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公开(公告)号：EP2484688A1
公开(公告)日：2012-08-08
申请号：EP11191554.2
申请日：2007-06-19
发明人： Shenk, Kevin D. , Parlati, Francesco , Zhou, Han-jie , Sylvain, Catherine , Smyth, Mark S. , Bennett, Mark K. , Laidig, Guy J.
IPC分类号： C07K5/068 , C07K5/072 , C07K5/078 , C07K5/062 , C07K5/065 , C07D303/32 , C07D405/12 , C07D409/12 , A61K38/05 , A61K31/336 , A61K31/404 , A61P35/00 , A61P37/00
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 of formula (I) 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：EP2970225B1
公开(公告)日：2018-08-15
申请号：EP14723553.5
申请日：2014-03-14
IPC分类号： C07D405/12 , A61K31/336 , A61K31/404 , C07D409/12 , C07D303/32 , A61P37/00
CPC分类号： C07K5/0806 , 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 , C07K5/0821
摘要： Provided herein are dipeptide and 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 proliferative diseases including cancer and autoimmune diseases.
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13.发明公开
公开(公告)号：EP3090737A1
公开(公告)日：2016-11-09
申请号：EP16171281.5
申请日：2009-10-21
IPC分类号： A61K31/167 , A61K31/165 , A61K31/45 , A61K31/573 , A61K38/08 , A61K38/04 , A61K38/55 , A61K45/06 , A61K38/06 , A61P35/00
CPC分类号： A61K38/07 , A61K31/165 , A61K31/167 , A61K31/198 , A61K31/335 , A61K31/337 , A61K31/45 , A61K31/454 , A61K31/573 , A61K31/704 , A61K45/06 , A61K2300/00
摘要： The invention provides combination therapy, wherein one or more other therapeutic agents are administered agents are administered with peptide epoxyketones or a pharmaceutically acceptable salt thereof. Another aspect of the invention relates to treating cancer with a peptide epoxyketone administered in combination with another therapeutic agent.
摘要翻译： 本发明提供组合疗法，其中一种或多种其它治疗剂是施用的药剂与肽环氧酮或其药学上可接受的盐一起施用。 本发明的另一方面涉及用另一种治疗剂组合施用的肽环氧酮治疗癌症。
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公开(公告)号：EP2484688B1
公开(公告)日：2016-06-08
申请号：EP11191554.2
申请日：2007-06-19
发明人： Shenk, Kevin D. , Parlati, Francesco , Zhou, Han-jie , Sylvain, Catherine , Smyth, Mark S. , Bennett, Mark K. , Laidig, Guy J.
IPC分类号： C07K5/068 , C07K5/072 , C07K5/078 , C07K5/062 , C07K5/065 , C07D303/32 , C07D405/12 , C07D409/12 , A61K38/05 , A61K31/336 , A61K31/404 , A61P35/00 , A61P37/00 , A61K38/00 , C07K5/083 , C07K5/087 , C07K5/103 , C07K5/093
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 of formula (I) 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式（I）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，其包括施用本发明的化合物。
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公开(公告)号：EP2869820A4
公开(公告)日：2016-02-17
申请号：EP13817628
申请日：2013-07-09
发明人： PHIASIVONGSA PASIT , LUEHR GARY , PENG GE , BY KOLBOT , ANIK SHABBIR T
IPC分类号： A61K47/48 , A61K31/452 , C07K5/103
CPC分类号： A61K47/549 , A61K38/06 , A61K38/07 , A61K47/48215 , A61K47/60 , C07K5/06078 , C07K5/0806 , C07K5/081 , C07K5/0821 , C07K5/1008 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K7/06
摘要： This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.
摘要翻译： 本公开的特征在于可用作环氧酮蛋白酶抑制剂的前药的化合物。
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公开(公告)号：EP2912025A1
公开(公告)日：2015-09-02
申请号：EP13849834.0
申请日：2013-10-24
发明人： JUMAA, Mouhannad , MUCHAMUEL, Tony , BEJUGAM, Naveen , WONG, Hansen , KIRK, Christopher J. , MANEK, Rahul Vishram , SHARMA, Sanjeev
IPC分类号： C07D277/00 , A61K38/06
CPC分类号： A61K9/0053 , A61K9/2013 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K38/05 , A61K38/06
摘要： This disclosure features modified release pharmaceutical formulations (e.g., extended release pharmaceutical formulations; e.g., solid dosage forms, e.g., tablets) that are useful for the oral administration of oprozomib, or a pharmaceutically acceptable salt thereof, to a human or animal subject as well as methods of making and using the formulations.
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公开(公告)号：EP2261236B1
公开(公告)日：2015-07-15
申请号：EP10179422.0
申请日：2005-12-07
CPC分类号： A61K31/336 , A61K9/0019 , A61K9/19 , A61K31/396 , A61K31/724 , A61K38/14 , A61K47/40 , C07K5/0812 , Y02A50/412 , A61K2300/00
摘要： Compositions comprising one or more practically insoluble proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin, substantially increase the solubility of these proteasome inhibitors and facilitate their administration. Such compositions optionally comprise a buffer. Methods of treatment using such compositions are also disclosed:
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18.发明公开
公开(公告)号：EP2555621A4
公开(公告)日：2014-07-02
申请号：EP11775425
申请日：2011-04-06
发明人： PHIASIVONGSA PASIT
IPC分类号： A01N43/20
CPC分类号： C07K5/0806
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公开(公告)号：EP2623113A3
公开(公告)日：2014-04-16
申请号：EP13157801.5
申请日：2006-11-09
IPC分类号： C07K5/062 , A61K38/55 , C07K5/08 , C07K5/10 , C07K5/065 , C07K5/078 , C07K5/083 , C07K5/087 , C07K5/097 , C07K5/117
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.
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公开(公告)号：EP2542238A1
公开(公告)日：2013-01-09
申请号：EP11715320.5
申请日：2011-03-01
IPC分类号： A61K31/4045 , A61K31/5375 , C07D209/20 , C07D295/104 , A61P37/00 , A61P35/00 , A61P29/00 , A61P31/00 , A61P25/00 , C07F5/04 , C07K5/065
CPC分类号： C07K5/0827 , C07D209/20 , C07D241/24 , C07D295/104 , C07D303/36 , C07D405/12
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相对于组成型蛋白酶体活性优先抑制免疫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，本发明涉及癌症的治疗，其包括施用本发明的化合物。
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