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公开(公告)号：US5026685A
公开(公告)日：1991-06-25
申请号：US219596
申请日：1988-07-15
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57545 , A61K38/00
摘要： Human Neuropeptide Y(NPY) has the formula: H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala- Pro-Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr- Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH.sub.2. Porcine and rat NPY have the same sequence except for Leu instead of Met in the 17-position. Porcine PYY is homologous having 11 different residues. NPY analogs wherein the N-terminus is shortened and which may contain one or more specific subsitutions for the naturally occurring residues, or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals, including humans, to substantially lower blood pressure over an extended period of time or to counteract hypertension.
摘要翻译： 人神经肽Y（NPY）具有下式：H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala- Pro-Ala-Glu-Asp-Met-Ala-Arg- Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH2。 猪和大鼠NPY具有相同的序列，除了Leu而不是17位的Met。 猪PYY具有11个不同残基的同源物。 NPY类似物，其中N末端被缩短并且可以含有分散在药学上可接受的液体或固体载体中的天然存在的残基或其药学上可接受的盐的一个或多个特异性亚基，可以包括人哺乳动物 在较长时间内显着降低血压或抵抗高血压。
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公开(公告)号：US4393050A
公开(公告)日：1983-07-12
申请号：US258878
申请日：1981-04-29
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。
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公开(公告)号：USRE30548E
公开(公告)日：1981-03-17
申请号：US071559
申请日：1979-08-31
IPC分类号： A61K38/00 , C07K14/655
CPC分类号： C07K14/6555 , A61K38/00
摘要： The present invention relates to peptides which possess biological activity in respect to the inhibition of growth hormone, insulin .[.secretion.]. and glucagon secretion .[.are provided.].. The peptides have fewer amino acid components than somatostatin and some of the peptides have dissociated activity. .Iadd.
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4.发明授权Synthetic calcitonin-gene-related peptides for lowering blood pressure or gastric acid secretion in mammals 失效用于降低哺乳动物血压或胃酸分泌的合成降钙素基因相关肽
公开(公告)号：US4530838A
公开(公告)日：1985-07-23
申请号：US512421
申请日：1983-07-08
申请人： Ronald M. Evans , Larry Swanson , Wylie W. Vale, Jr. , Michael G. Rosenfeld , Susan G. Amara , Marvin R. Brown , Jean E. F. Rivier
发明人： Ronald M. Evans , Larry Swanson , Wylie W. Vale, Jr. , Michael G. Rosenfeld , Susan G. Amara , Marvin R. Brown , Jean E. F. Rivier
IPC分类号： A61K38/00 , C07K14/575 , A61K37/02 , C07C103/52
CPC分类号： C07K14/57527 , A61K38/00
摘要： CGRP (calcitonin-gene-related peptide) has the formula: ##STR1## A related peptide has the residue Lys instead of Glu in the 35-position. CGRP or this homolog or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals, including humans, to influence memory, mood and pain appreciation and to achieve a substantial lowering of blood pressure or gastric acid secretion over an extended period of time. They also may be administered to affect ingestion behavior, taste and sensory perception.
摘要翻译： CGRP（降钙素基因相关肽）具有以下分子式：其中，ArgLeuAlaGlyLeuLeuSerArgSerGly GlyValValLysAspAsnPheValProThr + TR AsnValGlySerGluAlaPheNH2。 相关肽在35位具有残基Lys而不是Glu。 分散在药学上可接受的液体或固体载体中的CGRP或其同系物或其药学上可接受的盐可以施用于包括人在内的哺乳动物，以影响记忆，情绪和疼痛升高，并实现血压或胃酸分泌的显着降低 在很长一段时间内。 它们也可以被施用以影响摄取行为，味觉和感觉知觉。
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公开(公告)号：US4211693A
公开(公告)日：1980-07-08
申请号：US967505
申请日：1978-12-07
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。
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公开(公告)号：US4133782A
公开(公告)日：1979-01-09
申请号：US785533
申请日：1977-04-07
IPC分类号： A61K38/00 , C07K14/655 , C08L37/00 , C07C103/52
CPC分类号： C07K14/6555 , A61K38/00 , Y10S930/12 , Y10S930/16
摘要： The present invention relates to peptides having dissociated biological activity in respect to the inhibition of growth hormone, insulin, and glucagon secretion. The peptides are analogs of somatostatin.
