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105 条记录 (耗时 0.035 秒)

    Novel derivatives of gamma-endorphins, intermediates therefor, and compositions and methods employing said derivatives
    82.
    发明授权
    Novel derivatives of gamma-endorphins, intermediates therefor, and compositions and methods employing said derivatives 失效
    γ-内啡肽的新型衍生物，其中间体，以及使用所述衍生物的组合物和方法

    公开(公告)号：US4127518A

    公开(公告)日：1978-11-28

    申请号：US807120

    申请日：1977-06-16

    申请人： David H. Coy ,  Abba J. Kastin

    发明人： David H. Coy ,  Abba J. Kastin

    IPC分类号： A61K38/00 ,  C07K14/675 ,  C08L37/00 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/6755 ,  A61K38/00 ,  Y10S514/809 ,  Y10S930/28

    摘要： Novel .gamma.-endorphins represented by the formula 1H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Ywherein: X is a chiral residue of a D-amino acid selected from the group consisting of D-alanine, D-leucine, D-isoleucine, D-valine, D-phenylalanine, D-tyrosine, D-tryptophan, D-serine, D-threonine, D-methionine, D-glutamic acid, D-glutamine, D-proline D-aspartic acid, D-asparagine, D-lysine, D-arginine and D-histidine; and Y is selected from the group consisting of hydroxy, amino, loweralkylamino, diloweralkylamino and lower alkoxy; and the pharmaceutically acceptable salts thereof; intermediates useful in making the novel compounds; and pharmaceutical compositions and methods employing the novel compounds.

    摘要翻译： 由式1 H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Y表示的新型γ-内啡肽其中：X为 选自D-丙氨酸，D-亮氨酸，D-异亮氨酸，D-缬氨酸，D-苯丙氨酸，D-酪氨酸，D-色氨酸，D-丝氨酸，D-苏氨酸的D-氨基酸的手性残基 ，D-甲硫氨酸，D-谷氨酸，D-谷氨酰胺，D-脯氨酸D-天冬氨酸，D-天冬酰胺，D-赖氨酸，D-精氨酸和D-组氨酸; Y选自羟基，氨基，低级烷基氨基，二低级烷基氨基和低级烷氧基; 及其药学上可接受的盐; 用于制备新型化合物的中间体; 以及使用该新化合物的药物组合物和方法。

    MULTICOMPONENT COMPOSITIONS AND THE USES
    83.
    发明申请
    MULTICOMPONENT COMPOSITIONS AND THE USES 有权
    多组分组合物和用途

    公开(公告)号：US20140045752A1

    公开(公告)日：2014-02-13

    申请号：US13985051

    申请日：2012-02-16

    申请人： David H. Coy ,  Linchun Sun

    发明人： David H. Coy ,  Linchun Sun

    IPC分类号： A61K38/31 ,  A61K31/19

    CPC分类号： A61K38/31 ,  A61K31/19 ,  A61K45/06

    摘要： Multicomponent compositions and methods of use thereof are disclosed herein. Some embodiments of the present invention include multicomponent compositions comprising a first component and a second component, where the first component comprises a notch influencing molecule and the second component comprises a GPCR targeted molecule. Kits comprising the multicomponent composition are also disclosed. Methods for providing the multicomponent composition to one or more cells are additionally provided. Further embodiments include methods of using the multicomponent composition such as, for example, methods of administering the multicomponent composition and method of treating organisms (such as mammals) using the multicomponent composition.

    摘要翻译： 本文公开了多组分组合物及其使用方法。 本发明的一些实施方案包括包含第一组分和第二组分的多组分组合物，其中第一组分包含缺口影响分子，第二组分包含GPCR靶分子。 还公开了包含多组分组合物的试剂盒。 另外提供了将多组分组合物提供给一个或多个细胞的方法。 另外的实施方案包括使用多组分组合物的方法，例如使用多组分组合物施用多组分组合物的方法和治疗生物体（例如哺乳动物）的方法。

    USE OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND PACAP ANALOGS AS ADJUNCTIVE TREATMENTS WITH ANTICANCER AGENTS
    84.
    发明申请
    USE OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND PACAP ANALOGS AS ADJUNCTIVE TREATMENTS WITH ANTICANCER AGENTS 审中-公开
    作为辅助治疗剂，用抗炎剂代谢使用亚硝酸酯环化酶活化多肽（PACAP）和PACAP类似物

