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    Carbapenem derivatives
    3.
    发明授权
    Carbapenem derivatives 失效
    卡巴培南衍生物

    公开(公告)号：US06908913B2

    公开(公告)日：2005-06-21

    申请号：US10344729

    申请日：2001-11-22

    申请人： Yuko Kano ,  Yasuo Yamamoto ,  Takahisa Maruyama ,  Takehiko Sawabe ,  Eiki Shitara ,  Kazuhiro Aihara ,  Kunio Atsumi ,  Takashi Ida

    发明人： Yuko Kano ,  Yasuo Yamamoto ,  Takahisa Maruyama ,  Takehiko Sawabe ,  Eiki Shitara ,  Kazuhiro Aihara ,  Kunio Atsumi ,  Takashi Ida

    IPC分类号： A61P31/04 ,  C07D477/14 ,  C07D519/00 ,  A61K31/429 ,  C07D519/06

    CPC分类号： C07D477/14

    摘要： An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and β-lactamase producing bacteria and are stable to DHP-1. The carbapenem derivatives according to the present invention are compounds represented by formulae (I) and (II) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl, R2 and R3 each independently represent H; halogen; substituted or unsubstituted alkyl; cycloalkyl; substituted or unsubstituted alkylcarbonyl; carbamoyl; substituted or unsubstituted aryl; substituted or unsubstituted alkylthio; morpholinyl; alkylsulfonyl; or formyl, n is 0 (zero) to 4, and Hy represents a substituted or unsubstituted monocyclic or bicyclic heterocyclic group.

    摘要翻译： 本发明的目的是提供对MRSA，PRSP，流感病毒和产生β-内酰胺酶的细菌具有强抗生素活性并且对DHP-1稳定的碳青霉烯衍生物。 根据本发明的碳青霉烯衍生物是由式（I）和（II）表示的化合物或其药学上可接受的盐：其中R 1表示H或甲基，R 2， 和R 3各自独立地表示H; 卤素; 取代或未取代的烷基; 环烷基 取代或未取代的烷基羰基; 氨基甲酰基; 取代或未取代的芳基; 取代或未取代的烷硫基; 吗啉基 烷基磺酰基; 或甲酰基，n为0（零）至4，Hy表示取代或未取代的单环或双环杂环基。

    Malonic acid monoesters and process for producing the same
    5.
    发明授权
    Malonic acid monoesters and process for producing the same 失效
    丙二酸单酯及其制备方法

    公开(公告)号：US07553989B2

    公开(公告)日：2009-06-30

    申请号：US10531382

    申请日：2003-10-17

    申请人： Takehiko Sawabe ,  Kazuhiro Aihara ,  Kunio Atsumi ,  Keiichi Ajito

    发明人： Takehiko Sawabe ,  Kazuhiro Aihara ,  Kunio Atsumi ,  Keiichi Ajito

    IPC分类号： C07C69/34

    CPC分类号： C07D317/36 ,  C07C69/38 ,  C07C69/76 ,  C07C69/78 ,  C07C69/96

    摘要： The present invention relates to a compound represented by formula (1) or a salt thereof: wherein R represents a group that is easily removable upon hydrolysis in vivo. This compound is usable in the production of prodrug-type carbapenem antibacterial agents for oral administration. The use of this compound in the process of production of the antibacterial agents can realize enhanced production efficiency and reduced production cost.

    摘要翻译： 本发明涉及由式（1）表示的化合物或其盐：其中R表示在体内水解时容易除去的基团。 该化合物可用于生产用于口服给药的前药型碳青霉烯类抗生素。 在生产抗菌剂的过程中使用该化合物可以实现提高生产效率并降低生产成本。

    2-Thioethenyl substituted carbapenem derivatives
    6.
    发明申请
    2-Thioethenyl substituted carbapenem derivatives 失效
    2-噻吩基取代的碳青霉烯衍生物

    公开(公告)号：US20070004700A1

    公开(公告)日：2007-01-04

    申请号：US11401892

    申请日：2006-04-12

    申请人： Takahisa Maruyama ,  Yuko Kano ,  Takashi Ando ,  Toshiro Sasaki ,  Takehiko Sawabe ,  Nobuyoshi Baba ,  Hiromi Takata ,  Hisashi Suzuki ,  Kazuhiro Aihara ,  Toshiki Fujita

    发明人： Takahisa Maruyama ,  Yuko Kano ,  Takashi Ando ,  Toshiro Sasaki ,  Takehiko Sawabe ,  Nobuyoshi Baba ,  Hiromi Takata ,  Hisashi Suzuki ,  Kazuhiro Aihara ,  Toshiki Fujita

    IPC分类号： A61K31/407 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： [Objective] An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including bata-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis. [Structure] The present invention provides 2-ethenylthio-based carbapenem derivatives represented by the formula (I) or pharmaceutically acceptable salts thereof that are effective, for example, against pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including beta-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis:

    摘要翻译： [目的]本发明的目的是提供对于引起目前临床问题的各种抗性细菌有效的化合物，例如包括耐青霉素的肺炎链球菌（PRSP），流感嗜血杆菌，包括不产生氨苄青霉素的bata-内酰胺酶的肺炎球菌 流感嗜血杆菌（BLNAR）和莫拉氏菌（布拉汉氏菌）卡他氏菌。 [结构]本发明提供了式（I）表示的2-乙烯基硫代碳青霉烯衍生物或其药学上可接受的盐，其可有效地例如针对包括耐青霉素的肺炎链球菌（PRSP）在内的肺炎球菌，包括β-内酰胺酶的流感嗜血杆菌 - 非生产氨苄青霉素耐药性流感嗜血杆菌（BLNAR）和莫拉氏菌（Branhamella）卡他性：

