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11. 发明申请

WO2005115150A3 NOVEL LYSOPHOSPHATIDIC ACID RECEPTOR SELECTIVE ANTAGONISTS 审中-公开
标题翻译：新型赖氨酸受体选择性拮抗剂
公开(公告)号：WO2005115150A3
公开(公告)日：2006-05-04
申请号：PCT/US2005016011
申请日：2005-05-06
申请人： UNIV VIRGINIA , LYNCH KEVIN R , MACDONALD TIMOTHY L , HEASLEY BRIAN H
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L , HEASLEY BRIAN H
IPC分类号： A61K31/66 , A01N57/00 , C07F9/02 , C07F9/09 , C07F9/38 , C07F9/40 , C07F9/572 , C07F9/58 , C07F9/6506 , C07F9/655
CPC分类号： C07F9/65515 , C07F9/091 , C07F9/094 , C07F9/3891 , C07F9/404 , C07F9/5728 , C07F9/582 , C07F9/65062
摘要： The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
摘要翻译：本发明涉及包含溶血磷脂酸类似物的组合物和使用此类类似物作为LPA受体活性的激动剂或拮抗剂的方法。此外，本发明涉及LPA受体激动剂，其在各个LPA受体（即LPA1，LPA2和LPA3）上的选择度变化。更具体地说，本发明涉及LPA类似物，其中甘油被乙醇胺替代，并且多种取代已经在第二个碳原子连接。

12. 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

13. 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

14. 发明申请

WO2005115150A2 NOVEL LYSOPHOSPHATIDIC ACID RECEPTOR SELECTIVE ANTAGONISTS 审中-公开
标题翻译：新型赖氨酸受体选择性拮抗剂
公开(公告)号：WO2005115150A2
公开(公告)日：2005-12-08
申请号：PCT/US2005/016011
申请日：2005-05-06
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , HEASLEY, Brian, H.
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L. , HEASLEY, Brian, H.
IPC分类号： A01N57/00
CPC分类号： C07F9/65515 , C07F9/091 , C07F9/094 , C07F9/3891 , C07F9/404 , C07F9/5728 , C07F9/582 , C07F9/65062
摘要： The present invention is directed to compositions comprising lysophosphatidic acid analogs and methods of using such analogs as agonist or antagonists of LPA receptor activity. In addition the invention is directed to LPA receptor agonists that vary in the degree of selectivity at individual LPA receptors (i.e. LPA1, LPA2 and LPA3). More particularly the present invention is directed to LPA analogs wherein the glycerol is replaced with ethanolamine and a variety of substitutions have been linked at the second carbon atom.
摘要翻译：本发明涉及包含溶血磷脂酸类似物的组合物和使用这些类似物作为LPA受体活性的激动剂或拮抗剂的方法。此外，本发明涉及在各个LPA受体（即LPA1，LPA2和LPA3）上的选择性程度变化的LPA受体激动剂。更具体地说，本发明涉及LPA类似物，其中甘油被乙醇胺替代，并且多种取代已经在第二个碳原子连接。

