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105 条记录 (耗时 0.026 秒)

    Octadecapeptides, intermediates therefor, and compositions and methods employing said octadecapeptides
    41.
    发明授权
    Octadecapeptides, intermediates therefor, and compositions and methods employing said octadecapeptides 失效
    十八肽，其中间体，以及使用所述十八肽的组合物和方法

    公开(公告)号：US4127519A

    公开(公告)日：1978-11-28

    申请号：US807121

    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 ,  Y10S930/12 ,  Y10S930/28

    摘要： Novel octadecapeptides having the following amino acid sequenceH-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-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： 具有以下氨基酸序列H-Tyr-X-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-Phe-Y的新型十八肽其中：X 是D-氨基酸的手性残基，其选自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，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 their uses
    42.
    发明授权
    Multicomponent compositions and their uses 有权
    多组分组合物及其用途

    公开(公告)号：US09358272B2

    公开(公告)日：2016-06-07

    申请号：US13985051

    申请日：2012-02-16

    申请人： David H. Coy ,  Lichun Sun

    发明人： David H. Coy ,  Lichun Sun

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

    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 INHIBITORS OF CALCINEURIN OR INHIBITORS OF THE MAMMALIAN TARGET OF RAPAMYCIN (mTOR) COMPLEXES
    45.
    发明申请
    USE OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND PACAP ANALOGS AS ADJUNCTIVE TREATMENTS WITH INHIBITORS OF CALCINEURIN OR INHIBITORS OF THE MAMMALIAN TARGET OF RAPAMYCIN (mTOR) COMPLEXES 审中-公开
    作为ADAMYLATE CYCLASE-ACTIVATING POLYPEPTIDE（PACAP）和PACAP模拟物作为与RAPAMYCIN（mTOR）复合物的MAMMALIAN目标的CALCINEURIN或抑制剂的抑制剂的ADJUNCTIVE TREATORY的联合使用

    公开(公告)号：US20120309683A1

    公开(公告)日：2012-12-06

    申请号：US13577132

    申请日：2011-02-07

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

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

    IPC分类号： A61K38/17 ,  A61P9/00 ,  C07K14/435 ,  A61P13/12 ,  A61P1/16 ,  A61P1/00 ,  A61P25/00 ,  A61P11/00

    CPC分类号： A61K38/2235 ,  A61K38/13 ,  A61K45/06 ,  A61K2300/00

    摘要： This invention relates to methods and compositions for the treatment, management, reduction, or prevention of injuries to one or more major organs of the body, e.g., the brain, heart, lung, kidneys, liver, and gastrointestinal tract, of a mammal (e.g., a human) caused by one or more calcineurin or mammalian target of rapamycin (mTOR) complex inhibitors. The methods include administering an effective amount of one or more pituitary adenylate cyclase-activating polypeptide (PACAP)-like compounds to the mammal. Combination therapy with one or more PACAP-like compounds, either alone or in combination with one or more other prophylactic/therapeutic agents, plus one or more inhibitors of either calcineurin or the mTOR complexes can be used to treat organ transplantation, autoimmune diseases, graft-versus-host disease, Behçet's disease, hematological cancers, noninfectious uveitis, sarcoidosis, tuberous sclerosis complex, acute neurological diseases, age-related neurodegenerative diseases, Huntington's disease and other CAG codon repeat expansion diseases, keratoconjunctivitis sicca, and restenosis.

    摘要翻译： 本发明涉及用于治疗，管理，减少或预防哺乳动物身体的一个或多个主要器官（例如脑，心，肺，肾，肝和胃肠道）的损伤的方法和组合物（ 由一种或多种神经磷酸酶或哺乳动物雷帕霉素靶标（mTOR）复合物抑制剂引起的人类）。 所述方法包括向哺乳动物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。 单独或与一种或多种其他预防/治疗剂，一种或多种钙调神经磷酸酶或mTOR复合物抑制剂的一种或多种PACAP样化合物的联合治疗可用于治疗器官移植，自身免疫疾病，移植物 冠状动脉疾病，白塞病，血液癌，非感染性葡萄膜炎，结节病，结节性硬化综合征，急性神经系统疾病，年龄相关的神经变性疾病，亨廷顿舞蹈病和其他CAG密码子重复扩张疾病，结膜性角膜结膜炎和再狭窄。

    Flavivirus fusion inhibitors
    46.
    发明申请
    Flavivirus fusion inhibitors 有权
    黄病毒融合抑制剂

    公开(公告)号：US20090209464A1

    公开(公告)日：2009-08-20

    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： A61K38/16 ,  C07K14/00 ,  A61P31/12

    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。

    Somatostatin antagonists
    47.
    发明申请
    Somatostatin antagonists 审中-公开
    生长抑素拮抗剂

