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公开(公告)号：US5047502A
公开(公告)日：1991-09-10
申请号：US389093
申请日：1989-08-03
IPC分类号： A61K38/00 , C07K14/575
CPC分类号： C07K14/57572 , A61K38/00
摘要： Small cell lung carcinoma cells (SCLC) contain gastrin releasing peptide (GRP) receptors. The response of the cells to GRP is rapid growth. We have found a group of heptapeptides that act as GRP antagonists by blocking the binding of GRP to its receptor thereby inhibiting the growth of cells that are sensitive to the growth promoting acitivity of GRP.
摘要翻译： 小细胞肺癌细胞（SCLC）含有胃泌素释放肽（GRP）受体。 细胞对GRP的反应是快速增长。 我们已经发现一组作为GRP拮抗剂的七肽通过阻断GRP与其受体的结合，从而抑制对促进GRP活性的生长敏感的细胞的生长。
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公开(公告)号：US06130204A
公开(公告)日：2000-10-10
申请号：US51342
申请日：1998-04-06
IPC分类号： C12Q1/37 , A61K38/00 , A61K45/00 , A61K47/48 , A61K49/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07K5/10 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/47 , A61K38/07 , A61K38/08 , A61K38/48
CPC分类号： C07K14/47 , A61K47/48338 , C07K5/1016 , A61K38/00 , C07K2319/00 , Y10S930/28 , Y10S930/30
摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
摘要翻译： PCT No.PCT / US96 / 15713 Sec。 371日期：1998年4月6日 102（e）1998年4月6日PCT PCT 1996年10月2日PCT公布。 出版物WO97 / 12624 日期：1997年4月10日描述了包含被游离前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列的寡肽。 还描述了包含用于在体外和体内测定游离PSA蛋白酶活性的这种寡肽的测定法。 还描述了包含这种寡肽和已知细胞毒性剂的缀合物的治疗剂。
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公开(公告)号：US6143864A
公开(公告)日：2000-11-07
申请号：US468161
申请日：1995-06-06
IPC分类号： G01N33/566 , A61K31/195 , A61K38/00 , A61K38/08 , A61K47/48 , A61P13/08 , A61P35/00 , A61P43/00 , C07H15/24 , C07K7/06 , C07K7/08 , C07K14/47 , C07K17/08 , C12Q1/37 , G01N33/574 , A61K38/14 , C07K9/00
CPC分类号： C07K14/47 , A61K47/48238 , A61K47/48338 , A61K38/00
摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
摘要翻译： 描述了包含被游离前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列的寡肽。 还描述了包含用于在体外和体内测定游离PSA蛋白酶活性的这种寡肽的测定法。 还描述了包含这种寡肽和已知细胞毒性剂的缀合物的治疗剂。
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公开(公告)号：US5866679A
公开(公告)日：1999-02-02
申请号：US540412
申请日：1995-10-06
IPC分类号： C12Q1/37 , A61K38/00 , A61K45/00 , A61K47/48 , A61K49/00 , A61P13/02 , A61P15/00 , A61P35/00 , C07K5/10 , C07K5/107 , C07K7/06 , C07K7/08 , C07K14/47 , C07K5/09
CPC分类号： C07K14/47 , A61K47/48338 , C07K5/1016 , A61K38/00 , C07K2319/00 , Y10S930/28 , Y10S930/30
摘要： Oligopeptides which comprise amino acid sequences that are recognized and proteolytically cleaved by free prostate specific antigen (PSA) are described. Also described are assays which comprise such oligopeptides useful for determining free PSA protease activity in vitro and in vivo. Therapeutic agents which comprise conjugates of such oligopeptides and known cytotoxic agents are also described.
摘要翻译： 描述了包含被游离前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列的寡肽。 还描述了包含用于在体外和体内测定游离PSA蛋白酶活性的这种寡肽的测定法。 还描述了包含这种寡肽和已知细胞毒性剂的缀合物的治疗剂。
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公开(公告)号：US06177404B1
公开(公告)日：2001-01-23
申请号：US09051759
申请日：1998-08-03
申请人： Deborah DeFeo-Jones , Raymond E. Jones , Allen I. Oliff , Edward M. Scolnick , Victor M. Garsky
发明人： Deborah DeFeo-Jones , Raymond E. Jones , Allen I. Oliff , Edward M. Scolnick , Victor M. Garsky
IPC分类号： A61K3816
CPC分类号： A61K47/65
摘要： Novel pharmaceutical compositions useful for the treatment of benign prostatic hyperplasia which comprises novel oligopeptides, which are selectively cleaved by enzymatically active PSA, in conjugation with a cytotoxic agent are described. Methods of treating benign prostate hypertrophy are also disclosed.
