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    Peptides having thymopoietin-like activity
    3.
    发明授权
    Peptides having thymopoietin-like activity 失效
    具有胸腺生成素样活性的肽

    公开(公告)号：US4397842A

    公开(公告)日：1983-08-09

    申请号：US248759

    申请日：1981-03-30

    Applicant: Gideon Goldstein ,  George Heavner

    Inventor： Gideon Goldstein ,  George Heavner

    IPC: A61K38/00 ,  C07K14/66 ,  A61K37/00

    CPC classification number: C07K14/662 ,  A61K38/00 ,  Y10S930/18

    Abstract: There are disclosed peptides having the following formula:A--X--Z--Y--Bwherein A is ##STR1## X is a suitable neutral, aliphatic or aromatic amino acid residue; e.g., one selected from the group consisting of ALA, 2-Me-ALA, GLY, LEU, ILE, LYS, THR, SER, PHE, MET, D-ALA, D-LEU, D-ILE, D-LYS, D-THR, allo-THR, D-SER, D-PHE, D-MET, and SAR; Z is ##STR2## Y is GLY, SER, THR, LEU, ILE, VAL, OR SAR; B IS TYR-R', D-TYR-R', decarboxy-TYR, or ##STR3## m is 3 or 4; n is 1, 2, or 3; R''' is hydrogen, C.sub.1 -C.sub.7 alkyl, C.sub.6 -C.sub.12 aryl, or C.sub.1 -C.sub.7 alkanoyl; and R and R' are substituents which do not substantially affect the biological activity of the peptides, provided that R-ARG-LYS-ASP-VAL-TYR-R' is excluded. These peptides have the capability of inducing the differentiation of T-lymphocytes but not of complement receptor (CR.sup.+) B-lymphocytes and thus are useful in a number of therapeutic areas. Also provided are derivatives of the peptides, therapeutic compositions, and methods for use of the compositions.

    Abstract translation: 公开了具有下式的肽：A-X-Z-Y-B其中A是合适的中性，脂族或芳族氨基酸残基; 例如选自ALA，2-Me-​​ALA，GLY，LEU，ILE，LYS，THR，SER，PHE，MET，D-ALA，D-LEU，D-ILE，D-LYS，D -THR，allo-THR，D-SER，D-PHE，D-MET和SAR; Z是 Y是GLY，SER，THR，LEU，ILE，VAL或OR SAR; B是TYR-R'，D-TYR-R'，脱羧-TYR或者 m是3或4; n为1,2或3; R“是氢，C 1 -C 7烷基，C 6 -C 12芳基或C 1 -C 7烷酰基; 并且R和R'是不排除基本上影响肽的生物学活性的取代基，条件是R-ARG-LYS-ASP-VAL-TYR-R'。 这些肽具有诱导T淋巴细胞分化而不是补体受体（CR +）B淋巴细胞分化的能力，因此可用于许多治疗领域。 还提供了肽的衍生物，治疗组合物和组合物的使用方法。

    Peptides having thymopoietin-like activity
    4.
    发明授权
    Peptides having thymopoietin-like activity 失效
    具有胸腺生成素样活性的肽

    公开(公告)号：US4261886A

    公开(公告)日：1981-04-14

    申请号：US124959

    申请日：1980-03-13

    Applicant: Gideon Goldstein ,  George Heavner

    Inventor： Gideon Goldstein ,  George Heavner

    IPC: A61K38/00 ,  C07K14/66 ,  C07C103/52

    CPC classification number: C07K14/662 ,  A61K38/00 ,  Y10S930/18

    Abstract: There are disclosed peptides having the following formula: 12 A-X-Z-Y-Bwherein A is ##STR1## X is a suitable neutral, aliphatic or aromatic amino acid residue; e.g., one selected from the group consisting of ALA, 2-Me-ALA, GLY, LEU, ILE, LYS, THR, SER, PHE, MET, D-ALA, D-LEU, D-ILE, D-LYS, D-THR, allo-THR, D-SER, D-PHE, D-MET, and SAR; Z is ##STR2## Y is GLY, SER, THR, LEU, ILE, VAl, or SAR; B is TYR-R', D-TYR-R', decarboxy-TYR, or ##STR3## m is 3 or 4; n is 1, 2, or 3; R''' is hydrogen, C.sub.1 -C.sub.7 alkyl, C.sub.6 -C.sub.12 aryl, or C.sub.1 -C.sub.7 alkanoyl; and R and R' are substituents which do not substantially affect the biological activity of the peptides, provided that R-ARG-LYS-ASP-VAL-TYR-R' is excluded. These peptides have the capability of inducing the differentiation of T-lymphocytes but not of complement receptor (CR.sup.+) B-lymphocytes and thus are useful in a number of therapeutic areas. Also provided are derivatives of the peptides, therapeutic compositions, and methods for use of the compositions.

    Abstract translation: 公开了具有下式的肽：1 2 A-X-Z-Y-B其中A是合适的中性，脂族或芳族氨基酸残基; 例如选自ALA，2-Me-​​ALA，GLY，LEU，ILE，LYS，THR，SER，PHE，MET，D-ALA，D-LEU，D-ILE，D-LYS，D -THR，allo-THR，D-SER，D-PHE，D-MET和SAR; Z是 Y是GLY，SER，THR，LEU，ILE，VA1或SAR; B是TYR-R'，D-TYR-R'，脱羧-TYR或者 m是3或4; n为1,2或3; R“是氢，C 1 -C 7烷基，C 6 -C 12芳基或C 1 -C 7烷酰基; 并且R和R'是不排除基本上影响肽的生物学活性的取代基，条件是R-ARG-LYS-ASP-VAL-TYR-R'。 这些肽具有诱导T淋巴细胞分化而不是补体受体（CR +）B淋巴细胞分化的能力，因此可用于许多治疗领域。 还提供了肽的衍生物，治疗组合物和组合物的使用方法。

