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    Substituted oxazine and thiazine oxazolidinone antimicrobials
    1.
    发明授权
    Substituted oxazine and thiazine oxazolidinone antimicrobials 失效
    取代的恶嗪和噻嗪恶唑烷酮抗菌药

    公开(公告)号：US5880118A

    公开(公告)日：1999-03-09

    申请号：US886965

    申请日：1997-07-02

    申请人： Michael R. Barbachyn ,  Steven J. Brickner ,  Douglas K. Hutchinson

    发明人： Michael R. Barbachyn ,  Steven J. Brickner ,  Douglas K. Hutchinson

    IPC分类号： C07D263/20 ,  C07D413/10 ,  C07D417/10 ,  A61K31/42

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D417/10

    摘要： A compound of the Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein X, R, R.sup.1, R.sup.2, R.sup.3 and n are as defined in the disclosure. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci, and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

    摘要翻译： 式I的化合物或其药学上可接受的盐，其中X，R，R 1，R 2，R 3和n如本公开所定义。 恶嗪和噻嗪恶唑烷酮衍生物是对许多人类和兽医病原体有效的有用的抗微生物剂，包括革兰氏阳性好氧细菌如耐多重耐药性葡萄球菌，链球菌和肠球菌，以及厌氧生物如拟杆菌属（Bacteroides spp）。 和梭菌属（Clostridia spp。） 物种和耐酸生物如结核分枝杆菌，鸟分枝杆菌和分枝杆菌属。

    Esters of substituted-hydroxyacetyl piperazine phenyl oxazolidinones
    2.
    发明授权
    Esters of substituted-hydroxyacetyl piperazine phenyl oxazolidinones 失效
    取代羟基乙酰哌嗪苯基恶唑烷酮的酯

    公开(公告)号：US5652238A

    公开(公告)日：1997-07-29

    申请号：US640899

    申请日：1996-05-09

    申请人： Steven J. Brickner ,  Michael R. Barbachyn ,  Douglas K. Hutchinson

    发明人： Steven J. Brickner ,  Michael R. Barbachyn ,  Douglas K. Hutchinson

    IPC分类号： C07D263/24 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  A61P31/04 ,  C07D263/20 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07F9/6558 ,  C07D413/10 ,  C07D413/14

    CPC分类号： C07D263/20 ,  C07D413/12 ,  C07F9/65583

    摘要： A compound of structural Formula (I) or pharmaceutically acceptable salts thereof wherein: R is --C(O)--R.sup.1, --PO.sub.3 .dbd. or --P(O)(OH).sub.2 ; R.sup.1 is C.sub.1-6 alkyl, --N(R.sup.4).sub.2, C.sub.1-6 alkyl-N(R.sup.4).sub.2, --phenyl--N(R.sup.4).sub.2, --phenyl-NHC(O)CH.sub.2 NH.sub.2, --C.sub.2 H.sub.4 -morpholinyl, pyridinyl, C.sub.1-6 alkyl-OH, C.sub.1-6 alkyl-OCH.sub.3, C.sub.1-6 alkyl C(O)CH.sub.3, --O--C.sub.1-6 alkyl-OCH.sub.3, C.sub.0-3 alkyl-piperazinyl (optionally substituted with C.sub.1-3 alkyl), imidazolyl, C.sub.1-6 alkyl-COOH, --C(CH.sub.2 OH).sub.2 CH.sub.3 ; R.sup.2 and R.sup.3 are independently selected from hydrogen or F except at least one of R.sup.2 or R.sup.3 is F; R.sup.4 are independently selected from hydrogen or C.sub.1-6 alkyl. The compounds are water soluble and are useful antimicrobial agents, effective against a number of human veterinary pathogens, including multiply-resistant staphylococci, enterococci and streptococci, as well as anerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis.

    摘要翻译： PCT No.PCT / US94 / 10582 Sec。 371日期：1996年5月9日 102（e）日期1996年5月9日PCT 1994年9月27日PCT公布。 公开号WO95 / 14684 日期：1995年6月1日结构式（I）化合物或其药学上可接受的盐，其中：R为-C（O）-R1，-PO3 =或-P（O）（OH）2; R1是C1-6烷基，-N（R4）2，C1-6烷基-N（R4）2， - 苯基-N（R4）2， - 苯基-NHC（O）CH2NH2，-C2H4-吗啉基，吡啶基，C1- 6烷基-OH，C 1-6烷基-OCH 3，C 1-6烷基C（O）CH 3，-O-C 1-6烷基-OCH 3，C 3-8烷基 - 哌嗪基（任选被C 1-3烷基取代），咪唑基，C 1-6烷基-COOH， -C（CH 2 OH）2 CH 3; R2和R3独立地选自氢或F，但R 2或R 3中的至少一个为F; R 4独立地选自氢或C 1-6烷基。 这些化合物是水溶性的并且是有用的抗微生物剂，其对许多人类兽用病原体有效，包括耐多重抗性葡萄球菌，肠球菌和链球菌，以及厌氧生物如细菌和梭菌，以及耐酸生物如分枝杆菌 结核。

