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公开(公告)号：US20100144649A1
公开(公告)日：2010-06-10
申请号：US12708932
申请日：2010-02-19
申请人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
IPC分类号： A61K38/06 , A61K38/05 , C07K5/08 , C07D413/12 , C07D417/12 , C07D303/38 , A61P31/00 , A61P35/00 , A61P29/00 , A61P25/00
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
摘要翻译： 本发明的一个方面涉及优先抑制免疫蛋白酶体活性超过组成型蛋白酶体活性的抑制剂。 在某些实施方案中，本发明涉及治疗免疫相关疾病，包括施用本发明的化合物。 在某些实施方案中，本发明涉及治疗癌症，包括施用本发明的化合物。
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公开(公告)号：US08080545B2
公开(公告)日：2011-12-20
申请号：US12708753
申请日：2010-02-19
申请人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
IPC分类号： A61K31/5377
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
摘要翻译： 本发明的一个方面涉及优先抑制免疫蛋白酶体活性超过组成型蛋白酶体活性的抑制剂。 在某些实施方案中，本发明涉及治疗免疫相关疾病，包括施用本发明的化合物。 在某些实施方案中，本发明涉及治疗癌症，包括施用本发明的化合物。
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公开(公告)号：US20120088762A1
公开(公告)日：2012-04-12
申请号：US13328909
申请日：2011-12-16
申请人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
IPC分类号： A61K31/5377 , A61K31/404 , C07D303/38 , A61K31/336 , C07D413/12 , C07D417/12 , A61K31/427 , A61P37/06 , A61P1/00 , A61P3/10 , A61P25/00 , A61P17/06 , A61P19/02 , A61P37/08 , A61P11/06 , A61P17/00 , A61P37/00 , A61P31/18 , A61P35/00 , A61P35/02 , A61P29/00 , A61P11/08 , A61P1/18 , A61P9/10 , A61P31/04 , A61P31/12 , A61P33/00 , A61P25/28 , A61P25/16 , C07D405/12
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
摘要翻译： 本发明的一个方面涉及优先抑制免疫蛋白酶体活性超过组成型蛋白酶体活性的抑制剂。 在某些实施方案中，本发明涉及治疗免疫相关疾病，包括施用本发明的化合物。 在某些实施方案中，本发明涉及治疗癌症，包括施用本发明的化合物。
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公开(公告)号：US08357683B2
公开(公告)日：2013-01-22
申请号：US13328909
申请日：2011-12-16
申请人： Kevin D. Shenk , Francesco Parlati , Han-jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
IPC分类号： A61K31/5377 , A61K31/427 , A61K31/404 , A61K31/336 , C07D413/12 , C07D417/12 , C07D405/12 , C07D303/38
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
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公开(公告)号：US08080576B2
公开(公告)日：2011-12-20
申请号：US12708932
申请日：2010-02-19
申请人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
IPC分类号： A61K31/404 , A61K31/381 , A61K31/336 , C07D209/04 , C07D333/52 , C07D303/02
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
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公开(公告)号：US20100144648A1
公开(公告)日：2010-06-10
申请号：US12708753
申请日：2010-02-19
申请人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
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公开(公告)号：US07691852B2
公开(公告)日：2010-04-06
申请号：US11820490
申请日：2007-06-19
申请人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
发明人： Kevin D. Shenk , Francesco Parlati , Han-Jie Zhou , Catherine Sylvain , Mark S. Smyth , Mark K. Bennett , Guy J. Laidig
IPC分类号： A61K31/5377 , C07D413/02
CPC分类号： C07K5/1016 , A61K38/00 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/06 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06113 , C07K5/08 , C07K5/0806 , C07K5/0808 , C07K5/0812 , C07K5/0819 , C07K5/0821 , C07K5/1008 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.
摘要翻译： 本发明的一个方面涉及优先抑制免疫蛋白酶体活性超过组成型蛋白酶体活性的抑制剂。 在某些实施方案中，本发明涉及治疗免疫相关疾病，包括施用本发明的化合物。 在某些实施方案中，本发明涉及治疗癌症，包括施用本发明的化合物。
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公开(公告)号：US08716322B2
公开(公告)日：2014-05-06
申请号：US12084838
申请日：2006-11-09
申请人： Han-Jie Zhou , Congcong M. Sun , Kevin D. Shenk , Guy J. Laidig
发明人： Han-Jie Zhou , Congcong M. Sun , Kevin D. Shenk , Guy J. Laidig
IPC分类号： A61K31/425 , A61K31/41 , A61K31/42 , A61K31/415 , A61K31/34 , A61K31/38 , A61K31/535 , A61K31/69 , A61K31/56
CPC分类号： C07K5/08 , A61K31/69 , A61K38/00 , A61K38/06 , A61K38/55 , A61K45/06 , C07K5/06026 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0821 , C07K5/1024 , A61K2300/00
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. 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. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
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和选择性地抑制与蛋白酶体相关的N-末端亲核试剂（Ntn）水解酶的特异性活性。 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。 这些基于肽的蛋白酶体抑制剂的口服给药是可能的，因为它们的生物利用度谱。
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公开(公告)号：US07687456B2
公开(公告)日：2010-03-30
申请号：US11595804
申请日：2006-11-09
申请人： Han-Jie Zhou , Congcong M. Sun , Kevin D. Shenk , Guy J. Laidig
发明人： Han-Jie Zhou , Congcong M. Sun , Kevin D. Shenk , Guy J. Laidig
IPC分类号： A61K38/00
CPC分类号： C07K5/08 , A61K31/69 , A61K38/00 , A61K38/06 , A61K38/55 , A61K45/06 , C07K5/06026 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/0806 , C07K5/0808 , C07K5/081 , C07K5/0812 , C07K5/0821 , C07K5/1024 , A61K2300/00
摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. 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. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
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和选择性地抑制与蛋白酶体相关的N-末端亲核试剂（Ntn）水解酶的特异性活性。 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。 这些基于肽的蛋白酶体抑制剂的口服给药是可能的，因为它们的生物利用度谱。
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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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