15. 发明申请

WO2004010949A2 COMPOUNDS ACTIVE IN SPINIGOSINE 1-PHOSPHATE SIGNALING 审中-公开
标题翻译：化合物在磷酸肌醇1-磷酸酯信号传导中具有活性
公开(公告)号：WO2004010949A2
公开(公告)日：2004-02-05
申请号：PCT/US2003/023768
申请日：2003-07-30
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , LYNCH, Kevin, R. , MACDONALD, Timothy, L.
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L.
IPC分类号： A61K
CPC分类号： C07F9/65068 , C07F9/091 , C07F9/094 , C07F9/65062
摘要： The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure of Formula (I) wherein R 11 is C 5 -C 18 alkyl or C 5 -C 18 alkenyl; Q is selected from the group consisting of C 3 -C 6 optionally substituted cycloalkyl, C 3 -C 6 optionally substituted heterocyclic, C 3 -C 6 optionally substituted aryl C 3 -C 6 optionally substituted heteroaryl and -NH(CO)-; R 2 is selected from the group consisting of H, C 1 -C 4 alkyl, (C 1 -C 4 alkyl)OH and (C 1 -C 4 alkyl)NH 2 ; R 23 is H or C 1 -C 4 alkyl, and R 15 is selected from the group consisting of hydroxy, phosphonate, and of Formula (II) wherein X and R 12 is selected from the group consisting of O and S; or a pharmaceutically acceptable salt or tautomer thereof.
摘要翻译：本发明涉及具有S1P受体调节剂活性的S1P类似物以及这些化合物用于治疗与不适当的S1P受体活性相关的疾病的用途。所述化合物具有式（I）的通式结构，其中R 11为C 5 -C 18烷基或C 5-15芳基， C 18 -C 18链烯基; Q选自C 3 -C 6任选取代的环烷基，C 3 -C 6环烷基，C 3 -C 6环烷基，任选取代的杂环基，C 3 -C 6任选取代的芳基C 3 -C 6任选取代的杂芳基和 - NH（CO） - ; R 2选自H，C 1 -C 4烷基，（C 1 -C 4）烷基，C 1 -C 4烷基，（C 1 -C 4烷基）OH和（C 1 -C 4烷基）NH 2; R 23是H或C 1 -C 4烷基，并且R 15选自由以下组成的组：羟基，膦酸酯和式（II）的基团，其中X和R 12选自O和S; 或其药学上可接受的盐或互变异构体。

16. 发明申请

WO2003086408A1 USE OF A2A ADENOSINE RECEPTOR AGONISTS FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：使用A2A腺苷受体激动剂治疗炎性疾病
公开(公告)号：WO2003086408A1
公开(公告)日：2003-10-23
申请号：PCT/US2003/011146
申请日：2003-04-10
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , LINDEN, Joel, M. , SULLIVAN, Gail, W. , MACDONALD, Timothy, L. , SCHELD, Michael W. , OBRIG, Tom G. , RIEGER, Jayson M.
发明人： LINDEN, Joel, M. , SULLIVAN, Gail, W. , MACDONALD, Timothy, L. , SCHELD, Michael W. , OBRIG, Tom G. , RIEGER, Jayson M.
IPC分类号： A61K31/52
CPC分类号： A61K31/52 , C07H19/16 , Y02A50/473
摘要： The present invention provides a therapeutic method for treating biological diseases that includes the administration of an effective amount of a suitable antibiotic agent, antifungal agent or antiviral agent in conjunction with A 2A adenosine receptor agonist. If no anti-pathogenic agent is known the A 2A agonist can be used alone to reduce inflammation, as may occur during infection with antibiotic resistant bacteria, or certain viruses such as those that cause SARS or Ebola. Optionally, the method includes administration of a type IV PDE inhibitor
摘要翻译：本发明提供了治疗生物学疾病的治疗方法，其包括与A2A腺苷受体激动剂联合施用有效量的合适的抗生素，抗真菌剂或抗病毒剂。如果没有抗病原剂是已知的，则可以单独使用A2A激动剂来减少炎症，如在抗生素抗性细菌感染期间可能发生的，或某些病毒，例如导致SARS或埃博拉病毒的病毒。任选地，该方法包括施用IV型PDE抑制剂

