POLYPEPTIDE
    4.
    发明专利

    公开(公告)号:JPH01316399A

    公开(公告)日:1989-12-21

    申请号:JP5594189

    申请日:1989-03-08

    申请人: EISAI CO LTD

    摘要: NEW MATERIAL:A polypeptide (salt) expressed by formula I [A is formula II (G is L- or DC-type basic amino acid; R and R are H, lower alkyl or acyl), etc.; B is L-type basic amino acid, etc.; C is L-type Pro, etc.; D is L-type (non)natural type aromatic amino acid; E is L-type (N-alkyl)amino acid, etc. ; F is L- or D-type (N-alkyl)amino acid, etc.; R is formula III (R and R are H, lower alkyl), etc.]. USE:An antipsychotic and analgesic agents. PREPARATION:For example, ethyl ester of a C-terminal amino acid, etc., are reacted with an amino acid having a protected alpha-amino group at the second position from the C-terminal in the presence of N-methylmorpholine and ethyl chlorocarbonate, etc., and the alpha-amino-protecting group is then removed. The similar operation is repeated according to an amino acid sequence of a peptide to afford the peptide expressed by formula I.

    POLYPEPTIDE
    5.
    发明专利

    公开(公告)号:JPS62111997A

    公开(公告)日:1987-05-22

    申请号:JP25231585

    申请日:1985-11-11

    申请人: EISAI CO LTD

    摘要: NEW MATERIAL:A compound of formula I [R , R are H, lower alkyl, lower alkenyl; A, B are D- or L-basic aminoacid; C is alpha-aminoacid, beta-alanine, alpha- aminobutyric acid; D is -OR (R is H, lower alkyl), -E-OR (E is neutral to acidic aminoacid; R is H, lower alkyl); where the case is excluded where all of the aminoacid constituents are L-aminoacid of formula II (R is residual group, after the group of formula III is removed from the structural formula of aminoacids). EXAMPLE:CH3Tyr-Gly-Gly-Phe-Leu-Arg-CH3Arg-D-Ala-OH. USE:Analgesic. PREPARATION:For example, Z-CH3Arg(Tos)OH is used as a starting substance and converted into Boc-CH3Tyr(Cl2Bzl)-Gly-Gly-PHe-Leu-Arg(Tos)-CH2Arg(Tos)- D-Ala-OBu. Then, the product is allowed to react with HF.

    Secretin-relating derivative
    6.
    发明专利
    Secretin-relating derivative 失效
    相分离衍生物

    公开(公告)号:JPS59134763A

    公开(公告)日:1984-08-02

    申请号:JP797383

    申请日:1983-01-20

    申请人: Eisai Co Ltd

    摘要: NEW MATERIAL:The compound of formula I (X is a group which corresponds in the form of X-NH
    2 to secretin or a fragment devoid of 10 amino acids from its N-terminal; Y is residue corresponding in the form of Y-SH to β-galactosidase; Z is group of formula IIWformula IV).
    USE: An enzyme-labeling antigen for the enzymatic immunoassay of secretin. Secretin can be determined in high specificity and sensitivity with a simple and easy operation with easy calibration.
    PROCESS: The compound of formula I can be prepared by (1) reacting the crosslinking agent of formula V with secretin or secretin fragment of X-NH
    2 to introduce m-maleimidobenzoyl group to the N-terminal of secretin or secretin fragment, and (2) reacting the resultant compound of formula VI with β-D- galactosidase of formula Y-SH thereby adding the galactosidase to the maleimide group via the SH group of the galactosidase.
    COPYRIGHT: (C)1984,JPO&Japio

    摘要翻译: 新物质:式I化合物(X为X-NH 2与分泌素形式相对应的基团或其N-末端缺失10个氨基酸的片段; Y为Y-SH至 β-半乳糖苷酶; Z是式II-式IV)的基团。 用途:用于促胰液素的酶免疫测定的酶标记抗原。 通过简单的校准,可以通过简单易用的操作,确定具有高特异性和灵敏度的Secretin。 方法:式I化合物可以通过(1)使式V的交联剂与X-NH 2的促胰液素或胰蛋白酶片段反应,将m-马来酰亚胺苯甲酰基引入分泌素或胰蛋白酶片段的N末端,和(2 )使得到的式VI化合物与式Y-SH的β-D-半乳糖苷酶反应,从而通过半乳糖苷酶的SH基团将半乳糖苷酶加入到马来酰亚胺基团中。

    DECAPEPTIDE
    10.
    发明专利

    公开(公告)号:JPS58152852A

    公开(公告)日:1983-09-10

    申请号:JP3402782

    申请日:1982-03-05

    申请人: EISAI CO LTD

    IPC分类号: C07K7/06

    摘要: NEW MATERIAL:The decapeptide of formulaI(His is histidine; Ser is serine; Asp is aspartic acid; Gly is glycine; Thr is threonine; Phe is phenylalanine; Glu is glutamic acid; Leu is leucine). USE:Synthetic intermediate of secretin having pancreatic excretion promoting activity, gastrin-stimulated gastric juice secretion inhibiting activity, insulin- separating activity, pepsin-secretion stimulating activity, fat-decomposing activity, etc. PROCESS:The constituent amino acids are bonded together in the order through peptide bonds to obtain the decapeptide of formulaI. The protected secretin of formula IV can be prepared by condensing the fragment of formulaI with the fragment obtained by the condensation of the fragment of formula II with the fragment of formula III. The protected secretin can be converted to the highly pure and high activity synthetic secretin in high yield without loss by deactivation, by removing the protecting groups therefrom and purifying the product.