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1. 发明授权

US09205126B2 Compounds for enzyme inhibition 有权
公开(公告)号：US09205126B2
公开(公告)日：2015-12-08
申请号：US14038626
申请日：2013-09-26
申请人： Onyx Therapeutics, Inc.
发明人： Han-jie Zhou , Congcong M. Sun , Kevin D. Shenk , Guy J. Laidig
IPC分类号： A61K38/06 , A61K31/425 , A61K31/56 , A61K31/535 , A61K31/42 , A61K31/415 , A61K31/38 , A61K31/69 , A61K38/55 , C07K5/062 , C07K5/065 , C07K5/078 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/117 , A61K45/06 , 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.

2. 发明授权

US09051353B2 Crystalline tripeptide epoxy ketone protease inhibitors 有权
标题翻译：结晶三肽环氧酮蛋白酶抑制剂
公开(公告)号：US09051353B2
公开(公告)日：2015-06-09
申请号：US14035644
申请日：2013-09-24
申请人： Onyx Therapeutics, Inc.
发明人： Pasit Phiasivongsa , Louis C. Sehl
IPC分类号： A61K31/425 , C07D277/20 , C07K5/097 , C07D417/12
CPC分类号： C07K5/0802 , A61K31/427 , C07D417/12 , C07K1/026 , C07K5/0821 , Y02A50/409 , Y02A50/411 , Y02A50/491
摘要： The invention relates to crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.
摘要翻译：本发明涉及结晶三肽酮环氧化合物，其制备方法和相关的药物组合物。

3. 发明申请

US20140336106A1 TRIPEPTIDE EPOXY KETONE PROTEASE INHIBITORS 有权
标题翻译： TRIPEPTIDE环氧酮酮蛋白酶抑制剂
公开(公告)号：US20140336106A1
公开(公告)日：2014-11-13
申请号：US14210806
申请日：2014-03-14
申请人： Onyx Therapeutics, Inc.
发明人： Dustin McMinn , Henry Johnson , Simeon Bowers , David C. Moebius
IPC分类号： C07K5/083
CPC分类号： C07K5/0821 , A61K38/00 , A61K38/06 , C07D303/32 , C07D405/12 , C07D409/12 , C07K5/0202 , C07K5/0205 , C07K5/06026 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06113 , C07K5/06121 , C07K5/06139 , C07K5/06147 , C07K5/06173 , C07K5/06191 , C07K5/0806
摘要： Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.
摘要翻译：本文提供三肽环氧酮蛋白酶抑制剂，其制备方法，相关药物组合物及其使用方法。例如，本文提供了式（X）的化合物：及其药学上可接受的盐和包括其的组合物。本文提供的化合物和组合物可用于例如治疗包括炎症和神经变性疾病的疾病。

4. 发明申请

US20140080753A1 COMPOUNDS FOR ENZYME INHIBITION 审中-公开
标题翻译：用于酶抑制的化合物
公开(公告)号：US20140080753A1
公开(公告)日：2014-03-20
申请号：US14078378
申请日：2013-11-12
申请人： Onyx Therapeutics, Inc.
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： C07K5/08 , C07K5/06
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。

5. 发明申请

US20130041008A1 COMPOUNDS FOR ENZYME INHIBITION 有权
公开(公告)号：US20130041008A1
公开(公告)日：2013-02-14
申请号：US13646510
申请日：2012-10-05
申请人： Onyx therapeutics, Inc.
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： C07D303/36 , A61K31/4045 , A61K31/336 , A61P25/28 , A61P35/00 , A61P29/00 , A61P31/00 , C07D405/12 , C07D413/12
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.

6. 发明授权

US08324174B2 Compounds for enzyme inhibition 有权
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
IPC分类号： A61K38/06 , C07K5/10 , C07K1/00
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.

7. 发明授权

US08207124B2 Compounds for enzyme inhibition 有权
公开(公告)号：US08207124B2
公开(公告)日：2012-06-26
申请号：US13334263
申请日：2011-12-22
申请人： Mark S. Smyth , Guy J. Laidig
发明人： Mark S. Smyth , Guy J. Laidig
IPC分类号： A61K38/07 , C07K1/00 , C07K5/00
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.

8. 发明授权

US08198270B2 Compounds for proteasome enzyme inhibition 有权
标题翻译：蛋白酶体抑制的化合物
公开(公告)号：US08198270B2
公开(公告)日：2012-06-12
申请号：US11658983
申请日：2005-08-08
申请人： Mark S. Smyth , Guy J. Laidig
发明人： Mark S. Smyth , Guy J. Laidig
IPC分类号： A61K31/5377 , A61K31/4025
CPC分类号： C07K5/0812 , A61K31/4523 , A61K31/5377 , A61K38/00
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。

9. 发明申请

US20120101026A1 Compounds For Enzyme Inhibition 审中-公开
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.

10. 发明申请

US20120094928A1 COMPOUNDS FOR ENZYME INHIBITION 有权
公开(公告)号：US20120094928A1
公开(公告)日：2012-04-19
申请号：US13334263
申请日：2011-12-22
申请人： Mark S. Smyth , Guy J. Laidig
发明人： Mark S. Smyth , Guy J. Laidig
IPC分类号： A61K38/55 , A61P35/00 , C12N5/09
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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