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1. 发明申请

WO2008124150A1 METHOD OF TREATING ENTERITIS, INTESTINAL DAMAGE, AND DIARRHEA FROM C. DIFFICILE WITH AN A2A ADENOSINE RECEPTOR AGONIST 审中-公开
标题翻译：使用A2A腺苷受体激动剂治疗胆汁酸，肠内营养不良和脱水的方法
公开(公告)号：WO2008124150A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/004553
申请日：2008-04-09
申请人： GUERRANT, Richard L. , LINDEN, Joel M. , WARREN, Cirle A. , SULLIVAN, Gail W. , MACDONALD, Timothy L.
发明人： GUERRANT, Richard L. , LINDEN, Joel M. , WARREN, Cirle A. , SULLIVAN, Gail W. , MACDONALD, Timothy L.
IPC分类号： A61K31/70
CPC分类号： A61K31/70
摘要： A therapeutic method for treating intestinal damage, enteritis, diarrhea, or a combination thereof caused by a C. difficile is provided. The method includes administration to a patient in need thereof an effective amount of an A2A adenosine receptor agonist, optionally in combination with an effective amount of a stable glutamine derivative, e.g., alanyl-glutamine.
摘要翻译：提供了一种用于治疗由艰难梭菌引起的肠损伤，肠炎，腹泻或其组合的治疗方法。该方法包括向有需要的患者施用有效量的A2A腺苷受体激动剂，任选地与有效量的稳定的谷氨酰胺衍生物，例如丙氨酰 - 谷氨酰胺组合。

2. 发明申请

WO2006023272A1 2-POLYCYCLIC PROPYNYL ADENOSINE ANALOGS HAVING A2A AGONIST ACTIVITY 审中-公开
标题翻译：具有A2A激动剂活性的2-多环丙基腺苷类似物
公开(公告)号：WO2006023272A1
公开(公告)日：2006-03-02
申请号：PCT/US2005/027475
申请日：2005-08-02
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , RIEGER, Jayson M. , LINDEN, Joel M. , MACDONALD, Timothy L. , SULLIVAN, Gail W. , MURPHREE, Lauren J. , FIGLER, Robert Alan , THOMPSON, Robert Douglas
发明人： RIEGER, Jayson M. , LINDEN, Joel M. , MACDONALD, Timothy L. , SULLIVAN, Gail W. , MURPHREE, Lauren J. , FIGLER, Robert Alan , THOMPSON, Robert Douglas
IPC分类号： C07H19/16 , G01N33/50 , A61K31/7052
CPC分类号： C07H19/16
摘要： The invention provides compounds having the following general formula (I) wherein X, R 1 , R 2 , R 7 and Z are as described herein.
摘要翻译：本发明提供具有以下通式（I）的化合物，其中X，R

3. 发明申请

WO2010107736A2 BROAD SPECTRUM BENZOTHIOPHENE-NITROTHIAZOLIDE AND OTHER ANTIMICROBIALS 审中-公开
标题翻译：广泛光谱苯并噻唑和其他抗生素
公开(公告)号：WO2010107736A2
公开(公告)日：2010-09-23
申请号：PCT/US2010/027397
申请日：2010-03-16
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , HOFFMAN, Paul S. , GUERRANT, Richard L. , MACDONALD, Timothy L. , BALLARD, JR., Thomas Eric
发明人： HOFFMAN, Paul S. , GUERRANT, Richard L. , MACDONALD, Timothy L. , BALLARD, JR., Thomas Eric
IPC分类号： C07D417/12 , C07D417/10 , C07D417/14
CPC分类号： C07D417/14 , A61K31/381 , A61K31/426 , A61K31/427 , A61K31/4439 , C07D277/54 , C07D277/58 , C07D333/42 , C07D333/44 , C07D409/12 , C07D417/12 , Y02A50/47 , Y02A50/473 , Y02A50/491
摘要： The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
摘要翻译：本发明提供了基于硝基噻唑烷骨架的新型抗微生物化学物质，其对广泛的人类病原体表现出抗菌和抗寄生虫作用。新类化合物对革兰氏阳性细菌（包括MRSA耐药病原体）具有延长的作用。在革兰氏阳性生物中，它们特异性靶向和功能性地抑制微生物附着于表面和生物膜形成。在包括肠聚集大肠杆菌菌株的革兰氏阴性细菌中，这些化合物通过抑制丝氨酸亚基组装成粘合剂长丝而起二硅化物的作用。这些化合物中的几种显示出对革兰氏阳性细菌的强力抗微生物作用，可能涉及新的靶标。许多苯并噻吩衍生物以低微克每毫升范围表现出抗微生物活性，并阻止纳摩尔范围内的生物膜形成; 所考虑的范围完全在作为治疗剂的效用范围内。