    Immunostimulating peptides, a process for their preparation and pharmaceutical compositions containing them
    5.
    发明授权
    Immunostimulating peptides, a process for their preparation and pharmaceutical compositions containing them 失效
    免疫刺激肽，其制备方法和含有它们的药物组合物

    公开(公告)号：US5225400A

    公开(公告)日：1993-07-06

    申请号：US785026

    申请日：1991-10-30

    Applicant: Brunetto Brunetti ,  Marco Prada

    Inventor： Brunetto Brunetti ,  Marco Prada

    IPC: A61K38/00 ,  C07K5/093 ,  C07K7/06 ,  C07K14/66

    CPC classification number: C07K7/06 ,  C07K14/662 ,  C07K5/0819 ,  A61K38/00

    Abstract: Tripeptides having general formula II Glu-Lys-Arg in which: Glu is a glutamic acid residue, Lys is a lysine residue and Arg is an arginine residue are described. The aminoacids composing the tripeptides of the invention may be either of the natural, L-series or of the D-series or a racemic mixture of the two said series, but the aminoacids are preferably selected from the L-forms even though D- or DL aminoacids may also be considered. The invention refers also to the process for the preparation of said peptides as well as to their use as immunostimulant agents.

    Abstract translation: 具有通式II Glu-Lys-Arg的三肽，其中：Glu是谷氨酸残基，Lys是赖氨酸残基，Arg是精氨酸残基。 构成本发明的三肽的氨基酸可以是天然的，L系列的或D系的两种或两种所述的系列的外消旋混合物，但是氨基酸优选选自L-型，即使D-或 也可以考虑DL氨基酸。 本发明还涉及制备所述肽的方法以及它们作为免疫刺激剂的用途。

    Polypeptide compositions
    8.
    发明授权
    Polypeptide compositions 失效
    多肽组合物

    公开(公告)号：US4305852A

    公开(公告)日：1981-12-15

    申请号：US198415

    申请日：1980-10-20

    Applicant: Victor M. Garsky

    Inventor： Victor M. Garsky

    IPC: A61K38/00 ,  C07K14/66 ,  C08L37/00 ,  C07C103/52

    CPC classification number: C07K14/662 ,  A61K38/00 ,  Y10S930/18 ,  Y10S930/28

    Abstract: There are disclosed polypeptides having the formula:R-Arg-Lys-Asp-Val-D-Ala-R.sub.1whereinR is hydrogen, alkanoyl of 1-4 carbon atoms or aroyl of 6-10 carbon atoms; andR.sub.1 is amino, monoalkylamino of 1-4 carbon atoms, dialkylamino of 1-4 carbon atoms, hydroxy, alkoxy of 1-4 carbon atoms, ##STR1## the fully protected peptide-resin intermediates thereof, or pharmaceutically acceptable salts thereof. These polypeptides have the capability of inducing the differentiation of t-lymphocytes and thus are useful in a number of therapeutic areas.

    Abstract translation: 公开了具有下式的多肽：R-Arg-Lys-Asp-Val-D-Ala-R1其中R是氢，1-4个碳原子的烷酰基或6-10个碳原子的芳酰基; R1为氨基，1-4个碳原子的单烷基氨基，1-4个碳原子的二烷基氨基，羟基，1-4个碳原子的烷氧基，其完全保护的肽 - 树脂中间体或药学上 其可接受的盐。 这些多肽具有诱导t淋巴细胞分化的能力，因此可用于许多治疗领域。

    Process for the preparation of pentapeptides having an action on the immune system and intermediate products for this process
    10.
    发明授权
    Process for the preparation of pentapeptides having an action on the immune system and intermediate products for this process 失效
    制备对该过程具有免疫系统作用的五肽和中间产物的方法

    公开(公告)号：US4658016A

    公开(公告)日：1987-04-14

    申请号：US742441

    申请日：1985-06-07

    Applicant: Wolfgang Konig ,  Rolf Geiger ,  Rainer Obermeier ,  Hubert Mullner

    Inventor： Wolfgang Konig ,  Rolf Geiger ,  Rainer Obermeier ,  Hubert Mullner

    IPC: A61K38/00 ,  A61K38/22 ,  A61P37/00 ,  C07K7/06 ,  C07K14/66 ,  C07K1/02

    CPC classification number: C07K14/66 ,  C07K14/662 ,  Y02P20/55

    Abstract: The invention relates to a process for the preparation of peptides of the general formulaArg--Lys--S--Val--Yin which S denotes glutamic acid or .alpha.-aminoadipic acid and Y denotes tyrosine or tryptophan or esters or amides thereof, which comprises subjecting tetrapeptides of the formulaZ--Arg(Z'.sub.2)--Lys(Z')--S--(Bzl)--Val--OHin which Z' represents a protective group of the benzyl type, to a condensation reaction with corresponding tyrosine esters or amides or tryptophan esters or amides and removing the protective groups by hydrogenation. The invention furthermore relates to tetrapeptides as intermediate products of this process.

    Abstract translation: 本发明涉及制备通式Arg-Lys-S-Val-Y的肽的方法，其中S表示谷氨酸或α-氨基己二酸，Y表示酪氨酸或色氨酸或其酯或酰胺，其包括 式Z-Arg（Z'2）-Lys（Z'）-S-（Bzl）-Val-OH的四肽，其中Z'表示苄基类型的保护基，与相应的酪氨酸酯缩合反应或 酰胺或色氨酸酯或酰胺，并通过氢化除去保护基。 本发明还涉及作为该方法的中间产物的四肽。

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