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1. 发明授权

US5354871A Pyrroline N-oxide derivatives 失效
标题翻译：吡咯啉N-氧化物衍生物
公开(公告)号：US5354871A
公开(公告)日：1994-10-11
申请号：US46727
申请日：1993-04-16
申请人： Prabhat Arya , David Griller
发明人： Prabhat Arya , David Griller
IPC分类号： C07D207/46 , C07D495/04 , C07D403/12 , C07D495/02
CPC分类号： C07D495/04 , C07D207/46
摘要： Derivatives of 3,5-substituted pyrroline N-oxides having substituents in the 4-position have been prepared, with the 4-position substituents being selected from certain ester, polyether, and alkanoyl groups, the latter having components which bind to biological substrates. These specific derivatives are effective as spin traps for different types of free radicals to form persistent nitroxide adducts of extended half life. These adducts can be characterized by ESR spectrometry technique and provide information e.g. concerning the identification of free radicals.
摘要翻译：已经制备了在4-位具有取代基的3,5-取代的吡咯啉N-氧化物的衍生物，其中4-位取代基选自某些酯，聚醚和烷酰基，后者具有结合生物底物的成分。这些具体的衍生物作为不同类型的自由基的自旋捕获剂是有效的，以形成延长的半衰期的持久的氮氧化物加合物。这些加合物可以通过ESR分光技术进行表征，并提供信息。关于自由基的鉴定。

2. 发明申请

US20090068094A1 INHIBITORS OF ENDO-EXONUCLEASE ACTIVITY FOR TREATING CANCER 审中-公开
标题翻译：内切除酶活性抑制剂治疗癌症
公开(公告)号：US20090068094A1
公开(公告)日：2009-03-12
申请号：US12199603
申请日：2008-08-27
申请人： Terry Chow , Chiaoli Yeh , David Griller , Leonard Yuen
发明人： Terry Chow , Chiaoli Yeh , David Griller , Leonard Yuen
IPC分类号： A61K31/155 , A61K33/24 , A61K31/407 , A61K31/195 , A61K31/704 , A61K31/505 , A61K31/175 , A61K38/17 , A61K39/395 , A61K51/10 , A61K9/127 , A61K51/12 , A61P35/00
CPC分类号： A61K45/06 , A61K31/155 , A61K31/337 , A61K33/24 , A61K2300/00
摘要： The present invention relates to the treatment of cancer with compounds that inhibit the activity of endo-exonuclease. Endo-exonuclease has been shown to be necessary for the repair of damaged DNA. Compounds that inhibit the activity of endo-exonuclease have been shown to be particularly effective for treating cancer when used in combination with drugs that induce DNA breaks such as cisplatin and mitomycin C. These compounds have a synergistic effect when used in combination for inhibiting tumour growth. The invention includes pharmaceutical compositions for inhibiting tumour growth comprising a compound that inhibits endo-exonuclease activity. These pharmaceutical compositions preferably include compounds that induce DNA breaks. The invention includes methods of treating cancer with these pharmaceutical compositions and uses of these compositions to treat cancer. The preferred compounds that inhibit the activity of endo-exonuclease have low toxicity. One such compound is pentamidine. The invention also includes a method for diagnosing cancer and monitoring its progression. This aspect of the invention involves isolating serum from a patient; measuring the concentration of endo-exonuclease in said serum and determining whether said concentration is above a predetermined mean.
摘要翻译：本发明涉及用抑制内切核酸酶活性的化合物治疗癌症。内切核酸外切酶已被证明是修复受损DNA所必需的。当与使用顺铂和丝裂霉素C的DNA断裂药物组合使用时，抑制内切核酸外切酶活性的化合物已被证明对于治疗癌症是特别有效的。当组合用于抑制肿瘤生长时，这些化合物具有协同作用。本发明包括用于抑制肿瘤生长的药物组合物，其包含抑制内切核酸酶活性的化合物。这些药物组合物优选包括诱导DNA断裂的化合物。本发明包括用这些药物组合物治疗癌症的方法和这些组合物用于治疗癌症的方法。抑制内切核酸酶活性的优选化合物具有低毒性。一种这样的化合物是戊脒。本发明还包括用于诊断癌症并监测其进展的方法。本发明的这个方面涉及从患者中分离血清; 测量所述血清中内切核酸外切酶的浓度并确定所述浓度是否高于预定平均值。

