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1. 发明申请

WO2008014286A1 VINYL PHOSPHONATE LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS 审中-公开
标题翻译：乙烯基磷酸肌醇六磷酸受体拮抗剂
公开(公告)号：WO2008014286A1
公开(公告)日：2008-01-31
申请号：PCT/US2007/074262
申请日：2007-07-24
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , CARTER, Karen, M. , LYNCH, Kevin, R. , MACDONALD, Timothy, L.
发明人： CARTER, Karen, M. , LYNCH, Kevin, R. , MACDONALD, Timothy, L.
IPC分类号： C07F9/58 , A61K31/662 , A61P9/00 , A61P29/00 , A61P35/00
CPC分类号： C07F9/582
摘要： The present invention provides LPA analogs that are antagonists at the LPA receptors. The analogs have the formula (I) wherein Z is -CY=CH- or -G≡C-; wherein when Z is -CY=CH- then the double bond is in the trans (e) configuration; Y is hydrogen or halogen, and R 1 -R° and m and n are as defined in the application.
摘要翻译：本发明提供作为LPA受体拮抗剂的LPA类似物。类似物具有式（I）其中Z为-CY = CH-或-G = C-; 其中当Z为-CY = CH-时，双键为反式（e）构型; Y是氢或卤素，R 1 -R 0和m和n如申请中所定义。

2. 发明申请

WO2006063033A2 ARYL AMIDE SPHINGOSINE 1-PHOSPHATE ANALOGS 审中-公开
公开(公告)号：WO2006063033A2
公开(公告)日：2006-06-15
申请号：PCT/US2005/044231
申请日：2005-12-06
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , CLEMENS, Jeremy, J. , DAVIS, Michael, D.
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L. , CLEMENS, Jeremy, J. , DAVIS, Michael, D.
IPC分类号： A61P35/00 , A61K31/00
CPC分类号： C07F9/091 , C07F9/1651 , C07F9/3808 , C07F9/4006
摘要： The present invention provides compounds that have antagonist activity at the S1P 1 and/or S1P 3 receptors. These compounds have enhanced selectivity and potency at the S1P 1 and/or S1P 3 receptors.
摘要翻译：本发明提供了在S1P1和/或S1P3受体上具有拮抗活性的化合物。这些化合物在S1P1和/或S1P3受体上具有增强的选择性和效力。

3. 发明申请

WO2009146112A1 COMPOSITIONS AND METHODS FOR INHIBITING SPHINGOSINE KINASE 审中-公开
标题翻译：用于抑制丝氨酸激酶的组合物和方法
公开(公告)号：WO2009146112A1
公开(公告)日：2009-12-03
申请号：PCT/US2009/039334
申请日：2009-04-02
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , KHAREL, Yugesh , MATHEWS, Thomas, Peter , WAMHOFF, Brian, R.
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L. , KHAREL, Yugesh , MATHEWS, Thomas, Peter , WAMHOFF, Brian, R.
IPC分类号： C07D409/04 , C07D409/02 , C07D413/04 , C07D413/02 , A61K39/395 , A61P35/00 , A61P9/10
CPC分类号： C07D413/04 , C07D409/04
摘要： Amidine analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumor cells.
摘要翻译：提供了可以抑制鞘氨醇激酶1和鞘氨醇激酶2（SphK1和SphK2）活性的脒类似物。该化合物可以预防肿瘤细胞中的血管生成。

4. 发明申请

WO2009023854A1 BICYCLIC SPHINGOSINE 1-PHOSPHATE ANALOGS 审中-公开
标题翻译：双相磷脂酸1-磷酸酯类似物
公开(公告)号：WO2009023854A1
公开(公告)日：2009-02-19
申请号：PCT/US2008/073378
申请日：2008-08-15
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , BIOGEN IDEC MA INC. , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , GUCKIAN, Kevin , LIN, Edward, Yin-shiang
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L. , GUCKIAN, Kevin , LIN, Edward, Yin-shiang
IPC分类号： C07F9/09 , C07C215/08 , C07C215/10 , C07D271/06 , C07D333/16 , C07D413/04 , A61K31/133 , A61K31/381 , A61K31/4245 , A61K31/661 , A61P19/00
CPC分类号： C07C323/32 , C07C215/38 , C07C217/74 , C07D271/06 , C07D333/16 , C07D413/04 , C07F9/091
摘要： Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors. Formula (I):
摘要翻译：提供了在一种或多种S1P受体上具有激动剂活性的化合物。化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。式（I）：

