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1. 发明申请

US20050026827A1 Octapeptide bombesin analogs 审中-公开
标题翻译：八肽铃蟾肽类似物
公开(公告)号：US20050026827A1
公开(公告)日：2005-02-03
申请号：US10788563
申请日：2004-02-27
申请人： David Coy , Jacques-Pierre Moreau , Sun Kim
发明人： David Coy , Jacques-Pierre Moreau , Sun Kim
IPC分类号： A61K38/00 , C07K7/02 , C07K7/08 , C07K7/18 , C07K14/575 , C07K14/685 , A61K38/17
CPC分类号： C07K7/086 , A61K38/00 , C07K7/02 , C07K7/18 , C07K14/57572 , C07K14/685
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 β-amino acid, or a γ-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。而不是活性位点的氨基酸残基与相邻氨基酸残基之间的肽键。

2. 发明申请

US20050075480A1 Urotensin-II agonists and antagonists 失效
标题翻译：促肾上腺素Ⅱ激动剂和拮抗剂
公开(公告)号：US20050075480A1
公开(公告)日：2005-04-07
申请号：US10399542
申请日：2001-10-19
申请人： David Coy , Wojciech Rossowski , John Taylor
发明人： David Coy , Wojciech Rossowski , John Taylor
IPC分类号： A61K38/00 , A61K38/12 , A61P1/04 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/14 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07K7/06 , C07K7/52 , C07K7/64 , C07K14/575
CPC分类号： C07K7/52 , A61K38/00 , C07K14/57509
摘要： The present invention features a novel class of cyclic polypeptides that have U-II antagonist and agonist activity. The invention also features methods for treating physiological or psychological conditions characterized by an excess or under expression of Ur4otensin-II.
摘要翻译：本发明的特征在于具有U-II拮抗剂和激动剂活性的新一类环状多肽。本发明还具有用于治疗特征在于Ur4otensin-II过量或低表达的生理或心理状态的方法。

3. 发明申请

US20050070470A1 Diagnostic or therapeutic somatostatin or bombesin analog conjugates and uses thereof 有权
标题翻译：诊断或治疗性生长抑素或铃蟾肽类似物缀合物及其用途
公开(公告)号：US20050070470A1
公开(公告)日：2005-03-31
申请号：US10490326
申请日：2002-09-20
申请人： David Coy , Joseph Fuselier , William Murphy , Lichun Sun
发明人： David Coy , Joseph Fuselier , William Murphy , Lichun Sun
IPC分类号： A61K47/48 , A61B20060101 , A61B1/00 , A61K20060101 , A61K31/165 , A61K31/4745 , A61K31/519 , A61K38/00 , A61K38/08 , A61K38/10 , A61K38/31 , A61K47/42 , A61K49/00 , A61K51/00 , A61K51/08 , A61P1/00 , A61P9/00 , A61P11/00 , A61P13/08 , A61P15/00 , A61P25/00 , A61P27/02 , A61P35/00 , C07K7/06 , C07K7/08 , C07K14/655
CPC分类号： A61K51/088 , A61K47/58 , A61K47/60 , A61K47/64 , A61K51/083
摘要： Disclosed are peptide agents and uses thereof that are analogs of biologically active peptides such as somatostatin and bombesin. The compounds of the invention have the general formula X-Y-Z-Q, where X is a cytotoxic agent, therapeutic agent, detectable label or chelating group, and Q is a biologically active peptide. In peptide agents of the invention Y is optionally a hydrophilic polymer or peptide, and Z is a linking peptide bonded to Q at the amino terminus of Q, having two, three, four, or five, amino acid residues selected to link X to Q, while retaining the biological activity of Q. Methods of using these peptide agents in the diagnosis and treatment of diseases are also disclosed.
摘要翻译：公开了作为生物活性肽类似物的生物抑素和铃蟾肽的肽剂及其用途。本发明化合物具有通式X-Y-Z-Q，其中X为细胞毒性剂，治疗剂，可检测标记或螯合基团，Q为生物活性肽。在本发明的肽剂中，Y任选是亲水性聚合物或肽，Z是在Q的氨基末端键合至Q的连接肽，其具有选择用于连接X至Q的两个，三个，四个或五个氨基酸残基同时保留Q的生物活性。还公开了在诊断和治疗疾病中使用这些肽剂的方法。

