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    Novel nonapeptides, intermediates therefor, and compositions and methods employing said nonapeptides
    4.
    发明授权
    Novel nonapeptides, intermediates therefor, and compositions and methods employing said nonapeptides 失效
    新颖的肽，其中间体，以及使用所述非肽的组合物和方法

    公开(公告)号：US4139504A

    公开(公告)日：1979-02-13

    申请号：US807134

    申请日：1977-06-16

    Applicant: David H. Coy ,  Abba J. Kastin

    Inventor： David H. Coy ,  Abba J. Kastin

    IPC: A61K38/00 ,  C07K14/67 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/672 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/12

    Abstract: Novel nonapeptides having the following amino acid sequence:H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    Abstract translation: 具有以下氨基酸序列的新型肽：

    Peptides and therapeutic applications thereof
    8.
    发明授权
    Peptides and therapeutic applications thereof 失效
    肽及其治疗应用

    公开(公告)号：US4407794A

    公开(公告)日：1983-10-04

    申请号：US289383

    申请日：1981-08-03

    Applicant: Bernard Roques ,  Jeanne-Marie Lecomte

    Inventor： Bernard Roques ,  Jeanne-Marie Lecomte

    IPC: C07K14/655 ,  A61K38/00 ,  A61P25/00 ,  C07K7/06 ,  C07K14/575 ,  C07K14/67 ,  C07K14/70 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/672 ,  C07K14/702 ,  A61K38/00 ,  Y10S514/809

    Abstract: This invention relates to peptide derivatives of the formula:Tyr--A--Gly--B--C--D (I)in which:A is a D.Ala, AzaGly, Aib, D.Ser., D.Thr, D.Cys, homo Serine, .beta.Phe Ser, .beta.OH Leu, 4OH Ile, .alpha.,.beta.,.gamma. OHNor Val or OH Val residue in which the side-chain OH or SH groups, when same exist, may be free or protected (i) by a straight- or branched-chain alkyl containing 1-6 carbon atoms, (ii) by an unsubstituted phenyl radical or a phenyl radical substituted with one or more fluorine atoms, (iii) by an unsubstituted benzyl radical or a benzyl radical substituted with one or more fluorine atoms, (iv) by an aliphatic acyl radical having 1-6 carbon atoms or an acyl radical COX in which X is a phenyl, benzyl or benzhydryl radical, optionally substituted with one or more fluorine atoms,B is a L.Phe, pF.L.Phe or pentafluoro L.Phe residue,C is a Leu, N.Leu or Ile residue of D or L configuration,D is hydrogen or a group of the formula: ##STR1## in which n=0, 1 or 2, R is a hydrogen atom or a radical as defined for the protection of group OH of residue A,Y is a hydrogen atom, a group hydroxy, carboxy, carbamoyl, a group OR.sub.1, COOR.sub.1 or CONHR.sub.1 in which R.sub.1 represents a radical as defined for the protection of group OH of residue A, a phosphatidylethanolamine chain or a chain ##STR2## in which n is an integer from 0 to 3, R.sub.2 is a hydrogen atom or a straight alkyl radical containing 1-4 carbon atoms, and R.sub.3 is a hydrogen or oxygen atom or a straight alkyl residue containing 1-4 carbon atoms,and their pharmaceutically acceptable salts.Said compounds are therapeutically useful, typically an analgesic, psychotropic and anti-diarrheic agents.

    Abstract translation: 本发明涉及下式的肽衍生物：Tyr-A-Gly-BCD（I），其中：A为D.Ala，AzaGly，Aib，D.Ser。，D.Thr，D.Cys，高丝氨酸， βPhe Ser，βOH Leu，4OH Ile，α，β，γOHNor Val或OH Val残基，其中侧链OH或SH基团当存在时可以是游离的或受保护的（i）通过直链或 含有1-6个碳原子的支链烷基，（ii）未取代的苯基或被一个或多个氟原子取代的苯基，（iii）未取代的苄基或被一个或多个氟原子取代的苄基 ，（iv）具有1-6个碳原子的脂族酰基或酰基COX，其中X是苯基，苄基或二苯甲基，任选被一个或多个氟原子取代，B是L.Phe，pF。 L.Phe或五氟L.Phe残基，C是D或L构型的Leu，N.Leu或Ile残基，D是氢或下式的基团：其中n = 0,1或2， R是氢原子 如保护残基A的OH基团所定义的基团，Y是氢原子，羟基，羧基，氨基甲酰基，基团OR1，COOR1或CONHR1，其中R1表示为保护基团OH定义的基团 残基A，磷脂酰乙醇胺链或NH（CH2）nR3NR2R2 + RF，其中n为0-3的整数，R2为氢原子或含有1-4个碳原子的直链烷基，R3为氢或 氧原子或含有1-4个碳原子的直链烷基，及其药学上可接受的盐。 所述化合物是治疗上有用的，通常是镇痛药，精神药物和抗腹泻剂。

    Novel pentadecapeptides, intermediates therefor, and compositions and methods employing said pentadecapeptides
    10.
    发明授权
    Novel pentadecapeptides, intermediates therefor, and compositions and methods employing said pentadecapeptides 失效
    新的十五肽，其中间体，以及使用所述十五肽的组合物和方法

    公开(公告)号：US4127527A

    公开(公告)日：1978-11-28

    申请号：US807139

    申请日：1977-06-16

    Applicant: David H. Coy ,  Abba J. Kastin

    Inventor： David H. Coy ,  Abba J. Kastin

    IPC: A61K38/00 ,  C07K14/67 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/672 ,  A61K38/00 ,  Y10S514/809

    Abstract: Novel pentadecapeptides having the following amino acid sequence.H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    Abstract translation: 具有以下氨基酸序列的新型十五肽。

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