5. 发明申请

WO2011020116A1 IMIDAMIDE SPHINGOSINE KINASE INHIBITORS 审中-公开
标题翻译：咪嘧啶兴奋剂激酶抑制剂
公开(公告)号：WO2011020116A1
公开(公告)日：2011-02-17
申请号：PCT/US2010/045660
申请日：2010-08-16
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , MATHEWS, Thomas, P. , KENNEDY, Andrew , KHAREL, Yugesh
发明人： LYNCH, Kevin, R. , MACDONALD, Timothy, L. , MATHEWS, Thomas, P. , KENNEDY, Andrew , KHAREL, Yugesh
IPC分类号： A01N37/52 , A61K31/155
CPC分类号： C07D207/09 , A61K31/155 , A61K31/40 , C07C257/16 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2103/74 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74
摘要： Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphKl & SphK2) are provided. The compounds can prevent angiogenesis in tumors.
摘要翻译：提供可以抑制鞘氨醇激酶1和鞘氨醇激酶2（SphK1和SphK2）活性的亚胺酰胺（脒）类似物。这些化合物可以预防肿瘤中的血管生成。

6. 发明申请

WO2008064320A2 HYDRINDANE ANALOGS HAVING SPHINGOSINE 1-PHOSPHATE RECEPTOR AGONIST ACTIVITY 审中-公开
标题翻译：具有丝氨酸1-磷酸酯受体激动剂活性的盐酸模拟物
公开(公告)号：WO2008064320A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/085401
申请日：2007-11-21
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： C07C215/38 , C07C233/18 , C07D209/16 , C07D271/06 , C07D333/20
CPC分类号： C07D333/16 , C07C215/38 , C07C217/74 , C07C2602/08 , C07D209/16 , C07D271/06 , C07D413/04 , C07F9/091
摘要： Hydrindane analogs that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at SlP receptors.
摘要翻译：提供了在一种或多种S1P受体上具有激动剂活性的氢化茚类似物。化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

7. 发明申请

WO2007092638A1 BICYCLIC SPHINGOSINE 1-PHOSPHATE ANALOGS 审中-公开
标题翻译：双相SPHINGOSINE 1-磷酸酯类似物
公开(公告)号：WO2007092638A1
公开(公告)日：2007-08-16
申请号：PCT/US2007/003645
申请日：2007-02-09
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： C07D271/06 , C07D333/16 , C07D419/04 , C07F9/09 , C07C215/08 , C07C215/10 , A61P29/00 , A61P3/00 , A61P19/00 , A61K31/133 , A61K31/381 , A61K31/4245 , A61K31/661 , A61K31/6615
CPC分类号： C07D271/06 , C07C215/28 , C07C217/64 , C07D333/16 , C07D419/04 , C07F9/091 , C07F9/093
摘要： Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
摘要翻译：提供了在一种或多种S1P受体上具有激动剂活性的化合物。化合物是鞘氨醇类似物，磷酸化后，可以作为S1P受体的激动剂。

8. 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。

9. 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。

10. 发明申请

WO2013119946A1 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：WO2013119946A1
公开(公告)日：2013-08-15
申请号：PCT/US2013/025341
申请日：2013-02-08
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , SANTOS, Webster, L. , LYNCH, Kevin, R. , MACDONALD, Timothy, L. , KENNEDY, Andrew , KHAREL, Yugesh , RAJE, Mithun, Rajendra , HOUCK, Joseph
发明人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , 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。

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