公开(公告)号：US06683093B2

公开(公告)日：2004-01-27

申请号：US09989943

申请日：2001-11-21

申请人： Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Gary A. DeCrescenzo ,  Yvette M. Fobian ,  John N. Freskos ,  Daniel P. Getman ,  Joseph J. McDonald ,  Madeleine H. Li ,  Susan L. Hockerman ,  Carol Pearcy Howard ,  Steve A. Kolodziej ,  Deborah A. Mischke ,  Joseph G. Rico ,  Nathan W. Stehle ,  Michael B. Tollefson ,  William F. Vernier ,  Clara I. Villamil ,  Darren J. Kassab

发明人： Thomas E. Barta ,  Daniel P. Becker ,  Louis J. Bedell ,  Terri L. Boehm ,  Jeffery N. Carroll ,  Gary A. DeCrescenzo ,  Yvette M. Fobian ,  John N. Freskos ,  Daniel P. Getman ,  Joseph J. McDonald ,  Madeleine H. Li ,  Susan L. Hockerman ,  Carol Pearcy Howard ,  Steve A. Kolodziej ,  Deborah A. Mischke ,  Joseph G. Rico ,  Nathan W. Stehle ,  Michael B. Tollefson ,  William F. Vernier ,  Clara I. Villamil ,  Darren J. Kassab

IPC分类号： A61K31445

CPC分类号： C07D401/14 ,  C07D211/66 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/08 ,  C07D335/02 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.

摘要翻译： 本发明涉及芳族砜异羟肟酸盐（也称为芳香砜异羟肟酸）及其盐，其特别是倾向于抑制基质金属蛋白酶（也称为基质金属蛋白酶或MMP）活性和/或软骨聚集蛋白聚糖酶活性。 本发明还涉及一种治疗方法，其包括将有效量的MMP抑制和/或聚集蛋白聚糖酶抑制剂的化合物或盐施用于具有（或设置为具有）与MMP相关的病理状况的动物，特别是哺乳动物 活性和/或蛋白聚糖蛋白聚糖酶活性。

公开(公告)号：US07115378B2

公开(公告)日：2006-10-03

申请号：US10233885

申请日：2002-09-03

申请人： Dean J. Welsch ,  Kevin L. Duffin ,  Olga V. Nemirovskiy ,  Dawn R. Dufield ,  Teresa Sunyer ,  Carol Pearcy Howard

发明人： Dean J. Welsch ,  Kevin L. Duffin ,  Olga V. Nemirovskiy ,  Dawn R. Dufield ,  Teresa Sunyer ,  Carol Pearcy Howard

IPC分类号： G01N33/53

CPC分类号： G01N33/6842 ,  C07K14/78 ,  C07K16/18 ,  C12Q1/37 ,  G01N33/6821 ,  G01N33/6887 ,  G01N2333/78 ,  G01N2333/96486 ,  G01N2500/02 ,  G01N2800/102 ,  G01N2800/105 ,  G01N2800/52 ,  Y10T436/105831

摘要： A method for identifying and quantifying peptides resulting from enzyme cleavage of collagen type II by mass spectrometric analysis to detect characteristic peptide fragments of a carboxy-terminus having known mass to charge ratios to identify the peptide having that carboxy-terminus. Identification and quantification of the peptides in a biological sample is used to assess activity of proteolytic enzymes in diseases or physiological conditions such as osteoarthritis and rheumatoid arthritis and to assess the efficacy of enzyme blocking agents.