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    Cationic oligopeptides having microbicidal activity
    4.
    发明授权
    Cationic oligopeptides having microbicidal activity 失效
    具有杀菌活性的阳离子寡肽

    公开(公告)号：US4659692A

    公开(公告)日：1987-04-21

    申请号：US609410

    申请日：1984-05-11

    申请人： Robert I. Lehrer ,  Michael E. Selsted

    发明人： Robert I. Lehrer ,  Michael E. Selsted

    IPC分类号： A61K38/00 ,  C07K14/47 ,  A61K37/02 ,  C07K7/10

    CPC分类号： C07K14/4723 ,  A61K38/00 ,  Y10S930/19

    摘要： Novel microbicidal compositions are provided which find use as preservatives, disinfectants, antigens and the like. Particularly, cationic oligopeptides of up to about thirty-five amino acids are provided having amino acid sequences substantially comparable to the amino acid sequences of cationic oligopeptides produced by macrophage. A conserved framework structure is provided.The invention described herein was in the course, or under a grant from the United States Public Health Service and the National Institutes of Health.

    摘要翻译： 提供新的杀微生物组合物，其用作防腐剂，消毒剂，抗原等。 特别地，提供高达约35个氨基酸的阳离子寡肽，其具有与由巨噬细胞产生的阳离子寡肽的氨基酸序列基本上相当的氨基酸序列。 提供了一种保守的框架结构。 本文描述的发明是在美国公共卫生局和美国国立卫生研究院的授课中。

    Clavanins
    5.
    发明授权
    Clavanins 失效
    克拉夫人

    公开(公告)号：US6040293A

    公开(公告)日：2000-03-21

    申请号：US810324

    申请日：1997-02-28

    申请人： Robert I. Lehrer ,  Chengquan Zhao ,  In-Hee Lee

    发明人： Robert I. Lehrer ,  Chengquan Zhao ,  In-Hee Lee

    IPC分类号： A61K38/00 ,  C07K14/435 ,  C12N1/21 ,  C12N15/12 ,  C07K14/00 ,  A61K37/02

    CPC分类号： C07K14/43504 ,  A61K38/00

    摘要： Novel microbial peptides called clavanins are of the formula[X'.sub.1 X.sub.2 B'.sub.3 X.sub.4 X.sub.5 ]U.sub.6 B.sub.7 X.sub.8 X.sub.9 B.sub.10 B.sub.11 X.sub.12 U.sub.13 Z.sub.14 X.sub.15 X.sub.16 B*.sub.17 U.sub.18 X.sub.19 U.sub.20 B.sub.21 X.sub.22 X.sub.23 ( 1)(SEQ ID NO:1)including the salts, esters, amides and acylated forms thereofwherein X is a hydrophobic amino acid residue or modified form thereof;X' is a small or a hydrophobic amino acid residue or a modified form thereof;B is a basic amino acid residue or modified form thereof;B' is basic or a polar/large amino acid residue or modified form thereof; andB* is a basic or a hydrophobic amino acid residue or a modified form thereof;U is a small amino acid residue or modified form thereof;Z is a polar/large amino acid residue or modified form thereof, and wherein 1-5 amino acids is deleted from the N-terminus.

    摘要翻译： 称为克拉维宁的新型微生物肽具有式[X'1X2B'3X4X5] U6B7X8X9B10B11X12U13Z14X15X16B * 17U18X19U20B21X22X23（1）（1）（SEQ ID NO：1），其包括其盐，酯，酰胺和酰化形式，其中X是疏水性氨基酸残基或经修饰 形式; X'是小或疏水性氨基酸残基或其修饰形式; B是碱性氨基酸残基或其修饰形式; B'是碱性或极性/大氨基酸残基或其修饰形式; B *是碱性或疏水性氨基酸残基或其修饰形式; U是小氨基酸残基或其修饰形式; Z是极性/大的氨基酸残基或其修饰形式，其中1-5个氨基酸从N-末端缺失。

    Retrocyclins: antiviral and antimicrobial peptides
    7.
    发明授权
    Retrocyclins: antiviral and antimicrobial peptides 有权
    逆转录酶：抗病毒和抗菌肽

