83922-54-7Relevant academic research and scientific papers
SUBSTITUTED INHIBITORS OF MENIN-MLL AND METHODS OF USE
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Paragraph 0264, (2019/04/16)
The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL
Anti-inflammatory agents
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Page/Page column 98; 99, (2016/02/05)
Disclosed are novel compounds that are useful in regulating the expression of interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1), and their use in the treatment and/or prevention of cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s). Also, disclosed are compositions comprising the novel compounds, as well as methods for their preparation.
TREATMENT OF DISEASES BY EPIGENETIC REGULATION
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Paragraph 0596, (2013/11/05)
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
Mild Pd-catalyzed N -arylation of methanesulfonamide and related nucleophiles: Avoiding potentially genotoxic reagents and byproducts
Rosen, Brandon R.,Ruble, J. Craig,Beauchamp, Thomas J.,Navarro, Antonio
supporting information; experimental part, p. 2564 - 2567 (2011/06/25)
A convenient, general, and high yielding Pd-catalyzed cross-coupling of methanesulfonamide with aryl bromides and chlorides is reported. The use of this method eliminates concern over genotoxic impurities that can arise when an aniline is reacted with methanesulfonyl chloride. The application of this method to the synthesis of dofetilide is also reported.
Synthesis of (S)-(+)-sotalol and (R)-(-)-isoproterenol via a catalytic enantioselective Henry reaction
Blay, Gonzalo,Hernandez-Olmos, Victor,Pedro, Jose R.
body text, p. 578 - 581 (2010/08/06)
A unified approach for the synthesis of (S)-(+)-sotalol and (R)-(-)-isoproterenol has been developed. The enantioselective Henry reaction of the appropriate aldehyde in the presence of a camphor-derived amino pyridine-Cu(II) complex was the key step of th
HYDRAZONE DERIVATIVE
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Page/Page column 58, (2010/11/08)
A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
Synthesis of biologically active amines via rhodium-bisphosphite-catalyzed hydroaminomethylation
Briggs, John R.,Klosin, Jerzy,Whiteker, Gregory T.
, p. 4795 - 4798 (2007/10/03)
(Chemical Equation Presented) We report the use of a highly regioselective rhodium-bisphosphite catalyst for olefin hydroaminomethylation. This catalyst system was successfully applied in the synthesis of two biologically active tertiary amines, ibutilide and aripiprazole.
New 3- and 4-hydroxyfuranones as anti-oxidants and anti-inflammatory agents
Weber, Valerie,Rubat, Catherine,Duroux, Eliane,Lartigue, Claire,Madesclaire, Michel,Coudert, Pascal
, p. 4552 - 4564 (2007/10/03)
Two series of new furanones substituted by methylsulfonylphenyl or methylsulfamidophenyl moieties were found to protect against oxidation damage by inhibiting or quenching free radicals and reactive oxygen species in in vitro experiments. The effect on lipid peroxidation was also examined. In addition, we investigated the activity of products in two models of inflammation: phorbol ester-induced ear edema in mice and carrageenan-induced paw edema in rat. The most powerful compounds and with reducing activity against DPPH (IC50 = 1779 and 57 μM, respectively), superoxide anion quenching capacity (IC50 = 511 and 49 μM, respectively), lipid peroxidation inhibitory effect and anti-inflammatory properties (about 50-65% inhibition of edema at 200 mg/kg ip in both tests used) were selected for further pharmacological and toxicological tests because of their attractive profile for the treatment of inflammatory diseases.
HYDROXAMIC ACIDS USEFUL IN THE TREATMENT OF HYPER-PROLIFERATIVE DISORDERS
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Page 308, (2010/02/09)
This invention relates to a compound of Formula (I) and its use in treating hyper-proliferative disorders.
Substituent effects in infrared spectroscopy-VII. Meta and para substituted methanesulphonanilides
Laurence, C.,Berthelot, M.,Lucon, M.,Tsuno, Y.
, p. 791 - 796 (2007/10/02)
Substituent effects on the NH frequencies of the conformers of methanesulphonanilides, their cyclic dimers and their hydrogen bonded complexes with acetonitrile have been analysed by means of the Hammet equation.An electron-withdrawing substituent may either increase or decrease ν(NH) in the XC6H4NHY series according to the electronic nature of the Y group.This can be explained by the non-monotonic dependence of the NH stretching frequency on the ionic character of the NH bond.