3. 发明申请

US20120128667A1 PENTAMIDINE COMBINATIONS FOR TREATING CANCER 审中-公开
标题翻译：哌啶类联合治疗癌症
公开(公告)号：US20120128667A1
公开(公告)日：2012-05-24
申请号：US13318197
申请日：2010-05-03
申请人： Terry Chow , Chiaoli Yeh , David Griller
发明人： Terry Chow , Chiaoli Yeh , David Griller
IPC分类号： A61K31/155 , A61K31/7068 , A61K31/4545 , A61P35/04 , A61K31/505 , A61K39/395 , A61P35/00 , A61P35/02 , A61K31/282 , A61K31/519
CPC分类号： A61K9/0019 , A61K31/155 , A61K31/282 , A61K31/337 , A61K31/4745 , A61K31/513 , A61K31/7068 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the treatment of cancer, e.g., ovarian cancer, breast cancer, pancreatic cancer or colon cancer, with pentamidine and (a) oxaliplatin, (b) gemcitabine, (c) taxol, (d) 5-fluorouracil or (e) CPT 11.
摘要翻译：本发明涉及用戊脒和（a）奥沙利铂治疗癌症，例如卵巢癌，乳腺癌，胰腺癌或结肠癌，（b）吉西他滨，（c）紫杉醇，（d）5-氟尿嘧啶或（ e）CPT 11。

4. 发明授权

US4973783A Dehalogenation of halogenated aromatic compounds 失效
标题翻译：卤代芳族化合物的脱卤
公开(公告)号：US4973783A
公开(公告)日：1990-11-27
申请号：US324004
申请日：1989-03-16
申请人： David Griller , Jalal A. Hawari , Derek J. McPhee
发明人： David Griller , Jalal A. Hawari , Derek J. McPhee
IPC分类号： A62D3/00 , A62D3/34 , A62D3/37 , A62D101/22 , C07C1/26
CPC分类号： A62D3/34 , C07C1/26 , A62D2101/22
摘要： Various halogenated aromatic compounds, particularly polychlorinated biphls, and the like, are dehalogenated by reaction with alkali metal in the presence of liquid hydrosiloxane. A selected solvent or diluent may be present. The alkali metal halide reaction product may be removed by washing. It has been found substantially complete dehalogenation is achieved readily at ambient temperatures when the hydrosiloxane is present. The dehalogenated aromatic moiety normally is recovered intact. This method has been found very effective in the destruction and removal of PCB contaminants.
摘要翻译：各种卤代芳族化合物，特别是多氯联苯等通过在液态氢硅氧烷存在下与碱金属反应进行脱卤。可以存在所选择的溶剂或稀释剂。可以通过洗涤除去碱金属卤化物反应产物。已经发现，当存在氢硅氧烷时，在环境温度下容易实现基本上完全的脱卤。脱卤芳族部分通常被完整地回收。已经发现这种方法在PCB污染物的破坏和去除方面非常有效。

5. 发明授权

US07115665B1 Inhibitors of endo-exonuclease activity for treating cancer 有权
标题翻译：用于治疗癌症的内切核酸酶活性的抑制剂
公开(公告)号：US07115665B1
公开(公告)日：2006-10-03
申请号：US10129546
申请日：2000-11-16
申请人： Terry Chow , Chiaoli Yeh , David Griller , Leonard Yuen
发明人： Terry Chow , Chiaoli Yeh , David Griller , Leonard Yuen
IPC分类号： A61K31/04 , A61K31/14
CPC分类号： A61K31/04 , A61K31/14
摘要： The present invention relates to the treatment of cancer with compounds that inhibit the activity of endo-exonuclease. Endo-exonuclease has been shown to be necessary for the repair of damaged DNA. Compounds that inhibit the activity of endo-exonuclease have been shown to be particularly effective for treating cancer when used in combination with drugs that induce DNA breaks such as cisplatin and mitomycin C. These compounds have a synergistic effect when used in combination for inhibiting tumour growth. The invention includes pharmaceutical compositions for inhibiting tumour growth comprising a compound that inhibits endo-exonuclease activity. These pharmaceutical compositions preferably include compounds that induce DNA breaks. The invention includes methods of treating cancer with these pharmaceutical compositions and uses of these compositions to treat cancer. The preferred compounds that inhibit the activity of endo-exonuclease have low toxicity. One such compound is pentamidine. The invention also includes a method for diagnosing cancer and monitoring its progression. This aspect of the invention involves isolating serum from a patient; measuring the concentration of endo-exonuclease in said serum and determining whether said concentration is above a predetermined mean.
摘要翻译：本发明涉及用抑制内切核酸酶活性的化合物治疗癌症。内切核酸外切酶已被证明是修复受损DNA所必需的。当与使用顺铂和丝裂霉素C的DNA断裂药物组合使用时，抑制内切核酸外切酶活性的化合物已被证明对于治疗癌症是特别有效的。当组合用于抑制肿瘤生长时，这些化合物具有协同作用。本发明包括用于抑制肿瘤生长的药物组合物，其包含抑制内切核酸酶活性的化合物。这些药物组合物优选包括诱导DNA断裂的化合物。本发明包括用这些药物组合物治疗癌症的方法和这些组合物用于治疗癌症的方法。抑制内切核酸酶活性的优选化合物具有低毒性。一种这样的化合物是戊脒。本发明还包括用于诊断癌症并监测其进展的方法。本发明的这个方面涉及从患者中分离血清; 测量所述血清中内切核酸外切酶的浓度并确定所述浓度是否高于预定平均值。

