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18 条记录 (耗时 0.01 秒)

    CIS-SUBSTITUTED FLUOROMETHYLPYRROLIDINE DERIVATIVES
    2.
    发明公开
    CIS-SUBSTITUTED FLUOROMETHYLPYRROLIDINE DERIVATIVES 失效
    CIS的取代的FLUOROMETHYLPYRROLIDIN衍生物

    公开(公告)号：EP0995744A4

    公开(公告)日：2001-02-07

    申请号：EP98928627

    申请日：1998-06-23

    申请人： DAIICHI SEIYAKU CO

    发明人： TAKEMURA MAKOTO ,  TAKAHASHI HISASHI ,  OHKI HITOSHI ,  KIMURA KENICHI ,  MIYAUCHI RIE ,  TAKEDA TOSHIYUKI

    IPC分类号： C07D401/04 ,  A61K31/47 ,  C07D207/14

    CPC分类号： C07D401/04

    摘要： Quinolone derivatives represented by general formula (I), salts thereof, and hydrates thereof of both, having potent antimicrobial activities against various bacteria including resistant strains and being highly safe: wherein R1 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R2 represents a halogenomethoxyl or alkoxyl group; R3 represents an alkyl, alkenyl, halogenoalkyl, cyclic alkyl, heteroaryl, alkoxyl, or alkylamino group; R4 represents a hydrogen atom or a 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 group. The above substituents may be further substituted.

    CYCLOALKYLAMINOMETHYLPYRROLIDINE DERIVATIVES
    3.
    发明公开
    CYCLOALKYLAMINOMETHYLPYRROLIDINE DERIVATIVES 失效
    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。

    HETEROCYCLIC SPIRO DERIVATIVES
    4.
    发明公开
    HETEROCYCLIC SPIRO DERIVATIVES 失效
    杂环衍生物螺

    公开(公告)号：EP0816355A4

    公开(公告)日：1998-05-20

    申请号：EP96901553

    申请日：1996-02-06

    申请人： DAIICHI SEIYAKU CO

    发明人： TAKEMURA MAKOTO ,  KIMURA YOUICHI ,  OHKI HITOSHI

    IPC分类号： C07D401/04 ,  A61K31/47 ,  C07D471/04

    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 R2 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.

    8-CYANOQUINOLONECARBOXYLIC ACID DERIVATIVE
    6.
    发明公开
    8-CYANOQUINOLONECARBOXYLIC ACID DERIVATIVE 有权
    8CYANOCHINOLONCARBONSÄUREDERIVAT

    公开(公告)号：EP1669354A4

    公开(公告)日：2008-08-20

    申请号：EP04788328

    申请日：2004-09-29

    申请人： DAIICHI SEIYAKU CO

    发明人： TAKAHASHI HISASHI ,  MIYAUCHI RIE ,  TAKEMURA MAKOTO

    IPC分类号： C07D401/04 ,  A61K31/4709 ,  A61P31/04 ,  C07D215/22 ,  C07D215/233 ,  C07D215/56

    CPC分类号： C07D215/233 ,  A61K31/4709

    摘要： To provide a quinolone antibacterial drug and a therapeutic agent for infectious diseases, which exhibit potent antibacterial activity on Gram-positive and Gram-negative bacteria and which is highly safe. A compound represented by the following formula (1): (wherein R 1 represents a C3-C6 cycloalkyl group which may have a substituent or the like; R 2 represents a hydrogen atom or the like; R 3 and R 4 each independently represent a hydrogen atom or a C1-C6 alkyl group, or a substituted carboxyl group derived from an amino acid, a dipeptide, or a tripeptide, and, in the case where each of R 3 and R 4 represents a C1-C6 alkyl group, the alkyl group may be substituted by one or more atoms or groups selected from among a hydroxyl group, a halogen atom, a C1-C6 alkylthio group, and a C1-C6 alkoxy group; and n denotes an integer of 1 to 3), a salt thereof, and a hydrate of the compound or the salt. Also, antibacterial drugs and therapeutic agents for infectious diseases are prepared.

