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    Compositions having antibiotic properties
    1.
    发明授权
    Compositions having antibiotic properties 失效
    具有抗生素性质的组合物

    公开(公告)号：US4134972A

    公开(公告)日：1979-01-16

    申请号：US850742

    申请日：1977-11-11

    申请人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Peter S. Ringrose ,  Robert W. Lambert

    发明人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Peter S. Ringrose ,  Robert W. Lambert

    IPC分类号： A61K31/66 ,  A61K38/04 ,  C07F9/30 ,  C07F9/40 ,  C08G69/10 ,  A61K37/00 ,  A61K31/43 ,  A61K31/54

    CPC分类号： C08G69/10 ,  A61K31/66 ,  A61K38/04 ,  C07F9/301 ,  C07F9/4006 ,  Y10S930/19 ,  Y10S930/29

    摘要： Compositions having antibiotic properties containing as antibiotic potentiators peptides of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl, lower cycloalkyl, (lower cycloalkyl)-(lower alkyl), aryl or aryl(lower alkyl) group (said group being optionally substituted as the case may require by one or more amino, hydroxy, thio, methylthio, carboxy or guanidino groups so as to form the characterizing group of a naturally occurring L .alpha.-amino acid);R.sup.2 and R.sup.3 each represent the characterizing group of an .alpha.-amino acid of the type normally found in proteins with the proviso that R.sup.3 cannot represent a hydrogen atom when n is zero and R.sup.1 is a hydrogen atom or the phenyl group; R.sup.4 represents a hydroxy or methyl group; n stands for zero, 1, 2 or 3; and single asterisks denote that the configuration at the carbon atom so-marked is L when R.sup.2 or R.sup.3 as the case may be represents other than a hydrogen atom; and the double asterisk denotes that, when R.sup.1 represents other than a hydrogen atom, the configuration at the carbon atom so-marked is (R) (as hereinafter defined), and an antibiotic are disclosed.

    摘要翻译： 具有抗生素特性的组合物，其含有下式的抗生素增强剂肽：其中R 1表示氢原子或低级烷基，低级环烷基，（低级环烷基） - （低级烷基），芳基或芳基（低级烷基） 根据情况可以通过一个或多个氨基，羟基，硫代，甲硫基，羧基或胍基进行取代，以形成天然存在的Lα-氨基酸的表征基团）; R2和R3各自表示通常在蛋白质中发现的α-氨基酸的表征基团，条件是当n为0且R 1为氢原子或苯基时，R 3不能表示氢原子; R4表示羟基或甲基; n代表零，1,2或3; 并且单个星号表示当R2或R3表示除氢原子之外时，所标示的碳原子上的构型为L; 并且双星号表示当R 1表示除氢原子以外时，所示标记的碳原子上的构型为（R）（如下文定义），并且公开了抗生素。

    Acyl derivatives
    3.
    发明授权
    Acyl derivatives 失效
    酰基衍生物

    公开(公告)号：US4250085A

    公开(公告)日：1981-02-10

    申请号：US971156

    申请日：1978-12-20

    申请人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Robert W. Lambert ,  Peter S. Ringrose

    发明人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Robert W. Lambert ,  Peter S. Ringrose

    IPC分类号： C07K5/04 ,  A61K38/00 ,  A61P31/04 ,  C07F9/38 ,  C07K1/113 ,  C07K5/06 ,  C07K5/08 ,  C07C103/52 ,  A61K37/00 ,  C07G7/00

    CPC分类号： C07K5/0827 ,  C07F9/3808 ,  C07K5/06191 ,  A61K38/00 ,  Y02P20/55 ,  Y10S930/27

    摘要： Peptide derivatives provided by the present invention are compounds of the general formula ##STR1## wherein R.sup.1 represents a hydrogen atom or the methyl or hydroxymethyl group or a mono-, di- or trihalomethyl mgroup; R.sup.2 represents the characterizing group of an .alpha.-amino acid of the type normally found in proteins or a lower alkyl or hydroxy- (lower alkyl) group other than the characterising group of an .alpha.-amino acid of the type normally found in proteins; R.sup.3 represents a lower alkyl, lower cycloalkyl, lower alkenyl, aryl or aryl-(lower alkyl) group; R.sup.4 represents a hydrogen atom or a lower alkyl group; n stands for 1,2 or 3; the configuration at the carbon atom designated as (a) is (R) when R.sup.1 represents other than a hydrogen atom and the configuration at the carbon atom designated as (b) is (L) when R.sup.2 represents other than a hydrogen atom, and pharmaceutically acceptable salts thereof.The compounds exhibit activity as antibacterial agents against a range of gram-positive and gram-negative bacteria. Also disclosed are intermediates and a process for the production of the end product.

