CAS: 1643913-93-2; (E)-3-(6-Aminopyridin-3-yl)-N-((5-(4-(4,4-Difluoropiperidine-1-Carbonyl)Phenyl)-7-(4-Fluorophenyl)Benzofuran-2-yl)Methyl)Acrylamide

📜3-(6-Aminopyridin-3-yl)Acrylic Acid,(4-(2-(Aminomethyl)-7-(4-Fluorophenyl)Benzofuran-5-yl)Phenyl)(4,4-Difluoropiperidin-1-yl)Methanone置于3-(6-Aminopyridin-3-yl)Acrylic Acid体系中,化学反应生成(2E)-3-(6-氨基-3-吡啶基)-N-[[5-[4-[(4,4-二氟-1-哌啶基)羰基]苯基]-7-(4-氟苯基)-2-苯并呋喃基]甲基]-2-丙烯酰胺
参考文献:Multicyclic Compounds And Uses Thereof
标题:Multicyclic Compounds And Uses Thereof
摘要:本发明涉及多环化合物,其含有脲或胍基团,或其药学上可接受的盐或组成物,其结构式表示为(ia),或其药学上可接受的盐,以及包含该多环化合物的药物组合物.本发明还涉及一种治疗癌症(例如淋巴瘤,如袍细胞淋巴瘤),神经退行性疾病,炎症性疾病或免疫系统疾病(例如t细胞介导的自身免疫疾病)的方法,该方法包括向需要治疗的受体中注射本发明化合物的治疗有效量,或其药学上可接受的盐,或包含本发明化合物的组合物,或其药学上可接受的盐.

专利信息

专利号:US-10363247-B2
优先权日:2015-08-18
标 题:(S,E)-3-(6-aminopyridin-3-yl)-N-((5-(4-(3-fluoro-3-methylpyrrolidine-1-carbonyl)phenyl-7-(4-fluorophenyl)benzofuran-2-yl)methyl)acrylamide for the treatment of cancer
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted benzofuranyl compounds and, more particularly, to a compound represented by Structural Formula 1a: (I) or a pharmaceutically acceptable salt thereof. The invention also includes the synthesis and use of the compound of Structural Formula 1a, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of diseases or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, an inflammatory diseases or an immune system disease (e.g., a T-Cell mediated autoimmune disease) in a subject in need thereof. The method comprises administering to a subject in need thereof a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof, or a composition comprising a compound of the invention, or a pharmaceutically acceptable salt thereof.

专利号:US-2021072244-A1
优先权日:2018-01-04
标 题:Methods and compositions for treating melanoma resistant
发明人：BERTOLOTTO CORINE; OHANNA MICKAËL; BALLOTTI ROBERT
权利人:INST NAT SANTE RECH MED; UNIV COTE D'AZUR
摘要:The present invention relates to a method for treating a subject suffering from melanoma resistant by administering to said subject an inhibitor of NAMPT. Using a global metabolic profiling, inventors have showed that in addition to glycolysis, the BRAF inhibitor, PLX4032, promoted a complex metabolic rewiring of melanoma cells, including protein catabolism and fatty acid synthesis. Importantly, they observed that PLX4032 reduced the levels of nicotinamide adenine dinucleotide (NAD+), an important redox co-factor in numerous metabolic processes, including glycolysis, tricarboxylic acid cycle (TCA) cycle, glutamate metabolism and fatty acid betaoxidation. Pharmacological or genetic inhibition of NAMPT impaired melanoma cell growth, whereas the overexpression of NAMPT dampened the antiproliferative effect of PLX4032. In vivo, the inhibition of NAMPT also prevented the xenograft development of PLX4032-sensitive and -resistant melanoma cells, identifying NAMPT as a potential target for BRAFi-resistant melanomas.

专利号:US-9856241-B2
优先权日:2013-07-03
标 题:Substituted benzofuranyl and benzoxazolyl compounds and uses thereof
发明人：BALOGLU ERKAN; SHACHAM SHARON; SENAPEDIS WILLIAM; MCCAULEY DILARA; LANDESMAN YOSEF; GOLAN GALI; KALID ORI; SHECHTER SHARON
权利人:KARYOPHARM THERAPEUTICS INC
摘要:The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.