58026-14-5Relevant academic research and scientific papers
ARYL AND HETEROARYL-CARBOXAMIDE SUBSTITUTED HETEROARYL COMPOUNDS AS TYK2 INHIBITORS
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Page/Page column 168-169, (2021/10/15)
Novel carboxamide substituted compounds of Formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Tyrosine Kinase 2 (Tyk2).
SMALL MOLECULES FOR TREATING CANCER, INHIBITING CHEMOKINE ACTIVITY AND/OR INDUCING CELL DEATH
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Page/Page column 8; 61-62, (2020/11/30)
Compounds capable of, or usable in, inducing death of cancer cells and/or modulating a biological activity of a chemokine e.g., cell migration, and/or treating diseases and disorders associated with a biological activity of a chemokine and/or cell migrati
Regioselective Biomimetic Synthesis of Dimeric Oxyresveratrol Derivatives
Ran, Lu,Li, Hongpeng,Chao, Ge,Kang, Xiaodong,Lei, Tian,Li, Wenling
supporting information, p. 1809 - 1812 (2020/09/18)
Oxyresveratrol and its methylated derivative as coupling precursors were efficiently prepared in four steps, with Wittig reactions and subsequent isomerization reactions as the key steps. The coupling reactions of oxyresveratrol under various oxidative conditions gave a complex and inseparable mixture of coupling products. The oxidative dimerizations of methylated oxyresveratrols catalyzed by horseradish peroxidase-H 2O 2or FeCl 3·6H 2O in an acetone system predominantly produced the 8-5-coupled and 8-10-coupled dihydrobenzofuran-type dimers, respectively. This regioselective biomimetic strategy might be useful in synthesizing other dimeric oxyresveratrol derivatives.
Synthesis of p-O-Alkyl Salicylanilide Derivatives as Novel EGFR Inhibitors
Zhang, Li,Hou, Lin,Sun, Wenyan,Yu, Zidong,Wang, Jibo,Gao, Hua,Yang, Guiming
, p. 37 - 42 (2016/02/23)
(Table Presented) Epidermal growth factor receptor (EGFR), a validated target for anticancer drugs, plays a critical role in tumorigenesis and tumor development. A series of p-O-alkyl salicylanilide derivatives were designed and synthesized as novel EGFR inhibitors using a salicylic acid scaffold. A simulated six-membered ring strategy formed through intramolecular hydrogen bonds was employed to mimic the planar quinazoline of the EGFR antagonist, gefitinib. The derived compounds with hydroxyl at the ortho position were more potent than ones with methoxyl group. In particular, compounds 5d and 5b displayed significant EGFR inhibitory (IC50 values = 0.30 and 0.45 μM, respectively) activity as well as potent antiproliferative activity in A431 and HCT-116 tumor cells. These salicylanilides could be considered as promising lead compounds for developing novel EGFR inhibitors.
Concise synthesis of broussonone A
Jo, Hyeju,Choi, Minho,Viji, Mayavan,Lee, Young Hee,Kwak, Young-Shin,Lee, Kiho,Choi, Nam Song,Lee, Yeon-Ju,Lee, Heesoon,Hong, Jin Tae,Lee, Mi Kyeong,Jung, Jae-Kyung
, p. 15966 - 15975 (2015/12/01)
A concise and expeditious approach to the total synthesis of broussonone A, a p-quinol natural compound, has been developed. The key features of the synthesis include the Grubbs II catalyst mediated cross metathesis of two aromatic subunits, and a chemoselective oxidative dearomatizationin the presence of two phenol moieties. Especially, optimization associated with the CM reaction of ortho-alkoxystyrenes was also studied, which are known to be ineffective for Ru-catalyzed metathesis reactions under conventional reaction conditions because ortho-alkoxy group could coordinate to the ruthenium center, resulting in the potential complication of catalyst inhibition.
INDANYLOXYPHENYLCYCLOPROPANECARBOXYLIC ACIDS
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Paragraph 0362, (2014/01/07)
The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
NEW INDANYLOXYPHENYLCYCLOPROPANECARB OXYLIC ACIDS
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Page/Page column 58, (2014/01/07)
The present invention relates to compounds of general formula I, (I) wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
AGONISTS OF GPR40
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Page/Page column 145-146, (2012/02/05)
The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are there-fore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS
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Page/Page column 58, (2010/11/04)
Disclosed herein are substantially pure forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, stereoisomer or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.
Enantioselective total synthesis of hydramicromelin B
Huo, Xing,Ren, Xingfeng,Xu, Yanfen,Li, Xinyun,She, Xuegong,Pan, Xinfu
, p. 343 - 347 (2008/09/19)
The first total synthesis of hydramicromelin B is described. An AuCl3/AgOTf-catalyzed intramolecular reaction was used as key step for the construction the coumarin ring.
