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    Antimicrobial agents
    1.
    发明授权
    Antimicrobial agents 失效
    抗微生物剂

    公开(公告)号：US07323596B2

    公开(公告)日：2008-01-29

    申请号：US10433625

    申请日：2001-12-21

    申请人： Barry Porter ,  Paul Gane ,  Raymond Beckett ,  Kenneth Keavey ,  Jac Wijkmans ,  Lydia Saroglou

    发明人： Barry Porter ,  Paul Gane ,  Raymond Beckett ,  Kenneth Keavey ,  Jac Wijkmans ,  Lydia Saroglou

    IPC分类号： C07C239/00 ,  C07C259/00 ,  C07C303/00 ,  C07C307/00 ,  C07C309/00 ,  C07C311/00

    CPC分类号： C07D285/10 ,  C07C259/06 ,  C07C311/19 ,  C07D209/18 ,  C07D215/56 ,  C07D217/22 ,  C07D263/12 ,  C07D311/12 ,  C07D491/04

    摘要： Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(═O) or of formula C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(═O), a hydroxy or amino group; R2 represents a radical of formula R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or an optionally substituted c1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 ?alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent NH—, —O— or S— linkages, X represents NH—, —O— or S—, and m and n are independently 0 or 1; R3 represents hydrogen, C1-C6alkyl, or benzyl; and R4 is as defined in the specification.

    摘要翻译： 式（I）和（IA）的化合物具有抗菌或抗原虫活性：式（1）式（2）其中：Z表示式N（OH）CH（-O）或式C（-O）NH （哦）; R 1表示氢，甲基或三氟甲基，或除Z是式N（OH）CH（-O），羟基或氨基基团时; R 2表示式R 10 - （X）n - （ALK）m - 的基团，其中R C 1 -C 10烷基，C 2 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 6个烯基，C 2 -C 6炔基，环烷基，芳基或杂环基，ALK表示直链或支链二价C 1 - “C” - “C” - “00”“”=“2.46mm”wi =“1.44mm”file = “US07323596-20080129-P00001.TIF”alt =“自定义字符”img-content =“character”img-format =“tif”/> 6亚链烯基或C 2 -C 6个亚炔基，并且可以被一个或多个不相邻的NH-，-O-或S-键间隔，X表示NH-，-O-或S-，m和n独立地为0或 1; R 3表示氢，C 1 -C 6烷基或苄基; R 4和R 4如本说明书中所定义。

    Bacterial enzyme inhibitors
    3.
    发明授权
    Bacterial enzyme inhibitors 失效
    细菌酶抑制剂

    公开(公告)号：US07241921B2

    公开(公告)日：2007-07-10

    申请号：US10497494

    申请日：2002-11-27

    申请人： Paul Gane ,  Barry Porter ,  Henriette Willems ,  Raymond Paul Beckett ,  Kenneth Keavey

    发明人： Paul Gane ,  Barry Porter ,  Henriette Willems ,  Raymond Paul Beckett ,  Kenneth Keavey

    IPC分类号： C07C259/04 ,  A61K31/19

    CPC分类号： C07D213/40 ,  C07C275/24 ,  C07C2601/08 ,  C07D295/215

    摘要： Compounds of formula (I) are antibacterial agents: wherein: Z is —N(OH)CH(═O) or —C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl or, except when Z is a radical of formula —N(OH)CH(═O), a hydroxy, halo or amino group; R2, R3 and R4 independently represents hydrogen or a group R10—(D)n—(ALK)m— wherein R10, D, n, m and ALK are as defined in the claims; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom to which R4 and R5 are attached and the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen

    摘要翻译： 式（I）化合物是抗菌剂：其中：Z是-N（OH）CH（-O）或-C（-O）NH（OH）; 除了当Z是式-N（OH）CH（-O），羟基，卤素或氨基基团时，R 1表示氢，甲基或三氟甲基。 R 2，R 3和R 4独立地表示氢或基团R 10 - （D）

    Antibacterial agents
    5.
    发明申请
    Antibacterial agents 审中-公开
    抗菌剂

    公开(公告)号：US20060089363A1

    公开(公告)日：2006-04-27

    申请号：US10510600

    申请日：2003-04-09

    申请人： Andrew Ayscough ,  Kenneth Keavey

    发明人： Andrew Ayscough ,  Kenneth Keavey

    IPC分类号： A61K31/496 ,  A61K31/495 ,  C07D403/02 ,  C07D401/02 ,  A61K31/4545 ,  A61K31/445

    CPC分类号： C07D513/04 ,  C07D211/58 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14

    摘要： Compounds of formula (II) have antibacterial activity: wherein Q represents a radical of formula —N(OH)CH(═0) or formula —C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula —N(OH)CH(═0), a hydroxy, halo or amino group; R2 represents a group R10-(V)n-(ALK)m- wherein R10 represents hydrogen, or an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, V represents —NH—, —O— or —S—, m and n are independently 0 or 1; R3 represents the side chain of a natural or non-natural alpha amino acid; R4 represents hydrogen or C1-C3 alkyl; Y represents N or CH; ring A is optionally substituted on one or more ring carbon atoms by C1-C3 alkyl, C1-C3 alkoxy, or halo; and R5 represents a group (IIA): wherein m is 0 or 1; Alk1 represents a divalent C1-C3 alkylene radical; Z represents hydrogen or an optionally substituted cycloalkyl, phenyl or heterocyclic group.

    摘要翻译： 式（II）化合物具有抗菌活性：其中Q表示式-N（OH）CH（-O）或式-C（-O）NH（OH）的基团; R 1表示氢，甲基或三氟甲基，或除了当Z是式-N（OH）CH（-O），羟基，卤素或氨基基团时; R 2表示基团R 10 - （V）n - （ALK）m - 其中R 10 表示氢，或任选取代的C 1 -C 6烷基，C 2 -C 6烷基， C 1 -C 12烷基，C 2 -C 6炔基，环烷基，芳基或杂环基，ALK表示直链或支链二价C 1 -C 12烷基， -C 6亚烷基，C 2 -C 6亚烯基或C 2 -C 6亚炔基，并且可被一个或多个非 - 相邻的-NH-，-O-或-S-键，V表示-NH-，-O-或-S-，m和n独立地为0或1; R 3表示天然或非天然α氨基酸的侧链; R 4表示氢或C 1 -C 3烷基; Y表示N或CH; 环A任选在一个或多个环碳原子上被C 1 -C 3烷基取代，C 1 -C 3 - 烷氧基或卤素; 和R 5表示基团（IIA）：其中m为0或1; Alk 1表示二价C 1 -C 3亚烷基; Z表示氢或任选取代的环烷基，苯基或杂环基。