    公开(公告)号：US20110268789A1

    公开(公告)日：2011-11-03

    申请号：US13120862

    申请日：2009-09-25

    申请人： Min Li ,  Jerome L. Maderdrut ,  David H. Coy ,  Vecihi Batuman

    发明人： Min Li ,  Jerome L. Maderdrut ,  David H. Coy ,  Vecihi Batuman

    IPC分类号： A61K9/127 ,  A61K47/48 ,  A61K38/43 ,  A61K9/00 ,  A61K9/14 ,  A61K39/395 ,  A61P39/02 ,  A61K38/17 ,  A61K35/00

    CPC分类号： A61K38/16

    摘要： This invention relates to methods and compositions for the treatment, management or prevention of injuries to one or more of the organs of the body, such as the brain, heart, lung, kidneys, liver, and gastrointestinal tract, of humans or other mammals caused by one or more anticancer agents. The methods of this invention consist of the administration of an effective amount of one or more pituitary adenylate cyclase-activating polypeptide (PACAP)-like compounds, which includes native human PACAP38, native human PACAP27, native human vasoactive intestinal peptide (VIP), their agonists, analogs, fragments, and derivatives, with activities toward one or more of the PACAP/VIP receptors, including all of their various isoforms. This invention also provides pharmaceutical compositions of one or more PACAP-like compounds of the invention either alone or in combination with one or more other prophylactic/therapeutic agents useful for the treatment, management or prevention of injuries to the organs of the body of humans or other mammals undergoing cancer chemotherapy. Combination therapy with one or more PACAP-like compounds plus one or more anticancer agents can be used in the treatment of hematological cancers.

    摘要翻译： 本发明涉及用于治疗，管理或预防人或其它哺乳动物的一种或多种身体的器官如脑，心脏，肺，肾脏，肝脏和胃肠道的损伤的方法和组合物 通过一种或多种抗癌剂。 本发明的方法包括施用有效量的一种或多种垂体腺苷酸环化酶活化多肽（PACAP）样化合物，其包括天然人PACAP38，天然人PACAP27，天然人血管活性肠肽（VIP），它们 激动剂，类似物，片段和衍生物，具有对一种或多种PACAP / VIP受体的活性，包括其所有各种同种型。 本发明还提供本发明的一种或多种PACAP样化合物的药物组合物，其单独或与一种或多种其它预防/治疗剂组合使用，所述其它预防/治疗剂可用于治疗，管理或预防对人的身体的器官的损伤或 其他哺乳动物进行癌症化疗。 与一种或多种PACAP样化合物加上一种或多种抗癌剂的联合治疗可以用于治疗血液癌症。

    Flavivirus fusion inhibitors
    85.
    发明授权
    Flavivirus fusion inhibitors 有权
    黄病毒融合抑制剂

    公开(公告)号：US07854937B2

    公开(公告)日：2010-12-21

    申请号：US12229436

    申请日：2008-08-22

    申请人： Robert F. Garry ,  Srikanta Dash ,  David H. Coy ,  Jane A. McKeating

    发明人： Robert F. Garry ,  Srikanta Dash ,  David H. Coy ,  Jane A. McKeating

    IPC分类号： A61K39/12

    CPC分类号： C07K14/005 ,  A61K38/162 ,  A61K39/00 ,  C12N2770/24022 ,  C12N2770/24122 ,  C12N2770/24222 ,  C12N2770/24322 ,  C12N2770/36122 ,  Y02A50/394

    摘要： The present invention relates to peptides and methods of inhibiting fusion between the virion envelope of Flaviviruses and membranes of the target cell, the process that delivers the viral genome into the cell cytoplasm. The invention provides for methods which employ peptides or peptide derivatives to inhibit Flavivirus:cell fusion. The present invention is based in part on the discovery that E1 envelope glycoprotein of hepaciviruses and E2 envelope glycoprotein of pestivirus have previously undescribed structures, truncated class II fusion proteins. The present invention provides peptides and methods of treatment and prophylaxis of diseases induced by Flaviviruses.

    摘要翻译： 本发明涉及抑制黄病毒病毒粒子与目标细胞膜之间的融合的肽和方法，其将病毒基因组递送到细胞质中。 本发明提供了使用肽或肽衍生物抑制黄病毒：细胞融合的方法。 本发明部分地基于以下发现：瘟病毒的HCV病毒的E1包膜糖蛋白和E2包膜糖蛋白具有先前未被描述的结构，截短的II类融合蛋白。 本发明提供治疗和预防由黄病毒引起的疾病的肽和方法。

    Octapeptide bombesin analogs
    88.
    发明授权
    Octapeptide bombesin analogs 失效
    八肽铃蟾肽类似物

    公开(公告)号：US5877277A

    公开(公告)日：1999-03-02

    申请号：US337127

    申请日：1994-11-10

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

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

    IPC分类号： A61K38/00 ,  C07K7/02 ,  C07K7/08 ,  C07K7/18 ,  C07K14/575 ,  C07K14/685 ,  C07K5/00 ,  C07K7/00 ,  C07K7/06

    CPC分类号： C07K7/086 ,  C07K14/57572 ,  C07K14/685 ,  C07K7/02 ,  C07K7/18 ,  A61K38/00

    摘要： A linear (i.e., non-cyclic) analog of biologically active amphibian bombesin, mammalian gastrin-releasing peptide (GRP), or mammalian growth hormone releasing factor (GRF), 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 of naturally occurring bombesin, GRP, or GRF is unnecessary for in vivo biological activity. The analog has one of the following modifications: (a) a deletion of an amino acid residue within the active site and a modification of an amino acid residue outside of the active site, (b) a replacement of two amino acid residues within the active site with a synthetic amino acid, a .beta.-amino acid, or a .gamma.-amino acid residue, or (c) a non-peptide bond instead of a peptide bond between an amino acid residue of the active site and an adjacent amino acid residue.

