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公开(公告)号：US5998362A
公开(公告)日：1999-12-07
申请号：US926412
申请日：1997-09-09
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).
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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：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：US06174858B1
公开(公告)日：2001-01-16
申请号：US09193365
申请日：1998-11-17
IPC分类号： A61K3800
CPC分类号： C07K5/1016 , A61K38/00 , A61K47/65 , C07K5/1013 , C07K14/47 , Y10S530/828
摘要： Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. The conjugates of the invention are characterized by attachment of the cleavable oligopeptide to the oxygen atom at the 4-position on a vinca drug that has be desacetylated. 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）和已知的细胞毒性剂选择性蛋白水解切割的氨基酸序列的寡肽的化学共轭物。 本发明的缀合物的特征在于将可切割的寡肽与已经脱乙酰化的长春花药物的4-位上的氧原子连接。 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：US5948750A
公开(公告)日：1999-09-07
申请号：US950805
申请日：1997-10-14
CPC分类号： C07K14/47 , A61K47/48338 , A61K38/00
摘要： Chemical conjugates which comprise oligopeptides, having amino acid sequences that are selectively proteolytically cleaved by free prostate specific antigen (PSA) and known cytotoxic agents are disclosed. Such conjugates are useful in the treatment of prostatic cancer and benign prostatic hypertrophy (BPH).
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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：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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