    摘要翻译： 本发明提供的肽衍生物是通式为“IMAGE”的化合物，其中R 1表示氢原子或甲基或羟甲基或单，二或三卤甲基基团; R2代表通常存在于蛋白质中的α-氨基酸的表征基团或除通常在蛋白质中发现的α-氨基酸的特征基团以外的低级烷基或羟基 - （低级烷基）基团; R3表示低级烷基，低级环烷基，低级烯基，芳基或芳基 - （低级烷基）基团; R4代表氢原子或低级烷基; n代表1,2或3; 当R 1表示除氢原子之外时，指定为（a）的碳原子上的构型为（R），当R 2表示氢原子以外，以（b）表示的碳原子上的构型为（L） 其可接受的盐。 该化合物表现出针对一系列革兰氏阳性和革兰氏阴性细菌的抗菌剂的活性。 还公开了中间体和用于生产最终产品的方法。

    Compositions having antibiotic properties
    5.
    发明授权
    Compositions having antibiotic properties 失效
    具有抗生素性质的组合物

    公开(公告)号：US4127649A

    公开(公告)日：1978-11-28

    申请号：US799791

    申请日：1977-05-23

    申请人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Peter S. Ringrose ,  Robert W. Lambert

    发明人： Frank R. Atherton ,  Michael J. Hall ,  Cedric H. Hassall ,  Peter S. Ringrose ,  Robert W. Lambert

    IPC分类号： A61K31/66 ,  A61K38/00 ,  C07F9/30 ,  C07F9/40 ,  C07K5/06 ,  C08G69/10 ,  A61K37/00 ,  A61K31/43

    CPC分类号： C08G69/10 ,  A61K31/66 ,  C07F9/301 ,  C07F9/4006 ,  C07K5/06191 ,  A61K38/00

    摘要： Compositions having antibiotic properties containing as antibiotic potentiators peptides of the formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a lower alkyl, lower cycloalkyl, (lower cycloalkyl)-(lower alkyl), aryl or aryl-(lower alkyl) group (said group being optionally substituted as the case may require by one or more amino, hydroxy, thio, methylthio, carboxy or guanidino groups so as to form the characterizing group of a naturally occurring L .alpha.-amino acid);R.sup.2 and R.sup.3 each represent the characterizing group of an .alpha.-amino acid of the type normally found in proteins with the proviso that R.sup.3 cannot represent a hydrogen atom when n is zero and R.sup.1 is a hydrogen atom or the phenyl group; R.sup.4 represents a hydroxy or methyl group; n stands for zero, 1, 2 or 3; and single asterisks denote that the configuration at the carbon atom so-marked is L when R.sup.2 or R.sup.3 as the case may be represents other than a hydrogen atom; and the double asterisk denotes that, when R.sup.1 represents other than a hydrogen atom, the configuration at the carbon atom so-marked is (R) (as hereinafter defined),And an antibiotic are disclosed.

    摘要翻译： 具有抗生素特性的组合物，其含有下式的抗生素增效剂肽：其中R 1表示氢原子或低级烷基，低级环烷基，（低级环烷基） - （低级烷基），芳基或芳基 - （低级烷基） 基团可以被一个或多个氨基，羟基，硫代，甲硫基，羧基或胍基基团任选取代，以形成天然存在的Lα-氨基酸的表征基团）; R2和R3各自表示通常在蛋白质中发现的α-氨基酸的表征基团，条件是当n为0且R 1为氢原子或苯基时，R 3不能表示氢原子; R4表示羟基或甲基; n代表零，1,2或3; 并且单个星号表示当R2或R3表示除氢原子之外时，所标示的碳原子上的构型为L; 并且双星号表示当R1表示除氢原子以外的情况下，所示标记的碳原子上的构型为（R）（如下文定义），并且具有抗菌活性。