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33 条记录 (耗时 0.025 秒)

    Bradykinin analogs with non-peptide bond
    1.
    发明授权
    Bradykinin analogs with non-peptide bond 失效
    具有非肽键的缓激肽类似物

    公开(公告)号：US5750646A

    公开(公告)日：1998-05-12

    申请号：US408197

    申请日：1995-03-22

    申请人： David H. Coy ,  Jacques-Pierre Moreau ,  John E. Taylor ,  Sun Hyuk Kim

    发明人： David H. Coy ,  Jacques-Pierre Moreau ,  John E. Taylor ,  Sun Hyuk Kim

    IPC分类号： A61K38/00 ,  C07K7/18 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： C07K7/18 ,  A61K38/00

    摘要： A linear peptide which is an analog of a naturally occurring, biologically active peptide having an active site and a binding site responsible for the binding of the peptide to a receptor on a target cell, cleavage of a peptide bond in the active site to the naturally occurring peptide being unnecessary for in vivo biological activity, the analog having a non-peptide bond instead of a peptide bond between an amino acid of the active site and an adjacent amino acid, and having the same binding site as the naturally occurring peptide, so that the analog is capable of acting as a competitive inhibitor of the naturally occurring peptide by binding to the receptor and, by virtue of the non-peptide bond, failing to exhibit the in vivo activity of the naturally occurring peptide.

    摘要翻译： 线性肽，其是具有活性位点的天然存在的生物活性肽的类似物，以及负责肽与靶细胞上的受体结合的结合位点，将活性位点中的肽键切割成天然 发生的肽对于体内生物活性是不必要的，该类似物具有非肽键而不是活性位点的氨基酸与相邻氨基酸之间的肽键，并且具有与天然存在的肽相同的结合位点，因此 该类似物能够通过结合受体而作为天然存在的肽的竞争性抑制剂，并且由于非肽键，不能显示出天然存在的肽的体内活性。

    Opioid peptides
    2.
    发明授权
    Opioid peptides 失效
    阿片类肽

    公开(公告)号：US5663295A

    公开(公告)日：1997-09-02

    申请号：US352391

    申请日：1994-12-08

    申请人： Jacques-Pierre Moreau ,  Sun Hyuk Kim ,  John E. Taylor

    发明人： Jacques-Pierre Moreau ,  Sun Hyuk Kim ,  John E. Taylor

    IPC分类号： A61K38/00 ,  A61P25/00 ,  C07K5/02 ,  C07K5/027 ,  C07K5/065 ,  C07K5/087 ,  C07K5/107 ,  C07K7/06 ,  C07K14/575 ,  C07K14/655 ,  C07K7/00

    CPC分类号： C07K7/06 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/0812 ,  C07K5/1016 ,  A61K38/00

    摘要： Opioid peptides including those of the formula ##STR1## in which A.sub.1 is the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, azatyrosine, and 2,6-dimethyltyrosine; A.sub.2 is the identifying group of an amino acid selected from D-Ala and D-Arg; A.sub.3 is H, or the identifying group of an amino acid selected from of 3,4-dihydroxyphenylalanine and 3,4-dimethoxyphenylalanine, A.sub.4 is H, cyclohexylmethyl, the identifying group of an amino acid selected from 3,4-dihydroxyphenylalanine, 3,4-dimethoxyphenylalanine, Phe, and substituted Phe with its benzene ring substituted by halogen, NO.sub.2, OH, or CH.sub.3 ; A.sub.5 is the identifying group of a D- or L-amino acid selected from Leu, Nle, Lys, Met and Met(O), or is deleted together with R.sub.4 --CH attached thereto; each R.sub.1 and R.sub.2 is --H, --C(NH.sub.2).dbd.NH, or C.sub.1-12 alkyl; R.sub.3 is ##STR2## R.sub.4 is ##STR3## and R.sub.5 is --(CH.sub.2).sub.n+1 OH, ##STR4## wherein m is 0-6, n is 0-6, and X is H, C.sub.1-12 alkyl, C.sub.6-12 aryl, C.sub.7-18 aralkyl, C.sub.7-18 alkaryl, C.sub.7-18 alkayl, C.sub.6-17 pyridylalkyl, or C.sub.6-17 alkylpyridyl; provided that when one of R.sub.1 and R.sub.2 is --C(NH.sub.2).dbd.NH, the other must be H; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 阿片样肽包括式“IMAGE”的那些，其中A1是选自3,4-二羟基苯丙氨酸，3,4-二甲氧基苯丙氨酸，氨甲酰酪氨酸和2,6-二甲基酪氨酸的氨基酸的鉴定基团; A2是选自D-Ala和D-Arg的氨基酸的鉴定基团; A3是H，或选自3,4-二羟基苯丙氨酸和3,4-二甲氧基苯丙氨酸的氨基酸的鉴定基团，A4是H，环己基甲基，选自3,4-二羟基苯丙氨酸， 4-二甲氧基苯丙氨酸，Phe和取代的Phe，其苯环被卤素，NO 2，OH或CH 3取代; A5是选自Leu，Nle，Lys，Met和Met（O）的D-或L-氨基酸的鉴定基团，或与其连接的R4-CH一起缺失; 每个R 1和R 2是-H，-C（NH 2）= NH或C 1-12烷基; R3是，R4是，R5是 - （CH2）n + 1OH，其中m是0-6，n是0-6，X是H，C1-12烷基，C6-12 芳基，C7-18芳烷基，C7-18烷芳基，C7-18烷基，C6-17吡啶基烷基或C6-17烷基吡啶基; 条件是当R 1和R 2中的一个是-C（NH 2）= NH时，另一个必须是H; 或其药学上可接受的盐。