    Substituted oxazine and thiazine oxazolidinone antimicrobials
    3.
    发明授权
    Substituted oxazine and thiazine oxazolidinone antimicrobials 失效
    取代的恶嗪和噻嗪恶唑烷酮抗菌药

    公开(公告)号：US5688792A

    公开(公告)日：1997-11-18

    申请号：US617877

    申请日：1996-03-05

    申请人： Michael R. Barbachyn ,  Steven J. Brickner ,  Douglas K. Hutchinson

    发明人： Michael R. Barbachyn ,  Steven J. Brickner ,  Douglas K. Hutchinson

    IPC分类号： C07D263/20 ,  C07D413/10 ,  C07D417/10 ,  A61K31/535

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D417/10

    摘要： A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: X is O, S, SO, SO.sub.2, SNR.sup.10 or S(O)NR.sup.10 ; R is (a) hydrogen, (b) C.sub.1 -C.sub.8 alkyl optionally substituted with one or more of the following: F, Cl, hydroxy, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.8 acyloxy or --O--CH.sub.2 --Ph, (c) C.sub.3 -C.sub.6 cycloalkyl, (d) amino, (e) C.sub.1 -C.sub.8 alkylamino, (f) C.sub.1 -C.sub.8 dialkylamino or (g) C.sub.1 -C.sub.8 alkoxy; R.sup.1 is H, except when X is O then R.sup.1 can be H, CH.sub.3, CN, CO.sub.2 H, CO.sub.2 R or (CH.sub.2).sub.m R.sup.11 (m is 1 or 2); R.sup.2 is independently H, F or Cl; R.sup.3 is H except when X is O and R.sup.1 is CH.sub.3 then R.sup.3 can be H or CH.sub.3 ; R.sup.10 is independently H, C.sub.1 -C.sub.4 alkyl (optionally substituted with chloro, fluoro, hydroxy, C.sub.1 -C.sub.8 alkoxy, amino, C.sub.1 -C.sub.8 alkylamino, or C.sub.1 -C.sub.8 dialkylamino) or p-toluenesulfonyl; R.sup.11 is hydrogen, OH, OR, OCOR, NH.sub.2, NHCOR or N(R.sup.10).sub.2 ; and n is 0, 1 or 2. The oxazine and thiazine oxazolidinone derivatives are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.

    摘要翻译： PCT No.PCT / US94 / 08904 Sec。 371日期：1996年3月5日 102（e）1996年3月5日PCT PCT 1994年8月16日PCT公布。 WO95 / 07271 PCT出版物 日期：1995年3月16日结构式I化合物：其中X为O，S，SO，SO 2，SNR 10或S（O）NR 10; R为（a）氢，（b）任选被一个或多个下列基团取代的C 1 -C 8烷基：F，Cl，羟基，C 1 -C 8烷氧基，C 1 -C 8酰氧基或-O-CH 2 Ph，（c） C3-C6环烷基，（d）氨基，（e）C1-C8烷基氨基，（f）C1-C8二烷基氨基或（g）C1-C8烷氧基; R1是H，除非X是O，那么R 1可以是H，CH 3，CN，CO 2 H，CO 2 R或（CH 2）m R 11（m是1或2）; R2独立地为H，F或Cl; R3为H，但当X为O且R 1为CH 3时，R 3为H或CH 3; R 10独立地为H，C 1 -C 4烷基（任选被氯，氟，羟基，C 1 -C 8烷氧基，氨基，C 1 -C 8烷基氨基或C 1 -C 8二烷基氨基取代）或对甲苯磺酰基; R 11是氢，OH，OR，OCOR，NH 2，NHCOR或N（R 10）2; 并且n为0,1或2.恶嗪和噻嗪恶唑烷酮衍生物是有用的抗微生物剂，对许多人和兽医病原体有效，包括革兰氏阳性好氧细菌如耐多重耐药性葡萄球菌，链球菌和肠球菌以及厌氧 生物体如拟杆菌属（Bacteroides spp。） 和梭菌属（Clostridia spp。） 物种和耐酸生物如结核分枝杆菌，鸟分枝杆菌和分枝杆菌属。

