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31. 发明授权

US07829117B2 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
标题翻译：用于减少化学治疗剂不期望的毒性的化合物和方法
公开(公告)号：US07829117B2
公开(公告)日：2010-11-09
申请号：US11985241
申请日：2007-11-14
申请人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
发明人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
IPC分类号： A61K31/74
CPC分类号： A61K45/06 , A61K38/00
摘要： Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.
摘要翻译：公开了作为各种化学治疗剂的毒性还原剂和某些疾病和病症治疗的新型组合物和制剂。物质的组成是2-巯基乙磺酸钠的氨基酸和肽杂合二硫化物。

32. 发明申请

US20090232827A1 Compositions and methods of use of compounds to increase cancer patient survival time 有权
标题翻译：使用化合物增加癌症患者生存时间的组合物和方法
公开(公告)号：US20090232827A1
公开(公告)日：2009-09-17
申请号：US12218470
申请日：2008-07-15
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K39/395 , A61K31/105 , A61K31/095 , A61K31/505 , A61K31/7064 , A61K31/7076 , A61K31/337 , A61K31/282 , C12Q1/02 , A61P35/00 , C12Q1/68 , A61K33/24 , A61K31/704 , A61K31/437 , A61K38/43 , A61K38/16 , A61K38/02
CPC分类号： A61K33/24 , A61K31/095 , A61K31/105 , A61K31/282 , A61K31/337 , A61K31/437 , A61K31/505 , A61K31/704 , A61K31/7064 , A61K31/7076 , A61K38/05 , A61K38/06 , A61K45/06 , G01N33/57407 , G01N2333/90212 , A61K2300/00
摘要： The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in time of survival in cancer patients, wherein the cancer either: (i) overexpresses thioredoxin or glutaredoxin and/or (ii) exhibits evidence of thioredoxin- or glutaredoxin-mediated resistance to one or more chemotherapeutic interventions. The present invention also discloses and claims methods and kits for the administration of said compositions to properly treat cancer patients. Additionally, the present invention discloses and claims methods and kits for quantitatively determining the level of expression of thioredoxin or glutaredoxin in the cancer cells of a cancer patient, methods of using those determined levels in the initial diagnosis and/or planning of subsequent treatment methodologies for said cancer patient, as well as ascertaining the potential growth “aggressiveness” of the particular cancer and treatment responsiveness of the particular type of cancer. Further, the present invention discloses and claims novel pharmaceutical compositions, methods, and kits used for the treatment of patients with medical conditions and disease where there is the overexpression of thioredoxin and/or glutaredoxin, and wherein this overexpression is associated with deleterious physiological effects in the patients.
摘要翻译：本发明公开并要求组合物，治疗方法和试剂盒，其导致癌症患者的存活时间增加，其中所述癌症或者：（i）过表达硫氧还蛋白或谷氧还蛋白和/或（ii）显示硫氧还蛋白或对一种或多种化学治疗干预的谷氧还蛋白介导的抗性。本发明还公开并要求用于施用所述组合物以适当治疗癌症患者的方法和试剂盒。此外，本发明公开并说明了用于定量测定癌症患者癌细胞中硫氧还蛋白或谷氧还蛋白表达水平的方法和试剂盒，在初始诊断和/或规划后续治疗方法中使用确定水平的方法所述癌症患者以及确定特定癌症的潜在增长“侵略性”和特定类型癌症的治疗反应性。此外，本发明公开并要求用于治疗患有硫氧还蛋白和/或谷氧还蛋白过表达的医学病症和疾病的患者的新型药物组合物，方法和试剂盒，并且其中所述过表达与有害的生理作用相关病人。

