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    GOLD (I)-PHOSPHINE COMPOUNDS AS ANTI-BACTERIAL AGENTS
    1.
    发明申请
    GOLD (I)-PHOSPHINE COMPOUNDS AS ANTI-BACTERIAL AGENTS 审中-公开
    金（I） - 磷化合物作为抗菌剂

    公开(公告)号：WO2015181551A1

    公开(公告)日：2015-12-03

    申请号：PCT/GB2015/051551

    申请日：2015-05-28

    申请人： AUSPHERIX LIMITED

    发明人： HOLMES, Ian ,  NAYLOR, Alan ,  NEGOITA-GIRAS, Gabriel ,  POWELL, Jonathan ,  CHARLES, Ian ,  ALBER, Dagmar

    IPC分类号： A61K33/24 ,  A61P31/04

    CPC分类号： C07F1/005 ,  A61K31/28 ,  A61K31/35 ,  A61K31/437 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4465 ,  A61K31/505 ,  A61K31/661 ,  A61K31/665 ,  A61K31/675 ,  A61K33/42 ,  A61K45/06 ,  C07F1/12

    摘要： A compound of formula (I): for use in the prevention or treatment of a bacterial infection wherein: A is either S or Se; RA is selected from: wherein: each of Y 1 , Y 2 , Y 3 , Y 4 and Y 9 is independently selected from CH or N, wherein at least three of Y 1 , Y 2 , Y 3 , Y 4 and Y 9 is CH; V is selected from O, CH-OR 01 , N-CO 2 -R C2 or N-R N2 ; one of Y 5 , Y 6 , Y 7 and Y 8 is selected from CH and N, and the others are CH; X is selected from NH, S or O; R C1 is selected from O-R O2 or NHR N1 ; R O1 is selected from H and C 1-3 unbranched alkyl; R O2 is C 1-3 unbranched alkyl; R N1 is selected from H and C 1-3 unbranched alkyl; R N2 is C 1-3 unbranched alkyl; R C2 is either C 1-3 unbranched alkyl or C 3-4 branched alkyl; R C3 is selected from C 1-3 unbranched alkyl and C 2 H 4 CO 2 H; R C4 is either H or Me; R C5 is either H or Me; R C6 represents one or two optional methyl substituents; and n is an integer from 2 to 8.

    摘要翻译： 式（I）化合物：用于预防或治疗细菌感染，其中：A为S或Se; RA选自：其中：Y 1，Y 2，Y 3，Y 4和Y 9各自独立地选自CH或N，其中Y 1，Y 2，Y 3，Y 4和Y 9中的至少3个是CH; V选自O，CH-OR01，N-CO2-RC2或N-RN2; Y5，Y6，Y7和Y8中的一个选自CH和N，其余为CH; X选自NH，S或O; RC1选自O-RO2或NHRN1; RO1选自H和C 1-3无支链烷基; RO2是C1-3无支链烷基; RN1选自H和C1-3无支链烷基; RN2是C1-3非支链烷基; RC2是C1-3无支链烷基或C3-4支链烷基; RC3选自C 1-3无支链烷基和C 2 H 4 CO 2 H; RC4是H或Me; RC5是H或Me; RC6表示一个或两个任选的甲基取代基; n为2〜8的整数。

    GOLD (I)-PHOSPHINE COMPOUNDS AS ANTI-BACTERIAL AGENTS
    7.
    发明申请
    GOLD (I)-PHOSPHINE COMPOUNDS AS ANTI-BACTERIAL AGENTS 审中-公开
    金（I） - 磷化合物作为抗菌剂

    公开(公告)号：WO2015181550A1

    公开(公告)日：2015-12-03

    申请号：PCT/GB2015/051550

    申请日：2015-05-28

    申请人： AUSPHERIX LIMITED

    发明人： HOLMES, Ian ,  NAYLOR, Alan ,  NEGOITA-GIRAS, Gabriel ,  POWELL, Jonathan ,  CHARLES, Ian ,  ALBER, Dagmar

    IPC分类号： A61K33/24 ,  A61P31/04

    CPC分类号： C07F9/6561 ,  A61K31/66 ,  A61K31/665 ,  A61K31/675 ,  A61K45/06 ,  C07F9/28 ,  C07F9/592 ,  C07F9/65068 ,  C07F9/650917 ,  C07F9/65122 ,  C07F9/6552 ,  A61K2300/00

    摘要： A compound of formula (I) for use in the prevention or treatment of a bacterial infection wherein R P1 is either methyl, ethyl, isopropyl, cyclohexyl or phenyl; R P2 is selected from methyl, ethyl, isopropyl, cyclohexyl and phenyl; R P3 is either ethyl, isopropyl, cyclohexyl, phenyl or pyridyl; A is either S or Se; R A is selected from wherein each of Y 1 , Y 2 , Y 3 , Y 4 and Y 9 is independently selected from CH or N, wherein at least three of Y 1 , Y 2 , Y 3 , Y 4 and Y 9 are CH; V is selected from O, CH-OR O1 , N-CO 2 -R C2 or N-R N2 ; one of Y 5 , Y 6 , Y 7 and Y 8 is selected from CH and N, and the others are CH; X is selected from NH, S or O; R C1 is selected from O-R O2 or NHR N1 ; R O1 is selected from H and C 1-3 unbranched alkyl; R O2 is C 1-3 unbranched alkyl; R N1 is selected from H and C 1-3 unbranched alkyl; R N2 is C 1-3 unbranched alkyl; R C2 is either C 1-3 unbranched alkyl or C 3-4 branched alkyl; R C3 is selected from C 1-3 unbranched alkyl and C 2 H 4 CO 2 H; R C4 is either H or Me; R C5 is either H or Me; R C6 represents one or two optional methyl substituents; and n is an integer from 2 to 8.

    摘要翻译： 用于预防或治疗细菌感染的式（I）化合物，其中RP1为甲基，乙基，异丙基，环己基或苯基; RP2选自甲基，乙基，异丙基，环己基和苯基; RP3是乙基，异丙基，环己基，苯基或吡啶基; A是S或Se; RA选自其中Y1，Y2，Y3，Y4和Y9各自独立地选自CH或N，其中Y1，Y2，Y3，Y4和Y9中的至少三个为CH; V选自O，CH-ORO1，N-CO 2 -RC2或N-RN2; Y5，Y6，Y7和Y8中的一个选自CH和N，其余为CH; X选自NH，S或O; RC1选自O-RO2或NHRN1; RO1选自H和C 1-3无支链烷基; RO2是C1-3无支链烷基; RN1选自H和C1-3无支链烷基; RN2是C1-3非支链烷基; RC2是C1-3无支链烷基或C3-4支链烷基; RC3选自C 1-3无支链烷基和C 2 H 4 CO 2 H; RC4是H或Me; RC5是H或Me; RC6表示一个或两个任选的甲基取代基; n为2〜8的整数。