64010-38-4Relevant academic research and scientific papers
BET INHIBITORS FOR MODULATING DUX4 EXPRESSION IN FSHD
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Page/Page column 272; 273, (2020/07/14)
The present disclosure provides BET inhibitors of the formula: wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of treating a patient comprising administering a bromo- and extra-terminal (BET) domain inhibitor for the treatment of FSHD which modulates DUX4 expression. In some embodiments, the present methods comprise using one or more BET inhibitors as a therapeutic agent for the treatment of FSHD patients including patients who are being treated with one or more palliative treatments such as therapy and/or agents which lead to increased muscle mass.
Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile
Labeeuw, Olivier,Levoin, Nicolas,Poupardin-Olivier, Olivia,Calmels, Thierry,Ligneau, Xavier,Berrebi-Bertrand, Isabelle,Robert, Philippe,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
, p. 2548 - 2554 (2013/06/27)
Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series exhibited nanomolar binding affinities for human receptor, illustrating a new possible component for the H3 pharmacophore. As demonstrated with compound BP1.4160 (cyclohexanol 19), the introduction of an alcohol function counter-intuitively allowed to reach high in vivo efficiency and favorable pharmacokinetic profile with reduced half-life.
Process for the preparation of 3-aroyl-5-aminobenzofuran derivatives
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Page/Page column 32, (2012/06/01)
The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
PROCESS FOR THE PREPARATION OF 3-AROYL-5-AMINOBENZOFURAN DERIVATIVES
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Page/Page column 42, (2012/05/31)
The present invention relates to a process for the preparation of 3-aroyl -5- aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl) propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): A potent, selective histamine H3 receptor inverse agonist
Hudkins, Robert L.,Raddatz, Rita,Tao, Ming,Mathiasen, Joanne R.,Aimone, Lisa D.,Becknell, Nadine C.,Prouty, Catherine P.,Knutsen, Lars J. S.,Yazdanian, Mehran,Moachon, Gilbert,Ator, Mark A.,Mallamo, John P.,Marino, Michael J.,Bacon, Edward R.,Williams, Michael
experimental part, p. 4781 - 4792 (2011/09/21)
Optimization of a novel series of pyridazin-3-one histamine H3 receptor (H3R) antagonists/inverse agonists identified 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (8a, CEP-26401; irdabisant) as a lead candid
Novel and highly potent histamine H3 receptor ligands. Part 1: Withdrawing of hERG activity
Levoin, Nicolas,Labeeuw, Olivier,Calmels, Thierry,Poupardin-Olivier, Olivia,Berrebi-Bertrand, Isabelle,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
scheme or table, p. 5378 - 5383 (2011/10/12)
Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have developed a QSAR model specially dedicated to H3 receptor ligands. This model was designed to be di
COMPOUNDS COMPRISING A LACTAM OR A LACTAM DERIVATIVE MOIETY, PROCESSES FOR MAKING THEM, AND THEIR USES
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Page/Page column 84, (2008/06/13)
The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
Phenoxypropylpiperidines and -pyrrolidines and their use as histamine H3-receptor ligands
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Page/Page column 41, (2008/06/13)
The present patent application concerns compounds of formula (I), with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.
SUBSTITUTED ANILINIC PIPERIDINES AS MCH SELECTIVE ANTAGONISTS
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Page column 189, (2010/02/06)
This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands
Faghih, Ramin,Dwight, Wesley,Vasudevan, Anil,Dinges, Jurgen,Conner, Scott E.,Esbenshade, Timothy A.,Bennani, Youssef L.,Hancock, Arthur A.
, p. 3077 - 3079 (2007/10/03)
Biaryl nitrile amines were prepared and found to have high affinity and selectivity for human and rat histamine H3 receptors.