33. 发明授权

US07569606B2 Platinum complexes with mononitrile-containing ligands 失效
标题翻译：铂配合物与含有单腈的配体
公开(公告)号：US07569606B2
公开(公告)日：2009-08-04
申请号：US11405141
申请日：2006-04-17
申请人： Zejun Xiao , Frederick H. Hausheer , Pavankumar Petluru
发明人： Zejun Xiao , Frederick H. Hausheer , Pavankumar Petluru
IPC分类号： A61K31/28 , C07F15/00
CPC分类号： C07F15/0093
摘要： Disclosed herein are novel platinum-based complexes possessing one nitrile substituent group (mononitrile) covalently-bonded to the platinum, one or more nitrogen donor ligands capable of forming hydrogen bonds with the bases in DNA or RNA and leaving groups (i.e., L1 and L2 )which can be hydrolyzed iii vivo to active species, which can then form coordinate adducts with DNA or RNA at the Guanine or Adenine bases thereof. Also disclosed herein are the reaction schemes for the synthesis of said platinum complexes, as well as methods of treatment of various types of cancer by the administration of a pharmaceutically-effective dose of said novel platinum complexes.
摘要翻译：本文公开了具有与铂共价连接的一个腈取代基（单腈）的新型铂基络合物，能够与DNA或RNA中的碱形成氢键的离子基团（即L1和L2）的一个或多个氮供体配体），其可以体内水解成活性物质，其然后可以在鸟嘌呤或腺嘌呤碱基上与DNA或RNA形成配位加合物。本文还公开了用于合成所述铂络合物的反应方案，以及通过施用药学有效剂量的所述新型铂络合物治疗各种类型的癌症的方法。

34. 发明申请

US20090111735A1 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 审中-公开
标题翻译：用于减少化学治疗剂不期望的毒性的化合物和方法
公开(公告)号：US20090111735A1
公开(公告)日：2009-04-30
申请号：US12283995
申请日：2008-09-17
申请人： Frederick H. Hausheer , Hary Kochat , Qiuli Huang
发明人： Frederick H. Hausheer , Hary Kochat , Qiuli Huang
IPC分类号： A61K38/10 , A61K38/06 , A61K38/07 , A61P43/00 , A61K38/05 , A61K38/08
CPC分类号： A61K45/06 , A61K38/00
摘要： Novel compositions and formulations are disclosed that have use to mitigate or prevent physiologically deleterious side-effects and/or modulate the intracellular balance of oxidized and reduced thioredoxin (Trx) in patients with cancer who are receiving treatment with one or more chemotherapeutic agents. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium (mesna). In addition, methods of administration and kits comprising these novel mesna heteroconjugates are disclosed.
摘要翻译：已经公开了新的组合物和制剂，其用于减轻或预防生理上有害的副作用和/或调节正在接受用一种或多种化学治疗剂治疗的癌症患者中氧化和还原的硫氧还蛋白（Trx）的细胞内平衡。物质的组成是2-巯基乙磺酸钠（mesna）的氨基酸和肽杂合二硫化物。此外，公开了施用方法和包含这些新颖的mesna杂合物的试剂盒。

35. 发明申请

US20080193498A1 Chemoprotective methods and compositions 有权
标题翻译：化学保护方法和组合物
公开(公告)号：US20080193498A1
公开(公告)日：2008-08-14
申请号：US12075898
申请日：2008-03-14
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/105 , A61F2/00 , A61P39/00
CPC分类号： A61K31/105
摘要： Compositions and methods for reducing, preventing, mitigating, and/or delaying the onset of, attenuating the severity of, and/or hastening the resolution of, for example, one or more chemotherapy-associated toxicities in a subject receiving one or more chemotherapeutic agents. In addition compositions and methods for mitigating or preventing a novel form of chemotherapy-induced peripheral neuropathy are disclosed and claimed.
摘要翻译：用于减少，预防，减轻和/或延缓接受一种或多种化学治疗剂的受试者中例如一种或多种化疗相关毒性的分解的减轻，和/或加速其分解的组合物和方法。此外，公开并要求保护减轻或预防化疗诱发的周围神经病变的新形式的组合物和方法。

36. 发明申请

US20080161603A1 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
公开(公告)号：US20080161603A1
公开(公告)日：2008-07-03
申请号：US11985244
申请日：2007-11-14
申请人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
发明人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
IPC分类号： C07C205/02
CPC分类号： A61K45/06 , A61K38/00
摘要： Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.

