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21. 发明申请

US20120226031A1 PALMARUMYCIN BASED INHIBITORS OF THIOREDOXIN AND METHODS OF USING SAME 审中-公开
标题翻译：基于PALMARUMYCIN的三羟甲基纤维素抑制剂及其使用方法
公开(公告)号：US20120226031A1
公开(公告)日：2012-09-06
申请号：US13364499
申请日：2012-02-02
申请人： GARTH POWIS , PETER WIPF
发明人： GARTH POWIS , PETER WIPF
IPC分类号： C07D323/04 , C07D413/10 , C07H15/24 , C07D405/10
CPC分类号： C07D319/08 , A61K31/357 , A61K31/7048
摘要： Embodiments of the present invention relate to inhibitors of thioredoxin. Certain embodiments relate to palmarumycin based compounds and methods of using the same. Such compounds may be useful in inhibiting the overexpression of thioredoxin, inhibiting tumor growth and treating cancer.
摘要翻译：本发明的实施方案涉及硫氧还蛋白的抑制剂。某些实施方案涉及基于棕榈霉素的化合物及其使用方法。这些化合物可用于抑制硫氧还蛋白的过量表达，抑制肿瘤生长和治疗癌症。

22. 发明授权

US08124651B2 Palmarumycin based inhibitors of thioredoxin and methods of using same 有权
标题翻译：硫氧还蛋白的基于棕榈霉素的抑制剂及其使用方法
公开(公告)号：US08124651B2
公开(公告)日：2012-02-28
申请号：US12066426
申请日：2006-09-15
申请人： Garth Powis , Peter Wipf
发明人： Garth Powis , Peter Wipf
IPC分类号： A61K31/357 , C07D319/08
CPC分类号： C07D319/08 , A61K31/357 , A61K31/7048
摘要： Embodiments of the present invention relate to inhibitors of thioredoxin. Certain embodiments relate to palmarumycin based compounds and methods of using the same. Such compounds may be useful in inhibiting the overexpression of thioredoxin, inhibiting tumor growth and treating cancer.
摘要翻译：本发明的实施方案涉及硫氧还蛋白抑制剂。某些实施方案涉及基于棕榈霉素的化合物及其使用方法。这些化合物可用于抑制硫氧还蛋白的过量表达，抑制肿瘤生长和治疗癌症。

23. 发明申请

US20110092595A1 Compositions and Methods for Treating Lung Cancer 审中-公开
标题翻译：治疗肺癌的组合物和方法
公开(公告)号：US20110092595A1
公开(公告)日：2011-04-21
申请号：US12866877
申请日：2009-02-13
申请人： Garth Powis , Roy Herbst , Jörg Jacoby
发明人： Garth Powis , Roy Herbst , Jörg Jacoby
IPC分类号： A61K31/195 , A61P35/00
CPC分类号： A61K31/535
摘要： Embodiments of the present invention provide compositions and methods for treating lung cancer, including small cell and non-small cell lung cancer that may express HIF-1a by administering a therapeutically effective amount of PX-478.
摘要翻译：本发明的实施方案提供了通过施用治疗有效量的PX-478来治疗肺癌的组合物和方法，包括可表达HIF-1a的小细胞和非小细胞肺癌。

24. 发明授权

US07399785B2 N-oxides and derivatives of melphalan for treating diseased states associated with hypoxia inducible factor 失效
标题翻译：美法仑的N-氧化物和衍生物用于治疗与缺氧诱导因子相关的疾病状态
公开(公告)号：US07399785B2
公开(公告)日：2008-07-15
申请号：US10929156
申请日：2004-08-30
申请人： Lynn Kirkpatrick , Garth Powis , Sarah J. Welsh
发明人： Lynn Kirkpatrick , Garth Powis , Sarah J. Welsh
IPC分类号： A61K31/19
CPC分类号： A61K31/66 , A61K31/195 , C07F9/65846
摘要： This invention relates to compounds which are N-oxides and derivatives thereof, as well as their use to treat HIF related diseases. These compounds have the general formula set out below and are used to treat a variety of diseases associated with HIF: wherein R is an alkyl, aryl, arakyl or derivatives thereof such as CH3OCH2CH2—, CH3CH2OCH2CH2—, C6H5OCH2CH2—, C6H5CH2—, CH3(CH2)3OCH2CH2Cl; or any one of the following:
摘要翻译：本发明涉及作为N-氧化物及其衍生物的化合物及其用于治疗HIF相关疾病的用途。这些化合物具有下列通式，用于治疗与HIF相关的各种疾病：其中R是烷基，芳基，芳基或其衍生物，例如CH 3 OCH 2 CH 2 CH 2，CH 3 CH 2 CH 2 CH 2，CH 2，CH 2，CH 2， > - ，C 6 H 5，OCH 2 CH 2 - ， - C 6 - H 2 CH 2 - ，CH 3（CH 2）3 OCH 3 CH 2 - 2> 2 Cl 2; 或以下任何一种：

25. 发明授权

US07081475B2 Wortmannin analogs and methods of using same 失效
公开(公告)号：US07081475B2
公开(公告)日：2006-07-25
申请号：US10245779
申请日：2002-09-16
申请人： Garth Powis , Wipf Peter
发明人： Garth Powis , Wipf Peter
IPC分类号： A61K31/352 , C07D311/94
CPC分类号： A61K31/352 , A61K31/4025 , C07D311/94
摘要： Novel Wortmannin analogs and their use in inhibiting inhibiting PI-3-kinase activity in mammals as well as tumor formation in a subject are described herein.

26. 发明申请

US20050049309A1 Regulation of HIF protein levels via deubiquitination pathway 审中-公开
标题翻译：通过去泛素化途径调节HIF蛋白水平
公开(公告)号：US20050049309A1
公开(公告)日：2005-03-03
申请号：US10890756
申请日：2004-07-14
申请人： Lynn Kirkpatrick , Garth Powis , Sarah Welsh
发明人： Lynn Kirkpatrick , Garth Powis , Sarah Welsh
IPC分类号： A61K31/195 , A61K31/66 , C12N20060101
CPC分类号： A61K31/66
摘要： The hypoxia inducible factor-1 (HIF-1) transcription factor is an important regulator of the cellular response to hypoxia. The activity of HIF-1 is regulated by the level of the HIF-1α subunit, HIF-1α, which is rapidly degraded under normoxic conditions by the ubiquitin-proteasome pathway. HIF-1α levels increase under hypoxic conditions. Many human cancers also show constitutively increased HIF-1α levels. PX-478 or S-2-amino-3-[4′-N,N,-bis(2-chloroethyl)amino]phenyl propionic acid N-oxide dihydrochloride, is a novel anticancer agent, and is capably of decreasing both constitutive and hypoxia induced HIF-1α protein levels and HIF-1 transactivation in vitro and in vivo. In method embodiments, the administration of PX-478 is independent of the pathways of HIF-1α regulation involving the von Hippel-Lindau protein and p53. PX-478 causes an increase in polyubiquitinated HIF-1α levels due to inhibition of HIF-1α deubiquitination. The levels of other proteins whose proteasomal breakdown is mediated by ubiquitination are not affected by PX-478. Deubiquitination is a novel pathway for the regulation of cellular HIF-1α levels and PX-478 is a specific inhibitor of the pathway. Therapeutic compounds for regulating cellular HIF-1α levels and methods of regulating cellular HIF-1α levels are herein provided.
摘要翻译：缺氧诱导因子-1（HIF-1）转录因子是细胞对缺氧反应的重要调控因子。 HIF-1的活性受HIF-1α亚基HIF-1α的水平调节，HIF-1α在泛素 - 蛋白酶体途径的正常氧条件下迅速降解。低氧条件下HIF-1α水平升高。许多人类癌症也显示出组成型增加的HIF-1α水平。 PX-478或S-2-氨基-3- [4'-N，N，双（2-氯乙基）氨基]苯基丙酸N-氧化物二盐酸盐是一种新型抗癌剂，缺氧诱导HIF-1α蛋白水平和体外和体内HIF-1反式激活。在方法实施方案中，PX-478的施用与涉及von Hippel-Lindau蛋白和p53的HIF-1α调节途径无关。 PX-478由于抑制HIF-1α去泛素化而导致多泛素化的HIF-1α水平升高。蛋白酶体破坏由泛素介导的其他蛋白质的水平不受PX-478的影响。去泛素化是调节细胞HIF-1α水平的新途径，PX-478是该途径的特异性抑制剂。本文提供了用于调节细胞HIF-1α水平的治疗化合物和调节细胞HIF-1α水平的方法。

