against various bacteria and high safety, which comprise compounds of general formula (1), or salts of the compounds or hydrates thereof: wherein R and R are each hydrogen or alkyl; n is an integer of 1 to 3; R is alkyl, alkenyl, halogenoalkyl, cyclic alkyl, aryl, heteroaryl, alkoxyl or alkylamino; R is hydrogen or alkylthio; R is hydrogen, amino, hydroxyl, mercapto, halogenomethyl, alkyl, alkenyl, alkynyl or alkoxyl; X is halogeno or hydrogen; A is nitrogen or (II); X is hydrogen, amino, halogeno, cyano, halogenomethyl, halogenomethoxyl, alkyl, alkenyl, alkynyl or alkoxyl; and Y is hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, ethoxycarbonyl, cholyl, dimethylaminoethyl, 5-indanyl, phthalidyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, alkyl, alkoxymethyl or phenylalkyl.
摘要翻译：对各种细菌和高度安全性具有强效抗菌作用的抗菌药物，其包含通式（1）的化合物或其化合物或其水合物的盐：其中R 1和R 2各自为氢或烷基; n为1〜3的整数， R 3是烷基，烯基，卤代烷基，环烷基，芳基，杂芳基，烷氧基或烷基氨基; R 4是氢或烷硫基; R 5是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; X 1是卤代或氢; A是氮或（II）; X 2是氢，氨基，卤代，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; 并且Y是氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，取代基，二甲基氨基乙基，5-二氢化茚基，邻苯二甲酰基，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，，烷氧基甲基或苯基烷基。

7. 发明申请

WO1997019072A1 SUBSTITUTED AMINOCYCLOALKYLPYRROLIDINE DERIVATIVES 审中-公开
标题翻译：取代的氨基环丙基吡咯烷衍生物
公开(公告)号：WO1997019072A1
公开(公告)日：1997-05-29
申请号：PCT/JP1996003440
申请日：1996-11-22
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , TAKAHASHI, Hisashi , KIMURA, Kenichi , MIYAUCHI, Satoru , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Antibacterial drugs excellent in antibacterial activity and safety, comprising quinolone derivatives having various substituents including a substituted aminocycloalkylpyrrolidine and represented by general formula (I), salts thereof, or hydrates of both, wherein Q is formula (II) or (IV).
摘要翻译：其具有抗菌活性和安全性优异的抗菌药物，其中Q为式（II）或（IV），其中喹诺酮衍生物具有各种取代基，包括取代的氨基环烷基吡咯烷并由通式（I）表示，其盐或两者的水合物。

8. 发明申请

WO1996024593A1 HETEROCYCLIC SPIRO DERIVATIVES 审中-公开
标题翻译：杂环螺旋衍生物
公开(公告)号：WO1996024593A1
公开(公告)日：1996-08-15
申请号：PCT/JP1996000248
申请日：1996-02-06
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , TAKEMURA, Makoto , KIMURA, Youichi , OHKI, Hitoshi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Antibacterial compounds useful as medicines, animal drugs, aquacultural drugs or antibacterial preservatives; and antibacterial drugs or preparations containing the same, having an excellent activity against a wide variety of bacteria including particularly quinolone-resistant bacteria and being highly safe, more specifically quinolone derivatives that are represented by general formula (I) wherein R at the 7-position represents a group derived from a heterocyclic spiro compound and N at the 1-position bears a halogenocyclopropyl group and that comprise each preferably a single isomer.
摘要翻译：用作药物，动物药物，水产养殖药物或抗菌防腐剂的抗菌化合物; 和含有该抗菌药物或其制剂的抗菌药物或制剂，具有优异的抗多种细菌，特别是喹诺酮抗性细菌的活性，并且是高度安全的，更具体地，通式（I）表示的喹诺酮衍生物，其中R 2在 7-位表示衍生自杂环螺环化合物的基团，1-位上的N具有卤代环丙基，并且每个优选包含单个异构体。

