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公开(公告)号：EP4424677A1
公开(公告)日：2024-09-04
申请号：EP23159988.7
申请日：2023-03-03
申请人： RDP Pharma AG
发明人： CHANG, Cheng-Hao , WANG, Yu Fa , MARTI, Roger , MYLÈNE, Soudani , CRISP, Antony
IPC分类号： C07D303/32 , C07F9/113 , C07C43/315 , C07F9/10
CPC分类号： C07F9/10 , C07B2200/0720130101 , C07F9/113 , C07D303/32 , C07C43/315
摘要： The present invention relates to an improved method for the synthesis of (S) or (R)-edelfosine ((S) or (R)-CP201).
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公开(公告)号：EP4041747A1
公开(公告)日：2022-08-17
申请号：EP20874053.0
申请日：2020-10-09
IPC分类号： C07K5/08 , C07K7/06 , C07D303/32
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公开(公告)号：EP3613732A1
公开(公告)日：2020-02-26
申请号：EP19193077.5
申请日：2019-08-22
IPC分类号： C07D301/14 , C07D303/32
摘要： The object of the present invention is to provide an industrial and economical process for preparing (E2)-cis-6,7-epoxy-2-nonenal of the following formula (3):
The present invention provides a process for preparing (E2)-cis-6,7-epoxy-2-nonenal (3), comprising at least steps of:
subjecting (Z3,Z6)-3,6-nonadien-1-ol of the following formula (1) to oxidation:
to form (E2,Z6)-2,6-nonadienal of the following formula (2); and
epoxidizing the resulting (E2,Z6)-2,6-nonadienal to form the aforesaid (E2)-cis-6,7-epoxy-2-nonenal (3).-
公开(公告)号：EP3166933B1
公开(公告)日：2018-08-01
申请号：EP15821964.2
申请日：2015-07-14
IPC分类号： C07D303/32 , C07D413/14 , C07D413/12 , A61K31/336 , A61K31/5377 , A61P35/00 , A61P25/28 , C07K5/083 , C07K5/087 , C07K5/065
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0202 , C07K5/0806 , C07K5/0821
摘要： The present disclosure relates to novel compounds and pharmaceutical compositions thereof which are useful as inhibitors of proteasomes. The compounds provided herein have improved proteasome potency and selectivity, and increased aqueous solubility, and are useful in treating various conditions or diseases associated with proteasomes.
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5.发明授权5-[(3,3,3-Trifluoro-2-hydroxy-1-arylpropyl)amino]-1H-quinolin-2-ones, process for their production and their use as anti-inflammatory agents 有权5 - [（3,3,3-三氟-2-羟基-1-芳基丙基） - 氨基] -1H-喹啉-2-酮，它们的制备方法和它们作为抗炎剂
公开(公告)号：EP2234979B1
公开(公告)日：2016-05-25
申请号：EP08852223.0
申请日：2008-11-08
发明人： BERGER, Markus , REHWINKEL, Hartmut , ZOLLNER, Thomas , MAY, Ekkehard , HASSFELD, Jorma , SCHÄCKE, Heike
IPC分类号： C07D215/38 , C07D303/32 , C07D405/12 , C07C49/233 , A61K31/4704 , A61P29/00
CPC分类号： C07D215/38 , C07C45/00 , C07C45/58 , C07C45/71 , C07C49/82 , C07C49/84 , C07D303/32 , C07D405/12 , C07C47/575 , C07C47/565
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6.发明公开PROCESS FOR PREPARING CIS-5-[1-(4-CHLOROPHENYL)-METHYLENE]-1-HYDROXYMETHYL-2,2-DIMETHYLCYCLOPENTANOL 审中-公开VERFAHREN ZUR HERSTELLUNG VON CIS-5- [1-（4-氯苯基）甲基] -1-羟基甲基-2,2-二甲基环戊烷
公开(公告)号：EP2812299A1
公开(公告)日：2014-12-17
申请号：EP13702814.8
申请日：2013-02-07
发明人： ZIERKE, Thomas , KEMPER, Paul
IPC分类号： C07C29/132 , C07C29/14 , C07C33/50 , C07C35/50 , C07C45/58 , C07C47/457 , C07D249/08 , C07D301/02 , C07D301/12 , C07D301/19 , C07D303/32
CPC分类号： C07C29/132 , C07C29/14 , C07C45/58 , C07C2601/08 , C07C2601/10 , C07D249/08 , C07D301/02 , C07D301/12 , C07D301/19 , C07D303/32 , C07D405/06 , C07C35/50 , C07C49/457
摘要： The present invention relates to a process for preparing a diol of the formulae (la) (lb), or a mixture thereof, comprising the reaction of an epoxy alcohol of formulae (Va) or (Vb), or a mixture thereof, with alkali metal borohydride or earth alkaline borohydride, in particular sodium borohydride, and anhydrous aluminum(lll) chloride. The invention also relates to processes and intermediates for preparing an epoxy alcohol of formulae (Va) or (Vb). The invention furthermore relates to processes for preparing cis-metconazole in which a diol of the formulae (la) or (lb) is applied as a precursor.
摘要翻译： 本发明涉及一种制备式（Ia）或（Ib）的二醇或其混合物的方法，其包括式（Va）或（Vb）的环氧醇或其混合物与其混合物与 碱金属硼氢化物或碱土硼氢化物，特别是硼氢化钠，和无水氯化铝（III）。 本发明还涉及制备式（Va）或（Vb）的环氧醇的方法和中间体。 本发明还涉及其中应用式（Ia）或（Ib）的二醇作为前体的制备顺式 - 异康唑的方法。
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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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8.发明公开5-Ý(3,3,3-TRIFLUORO-2-HYDROXY-1-ARYLPROPYL)AMINO¨-1H-QUINOLIN-2-ONES, A PROCESS FOR THEIR PRODUCTION AND THEIR USE AS ANTI-INFLAMMATORY AGENTS 有权5 - [（3,3,3-三氟-2-羟基-1-芳基丙基） - 氨基] -1H-喹啉-2-酮，它们的制备方法和它们作为抗炎剂
公开(公告)号：EP2234979A1
公开(公告)日：2010-10-06
申请号：EP08852223.0
申请日：2008-11-08
发明人： BERGER, Markus , REHWINKEL, Hartmut , ZOLLNER, Thomas , MAY, Ekkehard , HASSFELD, Jorma , SCHÄCKE, Heike
IPC分类号： C07D215/38 , C07D303/32 , C07D405/12 , C07C49/233 , A61K31/4704 , A61P29/00
CPC分类号： C07D215/38 , C07C45/00 , C07C45/58 , C07C45/71 , C07C49/82 , C07C49/84 , C07D303/32 , C07D405/12 , C07C47/575 , C07C47/565
摘要： The present invention relates to compounds of formula (I), processes for their production and their use as anti-inflammatory agents.
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9.发明授权Triptolide analogs for the treatment of autoimmune and inflammatory disorders 有权雷公藤甲素类似物用于自身免疫性疾病和起重机的炎症的治疗
公开(公告)号：EP1659125B1
公开(公告)日：2010-06-02
申请号：EP05077239.1
申请日：2001-10-02
申请人： Emory University
IPC分类号： C07D493/10 , C07D493/20 , C07C39/04 , C07D303/32 , A61P29/00 , A61K31/336
CPC分类号： C07D303/04 , C07C37/002 , C07C45/46 , C07C2601/14 , C07D303/14 , C07D303/32 , C07D493/10 , C07C47/565 , C07C39/11 , C07C39/17
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公开(公告)号：EP2041158A2
公开(公告)日：2009-04-01
申请号：EP07809745.8
申请日：2007-06-19
申请人： Proteolix, Inc.
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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