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公开(公告)号:US6130315A
公开(公告)日:2000-10-10
申请号:US139009
申请日:1998-08-24
申请人: H. Michael Kolb , Joseph P. Burkhart , Michael J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
发明人: H. Michael Kolb , Joseph P. Burkhart , Michael J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
IPC分类号: A61K38/00 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07D498/10 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/08 , C07K5/083 , C07K5/097 , C07K7/00 , C07K1/02 , C07K1/107 , C07K5/10
CPC分类号: C07K5/0227 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06147 , C07K5/06191 , C07K5/0806 , C07K5/0823 , C07K5/0827 , A61K38/00
摘要: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
摘要翻译: 本发明涉及肽酶底物的类似物,其中含有底物肽的染色体酰胺键的酰胺基已被活化的亲电子酮部分代替。 肽酶底物的这些类似物为各种蛋白酶提供特异性酶抑制剂,其抑制将在各种疾病状态下具有有用的生理后果。
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公开(公告)号:US5849866A
公开(公告)日:1998-12-15
申请号:US481666
申请日:1995-06-07
申请人: H. Michael Kolb , Joseph P. Burkhart , Michel J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
发明人: H. Michael Kolb , Joseph P. Burkhart , Michel J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
IPC分类号: A61K38/00 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07D498/10 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/08 , C07K5/083 , C07K5/097 , C07C49/00 , C07C233/00 , C07K5/00 , C07K7/00
CPC分类号: C07K5/0227 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06147 , C07K5/06191 , C07K5/0806 , C07K5/0823 , C07K5/0827 , A61K38/00
摘要: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
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公开(公告)号:US5496927A
公开(公告)日:1996-03-05
申请号:US248847
申请日:1994-05-25
申请人: H. Michael Kolb , Joseph P. Burkhart , Michel J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
发明人: H. Michael Kolb , Joseph P. Burkhart , Michel J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
IPC分类号: A61K38/00 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07D498/10 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/08 , C07K5/083 , C07K5/097 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号: C07K5/0227 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06147 , C07K5/06191 , C07K5/0806 , C07K5/0823 , C07K5/0827 , A61K38/00
摘要: This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
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