    2-thioethenyl substituted carbapenem derivatives
    7.
    发明授权
    2-thioethenyl substituted carbapenem derivatives 失效
    2-硫代乙烯基取代的碳青霉烯衍生物

    公开(公告)号：US07687490B2

    公开(公告)日：2010-03-30

    申请号：US11401892

    申请日：2006-04-12

    申请人： Takahisa Maruyama ,  Yuko Kano ,  Takashi Ando ,  Takehiko Sawabe ,  Nobuyoshi Baba ,  Hiromi Takata ,  Hisashi Suzuki ,  Kazuhiro Aihara ,  Toshiki Fujita

    发明人： Takahisa Maruyama ,  Yuko Kano ,  Takashi Ando ,  Takehiko Sawabe ,  Nobuyoshi Baba ,  Hiromi Takata ,  Hisashi Suzuki ,  Kazuhiro Aihara ,  Toshiki Fujita

    IPC分类号： C07D477/20 ,  A61K31/426 ,  A61K31/454 ,  A61P31/04 ,  C07D277/56 ,  C07D277/26 ,  C07D277/30 ,  C07D277/40 ,  C07D417/06

    CPC分类号： C07D487/04

    摘要： An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including bata-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis.The present invention provides 2-ethenylthio-based carbapenem derivatives represented by the formula (I) or pharmaceutically acceptable salts thereof that are effective, for example, against pneumococci including penicillin resistant Streptococcus pneumoneae (PRSP), Haemophilus influenzae including beta-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae (BLNAR), and Moraxella (Branhamella) catarrhalis:

    摘要翻译： 本发明的目的是提供对于引起当前临床问题的各种耐药性细菌有效的化合物，例如包括耐青霉素的肺炎链球菌（PRSP），流感嗜血杆菌（Haemophilus influenzae），包括不含巴生酵母的氨苄青霉素抗性流感嗜血杆菌 BLNAR）和莫拉氏菌（Branhamella）卡他氏菌。 本发明提供了由式（I）表示的2-乙烯基硫代碳青霉烯衍生物或其药学上可接受的盐，其可有效地例如针对包括耐青霉素的肺炎链球菌（PRSP）在内的肺炎球菌，流感嗜血杆菌，包括β-内酰胺酶非生产氨苄青霉素 耐药性流感嗜血杆菌（BLNAR）和莫拉氏菌（Branhamella）卡他性：

    Carbapenem derivatives
    10.
    发明授权
    Carbapenem derivatives 失效
    卡巴培南衍生物

    公开(公告)号：US06310056B1

    公开(公告)日：2001-10-30

    申请号：US09355272

    申请日：1999-07-28

    申请人： Yuko Kano ,  Kazuhiro Aihara ,  Yumiko Toyooka ,  Toshiro Sasaki ,  Hiromasa Takizawa ,  Kenichi Fushihara ,  Kazuko Kobayashi ,  Kunio Atsumi ,  Katsuyoshi Iwamatsu ,  Takashi Ida

    发明人： Yuko Kano ,  Kazuhiro Aihara ,  Yumiko Toyooka ,  Toshiro Sasaki ,  Hiromasa Takizawa ,  Kenichi Fushihara ,  Kazuko Kobayashi ,  Kunio Atsumi ,  Katsuyoshi Iwamatsu ,  Takashi Ida

    IPC分类号： A61K31429

    CPC分类号： C07D519/00

    摘要： The carbapenem derivatives represented by the following formula (I) is disclosed. These compounds have strong anti-bacterial activities against bacteria including methicillin resistant Staphylococcus aureus, penicillin resistant Streptococcus pneumoniae, Enterococci, influenza, and &bgr;-lactamase producing bacteria, and have high stabilities to DHP-1 wherein R1 represents hydrogen or methyl, either one of R2, R3, R4, or R5 represents the bond to the 2-position on the carbapenem ring, and the remaining three respectively represent hydrogen, halogen, nitro, cyano, alkyl, cycloalkyl, alkylthio, alkenyl, formyl, alkylcarbonyl, alkoxycarbonyl, aminosulfonyl, aryl carbonyl, aryl, carbamoyl, N-lower alkylcarbamoyl, N,N-di-lower alkylaminocarbonyl, lower alkoxyiminomethyl, or hydroxyiminomethyl, R6 is not present or represents alkyl, cycloalkyl, or alkenyl, and R is not present, or represents hydrogen or a group which may be metabolically hydrolyzed in the body, provided that when R6 is not present, R represents hydrogen or a group which may be metabolically hydrolyzed in the body, and when R6 is present, R is not present, and the compound forms an inner salt.

    摘要翻译： 公开了由下式（I）表示的碳青霉烯衍生物。 这些化合物对包括耐甲氧西林金黄色葡萄球菌，青霉素耐药性肺炎链球菌，肠球菌，流感和β-内酰胺酶生产细菌在内的细菌具有很强的抗细菌活性，并且对于DHP-1具有高稳定性，其中R 1表示氢或甲基，R 2 ，R 3，R 4或R 5表示碳青霉烯环上2-位的键，其余3个分别表示氢，卤素，硝基，氰基，烷基，环烷基，烷硫基，烯基，甲酰基，烷基羰基，烷氧基羰基，氨基磺酰基， 芳基羰基，芳基，氨基甲酰基，N-低级烷基氨基甲酰基，N，N-二低级烷基氨基羰基，低级烷氧基亚氨基甲基或羟基亚氨基甲基，R6不存在或表示烷基，环烷基或烯基，R不存在，或表示氢或 可以在体内代谢水解的基团，条件是当R 6不存在时，R代表氢或可以代谢地水解的基团 e体，当R 6存在时，R不存在，且该化合物形成内盐。