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公开(公告)号：EP2880015A1
公开(公告)日：2015-06-10
申请号：EP13755978.7
申请日：2013-08-01
申请人： Fondazione Istituto Italiano Di Tecnologia , The Regents of the University of California , Alma Mater Studiorum -Universita' di Bologna
发明人： DE VIVO, Marco , SCARPELLI, Rita , CAVALLI, Andrea , MIGLIORE, Marco , PIOMELLI, Daniele , HABRANT, Damien , FAVIA, Angelo
IPC分类号： C07C271/28 , C07C271/42 , C07C271/44 , C07C271/56 , C07C271/58 , A61K31/325 , A61P35/00
CPC分类号： C07C271/56 , C07C271/28 , C07C271/44 , C07C271/58 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The invention provides novel multitarget inhibitors of the enzymes Fatty Acid Amide Hydrolase (FAAH), Cyclooxygenase-1 (COX-1) and/or Cyclooxygenase-2 (COX-2) having a specific carbamate moiety on the meta or ortho position of the A ring of a substituted biphenyl core and having an halogen in the ortho position of the B ring of the biphenyl core. The invention concerns also with therapeutical application of the multitarget inhibitors in particular in the prevention and treatment of cancer.
摘要翻译： 脂肪酸酰胺水解酶（FAAH），环氧合酶-1（COX-1）和/或环氧合酶-2（COX-2）的多靶抑制剂在取代的A环的间位或邻位上具有特定的氨基甲酸酯部分 联苯核心，在联苯核心的B环的邻位具有卤素。 还涉及多靶抑制剂的治疗应用，特别是预防和治疗癌症。
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2.发明授权
公开(公告)号：EP2880015B1
公开(公告)日：2017-09-27
申请号：EP13755978.7
申请日：2013-08-01
申请人： Fondazione Istituto Italiano Di Tecnologia , The Regents of the University of California , Alma Mater Studiorum -Università di Bologna
发明人： DE VIVO, Marco , SCARPELLI, Rita , CAVALLI, Andrea , MIGLIORE, Marco , PIOMELLI, Daniele , HABRANT, Damien , FAVIA, Angelo
IPC分类号： C07C271/28 , C07C271/42 , C07C271/44 , C07C271/56 , C07C271/58 , A61K31/325 , A61P35/00
CPC分类号： C07C271/56 , C07C271/28 , C07C271/44 , C07C271/58 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
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3.发明公开SUBSTITUTED BENZOXAZOLONE DERIVATIVES AS ACID CERAMIDASE INHIBITORS, AND THEIR USE AS MEDICAMENTS 有权AS苯并恶唑酮的酸性神经酰胺酶抑制剂取代衍生物及其作为药物
公开(公告)号：EP3143009A1
公开(公告)日：2017-03-22
申请号：EP15727567.8
申请日：2015-05-11
申请人： Fondazione Istituto Italiano di Tecnologia , The Regents of the University of California , Università degli Studi di Parma
发明人： PIOMELLI, Daniele , PIZZIRANI, Daniela , BACH, Anders , SCARPELLI, Rita , MELZIG, Laurin , MOR, Marco
IPC分类号： C07D263/58 , A61K31/423 , A61P35/00
摘要： The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases.
摘要翻译： 本发明涉及substituiertem benzoxazolones衍生物作为酸性神经酰胺酶抑制剂，含合成抑制剂和酸抑制神经酰胺的方法在神经酰胺水平的哪个调制病症的治疗的药物组合物是临床相关的。 因此本发明提供substituiertem benzoxazolones衍生物用于癌症，炎症，疼痛，炎性疼痛或肺疾病的治疗用途。
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4.发明公开INHIBITORS OF FATTY ACID AMIDE HYDROLASE (FAAH) ENZYME WITH IMPROVED ORAL BIOAVAILABILITY AND THEIR USE AS MEDICAMENTS 审中-公开酶学脂肪酸酰胺水解酶（FAAH）具有改进的口服生物利用度的抑制剂，它们作为药物
公开(公告)号：EP3129354A1
公开(公告)日：2017-02-15
申请号：EP15776702.1
申请日：2015-04-07
IPC分类号： C07C317/44
CPC分类号： C07C271/56 , C07C311/29 , C07C317/22 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： Described herein, inter alia, are compositions and methods useful for inhibiting fatty acid amide hydrolase.
