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    ANTIBACTERIAL 1-(4-MONO- AND DI-HALOMETHYLSULPHONYLPHENYL)-2-ACYLAMINO-3-FLUOROPROPONALS AND PREPARATION THEREOF
    2.
    发明申请
    ANTIBACTERIAL 1-(4-MONO- AND DI-HALOMETHYLSULPHONYLPHENYL)-2-ACYLAMINO-3-FLUOROPROPONALS AND PREPARATION THEREOF 失效
    抗真菌剂1-（4-单 - 和对 - 二甲基磺酰基苯基）-2-亚氨基-3-氟代丙烯酸酯及其制备方法

    公开(公告)号：US20080146527A1

    公开(公告)日：2008-06-19

    申请号：US12038105

    申请日：2008-02-27

    申请人： Dale E. Shuster ,  Scott Hecker ,  Tomasz W. Glinka ,  Rajeshwar Singh ,  Zhuoyi Su

    发明人： Dale E. Shuster ,  Scott Hecker ,  Tomasz W. Glinka ,  Rajeshwar Singh ,  Zhuoyi Su

    IPC分类号： A61K31/165 ,  C07F9/09 ,  A61K31/661 ,  A61P31/04

    CPC分类号： C07F9/094 ,  A61K31/165 ,  A61K31/661 ,  C07C317/32 ,  C07F9/091 ,  Y02A50/475

    摘要： Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

    摘要翻译： 具有化学结构的新型氟苯尼考化合物：或其药学上可接受的盐或其溶剂化物或其前药，其中R 1是CHCl 2，CHClF，CHF CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 3 CH （R 2）NH 2或CH X 1 X 2 2; 其中R 2是H，CH 3或CH 2 OH，X 1和X 2 是独立选择的卤素; 和R 3是CH 2 CH 2，CH 2 F，CHF 2，CHCl 2， SUB或CH 2 OH。 该化合物可用于治疗和/或预防广泛范围的患者中的细菌感染，例如但不限于鸟类，鱼类，贝类和哺乳动物。

    Antibacterial 1-(4-mono- and di-halomethylsulphonylphenyl)-2-acylamino-3-fluoroproponals and preparation thereof
    3.
    发明授权
    Antibacterial 1-(4-mono- and di-halomethylsulphonylphenyl)-2-acylamino-3-fluoroproponals and preparation thereof 失效
    抗菌1-（4-单和二卤甲基磺酰基苯基）-2-酰基氨基-3-氟丙酮及其制备方法

    公开(公告)号：US07361689B2

    公开(公告)日：2008-04-22

    申请号：US11018156

    申请日：2004-12-21

    申请人： Dale E. Shuster ,  Scott Hecker ,  Tomasz W. Glinka ,  Rajeshwar Singh ,  Zhuoyi Su

    发明人： Dale E. Shuster ,  Scott Hecker ,  Tomasz W. Glinka ,  Rajeshwar Singh ,  Zhuoyi Su

    IPC分类号： A61K31/16 ,  C07C317/34

    CPC分类号： C07F9/094 ,  A61K31/165 ,  A61K31/661 ,  C07C317/32 ,  C07F9/091 ,  Y02A50/475

    摘要： Novel florfenicol compounds having the chemical structure: or a pharmaceutically-acceptable salt thereof or a solvate thereof, or prodrug thereof, wherein R1 is CHCl2, CHClF, CHF2, CHBrCl, CH3, CH2N3, CH2CN, CH(R2)NH2 or CH X1X2; where R2 is H, CH3 or CH2OH, and X1 and X2 are independently selected halogens; and R3 is CH2Cl, CH2F, CHF2, CHCl2 or CH2OH are disclosed. The compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals.

