- Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment
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To address the multifactorial nature of Alzheimer's Disease (AD), a multi-target-directed ligand approach was herein developed. As a follow-up of our previous studies, a small library of newly designed 2-arylbenzofuran derivatives was evaluated towards ch
- Montanari, Serena,Mahmoud, Ali Mokhtar,Pruccoli, Letizia,Rabbito, Alessandro,Naldi, Marina,Petralla, Sabrina,Moraleda, Ignacio,Bartolini, Manuela,Monti, Barbara,Iriepa, Isabel,Belluti, Federica,Gobbi, Silvia,Di Marzo, Vincenzo,Bisi, Alessandra,Tarozzi, Andrea,Ligresti, Alessia,Rampa, Angela
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p. 243 - 258
(2019/06/14)
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- Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator
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Estrogen receptors (ERs) play a major role in the growth of human breast cancer cells. A selective estrogen receptor down-regulator (SERD) that acts as not only an inhibitor of ligand binding, but also induces the down-regulation of ER, would be useful fo
- Shoda, Takuji,Kato, Masashi,Fujisato, Takuma,Misawa, Takashi,Demizu, Yosuke,Inoue, Hideshi,Naito, Mikihiko,Kurihara, Masaaki
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p. 2914 - 2919
(2016/06/13)
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- MONOCYCLIC PYRIDINE DERIVATIVE
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The present invention provides a novel compound having FGFR inhibitory activity or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same. Specifically, the present invention provides a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein n represents 0 to 2; A represents an arylene group or a heteroarylene group; G represents a single bond, an oxygen atom or —CH2—; E represents a nitrogen-containing non-aromatic heterocycle; R1 represents an alkoxy group or the like; R2 represents a hydrogen atom or the like; and R3 represents a hydrogen atom, an alkyl group, an alkoxy group or the like, with the proviso that when E represents an azetidine ring and R2 or R3 is present on a nitrogen atom on the azetidine ring, the R2 or R3 does not represent a hydrogen atom.
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- Piperidine nucleophilic substitution without solvent: An efficient synthesis of raloxifene
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Mild and high-yielding synthesis is described for raloxifene via piperdine nucleophilic substitution of a new raloxifene intermediate 3-aroyl-2-aryl-substituted benzo[b]thiophenes, which is obtained by acylation of para-substituted benzoyl chlorides and 2-arylbenzo[b]thiophenes. The key step is solvent free and offers valuable advantages, such as low cost, and is suitable for industrial production.
- Yang, Yewei,Zhang, Tao,Huang, Wenhai,Shen, Zhenrong
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p. 3271 - 3276
(2015/10/06)
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- Benzothiophenes and related compounds as estrogen agonists
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The invention is a compound of Formula (I): wherein R is —OH, R1is —OH, R2is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1), or a pharmaceutical composition comprising a compou
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Page/Page column 42
(2010/02/07)
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- Processes for preparing benzothiophenes
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The present invention relates to intermediates and processes for preparing benzothiophenes.
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- Process for preparing benzothiophenes
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The present invention relates to intermediates and processes for preparing benzothiophenes of the following formula: wherein Y is chloro, bromo, iodo or -SO2R9; and, R9is C1-C4alkyl, trifluoromethyl,
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