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117 条记录 (耗时 0.027 秒)

    Peptides with para-substituted phenylalanine
    2.
    发明授权
    Peptides with para-substituted phenylalanine 失效
    具有对位取代苯丙氨酸的肽

    公开(公告)号：US4211693A

    公开(公告)日：1980-07-08

    申请号：US967505

    申请日：1978-12-07

    申请人： Jean E. F. Rivier ,  Marvin R. Brown ,  Wylie W. Vale, Jr.

    发明人： Jean E. F. Rivier ,  Marvin R. Brown ,  Wylie W. Vale, Jr.

    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： Somatostatin peptides are modified by substitution of para-methoxylated Phe or para-halogenated Phe for any Phe in the peptide. The modified somatostatin peptide analogs have the formulae: ##STR1## wherein R is hydrogen or an acyl group; R.sub.1 is selected from the group consisting of Lys or Des R.sub.1 ; R.sub.2 is selected from the group consisting of Asn, Ala or Des R.sub.2. The amino acids of the R.sub.2 group can be either the L-form or the D-form; R.sub.3 is selected from the group consisting of Trp or D-Trp; R.sub.4 is selected from the group consisting of Thr or Des R.sub.4 ; R.sub.5 is selected from the group consisting of Ser, D-Ser, Phe, X or Des R.sub.5 ; and X is selected from the group consisting of Phe, para-halogenated Phe and para-methoxylated Phe. Provided that at least one X is either para-halogenated Phe or para-methoxylated Phe.

    摘要翻译： 通过将肽中的任何Phe取代对甲氧基化的Phe或对位卤代Phe来修饰生长抑素肽。 修饰的生长抑素肽类似物具有下式：其中R是氢或酰基; R1选自Lys或Des R1; R2选自Asn，Ala或Des R2。 R2基团的氨基酸可以是L型或D型; R3选自Trp或D-Trp; R4选自Thr或Des R4; R5选自Ser，D-Ser，Phe，X或Des R5; X选自Phe，对位卤化Phe和对甲氧基化Phe。 条件是至少一个X是对位卤化Phe或对甲氧基化的Phe。

    CRF antagonists
    4.
    发明授权
    CRF antagonists 失效
    CRF拮抗剂

    公开(公告)号：US4605642A

    公开(公告)日：1986-08-12

    申请号：US583092

    申请日：1984-02-23

    申请人： Catherine L. Rivier ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marvin R. Brown

    发明人： Catherine L. Rivier ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marvin R. Brown

    IPC分类号： C07K1/06 ,  A61K38/00 ,  A61K38/04 ,  A61K38/22 ,  A61P5/00 ,  C07K1/02 ,  C07K1/04 ,  C07K14/00 ,  C07K14/575 ,  C07K7/10 ,  A61K37/24

    CPC分类号： C07K14/57509 ,  A61K38/00

    摘要： Several polypeptide analogs of the known members of the corticotropin releasing factor (CRF) family have been synthesized and tested including human and rat CRF which have the formula: H-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu-Ile-Ile-NH.sub.2. Peptides are herein disclosed that are potent competitive antagonists of CRF in mammals. One which has been found to be particularly potent is: H-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met-Leu-Glu-Met-Ala-Lys-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg-Leu-Leu-Leu-Glu-Glu-Ala-NH.sub.2. These antagonists or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans, to achieve a prevent elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of brain-mediated responses to stress over an extended period of time. They may also be used to affect mood, memory and learning, as well as diagnostically.

    摘要翻译： 已经合成并测试了促肾上腺皮质激素释放因子（CRF）家族的已知成员的几种多肽类似物，包括人和大鼠CRF，其具有下式：H-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp -Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn -Ar g-Lys-Leu-Met-Glu-Ile-Ile-NH 2。 本文公开了肽，其是哺乳动物中CRF的有竞争力的拮抗剂。 已发现特别有效的是：H-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met-Leu-Glu-Met-Ala-Lys-Ala-Glu-Gln -Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg-Leu-Leu-Leu-Glu-Glu-Ala-NH 2.这些拮抗剂或其药学或兽医学上可接受的盐， 可以将可接受的液体或固体载体施用于包括人在内的哺乳动物，以达到防止ACTH，β-内啡肽，β-促性腺激素，其他产物的前乳糖皮质激素基因和皮质酮水平的提高和/或降低脑 - 在长时间内介导对压力的反应。 它们也可能用于影响情绪，记忆和学习以及诊断。

    Analogs of extended N-terminal somatostatin
    5.
    发明授权
    Analogs of extended N-terminal somatostatin 失效
    延长N末端生长抑素的类似物

    公开(公告)号：US4393050A

    公开(公告)日：1983-07-12

    申请号：US258878

    申请日：1981-04-29

    申请人： Wylie W. Vale, Jr. ,  Jean E. F. Rivier ,  Marvin R. Brown

    发明人： Wylie W. Vale, Jr. ,  Jean E. F. Rivier ,  Marvin R. Brown

    IPC分类号： C07K14/575 ,  A61K38/00 ,  A61K38/04 ,  A61P5/00 ,  A61P5/02 ,  C07K14/655 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S514/866 ,  Y10S514/926 ,  Y10S514/927 ,  Y10S930/16

    摘要： Somatostatin-28 has the formula: ##STR1## Analogs have been synthesized that are more potent than somatostatin-28, and these analogs or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals in the same manner as somatostatin. In the analogs, Leu may be substituted in the 8-position in combination with D-Trp in the 22-position and/or Tyr in the 25-position. D-Cys may also be substituted in the 28-position, and D-Ser may be substituted in the 27-position. Certain residues may also be deleted. D-Trp.sup.22 somatostation-28 has surprisingly been found to be insulin-selective when administered in vivo and is useful for the treatment of insulinoma.