6. 发明申请

US20060276548A1 INHIBITORS OF ENDO-EXONUCLEASE ACTIVITY FOR TREATING CANCER 审中-公开
公开(公告)号：US20060276548A1
公开(公告)日：2006-12-07
申请号：US11420358
申请日：2006-05-25
申请人： Terry Chow , Chiaoli Yeh , David Griller , Leonard Yuen
发明人： Terry Chow , Chiaoli Yeh , David Griller , Leonard Yuen
IPC分类号： A61K31/155
CPC分类号： A61K45/06 , A61K31/155 , A61K31/337 , A61K33/24 , A61K2300/00
摘要： The present invention relates to the treatment of cancer with compounds that inhibit the activity of endo-exonuclease. Endo-exonuclease has been shown to be necessary for the repair of damaged DNA. Compounds that inhibit the activity of endo-exonuclease have been shown to be particularly effective for treating cancer when used in combination with drugs that induce DNA breaks such as cisplatin and mitomycin C. These compounds have a synergistic effect when used in combination for inhibiting tumour growth. The invention includes pharmaceutical compositions for inhibiting tumour growth comprising a compound that inhibits endo-exonuclease activity. These pharmaceutical compositions preferably include compounds that induce DNA breaks. The invention includes methods of treating cancer with these pharmaceutical compositions and uses of these compositions to treat cancer. The preferred compounds that inhibit the activity of endo-exonuclease have low toxicity. One such compound is pentamidine. The invention also includes a method for diagnosing cancer and monitoring its progression. This aspect of the invention involves isolating serum from a patient; measuring the concentration of endo-exonuclease in said serum and determining whether said concentration is above a predetermined mean.

7. 发明授权

US5178091A Product and method for detecting a low level of liquid in a liquid reservoir 失效
公开(公告)号：US5178091A
公开(公告)日：1993-01-12
申请号：US589499
申请日：1990-09-28
申请人： David Griller , Robert Gould
发明人： David Griller , Robert Gould
IPC分类号： G01F23/00 , G01F23/22 , G08B5/40
CPC分类号： G01F23/0046 , G01F23/0007 , G01F23/22 , G08B5/40
摘要： This invention relates to a novel means for detecting a low level of liquid in a reservoir. One application for the invention is to provide a way to indicate when the level of windshield washer fluid for a vehicle is at a low level. According to one of its broad aspects, the windshield washer fluid noticeable changes color on the windshield, when it is running low in the reservoir; for example, changing from very light blue to an intense red. There are known electrical and mechanical means for indicating the level of a fluid in a reservoir. However, these indicators of fluid level rely on special equipment such as floats and electrical contacts. An advantage of the present invention, is that it can be used with existing windshield washer reservoirs without the need for additional equipment and/or gauges in the interior of the vehicle. According to one aspect of this invention, the windshield washer reservoir contains a first liquid which usually would be ordinary windshield washer fluid, normally of a light blue or light green color and normally comprising a mixture of water, methyl alcohol and a dye. Added to this first liquid in the reservoir is a second liquid having a specific gravity different from and floating on top of the first liquid such that when the first liquid is exhausted, the windshield washer delivery system will then pump, on to the windshield, the second liquid. This provides an advance warning the windshield fluid is running low; however the second liquid will continue to be available to clean the windshield for as long as previously planned. The second liquid has a color that is noticeably different from that of the first liquid so that it is apparent the first liquid has been consumed. Hexyl alcohol is one example of a second liquid that is relatively immiscible with, and works well with ordinary windshield washer fluid as a first liquid. The hexyl alcohol based second liquid can be colored bright red, for example, with a dye that is relatively insoluble in the ordinary windshield washer fluid.

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