    公开(公告)号：US06713078B2

    公开(公告)日：2004-03-30

    申请号：US10141645

    申请日：2002-05-06

    申请人： Robert I. Lehrer ,  Alan J. Waring ,  Alexander M. Cole ,  Teresa B. Hong

    发明人： Robert I. Lehrer ,  Alan J. Waring ,  Alexander M. Cole ,  Teresa B. Hong

    IPC分类号： A01N2500

    CPC分类号： C07K14/4723 ,  A61K38/00 ,  C07K7/64

    摘要： Retrocyclin peptides are small antimicrobial agents with potent activity against bacteria and viruses. The peptides are nonhemolytic, and exhibit minimal in vitro cytotoxicity. A pharmaceutical composition comprising retrocyclin as an active agent is administered therapeutically to a patient suffering from a bacterial and/or viral infection, or to an individual facing exposure to a bacterial and/or viral infection, especially one caused by the HIV-1 retrovirus or other sexually-transmitted pathogens.

    摘要翻译： 逆转录肽是针对细菌和病毒的有效活性的小抗微生物剂。 肽是非溶血性的，并且表现出最小的体外细胞毒性。 包含逆转录酶作为活性剂的药物组合物治疗性地给予患有细菌和/或病毒感染的患者或面临暴露于细菌和/或病毒感染的个体，特别是由HIV-1逆转录病毒或 其他性传播病原体。

    Novispirins: antimicrobial peptides
    8.
    发明授权
    Novispirins: antimicrobial peptides 有权

    公开(公告)号：US06492328B2

    公开(公告)日：2002-12-10

    申请号：US09840009

    申请日：2001-04-19

    申请人： Robert I. Lehrer ,  Alan J. Waring ,  Brian F. Tack

    发明人： Robert I. Lehrer ,  Alan J. Waring ,  Brian F. Tack

    IPC分类号： A61K3800

    CPC分类号： C07K7/08 ,  A61K38/00 ,  Y02A50/473

    摘要： Novispirin peptides are antimicrobial agents with potent activity against Gram-negative bacteria. The peptides are nonhemolytic, exhibit reduced in vitro cytotoxicity relative to other antimicrobial peptides, and were well-tolerated in vivo after intravenous injection. Novispirins also bind lipopolysaccharide (LPS), a property that may mitigate symptoms associated with Gram-negative bacterial infection. A pharmaceutical composition comprising novispirin as an active agent is administered to a patient suffering from or predisposed to a microbial infection, particularly Gram-negative bacterial infections.

    Compositions and methods for treating and preventing microbial and viral infections
    9.
    发明授权
    Compositions and methods for treating and preventing microbial and viral infections 有权
    用于治疗和预防微生物和病毒感染的组合物和方法

    公开(公告)号：US6159936A

    公开(公告)日：2000-12-12

    申请号：US128345

    申请日：1998-08-03

    申请人： Robert I. Lehrer ,  Sylvia S. L. Harwig ,  Vladimir N. Kokryakov

    发明人： Robert I. Lehrer ,  Sylvia S. L. Harwig ,  Vladimir N. Kokryakov

    IPC分类号： A01N63/02 ,  A61K38/00 ,  C07K7/08 ,  C07K16/18 ,  C12N15/12 ,  C12P21/04 ,  A61K38/04 ,  C07K7/00 ,  C12P21/02

    CPC分类号： C07K7/08 ,  A01N63/02 ,  A61K38/00 ,  C07K16/18 ,  Y02A50/473 ,  Y02A50/481

    摘要： Peptide-based compounds containing four invariant cysteine residues which have been optionally oxidized to contain two intramolecular disulfide bonds, or modified forms where the cysteines are replaced are useful as preservatives and in preventing, treating, or ameliorating viral or microbial infection in animals and plants, and in inactivating endotoxin. These compounds, in one embodiment, are of the formula:A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --A.sub.5 --A.sub.6 --A.sub.7 --A.sub.8 --A.sub.9 --A.sub.10 --A.sub.11 --A.sub.12 --A.sub.13 --A.sub.14 --A.sub.15 --A.sub.16 --(A.sub.17 --A.sub.18) (1)and the N-terminal acylated and/or C-terminal amidated or esterified forms thereof, which is either in the optionally --SH stablizied linear or in a cystine-bridged formwherein each of A.sub.1 and A.sub.9 is independently a basic amino acid;each of A.sub.2 and A.sub.3 is independently a small amino acid;each of A.sub.5, A.sub.7, A.sub.12, A.sub.14 and A.sub.16 is independently a hydrophobic amino acid;A.sub.4 is a basic or a small amino acid;A.sub.10 is a basic or a small amino acid or is proline;A.sub.11 is a basic or hydrophobic amino acid;A.sub.17 is not present or, if present, is a small amino acid;A.sub.18 is not present or, if present, is a basic amino acid; or amodified form of formula (1) and the N-terminal acylated and/or C-terminal amidated or esterified forms thereof wherein each of 1-4 cysteines is independently replaced by a hydrophobic amino acid or a small amino acid.

