公开(公告)号：US07169818B2

公开(公告)日：2007-01-30

申请号：US10398305

申请日：2001-10-03

申请人： Kevin R. Lynch ,  Timothy L. Macdonald ,  Christopher E. Heise ,  Webster L. Santos ,  Mark D. Okusa

发明人： Kevin R. Lynch ,  Timothy L. Macdonald ,  Christopher E. Heise ,  Webster L. Santos ,  Mark D. Okusa

IPC分类号： A01N33/08

CPC分类号： C07K14/705 ,  C07F9/091 ,  C07F9/094 ,  C07F9/3808 ,  C07F9/3873 ,  C07F9/3882 ,  C07F9/5728 ,  C07F9/6506 ,  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。

公开(公告)号：US20170298032A1

公开(公告)日：2017-10-19

申请号：US15516333

申请日：2015-09-30

申请人： Kevin R. LYNCH ,  Webster L. SANTOS ,  University of Virginia Patent Foundation ,  Virginia Tech Intellectual Properties, Inc.

发明人： Kevin R. Lynch ,  Webster L. Santos

IPC分类号： C07D271/06 ,  C07C279/16 ,  A61K31/42 ,  C07D249/08 ,  A61K31/03

CPC分类号： C07D271/06 ,  A61K31/03 ,  A61K31/42 ,  C07C279/16 ,  C07D249/08 ,  C07D285/12 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

摘要： Sphingosine kinases are enzymes that catalyze the biosynthesis of sphingosine-1-phosphate. The invention provides compounds that are effective for inhibition of sphingosine kinase type 1, sphingosine kinase type 2, or both. Certain compounds are selective for sphingosine kinase type 2 relative to sphingosine kinase type 1. Compounds of the invention can be used in treatment of a range of diseases wherein increasing the level of sphingosine-1-phosphate in blood is medically indicated. Diseases that can be treated by administration of an effective dose of a compound of the invention include a neoplastic disease that involves excess vascular growth; macular degeneration or diabetic retinopathy; an allergic disease such as asthma, an inflammatory disease of the eye such as uveitis, scleritis, or vitritis; an inflammatory disease of the kidney; a fibrotic disease; atherosclerosis; or pulmonary arterial hypertension. A compound of the invention can be used to improve the integrity of a vascular barrier in a disease where the vascular barrier is disrupted, such as cancer or Alzheimer's disease.