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105 条记录 (耗时 0.028 秒)

    Urotensin-II agonists and antagonists
    1.
    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。

    Cyclic octapeptide neuromedin B receptor antagonists
    3.
    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.

    Bradykinin analogs with non-peptide bond
    7.
    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。

    Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof
    10.
    发明授权
    Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof 有权
    抑制生长素释放肽/生长激素分泌受体途径及其用途的方法

    公开(公告)号：US08883721B2

    公开(公告)日：2014-11-11

    申请号：US13320408

    申请日：2010-05-12

    申请人： Cyril Y. Bowers ,  David H. Coy ,  Simon J. Hocart ,  Gloria S. Tannenbaum

    发明人： Cyril Y. Bowers ,  David H. Coy ,  Simon J. Hocart ,  Gloria S. Tannenbaum

    IPC分类号： A61K38/08 ,  A61K38/10 ,  C07K7/06 ,  C07K7/08 ,  A61K31/00 ,  A61K45/06 ,  A61K31/404 ,  A61K38/16 ,  A61K38/25

    CPC分类号： A61K38/08 ,  A61K31/00 ,  A61K31/404 ,  A61K38/10 ,  A61K38/16 ,  A61K38/25 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18 (SEQ ID NO: 93), wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.

    摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18（SEQ ID NO：93），其中A11，A12 ，并且A13独立地不存在，氨基酸或氨基保护基; A15，A16，A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基共轭的 - （O）C1-C20烷基或二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。