37. 发明申请

US20080161525A1 Compounds and methods for reducing undesired toxicity of chemotherapeutic agents 有权
公开(公告)号：US20080161525A1
公开(公告)日：2008-07-03
申请号：US11985241
申请日：2007-11-14
申请人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
发明人： Frederick H. Hausheer , Harry Kochat , Qiuli Huang
IPC分类号： C08F112/08
CPC分类号： A61K45/06 , A61K38/00
摘要： Novel compositions and formulations are disclosed that have use as toxicity-reducing agents for various chemotherapeutic agents and as treatment for certain diseases and conditions. The compositions of matter are amino acid and peptide heteroconjugated disulfides of 2-mercaptoethane sulfonate sodium.

38. 发明授权

US06291441B1 Method of treating inflammatory bowel disorders 失效
标题翻译：炎症性肠病的治疗方法
公开(公告)号：US06291441B1
公开(公告)日：2001-09-18
申请号：US09671791
申请日：2000-09-27
申请人： Frederick H. Hausheer , Seetharamulu Peddaiahgari
发明人： Frederick H. Hausheer , Seetharamulu Peddaiahgari
IPC分类号： A61K3110
CPC分类号： A61K31/10 , A61K31/105 , Y10S514/925
摘要： This invention relates to a method of treating patients suffering from the inflammatory bowel disorders. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
摘要翻译：本发明涉及一种治疗患有炎症性肠病的患者的方法。该方法包括向需要治疗的患者施用有效量的根据说明书中阐述的式的硫醇或可还原的二硫化物化合物。

39. 发明授权

US06251881B1 Method of treating diabetic angiopathy 失效
标题翻译：治疗糖尿病性血管病的方法
公开(公告)号：US06251881B1
公开(公告)日：2001-06-26
申请号：US09422478
申请日：1999-10-21
申请人： Frederick H. Hausheer , Aulma Parker , Seetharamulu Peddaiaghari
发明人： Frederick H. Hausheer , Aulma Parker , Seetharamulu Peddaiaghari
IPC分类号： A61K3166
CPC分类号： A61K31/185 , A61K31/66
摘要： This invention relates to a method of treating patients afflicted with diabetic angiopathy. The method includes administering to a patient in need of treatment an effective amount of a thiol or reducible disulfide compound according to the formula set forth in the specification.
摘要翻译：本发明涉及治疗患有糖尿病血管病的患者的方法。该方法包括向需要治疗的患者施用有效量的根据说明书中阐述的式的硫醇或可还原的二硫化物化合物。

40. 发明授权

US6048849A Formulations and methods of reducing toxicity of antineoplastic agents 有权
公开(公告)号：US6048849A
公开(公告)日：2000-04-11
申请号：US225700
申请日：1999-01-06
申请人： Frederick H. Hausheer , Thomas J. Dodd
发明人： Frederick H. Hausheer , Thomas J. Dodd
IPC分类号： A61K31/02 , A61K31/131 , A61K31/136 , A61K31/166 , A61K31/175 , A61K31/185 , A61K31/196 , A61K31/198 , A61K31/255 , A61K31/28 , A61K31/282 , A61K31/337 , A61K31/36 , A61K31/40 , A61K31/407 , A61K31/4164 , A61K31/439 , A61K31/44 , A61K31/4745 , A61K31/495 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/662 , A61K31/675 , A61K31/7008 , A61K31/704 , A61K31/7048 , A61K31/7056 , A61K31/7068 , A61K31/7076 , A61K33/24 , A61K45/06 , A61P35/00 , A61P39/02 , A61P43/00 , A61K38/22
CPC分类号： A61K31/505 , A61K31/185 , A61K31/255 , A61K31/28 , A61K31/40 , A61K31/675 , A61K33/24 , A61K45/06 , Y10S514/946 , Y10S514/947
摘要： This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

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