    Cyclic octapeptide neuromedin B receptor antagonists
    7.
    发明授权
    Cyclic octapeptide neuromedin B receptor antagonists 失效
    循环八肽神经介肽B受体拮抗剂

    公开(公告)号：US5569741A

    公开(公告)日：1996-10-29

    申请号：US352392

    申请日：1994-12-08

    申请人： David H. Coy ,  John E. Taylor

    发明人： David H. Coy ,  John E. Taylor

    IPC分类号： A61K38/00 ,  A61K38/31 ,  A61P43/00 ,  C07K7/06 ,  C07K7/52 ,  C07K14/655 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

    CPC分类号： A61K38/31 ,  C07K14/6555

    摘要： A cyclic octapeptide of the formula: ##STR1## wherein: A.sup.1 is D-Nal or D-Trp;A.sup.3 is Phe, F.sub.5 -Phe, or X-Phe wherein X is a halogen, NO.sub.2, CH.sub.3, or OH;A.sup.5 is --NH--CH(Y)--CO-- wherein Y is (CH.sub.2).sub.m --R.sub.4 --N(R.sub.5)(R.sub.6) or (CH.sub.2).sub.n --R.sub.4 --NH--C(R.sub.7)--N(R.sub.5) (R.sub.6);A.sup.6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu;A.sup.8 is Nal or Trp;m is 1, 2, or 3;n is 1, 2, 3, 4 or 5;each of R.sub.1 and R.sub.2, independently, is H, E, COE, or COOE wherein E is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, phenyl, naphthyl, C.sub.7-12 phenylalkyl or alkylphenyl, C.sub.8-12 phenylalkenyl or alkenylphenyl, C.sub.8-12 phenylalkynyl or alkynylphenyl, C.sub.11-20 naphthylalkyl or alkylnaphthyl, C.sub.12-20 naphthylalkenyl or alkenylnaphthyl, or C.sub.12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R.sub.1 or R.sub.2 is COE or COOE, the other must be H;R.sub.4 is C.sub.6 H.sub.4 or absent;R.sub.7 is .dbd.NR.sub.8, .dbd.S, or .dbd.O; andeach of R.sub.3, R.sub.5, R.sub.6, and R.sub.8, independently, is H or E.

    摘要翻译： 下式的环状八肽：其中：A1为D-Nal或D-Trp; A3是Phe，F5-Phe或X-Phe，其中X是卤素，NO 2，CH 3或OH; A5是-NH-CH（Y）-CO-，其中Y是（CH2）m-R4-N（R5）（R6）或（CH2）n-R4-NH-C（R7）-N（R5） ）; A6是Thr，Leu，Ile，Nle，Val和Abu的D-或L-异构体; A8是Nal或Trp; m为1,2或3; n为1,2,3,4或5; R 1和R 2各自独立地是H，E，COE或COOE，其中E是C 1-12烷基，C 2-12烯基，C 2-12炔基，苯基，萘基，C 7-12苯基烷基或烷基苯基，C 8-12苯基烯基 或烯基苯基，C 8-12苯基炔基或炔基苯基，C 11-20萘基烷基或烷基萘基，C 12-20萘基烯基或链烯基萘基，或C 12-20萘基炔基或炔基萘基，条件是当R 1或R 2中的一个为COE或COOE时，另一个必须为H ; R4为C6H4或不存在; R 7 = NR 8，= S或= O; R 3，R 5，R 6和R 8各自独立地为H或E.

