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1. 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。

2. 发明申请

WO0229001A3 NOVEL LYSOPHOSPHATIDIC ACID RECEPTOR AGONISTS AND ANTAGONISTS 审中-公开
标题翻译：新型赖氨酸受体激动剂和拮抗剂
公开(公告)号：WO0229001A3
公开(公告)日：2003-08-21
申请号：PCT/US0130936
申请日：2001-10-03
申请人： UNIV VIRGINIAN PATENT FOUNDATI , LYNCH KEVIN R , MACDONALD TIMOTHY L , HEISE CHRISTOPHER E , SANTOS WEBSTER L , OKUSA MARK D
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L , HEISE CHRISTOPHER E , SANTOS WEBSTER L , OKUSA MARK D
IPC分类号： C07F9/09 , C07F9/38 , C07F9/572 , C07F9/6506 , C07F9/655 , C07K14/705 , A61K31/16 , A61K31/04 , A61K31/075 , A61K31/08 , A61K31/13 , C07C211/00 , C07C233/00
CPC分类号： C07K14/705 , C07F9/091 , C07F9/094 , C07F9/3808 , C07F9/3873 , C07F9/3882 , C07F9/5728 , C07F9/65062 , C07F9/65515
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。

3. 发明申请

WO2012129073A2 COMPOSITIONS AND METHODS FOR TISSUE ENGINEERING AND CELL BASED THERAPIES 审中-公开
标题翻译：组织工程和细胞治疗的组合物和方法
公开(公告)号：WO2012129073A2
公开(公告)日：2012-09-27
申请号：PCT/US2012029369
申请日：2012-03-16
申请人： UNIV VIRGINIA PATENT FOUND , BOTCHWEY III EDWARD A , LAUGHLIN MARY J , LYNCH KEVIN R , DAS ANUSUYA , AWOJOODU ANTHONY
发明人： BOTCHWEY III EDWARD A , LAUGHLIN MARY J , LYNCH KEVIN R , DAS ANUSUYA , AWOJOODU ANTHONY
IPC分类号： A61K31/13 , A61K31/137 , A61K31/4168 , A61P17/00 , A61P17/02
CPC分类号： A61K31/495 , A61K31/135 , A61K31/137 , A61K31/395 , A61K31/4164 , A61K31/66 , A61K45/06 , A61K2300/00
摘要： The present application discloses strategies to recruit and mobilize stem cells using S1P receptor selective agonists and antagonists as wells as regulators of chemokine receptors. In an in vivo ischemic model, S1P1/S1P3 activation with FTY720 impeded inflammatory cell infiltration and recruited endothelial progenitor cells (EPCs) with the potential to increase microvascular remodeling. S1P3 expression on marrow-derived cells was essential for this remodeling. Concurrent systemic S1P3 and CXCR4 antagonism mobilized hematopoietic stem cells (HSCs) with the ability to engraft and repopulate blood cells. Pre-treatment of donor HSCs with FTY720 increased homing toward SDF-1 and improved engraftment in marrow. FTY720-coated bone allografts coupled with systemic administration of VPC01091 enhanced bone allograft integration and new bone formation in bone defects. MSCs pre-treated with FTY720 exhibited increased migration toward SDF-1, a CXCR4+ ligand. The results show that S1P is a very powerful role player in pharmacological marrow-derived stem cell mobilization and recruitment.
摘要翻译：本申请公开了使用S1P受体选择性激动剂和拮抗剂作为趋化因子受体的调节剂募集和动员干细胞的策略。在体内缺血模型中，具有FTY720的S1P1 / S1P3激活阻碍炎性细胞浸润并引起具有增加微血管重塑潜力的内皮祖细胞（EPCs）。骨髓来源的细胞上的S1P3表达对于这种重塑是必不可少的。并发系统性S1P3和CXCR4拮抗剂动员造血干细胞（HSCs），具有移植和再填充血细胞的能力。 FTY720对供体HSC的预处理增加了对SDF-1的归巢，改善了骨髓移植。 FTY720包被的骨同种异体移植物与全身施用的VPC01091相结合，增强骨同种异体移植物整合和骨缺损中的新骨形成。用FTY720预处理的MSC表现出向SDF-1（CXCR4 +配体）的迁移增加。结果表明，S1P在药理学骨髓干细胞动员和招募中是非常有力的角色。