    摘要翻译： 具有化学结构的新型氟苯尼考化合物：或其药学上可接受的盐或其溶剂化物或其前药，其中R 1是CHCl 2，CHClF，CHF CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 2 CH 3 CH （R 2）NH 2或CH X 1 X 2 2; 其中R 2是H，CH 3或CH 2 OH，X 1和X 2 是独立选择的卤素; 和R 3是CH 2 CH 2，CH 2 F，CHF 2，CHCl 2， SUB或CH 2 OH。 该化合物可用于治疗和/或预防广泛范围的患者中的细菌感染，例如但不限于鸟类，鱼类，贝类和哺乳动物。

    Cephalosporin antibiotics
    5.
    发明授权
    Cephalosporin antibiotics 失效
    头孢菌素类抗生素

    公开(公告)号：US6087355A

    公开(公告)日：2000-07-11

    申请号：US730042

    申请日：1996-10-11

    申请人： In-Seop Cho ,  Scott J. Hecker ,  Tomasz W. Glinka ,  Ving J. Lee ,  Zhijia J. Zhang

    发明人： In-Seop Cho ,  Scott J. Hecker ,  Tomasz W. Glinka ,  Ving J. Lee ,  Zhijia J. Zhang

    IPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D277/40 ,  C07D277/44 ,  C07D277/46 ,  C07D501/00 ,  C07D501/24 ,  C07D501/59

    CPC分类号： C07D501/00

    摘要： The present invention includes novel compounds of formula ##STR1## where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, SO.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR2## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

    摘要翻译： 本发明包括新的式A化合物，其中A，B，D和E选自碳，氮和硫，R99选自硫，SO，SO 2，NH，N-烷基， 氧，C = C（顺式或反式）和C 3BOND C，R 12为NR 13 R 14。本发明还包括对广谱生物体表现出抗生素活性的药理学上可接受的盐，包括对β-内酰胺抗生素具有抗性的生物体， 作为抗菌剂是有用的。 本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

    Cephalosporin antibiotics
    7.
    发明授权
    Cephalosporin antibiotics 失效
    头孢菌素类抗生素

    公开(公告)号：US6030965A

    公开(公告)日：2000-02-29

    申请号：US940508

    申请日：1997-09-30

    申请人： In-Seop Cho ,  Scott J. Hecker ,  Tomasz W. Glinka ,  Ving J. Lee ,  Zhijia J. Zhang

    发明人： In-Seop Cho ,  Scott J. Hecker ,  Tomasz W. Glinka ,  Ving J. Lee ,  Zhijia J. Zhang

    IPC分类号： C07D501/00 ,  C07D501/59 ,  A61K31/545

    CPC分类号： C07D501/00

    摘要： The present invention includes novel compounds of formula where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, S0.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR1## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

    摘要翻译： 本发明包括新的式A化合物，其中A，B，D和E选自碳，氮和硫，R99选自硫，SO，SO 2，NH，N-烷基， 氧，C = C（顺式或反式）和C 3BOND C，R 12为NR 13 R 14。本发明还包括对广谱生物体表现出抗生素活性的药理学上可接受的盐，包括对β-内酰胺抗生素具有抗性的生物体， 作为抗菌剂是有用的。 本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

    Cephalosporin antibiotics
    10.
    发明授权
    Cephalosporin antibiotics 失效
    头孢菌素类抗生素

    公开(公告)号：US6057312A

    公开(公告)日：2000-05-02

    申请号：US728233

    申请日：1996-10-11

    申请人： In-Seop Cho ,  Scott J. Hecker ,  Tomasz W. Glinka ,  Ving J. Lee ,  Zhijia J. Zhang

    发明人： In-Seop Cho ,  Scott J. Hecker ,  Tomasz W. Glinka ,  Ving J. Lee ,  Zhijia J. Zhang

    IPC分类号： C07D277/20 ,  A61K31/00 ,  A61K31/545 ,  A61K31/546 ,  A61P31/00 ,  A61P31/04 ,  C07D277/40 ,  C07D277/44 ,  C07D277/46 ,  C07D501/00 ,  C07D501/24 ,  C07D501/59

    CPC分类号： C07D501/00

    摘要： The present invention includes novel compounds of formula ##STR1## where G, H, J, L and M are carbon or nitrogen, R.sup.99 is selected from the group consisting of sulfur, SO, SO.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR2## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

    摘要翻译： 本发明包括新的式G化合物，其中G，H，J，L和M是碳或氮，R99选自硫，SO，SO2，NH，N-烷基，氧，C = C 或反式），和C 3 B C，R 12为NR 13 R 14。本发明还包括对广谱生物体具有抗生素活性的药理学上可接受的盐，包括对β-内酰胺抗生素具有抗性的生物，并且可用作抗菌剂。 本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。