75369-41-4Relevant academic research and scientific papers
Design, synthesis and biological activity of multifunctional α,β-unsaturated carbonyl scaffolds for Alzheimer's disease
Bag, Seema,Ghosh, Sanjukta,Tulsan, Rekha,Sood, Abha,Zhou, Weihong,Schifone, Christine,Foster, Michelle,Levine III, Harry,T?r?k, Béla,T?r?k, Marianna
, p. 2614 - 2618 (2013)
A series of compounds containing an α,β-unsaturated carbonyl moiety, such as chalcones and coumarins were designed, synthesized and tested in a variety of assays to assess their potential as anti-Alzheimer's disease (AD) agents. The investigations include
PYRUVATE KINASE ACTIVATORS FOR USE IN TREATING BLOOD DISORDERS
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Page/Page column 4, (2019/03/05)
Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): Formula (I) wherein R', R2, L', and L2 are as defined herein.
CHEMICAL COMPOUNDS
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Page/Page column 51; 52, (2018/10/19)
The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers.
INHIBITORS OF HEPATITIS C VIRUS POLYMERASE
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Paragraph 240; 241; 242, (2016/10/11)
The present invention provides, among other things, compounds represented by the general Formula I: (I) and pharmaceutically acceptable salts thereof, wherein L and A (and further substituents) are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy
Baragana, Beatriz,Norcross, Neil R.,Wilson, Caroline,Porzelle, Achim,Hallyburton, Irene,Grimaldi, Raffaella,Osuna-Cabello, Maria,Norval, Suzanne,Riley, Jennifer,Stojanovski, Laste,Simeons, Frederick R. C.,Wyatt, Paul G.,Delves, Michael J.,Meister, Stephan,Duffy, Sandra,Avery, Vicky M.,Winzeler, Elizabeth A.,Sinden, Robert E.,Wittlin, Sergio,Frearson, Julie A.,Gray, David W.,Fairlamb, Alan H.,Waterson, David,Campbell, Simon F.,Willis, Paul,Read, Kevin D.,Gilbert, Ian H.
supporting information, p. 9672 - 9685 (2016/11/19)
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen against the blood stage of Plasmodium falciparum (3D7) and displayed moderate potency but with suboptimal physicochemical properties and poor microsomal stability. The screening hit (1, EC50 = 120 nM) was optimized to lead molecules with low nanomolar in vitro potency. Improvement of the pharmacokinetic profile led to several compounds showing excellent oral efficacy in the P. berghei malaria mouse model with ED90 values below 1 mg/kg when dosed orally for 4 days. The favorable potency, selectivity, DMPK properties, and efficacy coupled with a novel mechanism of action, inhibition of translation elongation factor 2 (PfEF2), led to progression of 2 (DDD107498) to preclinical development.
SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Paragraph 0333; 0334, (2014/09/30)
Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
COMPOUNDS USEFUL AS RETINOID-RELATED ORPHAN RECEPTOR GAMMA MODULATORS
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Page/Page column 38, (2012/08/08)
Disclosed are retinoid-related orphan receptor gamma (RORγ) modulators of Formula (I) and their use in the treatment of diseases mediated by RORγ, wherein the radicals have the meanings as defined in the invention.
Competition between azido cleavage and triplet nitrene formation in azidomethylacetophenones
Ranaweera, Ranaweera A. A. Upul,Zhao, Yu,Muthukrishnan, Sivaramakrishnan,Keller, Christopher,Gudmundsdottir, Anna D.
experimental part, p. 1645 - 1655 (2011/09/14)
Photolysis of p- and m-azidomethylacetophenone (1a, 1b) in argon-saturated solutions yields predominantly imine 2a, 2b, whereas irradiation of 1a, 1b in oxygen-saturated solutions results in heterocycles 3a, 3b, aldehydes 4a, 4b and nitriles 5a, 5b. Density functional theory calculations place the energy of the first and second excited state of the triplet ketones (T1K and T 2K) in 1a, 1b in close proximity to each other. The triplet transition state for cleaving the CN bond in 1a, 1b to form azido and benzyl radicals 1aB, 1bB is located only 3 kcal mol-1 (1 kcal = 4.184 kJ) above T1K, indicating that azido cleavage is feasible. The calculations place the energy of the triplet azido group (TA) in 1a, 1b ~25 kcal mol-1 below T1K; thus, this process is also easily accessible via energy transfer. Further, the transition state barrier for TA to expel N2 and form triplet nitrenes is less than 1 kcal mol-1 above TA in 1a, 1b. Laser flash photolysis of 1a, 1b reveals the formation of the triplet excited ketones of 1a, 1b, which decay to form benzyl radicals 1aB, 1bB and triplet alkylnitrenes. The triplet ketones and the benzyl radicals are quenched with molecular oxygen at rates close to diffusion, whereas the triplet nitrenes react more slowly with oxygen (~5 × 105 M-1s-1). We conclude that the triplet alkylnitrenes intercept the benzyl radicals to form 2 in argon-saturated solution, whereas the benzyl radicals are trapped to form 4 in oxygen-saturated solution; thus, the triplet nitrenes react with oxygen to form 3. CSIRO 2010.
LANTHANIDE(III) CHELATES COMPRISING BETA-DIKETONES AND CONJUGATES DERIVED THEREOF
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Page/Page column 10; 17, (2009/10/22)
This invention relates to luminescent lanthanide(III) chelates based on β-diketones comprising an azacycloalkane backbone and biomolecule conjugates and solid supports comprising these chelates. In contrast to lanthanide chelates based on monomeric β-diketones as well as lanthanide(III) chelates based on acyclic azaalkanes including several β-diketone subunits, the molecules of the present technology are luminescent even in the absence of additional chelators such as phosphine oxides.
Substituted isoxazolines, pharmaceutical compositions containing the same, methods of preparing the same, and uses of the same
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Page/Page column 20, (2008/06/13)
The invention relates to substituted isoxazolines according to the general formula (I) : in which A, R1, R2, R3, R4, Z, X, m, n, and p, are given in the claims, and salts thereof, to pharmaceutical compositions comprising said substituted isoxazolines, to methods of preparing said substituted isoxazolines as well as the use thereof for manufacturing a pharmaceutical composition for the treatment of diseases known to be at least in part mediated by HDAC activity or whose symptoms are known to be alleviated by HDAC inhibitors.