    公开(公告)号：US20080171853A1

    公开(公告)日：2008-07-17

    申请号：US12075319

    申请日：2008-03-11

    申请人： David H. Coy ,  Wiliam A. Murphy ,  Walajapet G. Rajeswaran

    发明人： David H. Coy ,  Wiliam A. Murphy ,  Walajapet G. Rajeswaran

    IPC分类号： C07K1/04 ,  C07K1/00

    CPC分类号： A61K38/08 ,  C07K14/655

    摘要： The present invention is directed to a method for synthesizing a peptide using solid-state chemistry in which at least one amide bond is N-methylated, wherein said method of synthesis utilizes N-Boc protected amino acids. For example, the a peptide is first synthesized using N-BOC protected amino acids and 4-methylbenzylhydrylamine functionalized 1% cross linked polystyrene resin until reaching the amide bond to be N-methylated. Then, the amino group at the desired methylation site is methylated. If desired, the synthesis of additional peptide using N-BOC protected amino acids may continued until the desired peptide is complete.

    摘要翻译： 本发明涉及使用其中至少一个酰胺键被N-甲基化的固态化学合成肽的方法，其中所述合成方法使用N-Boc保护的氨基酸。 例如，首先使用N-BOC保护的氨基酸和4-甲基苄基氢化胺官能化的1％交联聚苯乙烯树脂合成肽，直至达到酰胺键为N-甲基化。 然后，将所需甲基化位点处的氨基甲基化。 如果需要，可以继续使用N-BOC保护的氨基酸合成另外的肽，直到所需肽完成。

    Somatostatin antagonists
    48.
    发明授权
    Somatostatin antagonists 有权
    生长抑素拮抗剂

    公开(公告)号：US07378488B2

    公开(公告)日：2008-05-27

    申请号：US10469836

    申请日：2002-03-05

    申请人： David H. Coy ,  William A. Murphy ,  Walajapet G. Rajeswaran

    发明人： David H. Coy ,  William A. Murphy ,  Walajapet G. Rajeswaran

    IPC分类号： A61K38/16 ,  A61K38/00

    CPC分类号： A61K38/08 ,  C07K14/655

    摘要： The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic ∝-amino acid; A2 is an optionally substituted aromatic ∝-amino acid; A3 is Dab, Dap, Lys or Orn; A4 is β-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic -amino acid; and Y1 is OH, NH2 or NHR1, or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic -amino acid is optionally substituted with one or more substituents substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (c2-6)alkenyl, (c2-6)alkynyl, (C1-6)alkoxy, Bzl, O-Bzl, and NR9R10, where R9 ad R10 each is independently H, O, or (C1-6)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof.

    摘要翻译： 本发明涉及式（I）的生长抑素拮抗剂，其中A 1为任选取代的芳族α-氨基酸; A 2是任选取代的芳族α-氨基酸; Dab，Dap，Lys或Orn; Aβ4是β-羟基缬氨酸，Ser，Hser或Thr; A 5是任选取代的D-或L-芳族 - 氨基酸; 和Y 1是OH，NH 2或NHR 1或NHR 1，其中R 1 是（C 1-6）烷基; 其中每个所述任选取代的芳族 - 氨基酸任选地被一个或多个取代基取代，所述取代基各自独立地选自卤素，NO 2，OH，CN，（C 1-6） （C 2-6）烯基，（C 2-6 - ）炔基，（C 1-6 - ）烷基，（C 2-6） 烷氧基，Bzl，O-Bzl和NR 9 R 10，其中R 9和R 10各自为 独立地是H，O或（C 1-6 - ）烷基; 并且其中酰胺肽键和式（I）的A 1的氨基的胺氮任选被甲基取代，条件是存在至少一个所述甲基; 或其药学上可接受的盐，及其用途。

    Somatostatin agonists
    49.
    发明授权
    Somatostatin agonists 有权
    生长抑素激动剂

    公开(公告)号：US07312304B2

    公开(公告)日：2007-12-25

    申请号：US10474248

    申请日：2002-04-08

    申请人： David H. Coy ,  Walajapet G. Rajeswaran

    发明人： David H. Coy ,  Walajapet G. Rajeswaran

    IPC分类号： A61K38/22 ,  A61K38/04 ,  A61K38/00

    CPC分类号： C07K14/6555 ,  A61K38/00

    摘要： Claimed are a series of somatostatin agonists and uses thereof, according to formula (I), A1-cyclo[Cys-A2-D-Trp-A3-A4-Cys]-A5-Y1,   (I) wherein A1, A2, A3, A4, A5 and Y1 are as defined in specification provided that the amine nitrogen of at least one peptide bond is substituted with a methyl group or pharmaceutically acceptable salts thereof.

    摘要翻译： 根据式（I），所述是一系列生长抑素激动剂及其用途，<？在线公式描述=“在线公式”end =“lead”？> A 环[Cys-A 2-D-Trp-A 3 -S-4-Cys] -A 5 -I <1>，（I）<？in-line-formula description =“In-line formula”end =“tail”？>其中A 1， > 2 ，A 3，A 4，A 5和Y 1如下所定义。 规定，至少一个肽键的胺氮被甲基取代或其药学上可接受的盐。