Guerrero, Miguel’s team published research in Journal of Medicinal Chemistry in 62 | CAS: 906811-51-6

Journal of Medicinal Chemistry published new progress about 906811-51-6. 906811-51-6 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Amine,Benzene,Aldehyde, name is 2-Amino-5-bromo-3-fluorobenzaldehyde, and the molecular formula is C7H5BrFNO, Name: 2-Amino-5-bromo-3-fluorobenzaldehyde.

Guerrero, Miguel published the artcileDesign and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140), Name: 2-Amino-5-bromo-3-fluorobenzaldehyde, the publication is Journal of Medicinal Chemistry (2019), 62(4), 1761-1780, database is CAplus and MEDLINE.

κ Opioid receptor (KOR) antagonists are potential pharmacotherapies for the treatment of migraine and stress-related mood disorders including depression, anxiety, and drug abuse, thus the development of novel KOR antagonists with an improved potency/selectivity profile and medication-like duration of action has attracted the interest of the medicinal chem. community. In this paper, we describe the discovery of 1-(6-ethyl-8-fluoro-4-methyl-3-(3-methyl-1,2,4-oxadiazol-5-yl)quinolin-2-yl)-N-(tetrahydro-2H-pyran-4-yl)piperidin-4 amine (CYM-53093, BTRX-335140) as a potent and selective KOR antagonist, endowed with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rat pharmacodynamic experiments Orally administered CYM-53093 showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice. CYM-53093 exhibited a broad selectivity over a panel of off-target proteins. This compound is in phase 1 clin. trials for the treatment of neuropsychiatric disorders wherein dynorphin is thought to contribute to the underlying pathophysiol.

Journal of Medicinal Chemistry published new progress about 906811-51-6. 906811-51-6 belongs to bromides-buliding-blocks, auxiliary class Fluoride,Bromide,Amine,Benzene,Aldehyde, name is 2-Amino-5-bromo-3-fluorobenzaldehyde, and the molecular formula is C7H5BrFNO, Name: 2-Amino-5-bromo-3-fluorobenzaldehyde.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary