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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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公开(公告)号：EP3341007A1
公开(公告)日：2018-07-04
申请号：EP16842694.8
申请日：2016-08-26
申请人： Cornell University , Dana-Farber Cancer Institute, Inc. , Children's Medical Center Corporation
发明人： GRAY, Nathanael, S. , MELNICK, Ari, M. , WU, Hao , SCOTT, David, A. , HATCHER, John , CHENNAMADHAVUNI, Spandan , GABAS, Lorena, Fontan , QIAO, Qi , DU, Guangyan
CPC分类号： C07K5/1019 , A61K38/00 , A61K38/07 , A61K45/06 , A61P35/02 , C07K5/04 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06139 , C07K5/08 , C07K5/101
摘要： Provided herein are compounds of Formula (I) and pharmaceutical compositions thereof, which may be useful as MALT1 inhibitors. Also provided are for the treatment of proliferative disorders (e.g., cancer (e.g., non-Hodgkin' s lymphoma, diffuse large B-cell lymphoma, MALT lymphoma), benign neoplasm, a disease associated with angiogenesis,an autoimmune disease, an inflammatory disease, an autoinflammatory disease) by administering a compound of Formula (I).
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公开(公告)号：EP2859009B1
公开(公告)日：2017-10-18
申请号：EP13730439.0
申请日：2013-06-07
发明人： ACIRO, Caroline , STEADMAN, Victoria Alexandra , PETTIT, Simon Neil , POULLENNEC, Karine G. , LAZARIDES, Linos , DEAN, David Kenneth , DUNBAR, Neil Andrew , HIGHTON, Adrian John , KEATS, Andrew John , SIEGEL, Dustin Scott , KARKI, Kapil Kumar , SCHRIER, Adam James , JANSA, Petr , MACKMAN, Richard
IPC分类号： C07K5/062 , C07D487/08 , C07D498/08 , C07D498/18 , A61P31/14
CPC分类号： C07K5/06034 , A61K31/403 , A61K31/497 , A61K31/504 , A61K31/7056 , A61K31/7072 , A61K38/00 , A61K38/05 , A61K38/12 , A61K38/15 , A61K38/21 , A61K38/55 , A61K39/29 , A61K45/06 , C07D471/18 , C07D487/08 , C07D498/08 , C07D498/18 , C07D498/22 , C07K5/02 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06191 , C07K19/00 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/391 , Y02A50/395 , A61K2300/00
摘要： Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
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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：EP2771020A4
公开(公告)日：2015-11-11
申请号：EP12842936
申请日：2012-10-31
申请人： YU RUEY J , SCOTT EUGENE J VAN
发明人： YU RUEY J , VAN SCOTT EUGENE J
CPC分类号： A61K8/64 , A61K9/0014 , A61K38/05 , A61K2800/10 , A61K2800/92 , A61Q5/00 , A61Q19/00 , A61Q19/007 , A61Q19/008 , A61Q19/02 , A61Q19/06 , A61Q19/08 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06113 , C07K5/06147 , C07K5/06156 , C07K5/06165 , C07K5/06191
摘要： N-acyldipeptide derivatives are described. Compositions comprising the N-acyldipeptide derivatives are therapeutically effective for topical or systemic administration to alleviate or improve conditions, disorders, diseases, symptoms or syndromes associated with a tumor, cancer, immune, nervous, vascular, musculoskeletal or cutaneous system, or other tissue or system in a subject.
摘要翻译： 描述了通过局部给予N-酰基二肽衍生物来治疗老化相关皮肤变化和增加皮肤厚度的方法。 包含N-酰基二肽衍生物的组合物对于增加皮肤厚度以及用于治疗外在和内在老化和衰老相关的皮肤变化（例如细纹，皱纹，光老化，色素沉着过度，松弛，老年斑，斑点，斑驳皮肤和 橘皮组织。
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公开(公告)号：EP2906582A1
公开(公告)日：2015-08-19
申请号：EP13774418.1
申请日：2013-10-09
CPC分类号： C07K5/123 , A61K38/00 , C07K5/06026 , C07K5/0606 , C07K5/06078
摘要： The invention is concerned with the compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein X, Y, Z, R
1 , R
2 , R
3 and R
3 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease.摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中X，Y，Z，R 1，R 2，R 3和R 3在具体实施方式和权利要求书中定义。 另外，本发明涉及制备和使用式I化合物的方法以及含有这些化合物的药物组合物。 式I化合物是LMP7抑制剂，并且可用于治疗相关的炎症性疾病和病症，例如类风湿性关节炎，狼疮和肠易激惹起的疾病。
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7.发明公开Methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid 审中-公开用于递送3-氨基-1-Propanesulfonsäure的方法，化合物，组合物和媒体
公开(公告)号：EP2862581A3
公开(公告)日：2015-08-12
申请号：EP14200552.9
申请日：2007-10-12
发明人： Kong, Xianqi , Atfani, Mohamed , Bachand, Benoit , Bouzide, Abderrahim , Ciblat, Stephane , Levesque, Sophie , Migneault, David , Valade, Isabelle , Wu, Xinfu , Delorme, Daniel
IPC分类号： A61K47/48 , C07K5/06 , C07K5/08 , C07C309/15 , C07D207/16 , C07D209/20 , C07D217/24 , C07D233/64 , C07D291/02 , C07D333/24 , C12P11/00 , A61K38/07 , A61K38/08 , A61P25/28
CPC分类号： A61K31/145 , A61K47/54 , A61K47/542 , A61K47/545 , A61K47/549 , A61K47/554 , A61K47/64 , C07C309/15 , C07C309/18 , C07C309/19 , C07C309/24 , C07D207/16 , C07D209/20 , C07D217/24 , C07D233/64 , C07D285/36 , C07D285/38 , C07D291/02 , C07D323/02 , C07D333/24 , C07H7/02 , C07H15/12 , C07J9/005 , C07K5/06026 , C07K5/06052 , C07K5/0606 , C07K5/06069 , C07K5/06086 , C07K5/0806 , C07K5/081 , C12P11/00 , C12P13/001 , Y02P20/55
摘要： The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1 -propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compounds that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to, the prevention and treatment of Alzheimer's disease.
摘要翻译： 本发明涉及的方法，化合物，组合物和车辆用于递送3-氨基-1-丙受试者中的酸（3APS），优选人受试者。 本发明包括thatwill产生或产生3APS，无论是在体外或体内的化合物。 优选的化合物包括使用3APS的氨基酸前药，包括但不限于，阿尔茨海默氏病的预防和治疗。
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8.发明授权NEW CATHEPSIN S PROTEASE INHIBITORS, USEFUL IN THE TREATMENT OF E.G. AUTOIMMUNE DISORDERS, ALLERGY AND CHRONIC PAIN CONDITIONS 有权新的组织蛋白酶S蛋白酶抑制剂来治疗例如 自身免疫性疾病，过敏和慢性疼痛
公开(公告)号：EP2582660B1
公开(公告)日：2015-07-22
申请号：EP11795278.8
申请日：2011-06-16
申请人： Medivir UK Ltd
发明人： AYESA, Susana , GRABOWSKA,Urszula , HEWITT, Ellen , JÖNSSON, Daniel , KLASSON, Björn , KAHNBERG, Pia , LUNDGREN, Stina , TEJBRANT, Jan , WIKTELIUS, Daniel
IPC分类号： C07C237/14 , A61K31/16 , A61P11/00 , A61P37/00 , C07D233/58
CPC分类号： C07D233/61 , A61K38/55 , C07C231/12 , C07C235/80 , C07C237/22 , C07C271/22 , C07C275/18 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D213/81 , C07D233/60 , C07D277/56 , C07D305/08 , C07K5/06034 , C07K5/0606 , C07K5/06078 , C07K5/06139
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公开(公告)号：EP2736890A4
公开(公告)日：2015-07-15
申请号：EP12817817
申请日：2012-07-30
发明人： LAWTON DANIEL , NEARY MICHAEL , NIEMAN JAMES A
IPC分类号： C07D277/14 , A61K31/426 , A61P25/00
CPC分类号： A61K31/426 , A61K31/198 , A61K45/06 , C07D241/08 , C07D267/10 , C07D277/14 , C07K5/0606
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10.发明公开
公开(公告)号：EP2859009A1
公开(公告)日：2015-04-15
申请号：EP13730439.0
申请日：2013-06-07
申请人： Gilead Sciences, Inc. , Selcia Ltd
发明人： ACIRO, Caroline , STEADMAN, Victoria Alexandra , PETTIT, Simon Neil , POULLENNEC, Karine G. , LAZARIDES, Linos , DEAN, David Kenneth , DUNBAR, Neil Andrew , HIGHTON, Adrian John , KEATS, Andrew John , SIEGEL, Dustin Scott , KARKI, Kapil Kumar , SCHRIER, Adam James , JANSA, Petr , MACKMAN, Richard
IPC分类号： C07K5/062 , C07D487/08 , C07D498/08 , C07D498/18 , A61P31/14
CPC分类号： C07K5/06034 , A61K31/403 , A61K31/497 , A61K31/504 , A61K31/7056 , A61K31/7072 , A61K38/00 , A61K38/05 , A61K38/12 , A61K38/15 , A61K38/21 , A61K38/55 , A61K39/29 , A61K45/06 , C07D471/18 , C07D487/08 , C07D498/08 , C07D498/18 , C07D498/22 , C07K5/02 , C07K5/06052 , C07K5/0606 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06191 , C07K19/00 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/391 , Y02A50/395 , A61K2300/00
摘要： Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
摘要翻译： 提供式I的化合物及其药学上可接受的盐和酯。 提供的化合物，组合物和方法可用于治疗病毒感染，特别是丙型肝炎感染。
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