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    METHOD FOR PREPARING (R)-3-(3-FLUORO-4-(1-METHYL-5,6-DIHYDRO-1,2,4-TRIAZIN-4(1H)-YL)PHENYL)-5-(SUBSTITUTED METHYL)OXAZOLIDIN-2-ONE DERIVATIVES
    1.
    发明申请
    METHOD FOR PREPARING (R)-3-(3-FLUORO-4-(1-METHYL-5,6-DIHYDRO-1,2,4-TRIAZIN-4(1H)-YL)PHENYL)-5-(SUBSTITUTED METHYL)OXAZOLIDIN-2-ONE DERIVATIVES 有权
    制备（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三氮杂-4（1H） - 基）苯基）-5-（取代的甲基） ）OXAZOLIDIN-2-ONE衍生物

    公开(公告)号：US20130005967A1

    公开(公告)日：2013-01-03

    申请号：US13583492

    申请日：2011-03-08

    申请人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Hong Bum Lee ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    发明人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Hong Bum Lee ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    IPC分类号： C07D413/10 ,  C07D253/06

    CPC分类号： C07D255/02 ,  C07D253/06 ,  C07D413/10

    摘要： Provided are a method for preparing (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives, which are oxazolidinone antibiotic compounds having a cyclic amidrazone group, represented by Chemical Formula 1, and intermediates thereof, and uses 3,4-difluoro-4-nitrobenzen as a starting material. According to the preparation method of the present invention, (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives, which are useful as oxazolidinone antibiotics, can be prepared in high purity and high yield in a simpler manner than conventional methods.

    摘要翻译： 提供制备（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基）-5- （取代甲基）恶唑烷-2-酮衍生物，它们是由化学式1表示的具有环状氨基腙基的恶唑烷酮类抗生素化合物及其中间体，并以3,4-二氟-4-硝基苯为起始原料。 根据本发明的制备方法，将（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基 ）-5-（取代的甲基）恶唑烷-2-酮衍生物可以以比常规方法更简单的方式以高纯度和高产率制备，其可用作恶唑烷酮抗生素。

    Oxazolidinone derivative and medical composition containing same
    2.
    发明授权
    Oxazolidinone derivative and medical composition containing same 有权
    恶唑烷酮衍生物和含有它们的医药组合物

    公开(公告)号：US08846669B2

    公开(公告)日：2014-09-30

    申请号：US14008702

    申请日：2012-03-29

    申请人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sun Young Kim ,  Hong Bum Lee ,  Hyang Sook Lee ,  Kyuman Oh ,  Hye Jin Heo ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    发明人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sun Young Kim ,  Hong Bum Lee ,  Hyang Sook Lee ,  Kyuman Oh ,  Hye Jin Heo ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    IPC分类号： C07D413/14 ,  A61K31/53 ,  A61K31/5355

    CPC分类号： C07D413/14

    摘要： Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group.In Formula 1, R and Q are the same as defined in the detailed description.In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.

    摘要翻译： 公开了上述通式1所示的新型恶唑烷酮衍生物，特别是具有环状偕胺肟或环状氨基腙基的新型恶唑烷酮化合物。 在式1中，R和Q与详细描述中定义相同。 此外，公开了一种抗生素的药物组合物，其包含式1的新型恶唑烷酮衍生物，其前药，其水合物，其溶剂合物，其异构体或其药学上可接受的盐作为活性成分。 新型恶唑烷酮衍生物，其前体药剂，其水合物，其溶剂合物，其异构体及其药学上可接受的盐具有抗抗性细菌的抗菌谱，对革兰氏阳性和革兰氏阴性菌具有低毒性和强抗菌作用 因此可以有效地用作抗生素。

    NOVEL OXAZOLIDINONE DERIVATIVE AND MEDICAL COMPOSITION CONTAINING SAME
    3.
    发明申请
    NOVEL OXAZOLIDINONE DERIVATIVE AND MEDICAL COMPOSITION CONTAINING SAME 有权
    新型奥昔洛芬衍生物和含有它们的医药组合物

    公开(公告)号：US20140179691A1

    公开(公告)日：2014-06-26

    申请号：US14008702

    申请日：2012-03-29

    申请人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sun Young Kim ,  Hong Bum Lee ,  Hyang Sook Lee ,  Kyuman Oh ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim ,  Hye Jin Heo

    发明人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Sun Young Kim ,  Hong Bum Lee ,  Hyang Sook Lee ,  Kyuman Oh ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim ,  Hye Jin Heo

    IPC分类号： C07D413/14

    CPC分类号： C07D413/14

    摘要： Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group.In Formula 1, R and Q are the same as defined in the detailed description.In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient.The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.

