Process for converting preproinsulin analogs into insulins
    1.
    发明授权
    Process for converting preproinsulin analogs into insulins 失效
    将胰岛素类似物转化为胰岛素的方法

    公开(公告)号:US4639333A

    公开(公告)日:1987-01-27

    申请号:US659865

    申请日:1984-10-12

    IPC分类号: C12P21/02 C07K14/62 C07K7/40

    摘要: The invention relates to a process for the preparation of insulins from analogs of preproinsulins, which comprises reacting preproinsulin analogs, at a pH below the isoelectric point of the insulins in the presence of trypsin or a trypsin-like endopeptidase, with an ester of natural amino acids or their derivatives and then cleaving off the ester group and other protective groups which may optionally be present.

    摘要翻译: 本发明涉及从前胰岛素类似物制备胰岛素的方法,其包括在胰蛋白酶或胰蛋白酶样内肽酶存在下,将胰岛素类似物与胰岛素类胰蛋白酶存在下的pH低于胰岛素的等电点与天然氨基酸的酯反应 酸或其衍生物,然后断开酯基和可任选存在的其它保护基。

    Process for the preparation of insulin derivatives, the B chain of which
is lengthened c-terminally
    2.
    发明授权
    Process for the preparation of insulin derivatives, the B chain of which is lengthened c-terminally 失效
    胰岛素衍生物的制备方法,其B链延长c末端

    公开(公告)号:US5015728A

    公开(公告)日:1991-05-14

    申请号:US172236

    申请日:1988-03-23

    CPC分类号: C07K14/62 A61K38/00 Y02P20/55

    摘要: The invention relates to a process for the preparation of an insulin derivative of the formula I ##STR1## in which R.sup.1 denotes H or H-Phe, R.sup.30 represents the radical of a naturally occurring L-aminoacid and R.sup.31 represents a physiologically acceptable organic group of neutral or basic character consisting of 1 to 3 .alpha.-aminoacids in which the terminal carboxyl function is present in the free form and which insulin derivative has an isoelectric point above 5.8, which comprises reacting an insulin of the formula I in which R.sup.30 denotes the radical of a genetically codable L-aminoacid and R.sup.31 represents OH or a protective group of the carboxyl function, with a peptide or aminoacid derivatives of the formula R-R.sup.30 -R.sup.31 consisting of 2 to 4 .alpha.-aminocacids, in which the terminal carboxyl function is in free form, in the presence of a trypsin-like endopeptidase at a pH value below the isoelectric point of the starting insulin.

    摘要翻译: 本发明涉及一种制备式I(I)的胰岛素衍生物的方法,其中R1表示H或H-Phe,R30表示天然存在的L-氨基酸的基团,R31表示生理上可接受的 由1〜3个α-氨基酸组成的中性或碱性有机基团,其中末端羧基官能团以游离形式存在,哪种胰岛素衍生物具有高于5.8的等电点,其包括使式I的胰岛素与R30 表示可遗传编码的L-氨基酸的基团,R31表示OH或羧基官能团的保护基团,具有由2至4个α-氨基酸组成的式R-R30-R31的肽或氨基酸衍生物,其中末端 在胰蛋白酶样内肽酶的存在下,羧基功能是游离形式,其pH值低于起始胰岛素的等电点。

    Process for the preparation of pentapeptides having an action on the
immune system and intermediate products for this process
    3.
    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

    摘要: 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.

    摘要翻译: 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。

    Process for the preparation of insulin, analogs and derivatives thereof
    9.
    发明授权
    Process for the preparation of insulin, analogs and derivatives thereof 失效
    胰岛素,类似物及其衍生物的制备方法

    公开(公告)号:US4013628A

    公开(公告)日:1977-03-22

    申请号:US604667

    申请日:1975-08-14

    CPC分类号: C07K14/62 Y02P20/55

    摘要: A process for the manufacture of insulin and derivatives thereof by treating an insulin derivative, wherein the A-chain is cross-linked with the B-chain by means of a sulfonyl diethyl-bisoxycarbonyl bridge and the B-chain may contain an acyl group in the 1-position, with alkali metal hydroxides or quaternary organic bases having a pH value of more than 13.

    摘要翻译: 通过处理胰岛素衍生物制备胰岛素及其衍生物的方法,其中所述A链通过磺酰基二乙基 - 双氧羰基桥与所述B链交联,并且所述B链可含有酰基 1位,碱金属氢氧化物或pH值大于13的季有机碱。