摘要翻译： 本发明涉及在抑制生长激素，胰岛素和胰高血糖素分泌方面具有解离生物活性的肽。 肽是生长抑素的类似物。
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公开(公告)号：US4605642A
公开(公告)日：1986-08-12
申请号：US583092
申请日：1984-02-23
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。
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公开(公告)号：US4331661A
公开(公告)日：1982-05-25
申请号：US193621
申请日：1980-10-03
IPC分类号： A61K38/00 , C07K7/08 , A61K37/00 , C07C103/52
摘要： Peptides having thermoregulative and analgesic 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-Leu-Met-NH.sub.2wherein: R.sub.1 is an acyl moiety selected from the group consisting of formyl, acetyl, propionyl, acrylyl and benzoyl; R.sub.2 is selected from the group consisting of Gly and the D- and L-isomers of Ala, Asn, Gln, His, Leu, Met, Phe, Ser, Thr and Val; R.sub.3 is selected from the group consisting of D-Ala and Gly. Intermediates of the peptides are also provided.
摘要翻译： 当给动物施用时具有调温和镇痛特性的肽。 肽通过以下结构鉴定：R1-R2-Trp-Ala-Val-R3-His-Leu-Met-NH2其中：R1是选自甲酰基，乙酰基，丙酰基，丙烯酰基和苯甲酰基的酰基部分; R2选自Gly和Ala，Asn，Gln，His，Leu，Met，Phe，Ser，Thr和Val的D-和L-异构体; R3选自D-Ala和Gly。 还提供了肽的中间体。
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公开(公告)号：US5328899A
公开(公告)日：1994-07-12
申请号：US882923
申请日：1992-05-12
IPC分类号： A61K38/00 , C07K14/575 , A61K37/02 , C07K7/08 , C07K7/10
CPC分类号： C07K14/57545 , A61K38/00
摘要： Human Neuropeptide Y (NPY) has the formula: H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro- Ala-Glu-Asp-Met-Ala-Arg-Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile- Thr-Arg-Gln-Arg -Tyr-NH.sub.2. Porcine and rat NPY have the same sequence except for Leu instead of Met in the 17-position. Porcine PYY is homologous having 11 different residues. NPY analogs and N-terminally-shortened fragments, e.g. NPY(18-36), which contain one or more specific D-isomer substitutions for the naturally occurring residues (as well as pharmaceutically acceptable salts thereof), dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals, including humans, to substantially lower blood pressure over an extended period of time or to counteract hypertension.
摘要翻译： 人神经肽Y（NPY）具有下式：H-Tyr-Pro-Ser-Lys-Pro-Asp-Asn-Pro-Gly-Glu-Asp-Ala-Pro-Ala-Glu-Asp-Met-Ala-Arg- Tyr-Tyr-Ser-Ala-Leu-Arg-His-Tyr-Ile-Asn-Leu-Ile-Thr-Arg-Gln-Arg-Tyr-NH2。 猪和大鼠NPY具有相同的序列，除了Leu而不是17位的Met。 猪PYY具有11个不同残基的同源物。 NPY类似物和N-末端缩短的片段，例如 对于分散在药学上可接受的液体或固体载体中的天然存在的残基（以及其药学上可接受的盐）含有一个或多个特异性D-异构体取代的NPY（18-36）可以施用于包括人在内的哺乳动物 ，以在更长的时间内大幅降低血压或抵抗高血压。
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公开(公告)号：US4428942A
公开(公告)日：1984-01-31
申请号：US378748
申请日：1982-05-17
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。
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