摘要翻译： 描述了可用于治疗良性前列腺增生的新型药物组合物，其包含通过酶活性PSA选择性切割的与细胞毒性剂缀合的新型寡肽。 还公开了治疗良性前列腺肥大的方法。
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公开(公告)号：US06391305B1
公开(公告)日：2002-05-21
申请号：US09254892
申请日：1999-06-28
IPC分类号： A61K3814
CPC分类号： C07K7/06 , A61K38/00 , C07K5/1016
摘要： Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA), hydrophilic oligopeptide blocking groups and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
摘要翻译： 公开了包含具有由游离前列腺特异性抗原（PSA）选择性蛋白水解切割的氨基酸序列，亲水寡肽封闭基团和已知的细胞毒性剂的寡肽的化学共轭物。 这种缀合物可用于治疗前列腺癌和良性前列腺肥大（BPH）。
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公开(公告)号：US5599686A
公开(公告)日：1997-02-04
申请号：US267092
申请日：1994-06-28
CPC分类号： C07K14/47 , A61K47/48338 , A61K38/00
摘要： Assays which comprise oligopeptides and which are useful for determining free PSA protease activity in vitro and in vivo are described. Such oligopeptides comprise amino acid sequences that are recognized and proteolytically cleaved by free prostrate specific antigen (PSA). Also described are assays useful in identifying inhibitors of free PSA.
摘要翻译： 描述了包含寡肽并且其可用于在体外和体内测定游离PSA蛋白酶活性的测定。 这样的寡肽包括由游离的前列腺特异性抗原（PSA）识别和蛋白水解切割的氨基酸序列。 还描述了可用于鉴定游离PSA的抑制剂的测定法。
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公开(公告)号：US5238922A
公开(公告)日：1993-08-24
申请号：US770078
申请日：1991-09-30
IPC分类号： A61K38/55 , A61K38/00 , A61P35/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/083 , C07K5/087 , C07K5/10
CPC分类号： C07K5/0808 , C07K5/0207 , C07K5/06078 , A61K38/00
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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公开(公告)号：US4278596A
公开(公告)日：1981-07-14
申请号：US932089
申请日：1978-08-08
申请人： Victor M. Garsky
发明人： Victor M. Garsky
IPC分类号： A61K38/00 , C07K14/00 , C07K14/70 , C07C103/52 , A61K37/00
CPC分类号： C07K14/702 , A61K38/00 , Y10S514/809
摘要： Pentapeptides of the formula: ##STR1## wherein R.sup.1 is hydrogen, methyl, ethyl, propyl, 2-methyl-2-pentenyl, 2-methyl-1-pentenyl, cyclopropylmethyl, or cyclobutylmethyl; R.sup.2, R.sup.3, and R.sup.4 are, independently, hydrogen or methyl; and X is --OH, --NH.sub.2, --NHC.sub.n H.sub.2n+1 where n is 1, 2, 3, or 4, --OR.sup.3, or CH.sub.2 OR.sup.3, where R.sup.3 is hydrogen or lower alkyl of from 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof; have analgesic activity upon administration to warm-blooded animals.
摘要翻译： 式中：R 1为氢，甲基，乙基，丙基，2-甲基-2-戊烯基，2-甲基-1-戊烯基，环丙基甲基或环丁基甲基的五肽。 R2，R3和R4独立地是氢或甲基; 并且X是-OH，-NH 2，-NHC n H 2n + 1，其中n是1,2,3或4，-OR 3或CH 2 OR 3，其中R 3是氢或具有1至4个碳原子的低级烷基; 或其药学上可接受的盐; 对温血动物施用时具有止痛活性。
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10.发明授权Peptide conjugate compositions and methods for the prevention and treatment of alzheimer's disease 有权肽缀合物组合物和预防和治疗阿尔茨海默病的方法公开(公告)号：US07850973B2
公开(公告)日：2010-12-14
申请号：US11919897
申请日：2006-05-01
申请人： Victor M. Garsky , Joseph G. Joyce , Paul M. Keller , Gene Kinney , Xiaoping Liang , John W. Shiver
发明人： Victor M. Garsky , Joseph G. Joyce , Paul M. Keller , Gene Kinney , Xiaoping Liang , John W. Shiver
CPC分类号： A61K39/0007 , A61K2039/6068 , A61K2039/6087 , A61K2039/6093 , A61K2039/64
摘要： The invention provides compositions and methods for the treatment of diseases associated with amyloid deposits of Aβ in the brain of a patient, such as Alzheimer's disease. Such methods entail administering an immunogenic fragment of Aβ, lacking a T-cell epitope, capable of inducing a beneficial immune response in the form of antibodies to Aβ. In another aspect, the immunogenic fragment of Aβ is capable of elevating plasma Aβ levels. The immunogenic fragments comprise linear or multivalent peptides of Aβ. Pharmaceutical compositions comprise the immunogenic fragment chemically linked to a carrier molecule which may be administered with an adjuvant.
摘要翻译： 本发明提供了用于治疗与淀粉样蛋白沉积相关的疾病的组合物和方法。 在患者的脑中，如阿尔茨海默病。 这种方法需要施用能够以A和Bgr的抗体形式诱导有益的免疫应答的A＆bgr的免疫原性片段，缺少T细胞表位。 另一方面，A＆bgr的免疫原性片段 能够提升血浆A＆bgr; 水平。 免疫原性片段包含A和Bgr的线性或多价肽。 药物组合物包含与可与佐剂一起施用的载体分子化学连接的免疫原性片段。
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