4. 发明申请

WO2004010949A3 COMPOUNDS ACTIVE IN SPINIGOSINE 1-PHOSPHATE SIGNALING 审中-公开
标题翻译：螺旋体1-磷酸盐信号中的化合物
公开(公告)号：WO2004010949A3
公开(公告)日：2004-10-07
申请号：PCT/US0323768
申请日：2003-07-30
申请人： UNIV VIRGINIA , LYNCH KEVIN R , MACDONALD TIMOTHY L
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L
IPC分类号： C07D233/54 , C07F9/09 , C07F9/6506 , A61K31/4164 , C07F9/06
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 R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and -NH(CO)-; R2 is selected from the group consisting of H, C1 -C4 alkyl, (C1 -C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is selected from the group consisting of hydroxy, phosphonate, and of Formula (II) wherein X and R12 is selected from the group consisting of O and S; or a pharmaceutically acceptable salt or tautomer thereof.
摘要翻译：本发明涉及具有作为S1P受体调节剂的活性的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。化合物具有通式（I）的通式，其中R 11为C 5 -C 18烷基或C 5 -C 18烯基; Q选自C 3 -C 6任选取代的环烷基，C 3 -C 6任选取代的杂环，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） - ; R2选自H，C1-C4烷基，（C1-C4烷基）OH和（C1-C4烷基）NH2; R 23是H或C 1 -C 4烷基，R 15选自羟基，膦酸酯和式（II），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。

5. 发明申请

WO2008064337A3 BENZOCYCLOHEPTYL ANALOGS HAVING SPHINGOSINE 1-PHOSPHATE RECEPTOR ACTIVITY 审中-公开
标题翻译：具有1-磷酸鞘氨醇受体活性的苯并环庚烷类似物
公开(公告)号：WO2008064337A3
公开(公告)日：2008-10-09
申请号：PCT/US2007085433
申请日：2007-11-21
申请人： UNIV VIRGINIA , LYNCH KEVIN R , MACDONALD TIMOTHY L
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L
IPC分类号： C07C215/28 , A61K31/135 , A61P3/10 , A61P11/06 , A61P19/02 , A61P25/02 , A61P27/02 , A61P37/00 , A61P37/06 , C07C215/38
CPC分类号： C07C215/38 , C07C2602/12 , C07D271/06 , C07D333/16 , C07D413/04
摘要： Benzocycloheptyl analogs that have agonist activity at one or more of the S IP receptors are provided. The compounds are sphingosine analogs, which, after phosphorylation, can behave as agonists at SlP receptors.
摘要翻译：提供了对一种或多种S1P受体具有激动剂活性的苯并环庚基类似物。这些化合物是鞘氨醇类似物，其在磷酸化后可以用作S1P受体的激动剂。

6. 发明申请

WO2006063033A3 ARYL AMIDE SPHINGOSINE 1-PHOSPHATE ANALOGS 审中-公开
标题翻译：芳基酰胺类神经鞘氨醇1-磷酸类似物
公开(公告)号：WO2006063033A3
公开(公告)日：2006-11-09
申请号：PCT/US2005044231
申请日：2005-12-06
申请人： UNIV VIRGINIA , 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：本发明提供了对S1P SUB和/或S1P SUB受体具有拮抗活性的化合物。这些化合物对S1P SUB1和/或S1P SUB3受体具有增强的选择性和效力。