4. 发明申请

US20080090756A1 Somatostatin agonists 审中-公开
公开(公告)号：US20080090756A1
公开(公告)日：2008-04-17
申请号：US11973954
申请日：2007-10-11
申请人： David Coy , Walajapet Rajeswaran
发明人： David Coy , Walajapet Rajeswaran
IPC分类号： A61K38/12 , A61P1/00 , A61P3/00 , A61P35/00 , A61P5/00 , C07K7/50
CPC分类号： C07K14/6555 , A61K38/00
摘要： Claimed are a series of somatostatin agonists typically characterized by alkylation of the amide nitrogen, and uses thereof. Examples of claimed compounds are those according to formula (I), A1-cyclo{Cys-A2-D-Trp-A3-A4-Cys}-A5-Y1, (I) wherein: A1 is an optionally substituted D- or L-aromatic α-amino acid or optionally substituted D- or L-cyclo(C3-6)alkylalanine; A2 is an optionally substituted aromatic α-amino acid or optionally substituted cyclo(C3-6)alkylalanine; A3 is Lys or Orn; A4 is β-Hydroxyvaline, Ser, hSer, or Thr; A5 is β-Hydroxyvaline, Ser, hSer, or Thr; and Y1 is OH, NH2 or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic α-amino acid and each said optionally substituted cyclo(C3-6)alkylalanine is optionally substituted with one or more 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 and R10 each is independently H or (C1-6) alkyl; and wherein the amine nitrogen of each 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; and further provided that said compound is not D-Phe-cyclo{Cys-Phe-D-Trp-Lys-(N-Me-Thr)-Cys}-Thr-NH2; or a pharmaceutically acceptable salt thereof.

5. 发明申请

US20070287665A1 Urotensin-II agonists and antagonists 审中-公开
标题翻译：促肾上腺素Ⅱ激动剂和拮抗剂
公开(公告)号：US20070287665A1
公开(公告)日：2007-12-13
申请号：US11821823
申请日：2007-06-26
申请人： David Coy , Wojciech Rossowski , John Taylor
发明人： David Coy , Wojciech Rossowski , John Taylor
IPC分类号： A61K38/12 , A61P9/00 , C07K7/50
CPC分类号： C07K7/52 , A61K38/00 , C07K14/57509
摘要： The present invention features a novel class of cyclic polypeptides that have U-II antagonist and agonist activity. The invention also features methods for treating physiological or psychological conditions characterized by an excess or an under expression of Urotensin-II.
摘要翻译：本发明的特征在于具有U-II拮抗剂和激动剂活性的新一类环状多肽。本发明还具有用于治疗特征在于过度或未表达的促rotensin-II的生理或心理状态的方法。

6. 发明授权

US5776901A Polypeptide analogues having growth hormone releasing activity 失效
标题翻译：具有生长激素释放活性的多肽类似物
公开(公告)号：US5776901A
公开(公告)日：1998-07-07
申请号：US932494
申请日：1992-08-20
申请人： Cyril Y. Bowers , David Coy
发明人： Cyril Y. Bowers , David Coy
IPC分类号： A61K38/04 , A61K38/00 , A61K38/03 , A61K38/08 , A61P3/06 , A61P5/02 , C07K20060101 , C07K1/04 , C07K1/08 , C07K7/06 , C07K14/575 , C07K14/60 , C07K5/00 , C07K7/00
CPC分类号： C07K14/60
摘要： Novel peptides of the formula A.sub.1 -A.sub.2 -C.sub.1 -C.sub.2 -C.sub.3 -A.sub.5 are disclosed which promote the release of growth hormone when administered to animals. These peptides can be used therapeutically.
摘要翻译：公开了式A1-A2-C1-C2-C3-A5的新型肽，其在施用于动物时促进生长激素的释放。这些肽可用于治疗。

