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公开(公告)号:US20120101025A1
公开(公告)日:2012-04-26
申请号:US13341022
申请日:2011-12-30
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
IPC分类号: A61K38/06 , A61P17/06 , A61P11/08 , A61P11/00 , A61P31/18 , A61P25/28 , A61P25/00 , A61P9/10 , A61P25/02 , A61P25/16 , A61P31/04 , A61P33/00 , A61P31/12 , A61P21/00 , A61P35/00 , A61P27/02 , A61P9/04 , A61P17/00 , A61P37/00 , A61P37/06 , A61P19/02 , A61P1/00 , A61P31/00 , A61P13/12 , A61P1/16 , A61P11/06 , A61P37/08 , A61P1/18 , A61P29/00
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 chymotrypsin-like 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蛋白酶体的糜蛋白酶样活性。 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。
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公开(公告)号:US08088741B2
公开(公告)日:2012-01-03
申请号:US11596028
申请日:2005-05-09
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
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。
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公开(公告)号:US20120101026A1
公开(公告)日:2012-04-26
申请号:US13341056
申请日:2011-12-30
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , Kevin D. Shenk , Peggy A. Radel
IPC分类号: A61K38/06 , A61P31/18 , A61P11/00 , A61P17/06 , A61P25/28 , A61P21/00 , A61P35/00 , A61P27/02 , A61P37/00 , A61P37/06 , A61P11/06 , A61P19/02 , A61P9/10 , A61P9/04 , A61P9/00 , C07K5/083 , C12N9/99 , A61P25/16 , A61P31/00 , A61P13/12 , A61P37/08 , A61P31/12 , A61P1/18 , A61P1/16 , A61P29/00
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 chymotrypsin-like 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.
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公开(公告)号:US20120277146A1
公开(公告)日:2012-11-01
申请号:US13411044
申请日:2012-03-02
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
IPC分类号: A61K38/07 , A61P31/18 , A61P25/28 , A61P31/12 , A61P35/00 , A61P31/00 , A61P29/00 , A61P37/00 , C07K5/107 , A61P21/00
CPC分类号: C07K5/1016 , C07K5/0812 , C07K5/0827
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。
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公开(公告)号:US20120101050A1
公开(公告)日:2012-04-26
申请号:US13334372
申请日:2011-12-22
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
CPC分类号: C07K5/1016 , C07K5/0812 , C07K5/0827
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.
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公开(公告)号:US07232818B2
公开(公告)日:2007-06-19
申请号:US11106879
申请日:2005-04-14
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
IPC分类号: C07D413/12 , C07D405/12 , C07D303/36 , A61K31/5377 , A61K31/4025
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。
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公开(公告)号:US08324174B2
公开(公告)日:2012-12-04
申请号:US13334372
申请日:2011-12-22
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
CPC分类号: C07K5/1016 , C07K5/0812 , C07K5/0827
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.
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公开(公告)号:US08129346B2
公开(公告)日:2012-03-06
申请号:US11578626
申请日:2005-04-14
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
CPC分类号: C07K5/1016 , C07K5/0812 , C07K5/0827
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.
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公开(公告)号:US07491704B2
公开(公告)日:2009-02-17
申请号:US11786217
申请日:2007-04-11
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser
IPC分类号: A61K38/08
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。
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公开(公告)号:US20080200398A1
公开(公告)日:2008-08-21
申请号:US11578626
申请日:2005-04-14
申请人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , John S. Schneekloth Jr , John Clifford Chabala
发明人: Mark S. Smyth , Guy J. Laidig , Ronald T. Borchardt , Barry A. Bunin , Craig M. Crews , John H. Musser , John S. Schneekloth Jr , John Clifford Chabala
IPC分类号: A61K38/07 , C07K5/10 , A61P29/00 , A61P31/18 , A61P25/00 , A61P35/00 , A61P21/00 , A61P37/00
CPC分类号: C07K5/1016 , C07K5/0812 , C07K5/0827
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。
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