    摘要翻译： 喹啉类抗菌剂，对革兰氏阳性菌和革兰氏阴性菌具有强大的抗菌活性，安全性高; 和传染病治疗剂。 本发明提供由下述式（1）表示的化合物：（化学式1）（式中，R 1表示可以具有取代基的C 3-6环烷基等; R 2表示氢等; R 3和R 4分别独立地表示氢原子， 烷基或由氨基酸，二肽或三肽衍生的取代羧基，条件是当R3和R4为C1-6烷基时，则各烷基可被一个或多个选自羟基，卤代，C1- 6烷硫基和C1-6烷氧基;并且n是1至3的整数），该化合物的盐或任一种的水合物。

    SUBSTITUTED CYCLOBUTYLAMINE DERIVATIVES
    7.
    发明公开
    SUBSTITUTED CYCLOBUTYLAMINE DERIVATIVES 失效
    SUBSTITUIERTE CYCLOBUTYLAMINDERIVATE

    公开(公告)号：EP0990654A4

    公开(公告)日：2004-09-15

    申请号：EP98921863

    申请日：1998-05-28

    申请人： DAIICHI SEIYAKU CO

    发明人： TAKEMURA MAKOTO ,  TAKAHASHI HISAHI ,  SUGITA KAZUYUKI ,  MIYAUCHI RIE

    IPC分类号： A61K31/4709 ,  A61P31/04 ,  C07D401/04 ,  C07D498/06

    CPC分类号： C07D401/04

    摘要： Substituted cyclobutylamine derivatives with novel structures represented by general formula (I), wherein R1 to R4 and Q represent each a specific substituent and, in particular, Q represents a quinolone derivative of a specific structure. These derivatives are useful as antibacterial compounds which have excellent antibacterial actions over a wide scope of bacteria including gram-negative and gram-positive ones, exert potent antibacterial activities particularly on methicillin-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae and quinolone-resistant bacteria and are excellent in the in vivo dynamics and safety.

    摘要翻译： 具有由通式（I）表示的新结构的取代的环丁基胺衍生物，其中R 1至R 4和Q各自表示特定取代基，并且特别地，Q表示具体结构的喹诺酮衍生物。 这些衍生物作为抗菌化合物是有用的，其在广泛的细菌（包括革兰氏阴性和革兰氏阳性细菌）上具有优异的抗菌作用，对甲氧西林抗性金黄色葡萄球菌（MRSA），耐青霉素肺炎链球菌和喹诺酮 并且在体内动力学和安全性方面非常出色。

    PYRIDOBENZOXAZINE DERIVATIVES
    8.
    发明公开
    PYRIDOBENZOXAZINE DERIVATIVES 失效
    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。

    cis-SUBSTITUTED AMINOCYCLOPROPANE DERIVATIVES
    9.
    发明公开
    cis-SUBSTITUTED AMINOCYCLOPROPANE DERIVATIVES 失效
    CIS-SUBSTITUIERTE AMINOCYCLOPROPANDERIVATE

    公开(公告)号：EP0919553A4

    公开(公告)日：2002-06-12

    申请号：EP97930766

    申请日：1997-07-11

    申请人： DAIICHI SEIYAKU CO

    发明人： TAKEMURA MAKOTO ,  KIMURA YOUICHI ,  TAKAHASHI HISASHI ,  ISHIDA YOHHEI

    IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  C07D207/24 ,  C07D207/26 ,  C07D401/04 ,  C07D207/09 ,  C07D207/16 ,  C07D489/08 ,  C07D513/08

    CPC分类号： C07D207/26 ,  A61K31/4375 ,  A61K31/4709 ,  C07D207/24 ,  C07D401/04

    摘要： The present invention is to provide an antimicrobial agent having high safety as well as potent antimicrobial activity on broad range of microorganisms. A compound represented by the following formula, its salt and their hydrates: wherein R and R each independently represents a hydrogen atom or an alkyl group; n represents an integer of 1 to 3; R represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cycloalkyl group, an aryl group, a heteroaryl group, an alkoxyl group or an alkylamino group; R represents a hydrogen atom or an alkylthio group; R represents a hydrogen atom, an amino group, a hydroxyl group, a thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; X represents a halogen atom or a hydrogen atom; and A represents a nitrogen atom or a partial structure represented by formula (II): wherein X represents a hydrogen atom, an amino group, a halogen atom, a cyano group, a halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; and Y 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, a 3-acetoxy-2-oxobutyl group, an alkyl, an alkoxymethyl group or a phenylalkyl group.

    摘要翻译： 包含通式（1）化合物或其化合物或其水合物的盐的抗各种细菌和高安全性的抗菌药物：其中R 1和R 2各自为氢或烷基; n是1至3的整数; R3是烷基，烯基，卤代烷基，环状烷基，芳基，杂芳基，烷氧基或烷基氨基; R4是氢或烷硫基; R5是氢，氨基，羟基，巯基，卤代甲基，烷基，烯基，炔基或烷氧基; X1是卤代或氢; A是氮或（II）; X2是氢，氨基，卤素，氰基，卤代甲基，卤代甲氧基，烷基，烯基，炔基或烷氧基; 和Y是氢，苯基，乙酰氧基甲基，新戊酰氧基甲基，乙氧基羰基，胆酰基，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， ，烷氧基甲基或苯基烷基。