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公开(公告)号：US10308663B2
公开(公告)日：2019-06-04
申请号：US15737062
申请日：2016-06-16
IPC分类号： C07D495/04 , A61K31/4365 , A61P35/00
摘要： The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).
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公开(公告)号：US20180170946A1
公开(公告)日：2018-06-21
申请号：US15737062
申请日：2016-06-16
IPC分类号： C07D495/04 , A61P35/00
CPC分类号： C07D495/04 , A61K31/4365 , A61P35/00
摘要： The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesis of protein tyrosine phosphatase inhibitor and precursor compound thienopyridone (5).
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公开(公告)号：US5856506A
公开(公告)日：1999-01-05
申请号：US917453
申请日：1997-08-22
申请人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
发明人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
IPC分类号： A61K31/421 , A61P35/00 , A61P43/00 , C07D263/34 , C07D263/32
CPC分类号： C07D263/34
摘要： The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.
摘要翻译： 本发明涉及具有下式的化合物：本发明还提供了制备该化合物的方法。 该化合物可用作蛋白磷酸酶的抑制剂，例如PP1，PP2A，PP3，CDC25A和CDC25B。 本发明还涉及抑制蛋白质磷酸酶的方法，抑制细胞增殖的方法以及包含本发明化合物的药物组合物。
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公开(公告)号：US06673937B2
公开(公告)日：2004-01-06
申请号：US09910195
申请日：2001-07-19
申请人： John S. Lazo , Peter Wipf , Billy W. Day
发明人： John S. Lazo , Peter Wipf , Billy W. Day
IPC分类号： C07D40500
CPC分类号： C07D317/72 , A61K31/357 , A61K31/426 , C07D319/08 , C07D403/12 , C07D405/06 , C07D405/12 , C07D493/10
摘要： Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP1 and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1-tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-231 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin—thioredoxin reductase system.
摘要翻译： 双萘基醚的氧化环化允许8-9步骤中棕榈霉素CP1和脱氧阿司咪霉素A的简明综合，5-羟基-8-甲氧基-1-四氢萘酮的总产率为15-35％。 创建了一个古老的棕榈霉素类似物库。 这些萘醌螺旋酮对MCF-7和MDA-MB-231人乳腺癌细胞的生物学评价显示出几种低微摩尔生长抑制剂。 许多类似物抑制硫氧还蛋白硫氧还蛋白还原酶系统。
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公开(公告)号：US5952294A
公开(公告)日：1999-09-14
申请号：US690013
申请日：1996-07-31
申请人： John S. Lazo , Peter Wipf
发明人： John S. Lazo , Peter Wipf
IPC分类号： A61K38/00 , A61P35/00 , A61P35/02 , A61P43/00 , C07K5/02 , A61K38/03 , A61K39/385 , C07K5/00
CPC分类号： C07K5/0202 , A61K38/00
摘要： Peptidyl prodrugs of therapeutic agents having an activating function are sclosed. These therapeutic agents having activating functions include those having an amino, thiol, or hydroxyl function. Methods of making and using these prodrugs are also disclosed.
摘要翻译： 公开了具有激活功能的治疗剂的肽基前体药物。 具有活化功能的这些治疗剂包括具有氨基，硫醇或羟基官能团的那些。 还公开了制备和使用这些前药的方法。
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公开(公告)号：US6040323A
公开(公告)日：2000-03-21
申请号：US917454
申请日：1997-08-22
申请人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
发明人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
IPC分类号： A61K31/421 , A61P35/00 , A61P43/00 , C07D263/34 , A61K31/42
CPC分类号： C07D263/34
摘要： The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.
摘要翻译： 本发明涉及具有下式的化合物：本发明还提供制备该化合物的方法。 该化合物可用作蛋白磷酸酶的抑制剂，例如PP1，PP2A，PP3，CDC25A和CDC25B。 本发明还涉及抑制蛋白质磷酸酶的方法，抑制细胞增殖的方法以及包含本发明化合物的药物组合物。
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公开(公告)号：US5700821A
公开(公告)日：1997-12-23
申请号：US688530
申请日：1996-07-30
申请人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
发明人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
IPC分类号： A61K31/421 , A61P35/00 , A61P43/00 , C07D263/34 , A61K31/42 , C07D263/32
CPC分类号： C07D263/34
摘要： The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.
摘要翻译： 本发明涉及具有下式的化合物：本发明还提供了制备该化合物的方法。 该化合物可用作蛋白磷酸酶的抑制剂，例如PP1，PP2A，PP3，CDC25A和CDC25B。 本发明还涉及抑制蛋白质磷酸酶的方法，抑制细胞增殖的方法以及包含本发明化合物的药物组合物。
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公开(公告)号：US5925660A
公开(公告)日：1999-07-20
申请号：US917016
申请日：1997-08-22
申请人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
发明人： John S. Lazo , Robert L. Rice , April Cunningham , Peter Wipf
IPC分类号： A61K31/421 , A61P35/00 , A61P43/00 , C07D263/34 , A61K31/42 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495
CPC分类号： C07D263/34
摘要： The present invention is directed to compounds having the formula: ##STR1## The invention further provides a method of making the compounds. The compounds are useful as inhibitors of protein phosphatases, for example PP1, PP2A, PP3, CDC25A and CDC25B. The invention is further directed to a method of inhibiting a protein phosphatase, a method of inhibiting cell proliferation, and pharmaceutical compositions comprising the subject compounds.
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公开(公告)号：US20100298352A1
公开(公告)日：2010-11-25
申请号：US12775023
申请日：2010-05-06
申请人： Edward V. Prochownik , John S. Lazo
发明人： Edward V. Prochownik , John S. Lazo
IPC分类号： A61K31/52 , A61K31/353 , A61P35/00
CPC分类号： A61K31/353 , A61K31/52
摘要： A method of inhibiting a carcinoma in a subject, comprising administering to the subject at least one therapeutic agent that selectively targets carcinoma stem cells. Illustrative carcinoma stem cell-selective therapeutic agents include CGP74514A, rottlerin, and A-77636.
摘要翻译： 一种抑制受试者中的癌症的方法，包括向受试者施用选择性靶向癌细胞的至少一种治疗剂。 说明性的癌干细胞选择性治疗剂包括CGP74514A，转铁蛋白和A-77636。
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公开(公告)号：US5420228A
公开(公告)日：1995-05-30
申请号：US182862
申请日：1994-01-14
摘要： A fluorescent-labelled bleomycin analog useful as a probe for measuring cellular uptake of bleomycin and bleomycin derivatives, including methods of making and using same. The analog may further be used as a therapeutic agent as well as a diagnostic tool.
摘要翻译： 可用作测量博来霉素和博来霉素衍生物的细胞摄取的探针的荧光标记的博来霉素类似物，包括制备和使用它们的方法。 该类似物还可用作治疗剂以及诊断工具。
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