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21 条记录 (耗时 0.022 秒)

    Decapeptide analogs of somatostatin
    13.
    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。

    Synthetic natriuretic peptides
    14.
    发明授权
    Synthetic natriuretic peptides 失效
    合成利钠肽

    公开(公告)号：US4824937A

    公开(公告)日：1989-04-25

    申请号：US50208

    申请日：1987-05-14

    申请人： Romano Deghenghi ,  Hans U. Immer

    发明人： Romano Deghenghi ,  Hans U. Immer

    IPC分类号： C07K14/575 ,  A61K38/00 ,  A61P9/08 ,  A61P9/12 ,  C07K14/00 ,  C07K14/58 ,  C07K7/10

    CPC分类号： C07K14/582 ,  A61K38/00

    摘要： Synthetic natriuretic peptides (SNP) composed of 23 amino acid residues of which residues 2-23 have the natural L-configuration while the amino-terminal residue is derived from an unnatural amino acid having the D-configuration. The compounds possess diuretic, natriuretic, vasorelaxant, smooth muscle relaxant, hypotensive, and anti-hypertensive activities, and a process for their preparation is also disclosed, together with pharmaceutical preparations thereof and with their use in the practice of medicine. Salts of said synthetic natriuretic peptides with pharmaceutically acceptable acids are also disclosed.

    摘要翻译： 由23个氨基酸残基组成的合成利钠肽（SNP），其中残基2-23具有天然的L-构型，而氨基末端残基源自具有D-构型的非天然氨基酸。 该化合物具有利尿，利尿钠，血管舒张，平滑肌松弛剂，降血压和抗高血压活性，并且还公开了其制备方法及其药物制剂及其在药物实践中的用途。 还公开了所述合成利钠肽与药学上可接受的酸的盐。

    Preparation of (D-Trp .sup.6)-LH-RH via the heptapeptide H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2
    16.
    发明授权
    Preparation of (D-Trp .sup.6)-LH-RH via the heptapeptide H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 失效
    通过七肽H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH 2制备（D-Trp 6）-LH-RH

    公开(公告)号：US4301066A

    公开(公告)日：1981-11-17

    申请号：US147884

    申请日：1980-05-08

    申请人： Francesco Bellini ,  Hans U. Immer

    发明人： Francesco Bellini ,  Hans U. Immer

    IPC分类号： A61K38/00 ,  C07K7/23 ,  C07C103/52

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S930/13

    摘要： Herein is described a process for preparing the decapeptide Pry-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 ([D-Trp.sup.6 ]-LH-RH) by coupling Pyr-His-Trp-NHNH.sub.2 with H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2. [D-Trp.sup.6 ]-LH-RH had been established to be an efficient agent for causing release of lutenizing hormone and follicle-stimulating hormone in mammals.

    摘要翻译： 本文描述了通过偶联Pyr-His-Trp（[D-Trp6] -LH-RH）制备十肽Pry-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH 2 -NHNH 2与H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH 2。 [D-Trp6] -LH-RH已被确定为在哺乳动物中引起促黄体激素和促卵泡激素释放的有效药物。

    Process for producing triglycyl-lysine vasopressin and intermediates therefor
    17.
    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
    18.
    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