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    ANTIMICROBIAL AMINO ACID SEQUENCES DERIVED FROM ALPHA-MELANOCYTE-STIMULATING HORMONE
    52.
    发明申请
    ANTIMICROBIAL AMINO ACID SEQUENCES DERIVED FROM ALPHA-MELANOCYTE-STIMULATING HORMONE 审中-公开
    从阿尔法 - 梅毒刺激激素衍生的抗微生物氨基酸序列

    公开(公告)号：WO00059527A1

    公开(公告)日：2000-10-12

    申请号：PCT/US2000/006917

    申请日：2000-03-17

    IPC分类号： A61K9/02 ,  A61F13/20 ,  A61K9/00 ,  A61K9/06 ,  A61K9/107 ,  A61K9/12 ,  A61K9/20 ,  A61K38/00 ,  A61K38/07 ,  A61K38/34 ,  A61P13/00 ,  A61P15/00 ,  A61P15/18 ,  A61P29/00 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  A61P31/18 ,  C07K5/09 ,  C07K5/103 ,  C07K7/06 ,  C07K7/08 ,  C07K14/575 ,  A61K38/04

    CPC分类号： A61K38/34 ,  A61K9/0034 ,  A61K38/07

    摘要： The peptide a-melanocyte stimulating hormone (a-MSH) is found in barrier organs such as the gut and skin. The anti-inflammatory properties of the peptide make it useful for treating inflammation in human and veterinary disorders. It has been found that this peptide, and other peptides derived from a-MSH, possess antimicrobial activity against Staphylococcus aureus and Candida albicans. These a-MSH peptides exhibited antimicrobial effects over a broad concentration range, including the physiological (picomolar)range. Of particular interest are those peptides that include the amino acid sequence KPV, or those including the sequence MEHFRWG. Peptides having the most potent antimicrobial activity were those bearing the C-terminal amino acid sequence of a-MSH. Anti-inflammatory agents based on a-MSH peptides, with enhanced antimicrobial activity, would minimize the risk of further infection that is generally associated with treatments using coticosteroids or other nonsteroidal anti-inflammatory drugs.

    摘要翻译： 肽 - 黑素细胞刺激激素（a-MSH）被发现在屏障器官如肠和皮肤。 肽的抗炎性质使其可用于治疗人类和兽医疾病中的炎症。 已经发现，该肽和衍生自a-MSH的其它肽具有抗金黄色葡萄球菌和白色念珠菌的抗微生物活性。 这些a-MSH肽在广泛的浓度范围内显示出抗菌作用，包括生理（皮摩尔）范围。 特别感兴趣的是包括氨基酸序列KPV或包括序列MEHFRWG的那些肽。 具有最强抗微生物活性的肽是具有a-MSH的C-末端氨基酸序列的肽。 具有增强的抗微生物活性的基于a-MSH肽的抗炎剂可以将通常与使用类固醇或其他非甾体抗炎药物的治疗相关的进一步感染的风险降至最低。

    PROCESS FOR THE PREPARATION OF RESIN-BOUND CYCLIC PEPTIDES
    54.
    发明申请
    PROCESS FOR THE PREPARATION OF RESIN-BOUND CYCLIC PEPTIDES 审中-公开
    制备树脂环状胶囊的方法

    公开(公告)号：WO99052933A1

    公开(公告)日：1999-10-21

    申请号：PCT/US1999/008435

    申请日：1999-04-15

    IPC分类号： C07K17/08 ,  C07K1/04 ,  C07K5/062 ,  C07K5/078 ,  C07K5/09 ,  C07K5/113 ,  C07K7/04 ,  C07K7/06 ,  C07K7/08 ,  C07K7/54 ,  C07K14/635

    CPC分类号： C07K5/06182 ,  C07K1/04 ,  C07K7/54 ,  C07K14/635

    摘要： This invention is directed to a process for the solid phase, fragment-based synthesis of resin-bound cyclic peptide analogs of parathyroid hormones and analogs of parathyroid hormone-related proteins, which analogs contain at least one bridge between the side chains of two non-adjacent amino acid residues, and to peptide fragments useful therefor.

    摘要翻译： 本发明涉及一种用于甲状旁腺激素与甲状旁腺激素相关蛋白类似物的树脂结合环肽类似物的固相，片段基合成的方法，该类似物在两个非甲基化激素相关蛋白的侧链之间至少包含一个桥， 相邻的氨基酸残基，以及对其有用的肽片段。

    PEPTIDES WITH beta 1 INTEGRIN SUBUNIT DEPENDENT CELL ADHESION MODULATING ACTIVITY
    55.
    发明申请
    PEPTIDES WITH beta 1 INTEGRIN SUBUNIT DEPENDENT CELL ADHESION MODULATING ACTIVITY 审中-公开
    具有β1整合亚单位细胞粘附调节活性的肽

    公开(公告)号：WO99037669A1

    公开(公告)日：1999-07-29

    申请号：PCT/US1999/001236

    申请日：1999-01-21

    IPC分类号： A61K38/00 ,  A61P35/04 ,  C07K5/06 ,  C07K5/09 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K14/78 ,  A61K38/08

    CPC分类号： C07K7/06 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/0817 ,  C07K5/1008 ,  C07K14/78

    摘要： Peptides capable of modulating beta 1 integrin subunit dependent cell adhesion which includes a C-terminal aromatic amino acid residue and an amino acid residue having a lipophilic alkyl side chain as the penultimate C-terminal residue are provided. These "LipAr" C-terminated peptides are typically capable of modulating the beta 1 integrin subunit dependent adhesion of cells, such as Ramos cells.