9. 发明申请

WO1993000344A1 CARBAPENEM DERIVATIVE 审中-公开
公开(公告)号：WO1993000344A1
公开(公告)日：1993-01-07
申请号：PCT/JP1992000790
申请日：1992-06-19
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , NISHI, Toshiyuki; , KODA, Hiroko; , SUGITA, Kazuyuki; , ISHIDA, Yohhei; , TAKEMURA, Makoto; , HAYANO, Takeshi;
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D477/00
CPC分类号： C07D477/20 , Y02P20/55
摘要： Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta -methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxyl; R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.
摘要翻译：已知的碳青霉烯类衍生物如噻吩霉素具有缺点，它们在物理化学上不稳定，并易于被诸如肾脏的DHP之类的酶分解以产生不利影响如肾毒性，而1-β-甲基碳青霉烯化合物是稳定的并且具有有效的抗菌活性关于对DHP的稳定性和抗菌活性不令人满意。在这些情况下，本发明提供了一种通式（I）表示的抗生素，其对包括绿脓假单胞菌在内的各种细菌具有有效的抗菌活性，并且对于水解酶例如DHP及其盐（I）的安全性和稳定性优异，其中R 1表示低级烷基或任选保护的羟基低级烷基; R 2，R 13和R 14各自代表氢或低级烷基; R 3表示任选酯化的羧基; R 4，R 9，R 10和R 15各自表示氨基保护基，氢或低级烷基; R 5，R 6，R 11和R 12分别表示氢，羟基，低级烷基，羟基低级烷基或卤素，或者R 5和R 6和/ 11>和R 12可以结合在一起形成亚烷基; R 7表示氢，低级烷基，羧基，氨基甲酰基或-CONR 71 R 72; R 71和R 72表示氢或低级烷基; R 8表示氢，低级烷基或羟基低级烷基，或者R 8可与R 7结合形成亚烷基; Z表示单键，氧，硫，-CR 11 R 12 - ， - NR 13 CO - ， - CONR 14 - 或-NR 15 - 。 m和n表示0〜6的整数。

10. 发明申请

WO1992021659A1 PYRIDONECARBOXYLIC ACID DERIVATIVE 审中-公开
标题翻译：吡咯烷酮羧酸衍生物
公开(公告)号：WO1992021659A1
公开(公告)日：1992-12-10
申请号：PCT/JP1992000687
申请日：1992-05-27
申请人： DAIICHI PHARMACEUTICAL CO., LTD. , HAYAKAWA, Isao , KIMURA, Youichi , TAKAHASHI, Hisashi
发明人： DAIICHI PHARMACEUTICAL CO., LTD.
IPC分类号： C07D215/56
CPC分类号： C07D487/04 , C07D215/56 , C07D401/04 , C07D471/04 , Y02P20/55
摘要： Known synthetic antibacterials having a condensed pyridonecarboxylic acid skeleton include quinolone derivatives having various substituents at various positions of the skeleton. The possibility of the presence of diastereoisomerism in these derivatives, however, gives rise to a mixture of at least four diastereomers having properties differing from one another, resulting in the difficulty in applying the same as such as a medicine. Under these circumstances the present invention provides an antibacterial 1-(1,2-cis-2-fluorocyclopropyl) quinolone derivative represented by general formula (I) comprising a single diastereoisomer even when there are various diastereoisomers thereof. In formula (I), R represents methyl, difluoromethyl, etc.; R represents a saturated nitrogenous heterocyclic group; A represents C-X or nitrogen; X and X represent each independently halogen; and X and Z represent each hydrogen, etc.
摘要翻译：具有缩合吡啶酮羧酸骨架的已知合成抗菌剂包括在骨架的各个位置具有各种取代基的喹诺酮衍生物。然而，在这些衍生物中存在非对映异构体的可能性导致具有彼此不同的性质的至少四种非对映异构体的混合物，导致难以应用与药物相同的性质。在这些情况下，本发明提供了即使存在各种非对映异构体也包含单一非对映异构体的由通式（I）表示的抗菌1-（1,2-顺式2-氟环丙基）喹诺酮衍生物。在式（I）中，R 1表示甲基，二氟甲基等; R 2表示饱和含氮杂环基; A表示C-X 3或氮; X 1和X 2各自独立地表示卤素; X 3和Z代表每个氢等

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