公开(公告)号：US07125872B2

公开(公告)日：2006-10-24

申请号：US10745471

申请日：2003-12-22

申请人： Michael Kahn ,  Cyprian O. Ogbu ,  Masakatsu Eguchi ,  Hwa-Ok Kim ,  Patrick Douglas Boatman, Jr.

发明人： Michael Kahn ,  Cyprian O. Ogbu ,  Masakatsu Eguchi ,  Hwa-Ok Kim ,  Patrick Douglas Boatman, Jr.

IPC分类号： A01N43/58

CPC分类号： C07K7/06 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/437 ,  A61K31/5025 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04 ,  C07K1/047 ,  C07K5/0202 ,  C07K5/021 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0821 ,  C07K5/1024

摘要： There are disclosed β-sheet mimetics and methods relating to the same for imparting or stabilizing the β-sheet structure of a peptide, protein or molecule. In one aspect, β-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the β-sheet mimetic is a thrombin inhibitor.

公开(公告)号：US06548500B2

公开(公告)日：2003-04-15

申请号：US09742680

申请日：2000-12-19

申请人： Michael Kahn ,  Masakatsu Eguchi ,  Hwa-Ok Kim ,  Marcin Stasiak

发明人： Michael Kahn ,  Masakatsu Eguchi ,  Hwa-Ok Kim ,  Marcin Stasiak

IPC分类号： A61K314985

CPC分类号： C07D487/04 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/551 ,  A61K38/00 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06139 ,  C40B40/00 ,  Y10S514/825 ,  Y10S514/826 ,  Y10S514/903

摘要： Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.

公开(公告)号：US06245764B1

公开(公告)日：2001-06-12

申请号：US09009665

申请日：1998-01-20

申请人： Michael Kahn ,  Cyprian O. Ogbu ,  Masakatsu Eguchi ,  Hwa-Ok Kim ,  Patrick Douglas Boatman, Jr.

发明人： Michael Kahn ,  Cyprian O. Ogbu ,  Masakatsu Eguchi ,  Hwa-Ok Kim ,  Patrick Douglas Boatman, Jr.

IPC分类号： A01N4358

CPC分类号： C07K7/06 ,  A61K31/4035 ,  A61K31/4152 ,  A61K31/437 ,  A61K31/5025 ,  A61K38/005 ,  A61K38/04 ,  A61K38/55 ,  C07K1/047 ,  C07K5/0202 ,  C07K5/021 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/0821 ,  C07K5/1024

摘要： There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, &bgr;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &bgr;-sheet mimetic is a thrombin inhibitor.

摘要翻译： 公开了与赋予或稳定肽，蛋白质或分子的β-折叠结构相关的β-折叠模拟物和方法。 一方面，公开了通常用作蛋白酶抑制剂的β-片剂模拟物，更具体地，作为丝氨酸蛋白酶抑制剂如凝血酶，弹性蛋白酶和因子X抑制剂。 在一个实施方案中，β-折叠模拟物是凝血酶抑制剂。