    摘要翻译： 公开了上述通式1所示的新型恶唑烷酮衍生物，特别是具有环状偕胺肟或环状氨基腙基的新型恶唑烷酮化合物。 在式1中，R和Q与详细描述中定义相同。 此外，公开了一种抗生素的药物组合物，其包含式1的新型恶唑烷酮衍生物，其前药，其水合物，其溶剂合物，其异构体或其药学上可接受的盐作为活性成分。 新型恶唑烷酮衍生物，其前体药剂，其水合物，其溶剂合物，其异构体及其药学上可接受的盐具有抗抗性细菌的抗菌谱，对革兰氏阳性和革兰氏阴性菌具有低毒性和强抗菌作用 因此可以有效地用作抗生素。

    Method for preparing (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives
    4.
    发明授权
    Method for preparing (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives 有权
    制备（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基）-5-（取代的甲基 ）恶唑烷-2-酮衍生物

    公开(公告)号：US08703939B2

    公开(公告)日：2014-04-22

    申请号：US13583492

    申请日：2011-03-08

    申请人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Hong Bum Lee ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    发明人： Young Lag Cho ,  Sung Yoon Baek ,  Sang Eun Chae ,  Hong Bum Lee ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    IPC分类号： C07D253/065 ,  C07D413/10 ,  C07D413/14

    CPC分类号： C07D255/02 ,  C07D253/06 ,  C07D413/10

    摘要： Provided are a method for preparing (R)-3-(3-fluoro-4-(1-methyl-5, 6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl) oxazolidin-2-one derivatives, which are oxazolidinone antibiotic compounds having a cyclic amidrazone group, represented by Chemical Formula 1, and intermediates thereof, and uses 3,4-difluoro-4-nitrobenzen as a starting material. According to the preparation method of the present invention, (R)-3-(3-fluoro-4-(1-methyl-5, 6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl) oxazolidin-2-one derivatives, which are useful as oxazolidinone antibiotics, can be prepared in high purity and high yield in a simpler manner than conventional methods.

    摘要翻译： 提供制备（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基）-5- （取代甲基）恶唑烷-2-酮衍生物，它们是由化学式1表示的具有环状氨基腙基的恶唑烷酮类抗生素化合物及其中间体，并以3,4-二氟-4-硝基苯为起始原料。 根据本发明的制备方法，使用（R）-3-（3-氟-4-（1-甲基-5,6-二氢-1,2,4-三嗪-4（1H） - 基）苯基 ）-5-（取代的甲基）恶唑烷-2-酮衍生物可以以比常规方法更简单的方式以高纯度和高产率制备，其可用作恶唑烷酮抗生素。

    Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof
    9.
    发明授权
    Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone pharmaceutical compositions thereof 有权
    具有环偕胺肟或环状氨基腙的恶唑烷酮衍生物其药物组合物

    公开(公告)号：US08242113B2

    公开(公告)日：2012-08-14

    申请号：US13120568

    申请日：2009-09-22

    申请人： Young Lag Cho ,  Sang Eun Chae ,  Sung Yoon Baek ,  Yeon Ok Kim ,  Seong Jin Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    发明人： Young Lag Cho ,  Sang Eun Chae ,  Sung Yoon Baek ,  Yeon Ok Kim ,  Seong Jin Kim ,  Hyang Sook Lee ,  Ju Hyun Park ,  Tae Kyo Park ,  Sung Ho Woo ,  Yong Zu Kim

    IPC分类号： C07D403/08 ,  A61K31/5377

    CPC分类号： C07D403/08

    摘要： Disclosed is a novel oxazolidinone derivative, particularly a novel oxazolidinone compound with a cyclic amidoxime or cyclic amidrazone group. Also disclosed is a pharmaceutical antibiotic composition including a novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof as an effective ingredient. Because the novel oxazolidinone derivative, in vivo hydrolysable ester thereof, in vivo hydrolysable phosphate ester thereof, an isomer thereof or a pharmaceutically acceptable salt thereof exhibits a wide antibacterial spectrum against resistant bacteria, a low toxicity, and a strong antibacterial activity against Gram-positive and Gram-negative bacteria, it can be usefully used as an antibiotic.

    摘要翻译： 公开了一种新的恶唑烷酮衍生物，特别是具有环偕胺肟或环状氨基腙基团的新型恶唑烷酮化合物。 还公开了包含新的恶唑烷酮衍生物，其体内可水解的酯，其体内可水解的磷酸酯，其异构体或其药学上可接受的盐作为有效成分的药物抗生素组合物。 因为新的恶唑烷酮衍生物，其体内可水解的酯，其体内可水解的磷酸酯，其异构体或其药学上可接受的盐，表现出对抗细菌的抗菌谱广，毒性低，抗革兰氏阳性 和革兰阴性菌，可以有效地用作抗生素。