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1. 发明授权

US5214134A Process of linking nucleosides with a siloxane bridge 失效
标题翻译：用硅氧烷桥连接核苷酸的方法
公开(公告)号：US5214134A
公开(公告)日：1993-05-25
申请号：US581502
申请日：1990-09-12
申请人： Alexander L. Weis , Ashis K. Saha , Frederick H. Hausheer
发明人： Alexander L. Weis , Ashis K. Saha , Frederick H. Hausheer
IPC分类号： C07H20060101 , C07H23/00
CPC分类号： C07H23/00
摘要： A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.
摘要翻译：公开了将核苷与硅氧烷桥连接的方法，包括使3'-甲硅烷基化-5'-保护的核苷与未保护的核苷反应。甲硅烷基化和未保护的核苷可以是单体核苷或寡核苷酸或寡核苷酸类似物的末端核苷。还公开了合成具有硅氧烷核苷间键的寡核苷酸类似物的方法。合成方法包括用双官能甲硅烷基化试剂甲硅烷基化5'-保护的核苷以形成3'-甲硅烷基化核苷，在碱催化剂存在下使甲硅烷基化的核苷与未保护的核苷反应，并重复这些步骤以形成寡核苷酸类似物。还公开了用于制备具有硅氧烷核苷间键的寡核苷酸类似物的改进的固相合成方法。

2. 发明授权

US5567810A Nuclease resistant compounds 失效
标题翻译：核酸酶抗性化合物
公开(公告)号：US5567810A
公开(公告)日：1996-10-22
申请号：US456017
申请日：1995-05-31
申请人： Alexander L. Weis , Fred T. Oakes , Frederick H. Hausheer , Paul F. Cavanaugh, Jr. , Patricia S. Moskwa
发明人： Alexander L. Weis , Fred T. Oakes , Frederick H. Hausheer , Paul F. Cavanaugh, Jr. , Patricia S. Moskwa
IPC分类号： C07H21/00 , A61K31/045 , A61K31/715 , C07C31/20
CPC分类号： C07H21/00
摘要： Compounds, compositions and methods for inhibiting gene expression are disclosed. The compounds comprise oligonucleotide sequences of from about 9 to about 200 bases having a diol at either or both termini. Preferred diols are polyalkyleneglycols, preferably polyethyleneglycols. Pharmaceutical compositions comprising the compounds and a physiologically acceptable carrier and methods of inhibiting gene expression in mammals comprising administering such compounds are also provided. Methods for inhibiting nuclease cleavage of compounds are also provided.
摘要翻译：公开了抑制基因表达的化合物，组合物和方法。所述化合物包含约9至约200个碱基的寡核苷酸序列，在任一端或两端具有二醇。优选的二醇是聚亚烷基二醇，优选聚乙二醇。还提供了包含化合物和生理上可接受的载体的药物组合物和抑制哺乳动物中基因表达的方法，包括给予这些化合物。还提供了抑制化合物核酸酶切割的方法。

3. 发明授权

US5245022A Exonuclease resistant terminally substituted oligonucleotides 失效
标题翻译：核酸外切酶末端取代的寡核苷酸
公开(公告)号：US5245022A
公开(公告)日：1993-09-14
申请号：US562180
申请日：1990-08-03
申请人： Alexander L. Weis , Fred T. Oakes , Frederick H. Hausheer , Paul F. Cavanaugh, Jr. , Patricia S. Moskwa
发明人： Alexander L. Weis , Fred T. Oakes , Frederick H. Hausheer , Paul F. Cavanaugh, Jr. , Patricia S. Moskwa
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： Compounds, compositions and methods for inhibiting gene expression are disclosed. The compounds comprise oligonucleotide sequences of from about 9 to about 200 bases having a diol at either or both termini. Preferred diols are polyalkyleneglycols, preferably polyethyleneglycols. Pharmaceutical compositions comprising the compounds and a physiologically acceptable carrier and methods of inhibiting gene expression in mammals comprising administering such compounds are also provided. Methods for inhibiting nuclease cleavage of compounds are also provided.
摘要翻译：公开了抑制基因表达的化合物，组合物和方法。所述化合物包含约9至约200个碱基的寡核苷酸序列，在任一端或两端具有二醇。优选的二醇是聚亚烷基二醇，优选聚乙二醇。还提供了包含化合物和生理上可接受的载体的药物组合物和抑制哺乳动物中基因表达的方法，包括给予这些化合物。还提供了抑制化合物核酸酶切割的方法。

4. 发明申请

US20120070404A1 Increasing cancer patient survival time by administration of dithio-containing compounds 有权
标题翻译：通过给予含二硫化合物增加癌症患者的存活时间
公开(公告)号：US20120070404A1
公开(公告)日：2012-03-22
申请号：US12807931
申请日：2010-09-16
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： C07C321/14 , A61K38/02 , A61K38/16 , A61K39/395 , A61K38/20 , A61K33/24 , A61K38/50 , A61K31/517 , A61K38/22 , A61K38/21 , A61K38/43 , A61P35/00
CPC分类号： A61K45/06 , A61K31/517 , A61K33/24 , A61K38/05 , A61K38/212 , A61K2300/00
摘要： The present invention discloses and claims compositions, methods of treatment, and kits which cause an increase in the time of survival in cancer patients, wherein the cancer: (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，其中癌症：（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。

5. 发明申请

US20070219268A1 Anti-cancer activity augmentation compounds and formulations and methods of use thereof 审中-公开
标题翻译：抗癌活性增加化合物及其制剂及其使用方法
公开(公告)号：US20070219268A1
公开(公告)日：2007-09-20
申请号：US11724933
申请日：2007-03-16
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/255 , A61K31/095
CPC分类号： A61K31/095 , A61K9/0019 , A61K31/255 , A61K31/555 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The field of the present invention comprises pharmaceuticals and pharmaceutical treatments, including, for example, (i) compounds and formulations which cause the augmentation of anti-cancer activity (i.e., by enhancement of the lethal cytotoxic action in stimulatory [inducing oxidative stress] and/or depletive [decreasing anti-oxidative capacity] manner) of chemotherapeutic agents, in a selective manner; (ii) methods of administering said anti-cancer augmentation compounds and formulations; (iii) delivery devices containing said anti-cancer augmentation compounds and formulations; and (iv) methods of using said anti-cancer augmentation compounds, formulations, and devices to treat subjects in need thereof.
摘要翻译：本发明的领域包括药物和药物治疗，包括例如（i）引起抗癌活性增加的化合物和制剂（即，通过增强刺激性[诱导氧化应激]中的致死细胞毒性作用和 /或以选择性方式递送化学治疗剂的[降低抗氧化能力]方式）（ii）施用所述抗癌增强化合物和制剂的方法; （iii）含有所述抗癌增强化合物和制剂的递送装置; 和（iv）使用所述抗癌增强化合物，制剂和装置来治疗有需要的受试者的方法。

6. 发明授权

US07176192B2 Method for treating patients for radiation exposure 有权
标题翻译：治疗患者放射线暴露的方法
公开(公告)号：US07176192B2
公开(公告)日：2007-02-13
申请号：US10002526
申请日：2001-10-26
申请人： Frederick H. Hausheer
发明人： Frederick H. Hausheer
IPC分类号： A61K31/095 , A61K31/105 , A61K31/185 , A61K31/255 , A61K31/662
CPC分类号： A61K31/095 , A61K31/185 , A61K31/66
摘要： This invention relates to a method of treating a patient suffering from ionizing radiation exposure, or of treating a patient about to undergo ionizing radiation therapy. 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电离辐射暴露的患者或治疗接受电离辐射治疗的患者的方法。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。

7. 发明授权

US06525037B1 Method of treating atherosclerosis and complications resulting therefrom 有权
标题翻译：治疗动脉粥样硬化的方法及其引起的并发症
公开(公告)号：US06525037B1
公开(公告)日：2003-02-25
申请号：US09513540
申请日：2000-02-25
申请人： Frederick H. Hausheer , Seetharamulu Peddaiahgari
发明人： Frederick H. Hausheer , Seetharamulu Peddaiahgari
IPC分类号： A61K3166
CPC分类号： A61K31/255 , A61K31/66
摘要： This invention relates to a method of treating patients afflicted with atherosclerosis or to prevent the development of atherosclerosis in patients assessed to be high risk of developing the disease. 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动脉粥样硬化的患者或预防发展为高发病风险的患者动脉粥样硬化发展的方法。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。

8. 发明授权

US6040304A Formulations and methods of reducing toxicity of antineoplastic agents 有权
公开(公告)号：US6040304A
公开(公告)日：2000-03-21
申请号：US225695
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 , A61K31/35 , A61K31/55
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.

9. 发明授权

US6031006A Method of treating diabetic nephropathy 有权
标题翻译：治疗糖尿病肾病的方法
公开(公告)号：US6031006A
公开(公告)日：2000-02-29
申请号：US422486
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： A61K31/00 , A61K31/10
CPC分类号： A61K31/00
摘要： This invention relates to a method of treating patients afflicted with diabetic nephropathy. 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肾病的患者的方法。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。

10. 发明授权

US5880133A Pharmaceutical formulations of highly lipophilic camptothecin derivatives 失效
标题翻译：高亲脂性喜树碱衍生物的药物制剂
公开(公告)号：US5880133A
公开(公告)日：1999-03-09
申请号：US667424
申请日：1996-06-21
申请人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
发明人： Frederick H. Hausheer , Kochat Haridas , Dhanabalan Murali , Dasharatha Gauravaram Reddy
IPC分类号： A61K9/08 , A61K9/00 , A61K9/107 , A61K9/48 , A61K31/4745 , A61K31/475 , A61K47/00 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/22 , A61K47/26 , A61K47/28
CPC分类号： A61K9/0019 , A61K31/4745 , A61K47/18 , A61K47/22 , A61K9/1075 , A61K9/4858 , A61K47/10 , A61K47/12 , A61K47/26 , A61K47/28
摘要： Pharmaceutical formulations of Highly Lipophilic Camptothecin Derivatives (HLCD) include HLCD dissolved in N-methyl Pyrrolidinene (NMP). The formulations also include quantities of pharmaceutically acceptable excipients and diluents incorporated thereinto.
摘要翻译：高亲脂性喜树碱衍生物（HLCD）的药物制剂包括溶解在N-甲基吡咯烷（NMP）中的HLCD。制剂还包括并入其中的药学上可接受的赋形剂和稀释剂的量。

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