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    • 1. 发明授权
    • Urotensin-II agonists and antagonists
    • 促肾上腺素Ⅱ激动剂和拮抗剂
    • US07241737B2
    • 2007-07-10
    • US10399542
    • 2001-10-19
    • David H. CoyWojciech J. RossowskiJohn E. Taylor
    • David H. CoyWojciech J. RossowskiJohn E. Taylor
    • A61K38/08C07K7/06
    • C07K7/52A61K38/00C07K14/57509
    • 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.
    • 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。
    • 5. 发明授权
    • Cyclic octapeptide neuromedin B receptor antagonists
    • 循环八肽神经介肽B受体拮抗剂
    • US5569741A
    • 1996-10-29
    • US352392
    • 1994-12-08
    • David H. CoyJohn E. Taylor
    • David H. CoyJohn E. Taylor
    • A61K38/00A61K38/31A61P43/00C07K7/06C07K7/52C07K14/655C07K5/00C07K7/00C07K17/00
    • A61K38/31C07K14/6555
    • 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.
    • 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.
    • 9. 发明授权
    • Overhead flexible electric conductor
    • 架空柔性电导体
    • US4699461A
    • 1987-10-13
    • US711248
    • 1985-03-13
    • John E. TaylorIan W. Keene
    • John E. TaylorIan W. Keene
    • H01B7/17G02B6/44H01B5/10
    • G02B6/4422G02B6/4403G02B6/4407H01B5/108D07B1/147
    • 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.
    • 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。