公开(公告)号：EP2190852A1

公开(公告)日：2010-06-02

申请号：EP08798022.3

申请日：2008-08-15

申请人： University Of Virginia Patent Foundation ,  Biogen Idec MA Inc.

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):

公开(公告)号：EP1863463A1

公开(公告)日：2007-12-12

申请号：EP06735115.5

申请日：2006-02-14

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

发明人： LYNCH, Kevin, R. ,  MACDONALD, Timothy, L.

IPC分类号： A61K31/137 ,  A61K31/425 ,  A61K31/665 ,  A61K31/40 ,  A61K31/415 ,  A61K31/67 ,  A61K31/402 ,  A61K31/381 ,  A61K31/675 ,  A61K31/42 ,  A61K31/661 ,  A61P1/00 ,  A61K31/341 ,  A61K31/662 ,  A61P7/12

CPC分类号： C07D207/22 ,  C07C215/44 ,  C07D207/14 ,  C07D231/04 ,  C07D275/03 ,  C07D307/22 ,  C07F9/094 ,  C07F9/3882 ,  C07F9/547

摘要： The present invention provides sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type. The compounds invention include compounds having a phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.

公开(公告)号：EP1987013A1

公开(公告)日：2008-11-05

申请号：EP07763449.1

申请日：2007-02-09

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

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.

公开(公告)号：EP1827606A2

公开(公告)日：2007-09-05

申请号：EP05853218.5

申请日：2005-12-06

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

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 S1P1 and/or S1P3 receptors. These compounds have enhanced selectivity and potency at the S1P1 and/or S1P3 receptors.

公开(公告)号：EP1383778B1

公开(公告)日：2009-10-21

申请号：EP02704296.9

申请日：2002-01-30

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

发明人： MACDONALD, Timothy, L. ,  LYNCH, Kevin, R.

IPC分类号： C07F9/02

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, α-substituted methylene phosphonate, thiophoasphate and thiophosphonate; and R5 is C8-C22alkenyl.

公开(公告)号：EP2054424A1

公开(公告)日：2009-05-06

申请号：EP07813308.9

申请日：2007-07-24

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

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 R1-R° and m and n are as defined in the application.

公开(公告)号：EP1383778A2

公开(公告)日：2004-01-28

申请号：EP02704296.9

申请日：2002-01-30

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

发明人： MACDONALD, Timothy, L. ,  LYNCH, Kevin, R.

IPC分类号： C07F9/02 ,  C07C233/05 ,  A61K31/16 ,  A61K31/66

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, α-substituted methylene phosphonate, thiophoasphate and thiophosphonate; and R5 is C8-C22alkenyl.

公开(公告)号：EP1361872A2

公开(公告)日：2003-11-19

申请号：EP01977415.7

申请日：2001-10-03

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

发明人： LYNCH, Kevin, R. ,  MACDONALD, Timothy, L. ,  HEISE, Christopher, E. ,  SANTOS, Webster, L. ,  OKUSA, Mark, D.

IPC分类号： A61K31/16

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.

公开(公告)号：EP2822548A1

公开(公告)日：2015-01-14

申请号：EP13820704.8

申请日：2013-02-08

申请人： University of Virginia Patent Foundation

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, and methods of treating diseases and disorders by administering inhibitors of Sphingosine Kinase enzymatic activity.

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和SphK2）酶的化合物和药物组合物，并且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， 有效量的鞘氨醇激酶抑制剂。

公开(公告)号：EP1986623A2

公开(公告)日：2008-11-05

申请号：EP07717121.3

申请日：2007-01-29

申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION

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.