    摘要翻译： 生长抑素-28具有以下分子式：H-Ser-Ala-Asn-Ser-Asn-Pro-Ala-Met-Ala-Pro-Arg-Glu-Arg-Lys- 分散在药学上可接受的液体或固体载体中的这些类似物或其药学上可接受的盐可以以与生长抑素相同的方式施用于哺乳动物。 在类似物中，Leu可以在D位的8位上与22位和/或25位的Tyr结合取代。 D-Cys也可以在28位被取代，D-Ser可以在27位被取代。 某些残基也可能被删除。 D-Trp22生长激素-28在体内给药时已被惊人地发现是胰岛素选择性的，并且可用于治疗胰岛素瘤。

    Peptides having analgesic and thermoregulative properties
    7.
    发明授权
    Peptides having analgesic and thermoregulative properties 失效
    具有止痛和调温特性的肽

    公开(公告)号：US4207311A

    公开(公告)日：1980-06-10

    申请号：US856126

    申请日：1977-11-30

    申请人： Marvin R. Brown ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr.

    发明人： Marvin R. Brown ,  Jean E. F. Rivier ,  Wylie W. Vale, Jr.

    IPC分类号： A61K38/00 ,  C07K7/08 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/083 ,  A61K38/00

    摘要： Peptides having thermoregulative properties when administered to animals. The peptides are identified by the structure:R.sub.1 -R.sub.2 -Trp-Ala-Val-R.sub.3 -His-R.sub.4 -R.sub.5 -NH.sub.2 wherein: R.sub.1 is selected from the group consisting of hydrogen, an amino acid selected from the group consisting of p-Glu,Gln,Arg,Leu,Gly,Asn,Thr,Val, and Pro, and peptides having from 2 to 6 amino acids wherein the amino acids are selected from p-Glu,Gln,Arg,Leu,Gly,Asn,Thr,Val, and Pro, provided that when p-Glu is part of R.sub.1, p-Glu is located at the N terminus of the peptide; R.sub.2 is selected from the group consisting of D-pGlu, D-Gln and Gln; R.sub.3 is selected from the group consisting of D-Ala and Gly; R.sub.4 is selected from the group consisting of Phe and Leu and R.sub.5 is selected from Met and D-Met. Intermediates of the peptides are also provided.

    摘要翻译： 当给予动物时具有温度特性的肽。 肽通过以下结构鉴定：R1-R2-Trp-Ala-Val-R3-His-R4-R5-NH2其中：R1选自氢，选自对 - Glu，Gln，Arg，Leu，Gly，Asn，Thr，Val和Pro，以及具有2至6个氨基酸的肽，其中氨基酸选自p-Glu，Gln，Arg，Leu，Gly，Asn，Thr ，Val和Pro，条件是当p-Glu是R1的一部分时，p-Glu位于肽的N末端; R2选自D-pGlu，D-Gln和Gln; R3选自D-Ala和Gly; R4选自Phe和Leu，R5选自Met和D-Met。 还提供了肽的中间体。

    Analogs of somatostatin
    8.
    发明授权
    Analogs of somatostatin 失效
    生长抑素类似物

    公开(公告)号：US4428942A

    公开(公告)日：1984-01-31

    申请号：US378748

    申请日：1982-05-17

    申请人： Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marvin R. Brown

    发明人： Jean E. F. Rivier ,  Wylie W. Vale, Jr. ,  Marvin R. Brown

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

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16 ,  Y10S930/26

    摘要： Somatostatin-14 has the formula: ##STR1## Analogs that are more potent than somatostatin-14 in increasing electrolyte absorption in the gut without suppressing the secretion of GH, insulin and glucagon, or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals in the same manner as somatostatin to increase absorbtion of electrolytes for the treatment of diarrhea. In particular of the analogs, certain substitutions are made for Phe in the 11-position, sometimes in combination with deletions in the 4- and 5-positions and in the 12- and 13-positions. D-Cys may also be substituted in the 3- or 14-position. There may be some substitutions in the 6- and 10-positions, and the residues in the 1- and/or 2-positions may also be deleted or substituted.

    摘要翻译： 生长抑素-14具有以下分子式：在增加电解质吸收的肠道中比抑制生长抑素-14更有效的类似物，而不抑制分散在药学上可接受的液体中的GH，胰岛素和胰高血糖素或其药学上可接受的盐的分泌， 固体载体可以以与生长抑素相同的方式施用于哺乳动物以增加用于治疗腹泻的电解质的吸收。 特别是类似物，对11位的Phe进行某些取代，有时与4位和5位以及12位和13位的缺失相结合。 D-Cys也可以在3-或14-位取代。 在6-位和10位可能有一些取代，1-和/或2-位的残基也可以被缺失或取代。