135569-20-9Relevant academic research and scientific papers
Preparation method for apatinib
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, (2019/06/30)
The invention relates to a preparation method for apatinib. The preparation method comprises the following steps: performing condensation reaction on 4-(tert-butoxycarbonyl group) alkyl phenylacetateand 1,4-butane dihalide, thereby acquiring 1-[4-(tert-butoxycarbonyl group) phenyl] alkyl cyclopentane formate; performing deprotection reaction on the acquired product, thereby acquiring 1-(4-aminophenyl) alkyl cyclopentane formate; performing amidation reaction on the acquired product and 2-chloronicotinoyl chloride, thereby acquiring 1-{4-[(2-chlorine pyridine-3-group) carbonyl amino] phenyl} alkyl cyclopentane formate; performing substitution reaction on the acquired product and 4-aminomethyl pyridine, thereby acquiring 1-{4-[(2-((4-pyridyl methyl) amino) pyridine-3-group) carbonyl amino]phenyl} alkyl cyclopentane formate; performing amidation reaction on the acquired product, thereby acquiring 1-{4-[(2-((4-pyridyl methyl) amino) pyridine-3-group) carbonyl amino] phenyl} cyclopentaneformamide; lastly, dehydrating, thereby acquiring an end product.
Novel propanamides as fatty acid amide hydrolase inhibitors
Deplano, Alessandro,Morgillo, Carmine Marco,Demurtas, Monica,Bj?rklund, Emmelie,Cipriano, Mariateresa,Svensson, Mona,Hashemian, Sanaz,Smaldone, Giovanni,Pedone, Emilia,Luque, F. Javier,Cabiddu, Maria G.,Novellino, Ettore,Fowler, Christopher J.,Catalanotti, Bruno,Onnis, Valentina
supporting information, p. 523 - 542 (2017/05/29)
Fatty acid amide hydrolase (FAAH) has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol. FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects characterizing the agonists of the cannabinoid receptors. Here we present the discovery of a novel class of profen derivatives, the N-(heteroaryl)-2-(4-((2-(trifluoromethyl)pyridin-4-yl)amino)phenyl)propanamides, as FAAH inhibitors. Enzymatic assays showed potencies toward FAAH ranging from nanomolar to micromolar range, and the most compounds lack activity toward the two isoforms of cyclooxygenase. Extensive structure-activity studies and the definition of the binding mode for the lead compound of the series are also presented. Kinetic assays in rat and mouse FAAH on selected compounds of the series demonstrated that slight modifications of the chemical structure could influence the binding mode and give rise to competitive (TPA1) or non-competitive (TPA14) inhibition modes.
NOVEL HETEROCYCLIC COMPOUNDS AS GATA MODULATORS
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Page/Page column 27, (2010/06/19)
Novel heterocyclic compounds, sstereoisomers thereof and/or pharmaceutically acceptable salts of formula (I) and its stereoisomers are provided. Additionally, methods of forming novel heterocyclic compounds, stereoisomers thereof and/or pharmaceutically a
Novel Biccyclic Compounds As GATA Modulators
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Page/Page column 18, (2010/06/19)
Novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided.
Muscarinic Receptor Binding Profile of Para-Substituted Caramiphen Analogues
Hudkins, Robert L.,DeHaven-Hudkins, Diane L.,Stubbins, James F.
, p. 2984 - 2989 (2007/10/02)
Para-substituted analogues of the antimuscarinic agent caramiphen were synthesized and evaluated for their ability to bind to the M1 and M2 subtypes of the muscarinic receptor.The purpose of the set to look for a possible relationshi