摘要翻译： 描述中，除其他外，组合物和用于抑制脂肪酸酰胺水解酶有用的方法。
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公开(公告)号：EP2875006A1
公开(公告)日：2015-05-27
申请号：EP13739362.5
申请日：2013-05-27
申请人： Fondazione Istituto Italiano Di Tecnologia , The Regents of the University of California , Università degli Studi di Parma
发明人： PIOMELLI, Daniele , REALINI, Natalia , MOR, Marco , PAGLIUCA, Chiara , PIZZIRANI, Daniela , SCARPELLI, Rita , BANDIERA, Tiziano
IPC分类号： C07D239/54 , C07D239/557 , C07D239/553 , C07D239/545
CPC分类号： C07D239/54 , A61K31/513 , A61K31/5377 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D401/04 , C07D403/04
摘要： The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.
摘要翻译： 本发明在第一方面涉及本文定义的式I化合物，其药学上可接受的盐和含有这些化合物的药物组合物。 本发明还涉及用作酸性神经酰胺酶抑制剂的式I化合物，以及用于治疗其中神经酰胺水平的调节在临床上相关的癌症和其它疾病。
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7.发明公开
公开(公告)号：EP3988540A1
公开(公告)日：2022-04-27
申请号：EP21212118.0
申请日：2015-04-07
IPC分类号： C07C317/44 , A61K31/325 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36
摘要： Described herein, inter alia, are compositions and methods useful for inhibiting fatty acid amide hydrolase.
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公开(公告)号：EP2875006B1
公开(公告)日：2018-12-26
申请号：EP13739362.5
申请日：2013-05-27
申请人： Fondazione Istituto Italiano di Tecnologia , The Regents of the University of California , Università degli Studi di Parma
发明人： PIOMELLI, Daniele , REALINI, Natalia , MOR, Marco , PAGLIUCA, Chiara , PIZZIRANI, Daniela , SCARPELLI, Rita , BANDIERA, Tiziano
IPC分类号： C07D239/54 , C07D239/557 , C07D239/553 , C07D239/545 , A61K31/513 , A61K31/5377 , A61P35/00
CPC分类号： C07D239/54 , A61K31/513 , A61K31/5377 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D239/545 , C07D239/553 , C07D239/557 , C07D239/60 , C07D401/04 , C07D403/04
摘要： The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.
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9.发明公开
公开(公告)号：EP4031535A1
公开(公告)日：2022-07-27
申请号：EP20789304.1
申请日：2020-09-17
IPC分类号： C07D263/08 , C07D413/04 , C07D451/02 , C07D471/10 , C07D487/04 , C07D487/08 , C07D491/107 , A61P25/00 , A61P25/16 , A61P35/00 , A61P29/00
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10.发明授权DUAL INHIBITOR COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISORDERS AND ALZHEIMER'S DISEASE 有权双重抑制剂化合物用于治疗神经退行性疾病和阿尔茨海默病
公开(公告)号：EP3154953B1
公开(公告)日：2018-04-04
申请号：EP15731721.5
申请日：2015-06-12
发明人： CAVALLI, Andrea , PRATI, Federica , BOTTEGONI, Giovanni , FAVIA, Angelo Danilo , PIZZIRANI, Daniela , SCARPELLI, Rita , BOLOGNESI, Maria Laura
IPC分类号： C07D251/10 , A61K31/53
CPC分类号： C07D251/10 , A61K31/53 , A61K45/06 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The present invention relates to Compounds of Formula (I) and pharmaceutical compositions containing the same. It further relates to their use in the prevention or treatment of central nervous system diseases or disorders, in particular, cognitive, neurodegenerative or neuronal diseases or disorders.
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