27. 发明授权

US06703414B2 Device and method for treating restenosis 有权
标题翻译：治疗再狭窄的装置及方法
公开(公告)号：US06703414B2
公开(公告)日：2004-03-09
申请号：US10245780
申请日：2002-09-16
申请人： Garth Powis , Robert Abraham
发明人： Garth Powis , Robert Abraham
IPC分类号： A61K3140
CPC分类号： C07D311/94 , A61K31/35 , A61K31/40
摘要： A method of inhibiting restenosis in a subject following coronary angioplasty, atherectomy, or arterial bypass graft surgery comprised of administering wortmannin analogs of the present invention is described herein.
摘要翻译：冠状动脉血管成形术，粥样斑块切除术或包括施用本发明的渥曼青霉素类似物的动脉旁路移植手术后抑制受试者的再狭窄的方法在本文中描述。

28. 发明授权

US06379970B1 Analysis of differential protein expression 失效
标题翻译：差异蛋白表达分析
公开(公告)号：US06379970B1
公开(公告)日：2002-04-30
申请号：US09302475
申请日：1999-04-30
申请人： Daniel C. Liebler , Thomas D. McClure , Garth Powis
发明人： Daniel C. Liebler , Thomas D. McClure , Garth Powis
IPC分类号： G01N3300
CPC分类号： G01N27/44726 , C12Q1/6869 , Y10S435/804 , Y10T436/106664
摘要： A method of detecting peptide fragments of protein(s) that are differentially present in biological samples. The identity of the peptides may be determined and correlated with the protein(s) that are differentially present in the samples.
摘要翻译：检测差异地存在于生物样品中的蛋白质的肽片段的方法。可以确定肽的身份并与样品中差异存在的蛋白质相关。

29. 发明授权

US06372772B1 Inhibitors of redox signaling and methods of using same 失效
标题翻译：氧化还原信号的抑制剂及其使用方法
公开(公告)号：US06372772B1
公开(公告)日：2002-04-16
申请号：US09127219
申请日：1998-07-31
申请人： D. Lynn Kirkpatrick , Garth Powis
发明人： D. Lynn Kirkpatrick , Garth Powis
IPC分类号： A61K31415
CPC分类号： A61K31/423 , A61K31/00
摘要： The present invention is directed to a composition or formulation which inhibits or interferes with cellular redox function, and method of using same to restore normal cellular function. More specifically, the composition of the present invention interferes with or inhibits abnormal cellular proliferation and//restores or cellular apoptosis.
摘要翻译：本发明涉及抑制或干扰细胞氧化还原功能的组合物或制剂，以及使用其来恢复正常细胞功能的方法。更具体地，本发明的组合物干扰或抑制异常的细胞增殖和/或恢复或细胞凋亡。

30. 发明授权

US5227508A 3-deoxy-3-substituted analogs of phosphatidylinositol 失效
标题翻译：磷脂酰肌醇的3-脱氧-3-取代的类似物
公开(公告)号：US5227508A
公开(公告)日：1993-07-13
申请号：US825523
申请日：1992-01-24
申请人： Alan P. Kozikowski , Werner Tuckmantel , Abdul H. Faug , Garth Powis
发明人： Alan P. Kozikowski , Werner Tuckmantel , Abdul H. Faug , Garth Powis
IPC分类号： C07F9/117 , C07F9/24 , C07F9/40
CPC分类号： C07F9/2416 , C07F9/117 , C07F9/4018
摘要： The invention provides 3-deoxy-3-substituted analogs of phosphatidylinositol which are useful to inhibit the growth of mammalian cells, i.e., to treat neoplastic conditions and other proliferative disorders of mammalian cells.
摘要翻译：本发明提供磷脂酰肌醇的3-脱氧-3-取代的类似物，其可用于抑制哺乳动物细胞的生长，即治疗哺乳动物细胞的肿瘤病症和其它增殖性疾病。

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