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28 条记录 (耗时 0.023 秒)

    Process for producing triglycyl-lysine vasopressin and intermediates therefor
    2.
    发明授权
    Process for producing triglycyl-lysine vasopressin and intermediates therefor 失效
    制备三甘氨酰赖氨酸加压素及其中间体的方法

    公开(公告)号：US4093610A

    公开(公告)日：1978-06-06

    申请号：US763772

    申请日：1977-01-31

    申请人： Nedumparambil A. Abraham ,  Hans U. Immer ,  Kazimir Sestanj

    发明人： Nedumparambil A. Abraham ,  Hans U. Immer ,  Kazimir Sestanj

    IPC分类号： A61K38/00 ,  C07K7/16 ,  C07C103/52 ,  C07G7/00

    CPC分类号： C07K7/16 ,  A61K38/00 ,  Y10S930/15

    摘要： A new process for preparing the cyclic dodecapeptide triglycyl-lysine vasopressin of the formula ##STR1## which comprises the preparation of a first hexapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--NHNH.sub.2 and a second hexapeptide of formula H--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 by a series of condensations involving the reaction of an appropriately protected peptide unit having an activated carboxyl with an appropriately protected peptide having a free amino group. Subsequently, the first and second hexapeptides are condensed according to the azide coupling method to obtain the linear protected dodecapeptide of formula Boc--Gly--Gly--Gly--Cys(Trt)--Tyr--Phe--Gln(Mbh)--Asn(Mbh)--Cys(Trt)--Pro--Lys(Boc)--Gly--NH.sub.2 ; thereafter the linear protected dodecapeptide is transformed into the desired cyclic dodecapeptide, triglycyllysine vasopressin, by oxidizing and deprotecting processes.

    摘要翻译： 制备式“IMAGE”的环十二肽三缩水甘油基赖氨酸加压素的新方法，其包括制备式Boc-Gly-Gly-Gly-Cys（Trt）-Tyr-Phe-NHNH 2的第一六肽和第二个六肽 通过一系列缩合产生式H-Gln（Mbh）-Asn（Mbh）-Cys（Trt）-Pro-Lys（Boc）-Gly-NH 2）的反应，该缩合涉及适当保护的具有活性羧基的肽单元与适当的 具有游离氨基的保护肽。 随后，根据叠氮偶合法将第一和第二六肽缩合，得到式Boc-Gly-Gly-Gly-Cys（Trt）-Tyr-Phe-Gln（Mbh）-Asn（Mbh） - Cys（Trt）-Pro-Lys（Bo c）-Gly-NH 2; 此后，通过氧化和脱保护过程将线性保护的十二肽转化成所需的环十二肽，甘氨酰赖氨酸加压素。

    Derivatives of retro-enantio-somatostatin, intermediates therefor, and process therefor
    3.
    发明授权
    Derivatives of retro-enantio-somatostatin, intermediates therefor, and process therefor 失效
    复方生长抑素的衍生物，其中间体及其制备方法

    公开(公告)号：US4010260A

    公开(公告)日：1977-03-01

    申请号：US599448

    申请日：1975-07-28

    申请人： Hans U. Immer ,  Nedumparambil A. Abraham ,  Verner R. Nelson

    发明人： Hans U. Immer ,  Nedumparambil A. Abraham ,  Verner R. Nelson

    IPC分类号： A61K38/00 ,  C07K14/655 ,  C07C103/52 ,  A61K37/00

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16

    摘要： Compounds of the formula 1 or 1a ##STR1## IN WHICH R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 are disclosed. The compounds are obtained by a process which comprises the following step: preparing peptide fragments II, III, V and VII see below, by a series of condensations involving the reaction of an appropriately protected peptide having an activated ester group with an appropriately protected peptide having a free amino group; condensing ##STR2## by means of the azide method with ##STR3## followed by hydrogenolysis of the reaction product to obtain ##STR4## condensing the latter by means of the azide method with ##STR5## followed by treating the resulting compound with hydrazine hydrate to obtain ##STR6## condensing the latter by means of the azide method with ##STR7## in which R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 to obtain the linear protected peptide ##STR8## in which R is as defined herein; thereafter said linear peptide is transformed into the desired cyclic peptide of formula 1 by deprotecting and oxidizing processes. In addition, the linear, reduced form of the peptide of formula 1a is obtained by deprotection of the aforementioned linear peptide or by reduction of the cyclic peptide. The peptides of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly. Methods for their use are also disclosed.

    摘要翻译： 式1或1a的化合物

    Decapeptide analogs of somatostatin
    4.
    发明授权
    Decapeptide analogs of somatostatin 失效
    生长抑素的十肽类似物

    公开(公告)号：US4118380A

    公开(公告)日：1978-10-03

    申请号：US818500

    申请日：1977-07-25

    申请人： Hans U. Immer ,  Nedumparambil A. Abraham

    发明人： Hans U. Immer ,  Nedumparambil A. Abraham

    IPC分类号： A61K38/00 ,  C07K5/083 ,  C07K5/103 ,  C07K14/655 ,  C07C103/52

    CPC分类号： C07K5/1005 ,  C07K14/655 ,  C07K5/0806 ,  A61K38/00 ,  Y10S930/16

    摘要： Compounds of the formula 1 or 1a ##STR1##HSCH.sub.2 CH.sub.2 CO-A-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH.sub.2 CH.sub.2 SH (1a)in which A is Gly-Asn or Lys-Gly, or therapeutically acceptable salts thereof are disclosed. The compounds of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly in mammals. Compositions and methods for their use also are disclosed.

    摘要翻译： 式1或1a的化合物（1）HSCH2CH2CO-A-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-NHCH2CH2SH（1a）其中A是Gly-Asn或Lys-Gly，或 公开了其治疗上可接受的盐。 式1和1a的化合物可用于治疗糖尿病和哺乳动物肢端肥大症的治疗。 其使用的组合物和方法也被公开。