On June 5, 2014, Walsh, Shawn P.; Cato, Brian; Frie, Jessica L.; Kim, Dooseop; Pasternak, Alexander; Shi, Zhi-Cai published a patent.Recommanded Product: 868551-99-9 The title of the patent was Preparation of piperidine derivatives as inhibitors of the renal outer medullary potassium channel for treating cardiovascular diseases and edematous conditions. And the patent contained the following:
The present invention provides compounds of Formula I (wherein n = 0-1; the N-containing ring system is (un)substituted piperidinyl, etc.; R1 is -H, -OC1-3alkyl or -OH; R2 is -H or C1-3alkyl; R3 is -H, -F, -C1-3 alkyl or phenyl; or when n is 0, R2 and R3 are joined together to form a 4-6 member ring with the nitrogen and carbon to which each is attached; R4 and R5 are each independently -H or -C1-3-alkyl, or R4 and R5 are joined together with the carbon to which they are attached to form C3-6 cycloalkyl; Z1 is (un)substituted Ph, (un)substituted benzofuranyl, or (un)substituted benzopyranyl, and Z2 is a substituted N-containing heterocyclyl, (un)substituted Ph, etc.), and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention. Synthetic procedures for preparing I are exemplified. Example compound II was prepared by reacting intermediates 1-oxo-N-(piperidin-4-yl)-1,3-dihydroisobenzofuran-5-carboxamide hydrochloride and (4-methyl-1-oxo-1,3-dihydro-2-benzofuran-5-yl)acetaldehyde. In the ROMK channel functional thallium flux assay, II had an IC50 of 0.01 μM. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Recommanded Product: 868551-99-9
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