7. 发明申请

WO02064616A3 AGONISTS AND ANTAGONISTS OF SPHINGOSINE-1-PHOSPHATE RECEPTORS 审中-公开
标题翻译：天冬氨酸-1-磷酸受体的激动剂和拮抗剂
公开(公告)号：WO02064616A3
公开(公告)日：2002-11-14
申请号：PCT/US0202715
申请日：2002-01-30
申请人： UNIV VIRGINA PATENT FOUNDATION , MACDONALD TIMOTHY L , LYNCH KEVIN R
发明人： MACDONALD TIMOTHY L , LYNCH KEVIN R
IPC分类号： A61K47/42 , A61K31/436 , A61K31/52 , A61K31/573 , A61K31/661 , A61K31/675 , A61K38/00 , A61P1/00 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P13/02 , A61P13/08 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/02 , A61P31/04 , A61P31/10 , A61P31/12 , A61P31/18 , A61P33/02 , A61P35/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07C237/04 , C07F9/09 , C07F9/38 , C07F9/6506 , C07F9/02 , A61K31/16 , A61K31/66 , C07C233/05
CPC分类号： C07F9/65068 , C07C237/04 , C07F9/091 , C07F9/3808
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 (I), wherein R1 is C8-C22 alkyl, C8-C22 alkenyl or R12 is O, or R1 and R12 taken together form an optionally substituted aryl or an optionally substituted heteroaryl; R17 is H, alkyl or alkylaryl; R18 is N or CH; R2 and R3 are independently selected from the group consisting of H, NH2, and OH, with the proviso that at least one of R2 and R3 is NH2; R4 is selected from the group consisting of hydroxyl, phosphate, phosphonate methylene phosphonate, alpha -substituted methylene phosphonate, thiophoasphate and thiophosphonate; and R5 is C8-C22alkenyl.
摘要翻译：本发明涉及具有S1P受体调节剂活性的S1P类似物以及这类化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。所述化合物具有通式结构（I），其中R 1为C 8 -C 22烷基，C 8 -C 22烯基或R 12为O，或者R 1和R 12一起形成任选取代的芳基或任选取代的杂芳基; R17是H，烷基或烷芳基; R18是N或CH; R2和R3独立地选自由H，NH2和OH组成的组，条件是R2和R3中的至少一个是NH2; R4选自羟基，磷酸酯，膦酸酯亚甲基膦酸酯，α-取代的亚甲基膦酸酯，硫代磷酸酯和硫代膦酸酯; 和R5是C8-C22链烯基。

8. 发明申请

WO2007098474A8 PHENYL-CYCLOALKYL AND PHENYL-HETEROCYCLIC DERIVATIVES AS S1P RECEPTOR AGONISTS 审中-公开
标题翻译：作为S1P受体激动剂的苯丙氨酸和苯基间苯二酚衍生物
公开(公告)号：WO2007098474A8
公开(公告)日：2008-11-06
申请号：PCT/US2007062513
申请日：2007-02-21
申请人： UNIV VIRGINIA , LYNCH KEVIN R , MACDONALD TIMOTHY L
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L
IPC分类号： C07D271/06 , A61P35/00 , C07C251/32 , C07C255/50 , C07F9/02
CPC分类号： C07D271/06 , C07F9/65318
摘要： Compounds I and II 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I和II。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。

9. 发明申请

WO2008064320A3 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：WO2008064320A3
公开(公告)日：2008-10-30
申请号：PCT/US2007085401
申请日：2007-11-21
申请人： UNIV VIRGINIA , LYNCH KEVIN R , MACDONALD TIMOTHY L
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L
IPC分类号： C07C215/38 , A61K31/404 , A61K31/4245 , A61P19/00 , A61P37/00 , C07C233/18 , C07D209/16 , C07D271/06 , C07D333/20 , C07D413/04 , C07F9/117
CPC分类号： C07D333/16 , C07C215/38 , C07C217/74 , C07C2602/08 , C07D209/16 , C07D271/06 , C07D413/04 , C07F9/091
摘要： Hydrindane analogs of formula (IA) and (IB) 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式（IA）和（IB）的氢化茚二酮类似物。 '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。

10. 发明申请

WO2007089715A2 METHOD FOR TREATMENT OF NEUROPATHIC PAIN 审中-公开
标题翻译：治疗神经性疼痛的方法
公开(公告)号：WO2007089715A2
公开(公告)日：2007-08-09
申请号：PCT/US2007002422
申请日：2007-01-29
申请人： UNIV VIRGINIA , LYNCH KEVIN R , MACDONALD TIMOTHY L
发明人： LYNCH KEVIN R , MACDONALD TIMOTHY L
IPC分类号： A61K31/133 , A61K31/661 , A61P25/02
CPC分类号： A61K31/133 , A61K31/661
摘要： Compounds and methods useful for preventing and treating pain,e.g., neuropathic pain, in a subject in need thereof are provided. The compounds can be "SlP modulating" agents that are capable of inducing a detectable change in SlP receptor activity.
摘要翻译：提供了用于预防和治疗有此需要的受试者的疼痛，例如神经性疼痛的化合物和方法。该化合物可以是能够诱导S1P受体活性的可检测变化的“S1P调节”剂。

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