On November 4, 2021, Xu, Qing; Alt, Carsten; Li, Zhe; Nilar, Shahul; Rademacher, Peter Michael; Yee, Calvin Wesley published a patent.Category: pyrimidines The title of the patent was Prepartion of pyrimidines as ferroportin inhibitors. And the patent contained the following:
The invention is related to a method of inhibiting iron transport mediated by ferroportin in a subject, comprising administering to the subject an effective amount of a compound I [Z= N, CR5; R5 = H, halo, alkyl; R6 = independently at each occurrence halo, OH, (un)substituted alkoxy, alkyl, etc.; or two R6 groups, taken together with the atom to which each is attached, form an (un)substituted 5- or 6-membered monocyclic heterocyclyl fused with ring B, a C4-C7 cycloalkyl fused with ring B, a Ph fused with ring B, or a 5- to 6-membered monocyclic heteroaryl fused with ring B; n = 0-3; Y = (Y1)0-1; Y1-4 = independently CH, N, NH, O, S, SH, SR6, NR6, CR6; provided that 1 or 2 of Y1-4 can be N, NR6, NH, O, SH or SR6; R1, R2 = independently H, alkyl, haloalkyl, alkoxy, and OH; R1 and R2 taken together with the atom to which each is attached form ring A; wherein A = (un)substituted C5-C6 cycloalkyl, 5- or 6-membered heterocyclyl, Ph, and 5- or 6-membered heteroaryl; R3 = H , optionally deuterated C1-C3 alkyl, hydroxyalkyl, C1-C3 alkoxyalkyl, haloalkyl, cyclopropyl, phenyl; R4 = CH2CONH2 and derivatives, cycloalkyl, alkylsulfonylalkyl, etc.; or R3NR4 = (un)substituted4- to 12-membered heterocyclyl] and their pharmaceutical salts. The invention is laos relates to methods of administering them for prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries and to pharmaceutical compositions containing compounds I. Preparation of compounds I and their pharmaceutical acceptable salts is also given. Thus, II was prepared in 6 steps from 2-chloro-4-methylpyridine and diethylcarbonate using N-tert-Butyl-2-[(2-chloro-5H,6H,7H-cyclopenta[d]pyrimidin-4-yl)amino]acetamide (preparation given). II was tested in an in vitro ferroportin internalization assay (pEC50 = 7.7). The experimental process involved the reaction of 2,4-Dichloro-5,6-dimethylthieno[2,3-d]pyrimidine(cas: 42518-42-3).Category: pyrimidines
The Article related to pyrimdine cycloalkapyrimidine thienopyrimidine preparation ferroportin inhibitor, thienopyrimidine cyclopentapyrimidinyl amino acid amide preparation ferroportin inhibitor, hepcidin iron metabolism disorder cycloalkapyrimidine thienopyrimidine preparation, iron overload state thalassemia hemochromatosis treatment cycloalkapyridine thienopyrimidine preparation and other aspects.Category: pyrimidines
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia