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11. 发明申请

US20020136740A1 Vaccines containing ribavirin and methods of use thereof 失效
标题翻译：含有利巴韦林的疫苗及其使用方法
公开(公告)号：US20020136740A1
公开(公告)日：2002-09-26
申请号：US09929955
申请日：2001-08-15
发明人： Matti Sallberg , Catharina Hultgren
IPC分类号： A61K048/00 , A61K039/12 , A61K031/7056 , C12Q001/70 , A61K031/70 , A01N043/04 , C12P019/34 , A01N063/00 , A61K039/29
CPC分类号： A61K39/29 , A01K67/0271 , A61K31/7056 , A61K38/00 , A61K39/00 , A61K39/12 , A61K39/39 , A61K2039/53 , A61K2039/545 , A61K2039/55505 , A61K2039/55511 , A61K2039/57 , A61K2121/00 , A61K2123/00 , C07K14/005 , C07K16/109 , C12N7/00 , C12N2740/16134 , C12N2770/24022 , C12N2770/24221 , C12N2770/24222 , C12N2770/24234 , G06F19/00 , G06Q50/22 , Y02A50/464 , Y02A90/22 , Y02A90/26
摘要： Compositions and methods for enhancing the effect of vaccines in animals, such as domestic, sport, or pet species, and humans are disclosed. More particularly, vaccine compositions comprising ribavirin and an antigen, preferably an antigen that has an epitope present in Hepatitis C virus (HCV), are disclosed for use in treating and preventing disease, preferably HCV infection.
摘要翻译：公开了用于增强疫苗在家畜，运动或宠物物种和人类中的作用的组合物和方法。更具体地，公开了包含利巴韦林和抗原，优选具有存在于丙型肝炎病毒（HCV）中的表位的抗原的疫苗组合物用于治疗和预防疾病，优选HCV感染。

12. 发明申请

US20020068705A1 Tumor proliferation inhibitors 失效
标题翻译：肿瘤增殖抑制剂
公开(公告)号：US20020068705A1
公开(公告)日：2002-06-06
申请号：US09962181
申请日：2001-09-25
发明人： Edward H. Ruediger , Neelakantan Balasubramanian , Mikael Mahler , Carol Bachand , Francis Beaulieu
IPC分类号： A61K031/7056 , C07H019/044 , C07H019/056
CPC分类号： C07H19/23 , A61K31/7056
摘要： The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.
摘要翻译：本发明涉及吲哚并唑的新型糖衍生物及其药物组合物，其具有拓扑异构酶-1活性并且可用于抑制肿瘤细胞的增殖。

13. 发明申请

US20040259819A1 Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof 审中-公开
标题翻译：新型杂环核苷酸衍生物，含有这些化合物的药物及其用途
公开(公告)号：US20040259819A1
公开(公告)日：2004-12-23
申请号：US10734573
申请日：2003-12-12
申请人： Aventis Pharma Deutschland GmbH
发明人： Wendelin Frick , Heiner Glombik , Werner Kramer , Hubert Heuer , Harm Brummerhop , Oliver Plettenburg
IPC分类号： A61K031/7056 , C07H019/056
CPC分类号： C07H17/02 , C07H17/00
摘要： Novel heterocyclic fluoroglycoside derivatives, medicaments containing these compounds, and the use thereof. The invention relates to substituted heterocyclic fluoroglycoside derivatives of the formula I 1 in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation. The compounds are suitable for example as antidiabetics.
摘要翻译：新型杂环核苷酸衍生物，含有这些化合物的药物及其用途。本发明涉及其中基团具有所述含义的式I的取代的杂环氟代果糖衍生物及其生理上耐受的盐及其制备方法。该化合物适合于例如抗糖尿病药。

14. 发明申请

US20040242509A1 Method for treating a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate 有权
公开(公告)号：US20040242509A1
公开(公告)日：2004-12-02
申请号：US10802829
申请日：2004-08-03
发明人： Dale J. Kempf , Richard J. Bertz , Jeffrey F. Waring
IPC分类号： A61K031/7056 , A61K031/551
CPC分类号： A61K31/436 , A61K31/167 , A61K31/282 , A61K31/427 , A61K31/4418 , A61K31/496 , A61K31/506 , A61K31/565 , A61K31/7048 , A61K31/7068 , A61K31/708
摘要： The present invention is directed to a method for inducing UGT1A1 isoform expression for treatment of a disease, disorder or adverse effect caused by an elevated serum concentration of an UGT1A1 substrate comprising the step of administering to a subject an effective amount of ritonavir. In particular, the present invention is directed to a method of treating unconjugated hyperbilirubinemia by UGT1A1 induction comprising the step of administering to a subject an effective amount of ritonavir.

15. 发明申请

US20040213740A1 Light sensitive compounds for instant determination of organ function 失效
标题翻译：光敏化合物，用于即时测定器官功能
公开(公告)号：US20040213740A1
公开(公告)日：2004-10-28
申请号：US10751232
申请日：2004-01-02
申请人： Mallinckrodt Inc.
发明人： Samuel Achilefu , Raghavan Rajagopalan , Richard B. Dorshow , Joseph E. Bugaj , Hermo N. Jimenez , Muthunadar P. Periasamy
IPC分类号： A61K049/00 , A61K031/7056 , A61K031/428 , A61K031/423
CPC分类号： A61K49/0032 , C09B23/02
摘要： Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
摘要翻译：公开了在可见光区域吸收和发出荧光的高度亲水的吲哚和苯并吲哚衍生物。这些化合物可用于生理和器官功能监测。特别地，本发明的分子可用于肾脏和心脏疾病的光学诊断以及体内血液体积估计。

16. 发明申请

US20040152646A1 Carbohydrate prodrugs of fluorooxindoles 有权
标题翻译：氟氧吲哚的碳水化合物前药
公开(公告)号：US20040152646A1
公开(公告)日：2004-08-05
申请号：US10762907
申请日：2004-01-22
发明人： Kevin Gillman , Danielle M. Bocchino
IPC分类号： A61K031/7056 , C07H019/044
CPC分类号： C07H19/044
摘要： The present invention provides novel prodrug derivatives of fluorooxindoles having the general Formula I 1 wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer, and R1, R2, R3, R4 and X are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.
摘要翻译：本发明提供具有通式I的氟氧吲哚的新型前药衍生物，其中波浪键（）表示外消旋物，（R） - 对映体或（S） - 对映异构体，R 1，R 2，R 3，R 4和X如本文所定义，或其无毒的药学上可接受的盐或其溶剂化物，并且可用于治疗对钾通道开放有反应的病症。

17. 发明申请

US20040096436A1 Methods for inhibiting protein kinases in cancer cells 审中-公开
标题翻译：抑制癌细胞中蛋白激酶的方法
公开(公告)号：US20040096436A1
公开(公告)日：2004-05-20
申请号：US10632592
申请日：2003-08-01
申请人： REGENTS OF THE UNIVERSITY OF CALIFORNIA , SALMEDIX, INC.
发明人： Dennis A. Carson , Michael D. Rosenbach , Carlos J. Carrera , Lorenzo M. Leoni
IPC分类号： A61K031/7056 , A61K031/365 , A61K031/353 , A61K038/44 , A61K039/395
CPC分类号： A61K45/06 , A61K31/353 , A61K31/365 , A61K31/7056 , A61K39/395 , A61K2300/00
摘要： The present invention provides methods of treating cancer using inhibitors of protein kinases. The inhibitors of protein kinases are combined with agents that inhibit a cellular ATP synthetic pathway. Inhibitors of ATP synthesis include inhibitors of de novo purine biosynthesis, inhibitors of the salvage pathway of ATP biosynthesis, and inhibitors of the enzyme inosine monophosphate dehydrogenase.
摘要翻译：本发明提供使用蛋白激酶抑制剂治疗癌症的方法。蛋白激酶的抑制剂与抑制细胞ATP合成途径的试剂组合。 ATP合成的抑制剂包括从头嘌呤生物合成的抑制剂，ATP生物合成的补救途径的抑制剂和肌苷一磷酸脱氢酶的抑制剂。

18. 发明申请

US20040063646A1 Glucopyranosyloxypyrazole derivatives and use thereof in medicines 有权
标题翻译：吡喃葡萄糖氧吡唑衍生物及其在药物中的应用
公开(公告)号：US20040063646A1
公开(公告)日：2004-04-01
申请号：US10451926
申请日：2003-11-06
发明人： Hideki Fujikura , Nobuhiko Fushimi , Toshihiro Nishimura , Takeshi Nakabayashi , Masayuki Isaji
IPC分类号： A61K031/7056 , C07H017/02
CPC分类号： A61K45/06 , A61K31/7056 , C07H17/02 , A61K2300/00
摘要： The present invention provides glucopyranosyloxypyrazole derivatives represented by the general formula: 1 wherein R represents a hydrogen atom, a lower alkyl group or a group forming a prodrug: one of Q and T represents a group represented by the general formula: 2 (wherein P represents a hydrogen atom or a group forming a prodrug), while the other represents a lower alkyl group or a halo(lower alkyl) group; R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom; and with the proviso that P does not represent a hydrogen atom when R represents a hydrogen atom or a lower alkyl group, or pharmaceutically acceptable salts thereof, which exert an inhibitory activity in human SGLT2 and have an improved oral absorption, and therefore are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, and pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.
摘要翻译：本发明提供由以下通式表示的吡喃葡萄糖氧吡唑衍生物：其中R表示氢原子，低级烷基或形成前药的基团：Q和T之一表示由通式表示的基团：（其中P表示氢原子或形成前药的基团），而另一个表示低级烷基或卤代（低级烷基）基团; R 2表示氢原子，低级烷基，低级烷氧基，低级烷硫基，卤代（低级烷基）或卤素原子; 并且条件是当R表示氢原子或低级烷基时，P不表示氢原子，或其药学上可接受的盐，其在人SGLT2中具有抑制活性并具有改善的口服吸收，因此可用作用于预防或治疗与高血糖相关的疾病如糖尿病，糖尿病并发症或肥胖症的药剂及其药学上可接受的盐及其药学用途。

19. 发明申请

US20030212013A1 Use of amp kinase activators for treatment type 2 diabetes and insulin resistance 审中-公开
标题翻译：使用AMP激酶治疗2型糖尿病和胰岛素抵抗
公开(公告)号：US20030212013A1
公开(公告)日：2003-11-13
申请号：US10297114
申请日：2002-12-03
发明人： William W Winder
IPC分类号： A61K031/7056 , A61K031/7076
CPC分类号： A61K31/00 , A61K31/70
摘要： A method of treating type 2 diabetes in a mammal is provided. The method includes the step of administering a therapeutically effective amount of an AMP-activated protein kinase activator to the mammal. The mammal may be for example, a human, a rat, a mouse, and the like. The AMP-activated protein kinase activator can be subcutaneously injected into the mammal or administered in any other manner that provides for uptake of the AMP-activated protein kinase activator into the cells of the mammal. The activation of the AMP-activated protein kinase activator can produce the benefits of exercise training including the translocation of GLUT4 in the muscle cells of the mammal. A method of treating insulin resistance in a mammal is also provided. To treat the insulin resistance a therapeutically effective amount of an AMP-activated protein kinase activator is given to the mammal.
摘要翻译：提供了一种哺乳动物治疗2型糖尿病的方法。该方法包括向哺乳动物施用治疗有效量的AMP活化的蛋白激酶激活剂的步骤。哺乳动物可以是例如人，大鼠，小鼠等。可以将AMP-活化的蛋白激酶激活物皮下注射到哺乳动物中或以提供AMP-活化的蛋白激酶激活剂摄入哺乳动物细胞的任何其它方式施用。 AMP激活的蛋白激酶激活剂的活化可以产生运动训练的益处，包括在哺乳动物肌肉细胞中转运GLUT4。还提供了治疗哺乳动物胰岛素抵抗的方法。为了治疗胰岛素抵抗，向哺乳动物施用治疗有效量的AMP-活化的蛋白激酶激活剂。

20. 发明申请

US20030180819A1 Assays for cancer patient monitoring based on levels of analyte components of the plasminogen activator system in body fluid samples 审中-公开
标题翻译：基于体液样品中纤溶酶原激活物系统的分析物成分水平进行癌症患者监测的测定
公开(公告)号：US20030180819A1
公开(公告)日：2003-09-25
申请号：US10375646
申请日：2003-02-27
发明人： Walter P. Carney , Peter J. Hamer
IPC分类号： G01N033/574 , G01N033/53 , G01N033/537 , G01N033/543 , A61K031/7056
CPC分类号： G01N33/57484 , G01N33/86 , G01N2333/8132 , G01N2333/9723 , G01N2800/52 , Y10T436/25
摘要： The present invention describes clinically and medically important methods of examining, screening over time, and monitoring the outcome of a cancer patient who is undergoing treatment or therapy for his or her disease. More specifically, the invention provides a method of monitoring the progression of disease, or the effectiveness of cancer treatment, in a cancer patient by measuring the levels of one or more analytes of the plasminogen activator (uPA) system, namely, uPA, PAI-1 and the complex of uPA:PAI-1, in a sample taken from the cancer patient, preferably, before treatment, at the start of treatment, and at various time intervals during treatment. As a result of performing the method, an increase or elevation in the levels of one or more of the PA system analytes in the cancer patient compared with the levels one or more of the respective PA system analytes in normal control individuals serves as an indicator of cancer advancement or progression and/or a lack of treatment effectiveness for the patient.
摘要翻译：本发明描述临床和医学上重要的随时间的检查，筛选和监测正在接受治疗或治疗他或她的疾病的癌症患者的结果的重要方法。更具体地，本发明提供了通过测量纤溶酶原激活物（uPA）系统的一种或多种分析物的水平，即uPA，PAI-1，在癌症患者中监测疾病进展或癌症治疗的有效性的方法， 1和来自癌症患者的样品中的uPA：PAI-1的复合物，优选在治疗前，治疗开始时和治疗期间的各个时间间隔。作为执行该方法的结果，癌症患者中的一种或多种PA系统分析物的水平的增加或升高与正常对照个体中相应的PA系统分析物中的一个或多个水平相比作为癌症进展或进展和/或患者缺乏治疗有效性。

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