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    Antibacterial 1-(4-mono- and di-halomethylsulphonylphenyl)-2-acylamino-3-fluoroproponals and preparation thereof
    16.
    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

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

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

    IPC: A61K31/16 ,  C07C317/34

    CPC classification number: C07F9/094 ,  A61K31/165 ,  A61K31/661 ,  C07C317/32 ,  C07F9/091 ,  Y02A50/475

    Abstract: 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.

    Abstract translation: 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。

    4-oxa-1-azabicyclo [3,2,0] heptan-7-one derivatives as antitumor agents
    19.
    发明授权
    4-oxa-1-azabicyclo [3,2,0] heptan-7-one derivatives as antitumor agents 失效
    4-氧杂-1-氮杂双环[3,2,0]庚-7-酮衍生物作为抗肿瘤剂

    公开(公告)号：US5561126A

    公开(公告)日：1996-10-01

    申请号：US362490

    申请日：1995-03-16

    Applicant: Toshio Otani ,  Shinji Oie ,  Hiroshi Matsumoto ,  Mark Tempest ,  Ronald Micetich ,  Rajeshwar Singh ,  Tomohiro Yamashita

    Inventor： Toshio Otani ,  Shinji Oie ,  Hiroshi Matsumoto ,  Mark Tempest ,  Ronald Micetich ,  Rajeshwar Singh ,  Tomohiro Yamashita

    IPC: C07D503/00 ,  A61K31/42 ,  A61P35/00 ,  H61K31/395

    CPC classification number: A61K31/42

    Abstract: The present invention relates to the use of 4-oxa-1-azabicyclo [3,2,0] heptan-7-one derivatives of formula (I) or a pharmaceutically acceptable salt thereof, as antitumor agents. ##STR1## Wherein R is --OCOR.sub.1 group wherein R.sub.1 is hydrogen atom, a C.sub.1-9 alkyl group which may be substituted by either one or two substituents selected together from halogen atom, hydroxy, carboxy group or (3RS,5SR)-(4-oxo-1-azabicyclo[3,2,0]heptan-7-one-3-yl) methyloxycarbonyl, a C.sub.2-17 alkenyl group, which may be substituted by carboxy group or (3RS,5SR)-(4-oxa-1-azabicyclo [3,2,0]heptan-7-one-3-yl)methyloxycarbonyl, A C.sub.2-4 alkynyl group, a C.sub.3-6 cycloalkyl group which may be substituted by carboxy group or phenyl group which may have 1, 2 or 3 substituents selected from the group consisting of cyano group, halogen atom, C.sub.1-6 alkoxy group which may be substituted by carboxy group, C.sub.1-6 alkyl group, amino group or hydroxy group.--OR.sub.2 wherein R.sub.2 is a hydrogen atom or benzyl group which may be substituted by 1 or 2 C.sub.1-6 alkoxy group.--S(O).sub.n R.sub.3 wherein R.sub.3 is phenyl group or a benzyl group which may be substituted by C.sub.1-6 alkyl group, n is 0, 1, or 2;or --CH.sub.2 OH.

    Abstract translation: PCT No.PCT / GB93 / 01435 Sec。 371日期1995年3月16日 102（e）1995年3月16日PCT PCT 1993年7月8日PCT公布。 公开号WO94 / 01109 1994年1月20日的日本本发明涉及式（I）的4-氧杂-1-氮杂双环[3,2,0]庚-7-酮衍生物或其药学上可接受的盐作为抗肿瘤剂。 （I）其中R是-OCOR1基团，其中R1是氢原子，可以被一个或两个选自卤原子，羟基，羧基或（3RS，5SR）的取代基取代的C1-9烷基， - （4-氧代-1-氮杂双环[3,2,0]庚-7-酮-3-基）甲氧基羰基，可被羧基取代的C 2-7烯基或（3RS，5SR） - （ 4-氧杂-1-氮杂双环[3,2,0]庚-7-酮-3-基）甲氧基羰基，C 2-4炔基，可被羧基或苯基取代的C 3-6环烷基， 可以具有1,2或3个选自氰基，卤素原子，可被羧基，C 1-6烷基，氨基或羟基取代的C 1-6烷氧基的取代基。 -OR 2，其中R 2是可被1或2个C 1-6烷氧基取代的氢原子或苄基。 -S（O）n R 3，其中R 3是苯基或可被C 1-6烷基取代的苄基，n是0,1或2; 或-CH 2 OH。

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