7. 发明申请

US20080020970A1 Somatostatin antagonists 有权
标题翻译：生长抑素拮抗剂
公开(公告)号：US20080020970A1
公开(公告)日：2008-01-24
申请号：US11894231
申请日：2007-08-20
申请人： David Coy , William Murphy , Walajapet Rajeswaran
发明人： David Coy , William Murphy , Walajapet Rajeswaran
IPC分类号： A61K38/00 , A61P9/00
CPC分类号： A61K38/08 , C07K14/655
摘要： A1-cyclo{D-Cys-A2-D-Trp-A3-A4-Cys}-A5-Y1 (I) The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic ax-amino acid; A2 is an optionally substituted aromatic α-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, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic-amino acid is optionally substituted with one or more 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： <？in-line-formula description =“In-line Formulas”end =“lead”？> A <1> Trp-A <3> -line-formula description =“In-line Formulas”end =“tail”？本发明涉及根据式（I）的生长抑素拮抗剂，其中A 1是任选取代的芳族斧氨酸; 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; 并且Y 1是OH，NH 2或NHR 1，其中R 1是（C 1） -6 N）烷基; 其中每个所述任选取代的芳族 - 氨基酸任选被一个或多个独立地选自卤素，NO 2，OH，CN，（C 1-6）烷基的取代基取代，（C 2-6 - ）烷基，（C 2-6）烯基，（C 2-6）炔基，（C 1-6 - ）烷氧基，Bzl，O-Bzl和NR 9 R 10，其中R 9和R 10各自独立地为 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。

8. 发明申请

US20070259811A1 Method of modulating the proliferation of medullary thyroid carcinoma cells 有权
标题翻译：调节甲状腺髓样癌细胞增殖的方法
公开(公告)号：US20070259811A1
公开(公告)日：2007-11-08
申请号：US11799594
申请日：2007-05-02
申请人： Ettore Degli Uberti , Maria Zatelli , Michael Culler , David Coy
发明人： Ettore Degli Uberti , Maria Zatelli , Michael Culler , David Coy
IPC分类号： A61K38/12 , A61P35/00 , C12N5/02
CPC分类号： A61K38/31 , A61K38/08
摘要： The present invention is directed to a method of decreasing the rate of proliferation of medullary thyroid carcinoma cells which comprises contacting medullary thyroid carcinoma cells with one or more SSTR2 agonist. A somatostatin receptor antagonist having the formula Cpa-cyclo(D-Cys-4-Pal-D-Trp-Lys-Thr-Cys)-Nal-NH2 is also disclosed.
摘要翻译：本发明涉及一种降低髓样甲状腺癌细胞增殖速率的方法，其包括使髓样甲状腺癌细胞与一种或多种SSTR2激动剂接触。还公开了具有式Cpa-cyclo（D-Cys-4-Pal-D-Trp-Lys-Thr-Cys）-Nal-NH 2的生长抑素受体拮抗剂。

9. 发明申请

US20060009622A1 Conjugates of therapeutic or cytotoxic agents and biologically active peptides 有权
标题翻译：治疗或细胞毒素和生物活性肽的共轭物
公开(公告)号：US20060009622A1
公开(公告)日：2006-01-12
申请号：US10506223
申请日：2003-03-03
申请人： Joseph Fuselier , David Coy
发明人： Joseph Fuselier , David Coy
IPC分类号： A61K38/17 , C07K14/47
CPC分类号： A61K47/642 , A61K47/65
摘要： The invention features conjugates of therapeutic or cytotoxic agents and biologically active peptides and methods of use thereof.
摘要翻译：本发明涉及治疗性或细胞毒性剂和生物活性肽的缀合物及其使用方法。

10. 发明申请

US20050271677A1 Flavivirus fusion inhibitors 有权
标题翻译：黄病毒融合抑制剂
公开(公告)号：US20050271677A1
公开(公告)日：2005-12-08
申请号：US10532480
申请日：2003-11-07
申请人： Robert Garry , Srikanta Dash , David Coy
发明人： Robert Garry , Srikanta Dash , David Coy
IPC分类号： A61K38/00 , A61K38/16 , A61K39/00 , A61K39/12 , A61K39/193 , A61K39/29 , A61K39/295 , A61K39/38 , A61P31/14 , C07K14/18 , C07K16/10 , C12Q20060101
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：瘟病毒的乙型肝炎病毒的E 1包膜糖蛋白和E 2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。

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