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    Process for the manufacture of insulin, analogs and derivatives thereof
    2.
    发明授权
    Process for the manufacture of insulin, analogs and derivatives thereof 失效
    制备胰岛素，类似物及其衍生物的方法

    公开(公告)号：US3883500A

    公开(公告)日：1975-05-13

    申请号：US41031073

    申请日：1973-10-29

    Applicant: HOECHST AG

    Inventor： GEIGER ROLF ,  JAGER GEORG

    IPC: C07K14/575 ,  C07K1/113 ,  C07K14/62 ,  C07C103/52 ,  A61K17/04 ,  C07G7/00

    CPC classification number: C07K14/62 ,  Y02P20/55 ,  Y10S930/26

    Abstract: D R A W I N G
    A method for making insulin and certain derivatives thereof from a compound of the formula (I)

    D R A W I N G
    wherein X is hydrogen or an S-protective group and n is an integer from two to four, which comprises cleaving any Sprotective groups present and dehydrogenating -SH groups to form S-S bonds to form a compound of the formula (II)

    BRIDGE BY TREATING THE LATTER COMPOUND WITH AN ACID. Compounds of the formula II.

    and then eliminating the

    Abstract translation: 一种由式（I）化合物制备胰岛素及其某些衍生物的方法，其中X为氢或S-保护基，n为2至4的整数，其包括切断存在的任何S-保护基团并脱氢 - SH基团形成SS键以形成式（II）的化合物，然后通过用酸处理化合物来消除桥。 式II的化合物。

    Process for the manufacture of insulin, analogs and derivatives thereof
    5.
    发明授权
    Process for the manufacture of insulin, analogs and derivatives thereof 失效
    制备胰岛素，类似物及其衍生物的方法

    公开(公告)号：US3883496A

    公开(公告)日：1975-05-13

    申请号：US40891373

    申请日：1973-10-23

    Applicant: HOECHST AG

    Inventor： GEIGER ROLF

    IPC: C07D499/44 ,  A61K38/28 ,  A61P3/08 ,  C07D501/20 ,  C07D501/60 ,  C07K1/113 ,  C07K14/575 ,  C07K14/62 ,  A61K17/04 ,  C07C103/52

    CPC classification number: C07K14/62 ,  Y02P20/55 ,  Y10S930/26

    Abstract: BRIDGE BY Edman degradation. Compounds of the formula II.

    and then eliminating the

    wherein Ac is an N-protective group removable by proton solvolysis, X is hydrogen or an S-protective group, and W is (CH2)-n where n is an integer from zero to four and one -CH2member thereof may be replaced by -S- or -SO2-, which comprises solvolyzing the Ac groups and dehydrogenating the -SX groups to S-S bonds to form a compound of the formula (II)

    A method for making insulin and certain derivatives thereof from a compound of the formula (I)

    Abstract translation: 一种由式（I）化合物制备胰岛素及其某些衍生物的方法，其中Ac是通过质子溶解分解可除去的N-保护基，X是氢或S-保护基，W是 - （CH2）-n 其中n为0至4的整数，并且其一个-CH 2 - 成员可以被-S-或-SO 2 - 取代，其包括使Ac基团溶解分解并将-SX基团脱氢成SS键，以形成式 （II），然后消除BRIDGE BY Edman降解。 式II的化合物。

    Position 1 analogs of {8 phenylglycyl{9 -angiotension II
    8.
    发明授权
    Position 1 analogs of {8 phenylglycyl{9 -angiotension II 失效
    位置1的{8苯基甘氨酰{9-血管紧张素II

    公开(公告)号：US3920627A

    公开(公告)日：1975-11-18

    申请号：US46783274

    申请日：1974-05-07

    Applicant: HOECHST AG

    Inventor： WISSMANN HANS ,  GEIGER ROLF ,  LINDNER ERNST ,  SCHOLKENS BERNWARD

    IPC: C07K7/06 ,  A61K38/00 ,  A61P5/00 ,  C07C231/00 ,  C07K1/113 ,  C07K7/14 ,  C07C103/52 ,  A61K37/26

    CPC classification number: C07K7/14 ,  A61K38/00 ,  Y02P20/55

    Abstract: Peptides of the formula I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH (I) in which X represents the radical of an aliphatic carboxylic acid of up to 5 carbon atoms or the phthalic acid radical, and Phegly-OH represents L-C-phenylglycine, and a process of preparing them by condensing the O-tert. butyl ester of compound I, in which tyrosine is protected by tert. butyl, and X represents hydrogen, with carboxylic acids of the formula X-OH, in which X has the first mentioned meaning, according to the condensation methods usually employed in peptide chemistry.

    Abstract translation: 式I X-Arg-Val-Tyr-Ile-His-Pro-Phegly-OH（I）的肽，其中X表示至多5个碳原子的脂肪族羧酸基团或邻苯二甲酸基团，Phegly -OH表示LC-苯基甘氨酸，以及通过将O-叔丁基缩合制备它们的方法。 化合物I的丁酯，其中酪氨酸被叔保护。 丁基，X表示氢，根据肽化学中通常使用的缩合方法，具有式X-OH的羧酸，其中X具有第一个提及的含义。

    Method for the aminolysis of activated esters in the presence of N-hydroxy compounds as catalysts
    9.
    发明授权
    Method for the aminolysis of activated esters in the presence of N-hydroxy compounds as catalysts 失效
    在N-羟基化合物作为催化剂存在下活化酯的氨解方法

    公开(公告)号：US3872074A

    公开(公告)日：1975-03-18

    申请号：US26444172

    申请日：1972-06-20

    Applicant: HOECHST AG

    Inventor： KONIG WOLFGANG ,  GEIGER ROLF ,  WISSMANN HANS

    IPC: A61K38/00 ,  C07K1/10 ,  C07K5/06 ,  C07K14/625 ,  C07K14/695 ,  C07C103/52 ,  C07G7/00

    CPC classification number: C07K5/06043 ,  A61K38/00 ,  C07K1/10 ,  C07K14/625 ,  C07K14/695

    Abstract: A process for the manufacture of peptides by reacting a protected amino acid or a protected peptide ester with an optionally protected amino acid or a peptide having a free amino group, which may be bound to a polymer support, by adding a heterocyclic compound of the formula

    D R A W I N G
    WHEREIN X stands for the groups C O, C S or -N and X and N are members of a 5- or 6-membered heterocyclic ring optionally substituted and fused with a benzene nucleus and/or optionally containing 1 or 2 further hetero atoms, and the pK-value whereof lies between 3.7 and 4.2, as catalysts for the condensation.

    Abstract translation: 通过将受保护的氨基酸或受保护的肽酯与任选保护的氨基酸或具有游离氨基的肽（其可以结合到聚合物载体）反应，通过加入式 其中X代表基团C = O，C = S或-N =且X和N是任选被取代并与苯核稠合的5或6元杂环的成员和/或任选地含有1或2个 杂原子，其pK值在3.7和4.2之间，作为缩合的催化剂。

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