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    • 2. 发明授权
    • Use of Ginkgo extract
    • 使用银杏提取物
    • US07078434B1
    • 2006-07-18
    • US10018448
    • 2000-08-11
    • Katy DrieuVassilios Papadopoulos
    • Katy DrieuVassilios Papadopoulos
    • A61K31/34A61K36/16
    • A61K31/34A61K36/16
    • The present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated Ginkgolide B (GKB), a component of the extract of Ginkgo biloba leaves in a method for decreasing the expression of peripheral-type benzodiazepine receptor (PBR) in cells of a patient in need thereof. Further, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method for decreasing the proliferation of cancer cells in a patient. More particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method of decreasing cancer cell proliferation in a patient wherein the cancer cell is human breast cancer cell. Even more particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in method of decreasing cancer cell proliferation in a patient wherein the cancer cell is of the aggressive and invasive phenotype and expresses high levels of PBR in comparison to non-aggressive cancer cell.
    • 本发明涉及银杏提取物或银杏叶提取物的分离银杏内酯B(GKB)提取物在细胞中降低外周型苯二氮受体(PBR)表达的方法中的用途。 的需要的患者。 此外,本发明涉及银杏叶提取物或分离的GKB在减少患者癌细胞增殖的方法中的用途。 更具体地,本发明涉及银杏叶提取物或分离的GKB在癌细胞是人乳腺癌细胞的患者中降低癌细胞增殖的方法中的用途。 更具体地,本发明涉及银杏提取物或分离的GKB在降低癌细胞增殖的方法中的用途,其中癌细胞具有侵袭性和侵袭性表型,并且表达高水平的PBR 与非侵袭性癌细胞的比较。
    • 6. 发明申请
    • Octapeptide bombesin analogs
    • 八肽铃蟾肽类似物
    • US20050026827A1
    • 2005-02-03
    • US10788563
    • 2004-02-27
    • David CoyJacques-Pierre MoreauSun Kim
    • David CoyJacques-Pierre MoreauSun Kim
    • A61K38/00C07K7/02C07K7/08C07K7/18C07K14/575C07K14/685A61K38/17
    • C07K7/086A61K38/00C07K7/02C07K7/18C07K14/57572C07K14/685
    • 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.
    • 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。
    • 8. 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。