    摘要翻译： 含有四个不变半胱氨酸残基的基于肽的化合物，其被任选地氧化成含有两个分子内二硫键，或其中替代半胱氨酸的修饰形式可用作防腐剂，并且用于预防，治疗或改善动物和植物中的病毒或微生物感染， 并灭活内毒素。 这些化合物在一个实施方案中具有下式：A1-A2-A3-A4-A5-A6-A7-A8-A9-A10-A11-A12-A13-A14-A15-A16-（A17-A18）（ 1）和其N-末端酰化和/或C末端酰胺化或酯化形式，其以任选-SH稳定的线性或胱氨酸桥接形式，其中A1和A9各自独立地为碱性氨基酸; A2和A3各自独立地是小氨基酸; A5，A7，A12，A14和A16各自独立地是疏水性氨基酸; A4是碱性或小氨基酸; A10是碱性或小氨基酸，或是脯氨酸; A11是碱性或疏水性氨基酸; A17不存在，或者如果存在，则是小氨基酸; A18不存在，或者如果存在，则是碱性氨基酸; 或式（1）的修饰形式和其N-末端酰化和/或C-末端酰胺化或酯化形式，其中1-4个半胱氨酸中的每一个独立地被疏水性氨基酸或小氨基酸替代。

    Clavaspirins
    10.
    发明授权
    Clavaspirins 失效
    克拉霉素

    公开(公告)号：US5998374A

    公开(公告)日：1999-12-07

    申请号：US808277

    申请日：1997-02-28

    申请人： Robert I. Lehrer ,  In-Hee Lee ,  Chengquan Zhao

    发明人： Robert I. Lehrer ,  In-Hee Lee ,  Chengquan Zhao

    IPC分类号： A61K38/00 ,  A61P43/00 ,  C07K14/435 ,  C12N15/12 ,  A61K38/17

    CPC分类号： C07K14/43504 ,  A61K38/00

    摘要： Novel microbial peptides called clavaspirins are of the formula (SEQ ID NO:1)X'.sub.1 X.sub.2 B'.sub.3 X.sub.4 X.sub.5 U.sub.6 U.sub.7 X.sub.8 X.sub.9 B.sub.10 X'.sub.11 X.sub.12 U.sub.13 B.sub.14 X.sub.15 X.sub.16 B*.sub.17 B.sub.18 X.sub.19 U.sub.20 X.sub.21 X'.sub.22 X.sub.23 (1)including the salts, esters, amides and acylated forms thereofwherein X is a hydrophobic amino acid residue or modified form thereof;X' is a small or a hydrophobic amino acid residue or a modified form thereof;B is a basic amino acid residue or modified form thereof;B' is basic or a polar/large amino acid residue or modified form thereof;B* is a basic or a hydrophobic amino acid residue or a modified form thereof; andU is a small amino acid residue or modified form thereof.

    摘要翻译： 称为克拉斯匹林的新型微生物肽具有式（SEQ ID NO：1）X'1X2B'3X4X5U6U7X8X9B10X'11X12U13B14X15X16B * 17B18X19U20X21X'22X23（1），其包括其盐，酯，酰胺和酰化形式，其中X是疏水性氨基酸残基或 其修改形式; X'是小或疏水性氨基酸残基或其修饰形式; B是碱性氨基酸残基或其修饰形式; B'是碱性或极性/大氨基酸残基或其修饰形式; B *是碱性或疏水性氨基酸残基或其修饰形式; U是小氨基酸残基或其修饰形式。