    摘要翻译： 具有活性位点和负责肽结合的结合位点的生物活性水陆两栖铃蟾肽，哺乳动物胃泌素释放肽（GRP）或哺乳动物生长激素释放因子（GRF）的线性（即非循环）类似物 到目标细胞上的受体。 在天然存在的铃蟾肽，GRP或GRF的活性位点中肽键的切割对于体内生物活性是不必要的。 类似物具有以下修饰之一：（a）活性位点内的氨基酸残基的缺失和活性位点之外的氨基酸残基的修饰，（b）在活性位点内置换两个氨基酸残基 具有合成氨基酸，β-氨基酸或γ-氨基酸残基的位点，或（c）非肽键代替活性位点的氨基酸残基与相邻氨基酸残基之间的肽键 。

    Octapeptide analogs of somatostatin having threonine at the sixth position
    89.
    发明授权
    Octapeptide analogs of somatostatin having threonine at the sixth position 失效
    生长抑素的八肽类似物在第六位具有苏氨酸

    公开(公告)号：US5506339A

    公开(公告)日：1996-04-09

    申请号：US840621

    申请日：1992-02-21

    申请人： David H. Coy ,  William A. Murphy

    发明人： David H. Coy ,  William A. Murphy

    IPC分类号： A61K38/04 ,  A61K31/00 ,  A61K38/00 ,  A61P5/00 ,  A61P5/02 ,  C07K14/575 ,  C07K14/655

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

    摘要： A compound of the formula: ##STR1## wherein each A.sub.1 and A.sub.2, independently, is H, C.sub.1-12 alkyl, C.sub.7-10 phenylalkyl, R.sub.1 CO (where R.sub.1 is C.sub.1-20 alkyl, C.sub.3-20 alkenyl, C.sub.3-20 alkinyl, phenyl, naphthyl, or C.sub.7-10 phenylalkyl), or R.sub.2 OCO (where R.sub.2 is C.sub.1-10 alkyl or C.sub.7-10 phenylalkyl), provided that when one of A.sub.1 or A.sub.2 is R.sub.1 CO or R.sub.2 OCO, the other must be H;each X.sub.1 and X.sub.2, independently, is H, F, Cl, Br, OH, CH.sub.3, or CF.sub.3, provided that at least one of X.sub.1 and X.sub.2 must be H;A.sub.3 is Phe or Tyr; andA.sub.4 is OH, NH.sub.2, or NH-R.sub.3 (wherein R.sub.3 is a saturated aliphatic C.sub.1-8 alkyl);or a pharmaceutically acceptable salt thereof. A therapeutic composition containing the compound of the present invention and a method of using the same are also described.

    摘要翻译： 其中每个A1和A2独立地是H，C1-12烷基，C7-10苯基烷基，R1CO（其中R1是C1-20烷基，C3-20烯基，C3-20炔基， 苯基，萘基或C7-10苯基烷基）或R2OCO（其中R2为C1-10烷基或C7-10苯基烷基），条件是当A1或A2之一为R1CO或R2OCO时，另一个必须为H; 每个X 1和X 2独立地是H，F，Cl，Br，OH，CH 3或CF 3，条件是X 1和X 2中的至少一个必须是H; A3是Phe或Tyr; 并且A4是OH，NH 2或NH-R 3（其中R 3是饱和脂族C 1-8烷基）; 或其药学上可接受的盐。 还描述了含有本发明化合物的治疗组合物及其使用方法。

    Growth hormone-releasing peptides and method of treating animals, therewith
    90.
    发明授权
    Growth hormone-releasing peptides and method of treating animals, therewith 失效
    生长激素释放肽和治疗动物的方法

    公开(公告)号：US5416073A

    公开(公告)日：1995-05-16

    申请号：US807821

    申请日：1985-12-16

    申请人： David H. Coy ,  William A. Murphy

    发明人： David H. Coy ,  William A. Murphy

    IPC分类号： A61K38/00 ,  C07K14/60 ,  A61K38/27 ,  C07K7/00

    CPC分类号： C07K14/60 ,  A61K38/00

    摘要： The present invention relates to novel growth hormone-releasing peptides and method for increasing the release of growth hormone levels in mammals, as well as method for increasing milk production in dairy cows and increasing growth rates of animals, such as cattle, sheep, swine, and others. The novel peptides of this invention surprisingly are effective for releasing growth hormone levels in animals by replacing the natural amino acids in positions 1, 2, 3, 8, 9, 10, 12, 21 and 27, as well as derivatizing the N-terminal amino acid residue in human pancreatic islet tumor origin growth hormone-releasing factor.

    摘要翻译： 本发明涉及新型生长激素释放肽和增加哺乳动物生长激素水平释放的方法，以及增加奶牛产奶量和增加动物如牛，绵羊，猪， 和别的。 本发明新颖的肽令人惊奇的是通过替代1,2,3,4,8,9,10,12,21和27位的天然氨基酸以及衍生N末端有效释放动物中的生长激素水平 人胰岛细胞中的氨基酸残基起源于生长激素释放因子。