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1. 发明申请

US20070191284A1 Compounds for enzyme inhibition 有权
公开(公告)号：US20070191284A1
公开(公告)日：2007-08-16
申请号：US11786217
申请日：2007-04-11
申请人： Mark Smyth , Guy Laidig , Ronald Borchardt , Barry Bunin , Craig Crews , John Musser
发明人： Mark Smyth , Guy Laidig , Ronald Borchardt , Barry Bunin , Craig Crews , John Musser
IPC分类号： A61K38/04 , C07K5/04
CPC分类号： C07K5/1016 , A61K38/00 , A61K38/07 , C07K5/0812 , C07K5/1008 , C07K5/1024
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

2. 发明申请

US20050245435A1 Compounds for enzyme inhibition 有权
标题翻译：用于酶抑制的化合物
公开(公告)号：US20050245435A1
公开(公告)日：2005-11-03
申请号：US11106879
申请日：2005-04-14
申请人： Mark Smyth , Guy Laidig , Ronald Borchardt , Barry Bunin , Craig Crews , John Musser , John Schneekloth , John Chabala
发明人： Mark Smyth , Guy Laidig , Ronald Borchardt , Barry Bunin , Craig Crews , John Musser , John Schneekloth , John Chabala
IPC分类号： A61K38/00 , A61K38/04 , C07K5/04 , C07K5/087
CPC分类号： C07K5/1016 , A61K38/00 , A61K38/07 , C07K5/0812 , C07K5/1008 , C07K5/1024
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。基于肽的化合物包括至少三个肽单元，环氧化物或氮丙啶，并且在N-末端官能化。除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

3. 发明申请

US20080090785A1 Compounds For Enzyme Inhibition 有权
标题翻译：化合物用于酶抑制
公开(公告)号：US20080090785A1
公开(公告)日：2008-04-17
申请号：US11596028
申请日：2005-05-09
申请人： Mark Smyth , Guy Laidig , Ronald Borchardt , Barry Bunin , Craig Crews , John Musser , Kevin Shenk , Peggy Radel
发明人： Mark Smyth , Guy Laidig , Ronald Borchardt , Barry Bunin , Craig Crews , John Musser , Kevin Shenk , Peggy Radel
IPC分类号： A61K31/665 , A61K31/336 , A61K31/381 , A61K31/4523 , A61K31/4535 , A61P25/00 , A61P31/18 , C07D241/14 , C07D303/36 , C07D409/14 , C07D409/12 , C07D403/12 , C07D401/12 , C07D325/00 , C07D265/30 , A61P35/00 , A61P29/00 , A61P21/00 , A61K31/496 , A61K31/497 , A61K31/5355
CPC分类号： C07K5/0812 , C07K5/06034 , C07K5/0827 , Y02A50/412
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsinlike activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.
摘要翻译：包括含杂原子的三元环的基于肽的化合物有效地选择性地抑制N末端亲核试剂（Ntn）水解酶的比活性。具有多种活性的那些Ntn的活性可被所描述的化合物差别地抑制。例如，本发明化合物可以选择性地抑制20S蛋白酶体的胰凝乳蛋白酶样活性。肽类化合物包括环氧化物或氮丙啶，并且在N-末端官能化。除了其他治疗用途之外，预期基于肽的化合物显示抗炎性质和抑制细胞增殖。

4. 发明申请

US20060281722A1 Compounds and uses thereof 审中-公开
标题翻译：化合物及其用途
公开(公告)号：US20060281722A1
公开(公告)日：2006-12-14
申请号：US11352846
申请日：2006-02-13
申请人： Michael Foley , Curtis Keith , Ronald Borchardt
发明人： Michael Foley , Curtis Keith , Ronald Borchardt
IPC分类号： A61K31/573 , A61K31/553 , A61K31/198
CPC分类号： C07D317/64 , C07C229/12 , C07C279/04 , C07C2603/32 , C07D267/16 , C07D267/20
摘要： The invention features charge-modified antidepressants and compounds conjugated to either a charged group or a bulky group in a manner that resists in vivo cleavage. The invention provides a method for treating a patient having an inflammatory disease by administering to the patient a compound of the invention.
摘要翻译：本发明的特征在于电荷修饰的抗抑郁剂和化合物以与抗体活化的方式结合的带电基团或大体积基团结合。本发明提供了通过向患者施用本发明化合物来治疗患有炎性疾病的患者的方法。

5. 发明申请

US20070176071A1 Container clip 审中-公开
标题翻译：集装箱夹
公开(公告)号：US20070176071A1
公开(公告)日：2007-08-02
申请号：US11343067
申请日：2006-01-30
申请人： Ronald Borchardt , Jeffrey Minnette , Clayton Robinson , Randall Julian
发明人： Ronald Borchardt , Jeffrey Minnette , Clayton Robinson , Randall Julian
IPC分类号： A47G1/10
CPC分类号： B65D71/50
摘要： The present invention is directed to a novel packaging clip for retaining a plurality of containers. The clip comprises a rectangular frame made of a resilient material and having length and width dimensions. The rectangular frame has a plurality of circular apertures having open mouths and two arms adjacent to and forming the open mouths. The number of arms is one more than the number of circular apertures. The circular apertures have inner diameters that are substantially equivalent to the diameters of the containers to be retained by the clip. The open mouths of the circular apertures are positioned along the length dimension of the frame so that the mouths open in only one direction. Additionally, the open mouths of the circular apertures are smaller than the inner diameter of the circular apertures and smaller than the diameter of the containers to be retained by the clip.
摘要翻译：本发明涉及一种用于保持多个容器的新颖的包装夹。夹子包括由弹性材料制成并具有长度和宽度尺寸的矩形框架。矩形框架具有多个具有开口的圆形孔和邻近并形成开口的两个臂。臂数比圆孔数多一个。圆形孔具有基本上等于待夹子保持的容器的直径的内径。圆形开孔的开放口沿着框架的长度尺寸定位，使得嘴仅沿一个方向打开。此外，圆形孔的开放口小于圆形孔的内径，并且小于由夹子保持的容器的直径。

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