17. 发明申请

WO2013119946A8 LONG CHAIN BASE SPHINGOSINE KINASE INHIBITORS 审中-公开
标题翻译：长链碱性激酶激酶抑制剂
公开(公告)号：WO2013119946A8
公开(公告)日：2014-10-30
申请号：PCT/US2013025341
申请日：2013-02-08
申请人： UNIV VIRGINIA PATENT FOUND , SANTOS WEBSTER L , LYNCH KEVIN R , MACDONALD TIMOTHY L , KENNEDY ANDREW , KHAREL YUGESH , RAJE MITHUN RAJENDRA , HOUCK JOSEPH
发明人： SANTOS WEBSTER L , LYNCH KEVIN R , MACDONALD TIMOTHY L , KENNEDY ANDREW , KHAREL YUGESH , RAJE MITHUN RAJENDRA , HOUCK JOSEPH
IPC分类号： A61K31/155
CPC分类号： C07D413/04 , C07C251/02 , C07C251/12 , C07C257/14 , C07C257/16 , C07C271/20 , C07C275/70 , C07C279/00 , C07C279/16 , C07C279/18 , C07C281/16 , C07C2601/02 , C07C2601/14 , C07D249/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D413/06
摘要： The invention relates to inhibitors of sphingosine kinase enzymatic activity, compounds and pharmaceutical compositions that inhibit sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) enzymes and further relates to methods of treating diseases and disorders mediated by sphingosine 1 phosphate activity, comprising administering an effective amount of sphingosine kinase inhibitors.
摘要翻译：本发明涉及鞘氨醇激酶酶活性抑制剂，抑制鞘氨醇激酶1和鞘氨醇激酶2（SphK1＆SphK2）酶的化合物和药物组合物，还涉及治疗由鞘氨醇1磷酸酯活性介导的疾病和病症的方法，包括给予有效量的鞘氨醇激酶抑制剂。

18. 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。

19. 发明申请

WO2006023883A3 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：WO2006023883A3
公开(公告)日：2006-07-27
申请号：PCT/US2005029862
申请日：2005-08-22
申请人： UNIV VIRGINIA , 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： C07C211/03
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型钙通道流入细胞外钙的哺乳动物相关的疾病或病症的用途，其中R 1， C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，羟基或C 1 -C 4烷氧基; Z是NH，NCH 3，O，S或CH 2; Y是NH，O或CH 2，条件是Y和Z不相同; R 2是H，卤素，NH 2，C 1 -C 4烷基，羟基或C 1 -C 4烷基， C 1 -C 4烷氧基; m和n独立地选自1-5的整数，条件是m + n = 2-9的整数; 且R 3为H，卤素，NH 2，C 1 -C 4烷基，羟基或C C 1 -C 4烷氧基。

20. 发明申请

WO03061655A8 2-AMINOTHIAZOLE ALLOSTERIC ENHANCERS OF A1 ADENOSINE RECEPTORS 审中-公开
标题翻译： A1亚单位受体的2-氨基噻唑单抗增强剂
公开(公告)号：WO03061655A8
公开(公告)日：2006-06-22
申请号：PCT/US0301396
申请日：2003-01-16
申请人： UNIV VIRGINIA , LINDEN JOEL , MURPHREE LAUREN , CHORDIA MAHENDRA D , MACDONALD TIMOTHY L
发明人： LINDEN JOEL , MURPHREE LAUREN , CHORDIA MAHENDRA D , MACDONALD TIMOTHY L
IPC分类号： C07D277/60 , A61K31/428 , A61P9/00 , A61P9/06 , A61P9/10 , A61P15/08 , A61P25/02 , A61P25/20 , A61P27/16 , A61P29/00 , A61P43/00 , C07D277/84 , C07D417/04
CPC分类号： C07D277/60 , C07D277/84
摘要： The present invention relates generally to a class of 2-aminothiazole derivatives which have recently been identified as allosteric enhancers of the A 1 adenosine receptor. These compounds, and therapeutic compositions containing them, are useful for treating conditions in which activation of the A 1 adenosine receptor would be beneficial, for example, those conditions in which stimulation of angiogenesis would improve blood flow to ischemic tissues.
摘要翻译：本发明一般涉及最近被鉴定为Aβ1腺苷受体的变构增强子的一类2-氨基噻唑衍生物。这些化合物和含有它们的治疗组合物可用于治疗其中A 1 N 2腺苷受体的活化将是有益的条件，例如，其中血管生成刺激将改善血液流向缺血的那些条件组织。

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