    Oxazolidinone antimicrobials containing substituted diazine moieties
    5.
    发明授权
    Oxazolidinone antimicrobials containing substituted diazine moieties 失效
    含有取代的二嗪部分的恶唑烷酮抗微生物剂

    公开(公告)号：US5547950A

    公开(公告)日：1996-08-20

    申请号：US332822

    申请日：1994-10-31

    申请人： Douglas K. Hutchinson ,  Michael R. Barbachyn ,  Steven J. Brickner ,  Ronald B. Gammill ,  Mahesh V. Patel

    发明人： Douglas K. Hutchinson ,  Michael R. Barbachyn ,  Steven J. Brickner ,  Ronald B. Gammill ,  Mahesh V. Patel

    IPC分类号： A61K31/395 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61P31/00 ,  A61P31/04 ,  C07D263/20 ,  C07D263/24 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D413/00

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12

    摘要： A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is chosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.

    摘要翻译： 结构式I的化合物或其药学上可接受的盐，其中：每个n独立地为1至3; Y选自本文定义的a-n; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR1，CO 2 R 1，CN，SR 1或R 1（其中R 1是氢或C 1-4烷基）取代; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。 具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及 耐酸生物如结核分枝杆菌和鸟分枝杆菌。

    Oxazolidinone antimicrobials containing substituted diazine moieties
    7.
    发明授权
    Oxazolidinone antimicrobials containing substituted diazine moieties 失效
    含有取代的二嗪部分的恶唑烷酮抗微生物剂

    公开(公告)号：US5700799A

    公开(公告)日：1997-12-23

    申请号：US610031

    申请日：1996-03-04

    申请人： Douglas K. Hutchinson ,  Michael R. Barbachyn ,  Steven J. Brickner ,  Ronald B. Gammill ,  Mahesh V. Patel

    发明人： Douglas K. Hutchinson ,  Michael R. Barbachyn ,  Steven J. Brickner ,  Ronald B. Gammill ,  Mahesh V. Patel

    IPC分类号： A61K31/395 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61P31/00 ,  A61P31/04 ,  C07D263/20 ,  C07D263/24 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D245/02

    CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12

    摘要： A compound of structural Formula I: ##STR1## or pharmaceutically acceptable salts thereof wherein: each n is independently 1 to 3; Y is choosen from a-n as defined herein; wherein each occurrence of said C.sub.1-6 alkyl may be substituted with one or more F, Cl, Br, I, OR.sup.1, CO.sub.2 R.sup.1, CN, SR.sup.1, or R.sup.1 (where R.sup.1 is a hydrogen or C.sub.1-4 alkyl); X and Z are independently C.sub.1-6 alkyl, C.sub.3-12 cycloalkyl or hydrogen, or X and Z form a C.sub.0-3 bridging group, preferably X and Z are hydrogen; U, V and W are independently C.sub.1-6 alkyl, F, Cl, Br, hydrogen or a C.sub.1-6 alkyl substituted with one or more of F, Cl, Br or I, preferably U and V are F and W is hydrogen; R is hydrogen, C.sub.1-12 alkyl, C.sub.3-12 cycloalkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkyl substituted with one or more F, Cl, Br, I or OH; and q is 0 to 4 inclusive. Oxazolidinone derivatives possessing a substituted diazine moiety bonded to the N-aryl ring are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including multiply-resistant staphylococci and streptococci, as well as anaerobic organisms such as bacteroides and clostridia species, and acid-fast organisms such as Mycobacterium tuberculosis and Mycobacterium avium.

    摘要翻译： 结构式I的化合物或其药学上可接受的盐，其中：每个n独立地为1至3; 从本文定义的a-n中选择Y; 其中所述C 1-6烷基的每次出现可以被一个或多个F，Cl，Br，I，OR1，CO 2 R 1，CN，SR 1或R 1（其中R 1是氢或C 1-4烷基）取代; X和Z独立地是C 1-6烷基，C 3-12环烷基或氢，或X和Z形成C0-3桥连基，优选X和Z是氢; U，V和W独立地是C 1-6烷基，F，Cl，Br，氢或被F，Cl，Br或I中的一个或多个取代的C 1-6烷基，优选U和V是F，W是氢; R是氢，C 1-12烷基，C 3-12环烷基，C 1-6烷氧基，被一个或多个F，Cl，Br，I或OH取代的C 1-6烷基; q为0〜4。 具有与N-芳基环结合的取代的二嗪部分的恶唑烷酮衍生物是有效的抗微生物剂，其对许多人类和兽医病原体有效，包括多重耐药性葡萄球菌和链球菌，以及厌氧生物体如杀菌剂和梭菌属物种，以及 耐酸生物如结核分枝杆菌和鸟分枝杆菌。