    摘要翻译： 提供了能够调节β1整联蛋白亚基依赖性细胞粘附的肽，其包括C末端芳族氨基酸残基和具有亲脂性烷基侧链的氨基酸残基作为倒数第二个C-末端残基。 这些“LipAr”C末端肽通常能够调节β1整联蛋白亚基依赖性细胞粘附，如Ramos细胞。

    LIQUID PHASE PROCESS FOR THE PREPARATION OF GnRH PEPTIDES
    56.
    发明申请
    LIQUID PHASE PROCESS FOR THE PREPARATION OF GnRH PEPTIDES 审中-公开
    用于制备GnRH肽的液相过程

    公开(公告)号：WO99026964A1

    公开(公告)日：1999-06-03

    申请号：PCT/US1998/024623

    申请日：1998-11-18

    IPC分类号： C07K5/09 ,  C07K5/103 ,  C07K5/107 ,  C07K7/23 ,  C07K5/08 ,  C07K5/10

    CPC分类号： C07K5/0815 ,  C07K5/101 ,  C07K5/1013 ,  C07K5/1016 ,  C07K7/23 ,  Y02P20/55

    摘要： A liquid phase process for preparing GnRH peptide analogs of the formula (1): G-AA1-(A)D-Phe-AA3-AA4-(R2)-AA5-AA6-AA7-AA8-Pro-AA10-NH2, which comprises: (a) reacting a peptide of the formula: T-(R2)AA5-AA6-X, where T is (P2)AA4 or P2 and X is AA7-OH or is -OH, with a peptide of the formula: X'-AA8-Pro-AA10-NH2 or acid-addition salt form thereof, where X' is AA7 when X is absent and X' is absent when X is AA7-OH; in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula: T-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2, (b) removing the P2, protecting group at the N-terminus, and (c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula: G-AA1-(R1)D-Phe-AA3-T' or acid-addition salt form thereof, where T' is AA4-OH when T is absent and is absent when T is P2-AA4, in a liquid reaction medium to obtain a GnRH peptide of the formula: G-AA1-(A)D-Phe-AA3-AA4-(R2)AA5-AA6-AA7-AA8-Pro-AA10-NH2.

    摘要翻译： 用于制备式（1）的GnRH肽类似物的液相方法：G-AA1-（A）D-Phe-AA3-AA4-（R2）-AA5-AA6-AA7-AA8-Pro-AA10-NH2，其 包括：（a）使下式的肽与下式的肽反应：式（T-2）AA5-AA6-X的肽，其中T是（P2）AA4或P2，X是AA7-OH或-OH， X'-AA8-Pro-AA10-NH2或其酸加成盐形式，其中当X不存在时X'为AA 7，X为AA 7 -OH时X'为不存在; 在液体反应介质中，在肽偶联剂和强有机胺碱的存在下，得到下式的产物：（（R 2）AA 5 -A AA 6 -A AA 7 -A AA 8 -Pro-AA 10 -NH 2，（b） 在N末端的P2保护基，和（c）使步骤（b）的产物或其酸加成盐与下式的肽反应：G-AA1-（R1）D-Phe-AA3- T'或其酸加成盐形式，其中当T不存在时T'为AA4-OH，当T为P2-AA4时不存在，在液体反应介质中得到G-AA1-（ A）D-PHE-AA3-AA4-（R2）AA5-AA6-AA7-AA8-PRO-AA10-NH 2。

    ANTIPYRETIC AND ANTI-INFLAMMATORY PEPTIDES
    59.
    发明申请
    ANTIPYRETIC AND ANTI-INFLAMMATORY PEPTIDES 审中-公开
    抗炎和抗炎药物

    公开(公告)号：WO8800833A3

    公开(公告)日：1988-05-19

    申请号：PCT/US8701994

    申请日：1987-08-07

    申请人： UNIV TEXAS

    发明人： LIPTON JAMES M

    IPC分类号： A61K38/35 ,  A61K38/00 ,  A61P29/00 ,  C07K5/08 ,  C07K5/09 ,  C07K14/575 ,  A61K37/02

    CPC分类号： C07K5/0815 ,  A61K38/00

    摘要： An antipyretic tripeptide, having the amino acid sequence lysine-proline-valine, and a method for utilizing the tripeptide to reduce fever and inflammation in mammals. The tripeptide can either be isolated from natural sources or chemically synthesized. A ''protected'' tripeptide having greater antipyretic potency and duration of action is also disclosed. The ''protected'' tripeptide contains an acyl group, such as an acetyl or a dibenzyl oxy carboxyl group, at its amino terminals and is amidated or esterified at its carboxyl terminals. Further, improved antipyretic potency and direction of action can be achieved through the co-administration of copper salts with the tripeptide.