On May 20, 2021, Bestvater, Brian P.; Du, Zhimin; Farand, Julie; Notte, Gregory; Tang, Doris T.; Venkataramani, Chandrasekar; Wang, Peiyuan; Yang, Kin S.; Zagorska, Anna; Phillips, Barton W. published a patent.COA of Formula: C7H8FNO The title of the patent was Preparation of triazole carbamate pyridyl sulfonamides as LPA receptor antagonists and uses thereof. And the patent contained the following:
The present disclosure relates generally to compounds I [R1 = (un)substituted alkyl, cycloalkyl, 6-10 membered aryl, etc.; R2 = H, (un)substituted alkyl, cycloalkyl; R3 = H, halo, (un)substituted alkyl, etc.; R4 = D, halo, (un)substituted alkyl, etc.; n = 0-2; R5 = (un)substituted alkyl, cycloalkyl, 3-6 membered heterocyclyl having 1-2 heteroatoms independently selected from N, O, and S; X = NH or O; Y = H or (un)substituted alkyl; Z = (un)substituted alkyl, alkoxy, cycloalkyl, etc.; or Y and Z together with the carbon to which they are attached form (un)substituted cycloalkyl, aryl, 3-12 membered heterocyclyl having 1-4 heteroatoms independently selected from N, O, and S, or 5-12 membered heteroaryl having 1-4 heteroatoms independently selected from N, O, and S] or pharmaceutically acceptable salts thereof, that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. E.g., a multi-step synthesis of (R)-II, starting from 2H-1,2,3-triazole, was described. Exemplified compounds I were tested for their in vitro LPAR1 activity (data given). The disclosure further relates to the use of the compounds I for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alc. steatohepatitis (NASH). Pharmaceutical compositions comprising compound I, alone or in combination with other therapeutic agents, were disclosed. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).COA of Formula: C7H8FNO
The Article related to triazole carbamate pyridyl sulfonamide preparation lpa lpar1 receptor antagonist, lysophosphatidic acid receptor lpar1 antagonist triazole carbamate pyridyl sulfonamide, fibrosis liver disease treatment triazole carbamate pyridyl sulfonamide preparation, nonalcoholic steatohepatitis nash treatment triazole carbamate pyridyl sulfonamide preparation and other aspects.COA of Formula: C7H8FNO
Referemce:
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Alcohols – Chemistry LibreTexts