    Urotensin-II agonists and antagonists
    9.
    发明授权
    Urotensin-II agonists and antagonists 失效
    促肾上腺素Ⅱ激动剂和拮抗剂

    公开(公告)号：US07241737B2

    公开(公告)日：2007-07-10

    申请号：US10399542

    申请日：2001-10-19

    申请人： David H. Coy ,  Wojciech J. Rossowski ,  John E. Taylor

    发明人： David H. Coy ,  Wojciech J. Rossowski ,  John E. Taylor

    IPC分类号： A61K38/08 ,  C07K7/06

    CPC分类号： C07K7/52 ,  A61K38/00 ,  C07K14/57509

    摘要： The present invention is directed to a novel class of cyclic polypeptides of the formula: (R1)a-AA1-cyclo[AA2-AA3-AA4-AA5-AA6-Cys]-AA7-R2, pharmaceutically acceptable salts thereof, wherein the variables are as defined in the specification, which inhibit the effects of urotensin-II and are useful for treating a variety of diseases and/or conditions characterized by an excess of urotensin-II including ischaemic heart disease, congestive heart failure, portal hypertension, variceal bleeding, hypotension, angina pectoris, myocardial infarction, ulcers, anxiety, schizophrenia, manic depression, delirium, dementia, mental retardation and/or dyskinesias.

    摘要翻译： 本发明涉及一类新型的下式的环状多肽：（R 1）a-A 1 - 环[AA] SUP→2→A→3→A→4→A→5→A→6→Cys〕 其中所述变量如本说明书中所定义，其抑制泌尿生长素-2的作用，并且可用于治疗 多种疾病和/或病症，其特征在于过量的泌尿生长素II，包括缺血性心脏病，充血性心力衰竭，门静脉高压，静脉曲张出血，低血压，心绞痛，心肌梗死，溃疡，焦虑，精神分裂症，躁狂抑郁，del妄，痴呆 ，精神发育迟滞和/或运动障碍。

    Overhead flexible electric conductor
    10.
    发明授权
    Overhead flexible electric conductor 失效
    架空柔性电导体

    公开(公告)号：US4699461A

    公开(公告)日：1987-10-13

    申请号：US711248

    申请日：1985-03-13

    申请人： John E. Taylor ,  Ian W. Keene

    发明人： John E. Taylor ,  Ian W. Keene

    IPC分类号： H01B7/17 ,  G02B6/44 ,  H01B5/10

    CPC分类号： G02B6/4422 ,  G02B6/4403 ,  G02B6/4407 ,  H01B5/108 ,  D07B1/147

    摘要： An overhead electric conductor comprises a central tubular metal core, at least one layer of helically wound bare metal wires surrounding the core and, loosely housed in the bore of the core, at least one optical fibre element. The optical fibre element comprises a flexible tube of elongate transverse cross-section in which is loosely housed an optical fibre ribbon structure and which is resiliently set in such a form that it follows a path of smoothly curved undulations, the axes of curvature of which lie parallel to one another and normal to the axis of the tube. Should a tensile force applied to the overhead conductor be transferred to the loosely housed optical fibre element, the flexible tube of the element will tend to straighten in a lengthwise direction against the action of its resilient set thereby to reduce any tensile force that might otherwise be applied to the optical fibres and, when the tensile force is removed, the tube will return under the action of its resilient set towards its original form.

    摘要翻译： 架空电导体包括中心管状金属芯，围绕芯的至少一层螺旋缠绕的裸金属线，并松散地容纳在芯的孔中，至少一个光纤元件。 光纤元件包括细长横截面的柔性管，其中松散地容纳光纤带结构，并且弹性地设置成使得其遵循平滑弯曲的起伏的路径，其曲率轴线位于 彼此平行并垂直于管轴。 如果施加到架空导体的拉力传递到松散收容的光纤元件，则该元件的柔性管将倾向于抵抗其弹性组的作用沿长度方向拉直，从而减小否则可能的任何张力 应用于光纤，并且当拉力被去除时，管将在其弹性组件的作用下返回到其原始形式。