4. 发明申请

WO2012040170A2 COMPOSITIONS AND METHODS FOR TREATING TUBERCULOSIS 审中-公开
标题翻译：治疗结核病的组合物和方法
公开(公告)号：WO2012040170A2
公开(公告)日：2012-03-29
申请号：PCT/US2011/052308
申请日：2011-09-20
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , HOFFMAN, Paul S. , MACDONALD, Timothy L. , HOUPT, Eric R. , BALLARD, JR., Thomas Eric
发明人： HOFFMAN, Paul S. , MACDONALD, Timothy L. , HOUPT, Eric R. , BALLARD, JR., Thomas Eric
IPC分类号： A61K31/426 , A61K31/381 , A61P31/06 , A61P31/00
CPC分类号： A61K31/381 , A61K31/426 , A61K31/427 , A61K2300/00
摘要： The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein. The derivatives were synthesized using a di-nitro-thiophene or 4-Chloro-5-Nitro-thiazole scaffold and R groups connected via a peptide bond (NHCO) to cyclic compounds such as benzene, thiophene or furans. Many of these compounds have broad spectrum activity against Gram positive bacteria including Staphylococcus aureus (MRSA) and Staphylococcus epidermidis. Several of these lead compounds were not toxic for mice at 200 mg/Kg doses administered over a period of three days.
摘要翻译：本发明提供了基于显示抗分枝杆菌活性的硝基噻唑内酯骨架的抗微生物化学实体的用途，所述抗微生物化学实体包括引起结核病的分枝杆菌。合成多种化合物并筛选抗结核活性。本文公开了一系列具有抗结核活性的化合物，包括六种导致完全抑制5微克/ ml或更少的细菌生长的导致。对这些化合物中的三种进行测试以确定MIC，并且这些化合物针对药物敏感的结核分枝杆菌菌株和包括XDR菌株在内的多药耐药性（MDR）菌株，均在1和4微克/ ml之间。所开发的化合物衍生自母体化合物硝唑尼特，其在本文使用的严格测试形式中没有抑制活性。使用二硝基 - 噻吩或4-氯-5-硝基 - 噻唑骨架和R基团通过肽键（NHCO）连接环状化合物如苯，噻吩或呋喃来合成衍生物。许多这些化合物对革兰氏阳性菌包括金黄色葡萄球菌（MRSA）和表皮葡萄球菌具有广谱活性。这些先导化合物中的几种在三天内以200mg / Kg剂量施用对小鼠无毒。

5. 发明申请

WO2006023883A2 T TYPE CALCIUM CHANNEL INHIBITORS 审中-公开
标题翻译： T型钙通道抑制剂
公开(公告)号：WO2006023883A2
公开(公告)日：2006-03-02
申请号：PCT/US2005/029862
申请日：2005-08-22
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , GRAY, Lloyd S. , MACDONALD, Timothy L. , HAVERSTICK, Doris M. , PATTERSON, Jaclyn R. , MCCALMONT, William F.
发明人： GRAY, Lloyd S. , MACDONALD, Timothy L. , HAVERSTICK, Doris M. , PATTERSON, Jaclyn R. , MCCALMONT, William F.
IPC分类号： C07C217/54
CPC分类号： A61K31/14 , A61K31/085 , A61K31/12 , A61K31/137 , A61K31/138 , A61K45/06 , C07C217/58 , C07C217/60 , C07C217/62 , A61K2300/00
摘要： The present invention provides novel T type calcium channel inhibitors of formula (I), the use thereof in the treatment of a disease or condition in a mammal associated with influx of extracellular calcium via T type calcium channels, wherein R 1 is C 1 -C 4 alkyl, hydroxy, or C 1 -C 4 alkoxy; Z is NH, NCH 3 , O, S, or CH 2 ; Y is NH, O, or CH 2 with the proviso that Y and Z are not the same; R 2 is H, halo, NH 2 , C 1 -C 4 alkyl, hydroxy, or C 1 -C 4 alkoxy; m and n are independently selected from integers ranging from 1-5 with the proviso that m + n = an integer ranging from 2-9; and R 3 is H, halo, NH 2 , C 1 -C 4 alkyl, hydroxy, or C 1 -C 4 alkoxy.
摘要翻译：本发明提供式（I）的新型T型钙通道抑制剂，其用于治疗与通过T型钙通道流入胞外钙相关的哺乳动物疾病或病症的用途，其中R

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