Category: 5335-40-0

Arikawa, Yasuyoshi; Nishida, Haruyuki; Kurasawa, Osamu; Hasuoka, Atsushi; Hirase, Keizo; Inatomi, Nobuhiro; Hori, Yasunobu; Matsukawa, Jun; Imanishi, Akio; Kondo, Mitsuyo; Tarui, Naoki; Hamada, Teruki; Takagi, Terufumi; Takeuchi, Toshiyuki; Kajino, Masahiro published the artcile< Discovery of a Novel Pyrrole Derivative 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine Fumarate (TAK-438) as a Potassium-Competitive Acid Blocker (P-CAB)>, Recommanded Product: 3-(Methylsulfonyl)benzenesulfonyl Chloride, the main research area is pyrrole fluorophenylpyridinylsulfonyl preparation gastric acid secretion inhibitor; proton potassium ATPase gastric inhibitor pyrrole fluorophenylpyridinylsulfonyl.

In our pursuit of developing a novel and potent potassium-competitive acid blocker (P-CAB), we synthesized pyrrole derivatives focusing on compounds with low log D and high ligand-lipophilicity efficiency (LLE) values. Among the compounds synthesized, the compound I exhibited potent H+,K+-ATPase inhibitory activity and potent gastric acid secretion inhibitory action in vivo. Its maximum efficacy was more potent and its duration of action was much longer than those of proton pump inhibitors (PPIs). Therefore, compound I (1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine fumarate, TAK-438) was selected as a drug candidate for the treatment of gastroesophageal reflux disease (GERD), peptic ulcer, and other acid-related diseases.

Journal of Medicinal Chemistry published new progress about Digestive tract disease. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Recommanded Product: 3-(Methylsulfonyl)benzenesulfonyl Chloride.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Shao, Pengcheng P.; Ye, Feng; Chakravarty, Prasun K.; Varughese, Deepu J.; Herrington, James B.; Dai, Ge; Bugianesi, Randal M.; Haedo, Rodolfo J.; Swensen, Andrew M.; Warren, Vivien A.; Smith, McHardy M.; Garcia, Maria L.; McManus, Owen B.; Lyons, Kathryn A.; Li, Xiaohua; Green, Mitchell; Jochnowitz, Nina; McGowan, Erin; Mistry, Shruti; Sun, Shu-Yu; Abbadie, Catherine; Kaczorowski, Gregory J.; Duffy, Joseph L. published the artcile< Aminopiperidine Sulfonamide Cav2.2 Channel Inhibitors for the Treatment of Chronic Pain>, Electric Literature of 5335-40-0, the main research area is aminopiperidine sulfonamide preparation calcium channel analgesic SAR.

The voltage-gated calcium channel Cav2.2 (N-type calcium channel) is a critical regulator of synaptic transmission and has emerged as an attractive target for the treatment of chronic pain. We report here the discovery of sulfonamide-derived, state-dependent inhibitors of Cav2.2. In particular, 19 (I) is an inhibitor of Cav2.2 that is selective over cardiac ion channels, with a good preclin. PK and biodistribution profile. This compound exhibits dose-dependent efficacy in preclin. models of inflammatory hyperalgesia and neuropathic allodynia and is devoid of ancillary cardiovascular or CNS pharmacol. at the doses tested. Importantly, 19 exhibited no efficacy in Cav2.2 gene-deleted mice. The discovery of metabolite 26 confounds further development of members of this aminopiperidine sulfonamide series. This discovery also suggests specific structural liabilities of this class of compounds that must be addressed.

Journal of Medicinal Chemistry published new progress about Allodynia. 5335-40-0 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H7ClO4S2, Electric Literature of 5335-40-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics