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公开(公告)号：US20170260230A1
公开(公告)日：2017-09-14
申请号：US15606076
申请日：2017-05-26
发明人： Han-Jie Zhou , Congcong M. Sun , Kevin D. Shenk , Guy J. Laidig
IPC分类号： C07K5/08 , C07K5/062 , C07K5/065 , C07K5/078 , A61K38/06 , C07K5/087 , C07K5/097 , C07K5/117 , A61K31/69 , A61K38/55 , C07K5/083
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：US20160213610A1
公开(公告)日：2016-07-28
申请号：US15008634
申请日：2016-01-28
发明人： Mouhannad Jumaa , Tony Muchamuel , Naveen Bejugam , Hansen Wong , Christopher J. Kirk , Rahul Vishram Manek , Sanjeev Sharma
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.
摘要翻译： 该公开内容特征在于可用于将人类或动物受试者口服阿曲单核苷或其药学上可接受的盐的改良释放药物制剂（例如，延长释放药物制剂，例如固体剂型，例如片剂） 作为制备和使用制剂的方法。
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公开(公告)号：US09205126B2
公开(公告)日：2015-12-08
申请号：US14038626
申请日：2013-09-26
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.
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公开(公告)号：US20150209282A1
公开(公告)日：2015-07-30
申请号：US14414568
申请日：2013-07-17
发明人： Katherine A. Chu , Elena T. Chan , Ying Fang , Mouhannad Jamaa , Christopher Justin Kirk , Tony Muchamuel , Zhengping Wang , Jing Jiang , Jeffrey Joseph Jones
CPC分类号： A61K9/127 , A61K9/1271 , A61K9/1277 , A61K38/07 , A61K45/06 , A61K47/22 , A61K47/6951
摘要： Liposomal compositions comprising peptide epoxyketone compounds are described, as well as methods of making and using such liposomal compositions. These liposomal compositions enhance the therapeutic window of peptide epoxyketone compounds by improving in vivo half-life relative to non-liposomal compositions comprising peptide epoxyketone compounds, providing desirable pharmacodynamic profiles, and providing anti-tumor activity in a human tumor xenograft model, greater than or equal to non-liposomal compositions comprising peptide epoxyketone compounds. Further, experiments performed in support of the present invention demonstrated improved tolerability of liposomal compositions comprising peptide epoxyketone compounds.
摘要翻译： 描述了包含肽环氧酮化合物的脂质体组合物，以及制备和使用这些脂质体组合物的方法。 这些脂质体组合物通过相对于包含肽环氧酮化合物的非脂质体组合物提供体内半衰期来提高肽环氧酮化合物的治疗窗口，提供所需的药效学特征，并在人肿瘤异种移植模型中提供抗肿瘤活性，大于或 等于包含肽环氧酮化合物的非脂质体组合物。 此外，支持本发明的实验证明了包含肽环氧酮化合物的脂质体组合物的耐受性得到改善。
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公开(公告)号：US20150175656A1
公开(公告)日：2015-06-25
申请号：US14639603
申请日：2015-03-05
发明人： Phiasivongsa Pasit , Louis C. Sehl
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。
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公开(公告)号：US09051353B2
公开(公告)日：2015-06-09
申请号：US14035644
申请日：2013-09-24
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。
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公开(公告)号：US20140336106A1
公开(公告)日：2014-11-13
申请号：US14210806
申请日：2014-03-14
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。
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公开(公告)号：US20140105921A1
公开(公告)日：2014-04-17
申请号：US13938075
申请日：2013-07-09
发明人： Pasit Phiasivongsa , Gary Luehr , Ge Peng , Kolbot By , Shabbir T. Anik
CPC分类号： C07K5/08 , A61K38/06 , A61K38/07 , A61K47/549 , A61K47/60 , A61K47/64 , A61K47/6889 , C07K5/06078 , C07K5/0806 , C07K5/081 , C07K5/0821 , C07K5/10 , 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：US20140080753A1
公开(公告)日：2014-03-20
申请号：US14078378
申请日：2013-11-12
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.
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：US20130041008A1
公开(公告)日：2013-02-14
申请号：US13646510
申请日：2012-10-05
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.
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