On May 7, 2020, Hehn, Joerg P.; Blum, Andreas; Hucke, Oliver; Peters, Stefan published a patent.Recommanded Product: 1251006-64-0 The title of the patent was Preparation of pyridine-3-sulfonamide derivatives as amine oxidase copper containing 3 (AOC3) inhibitors and pharmaceutical compositions and uses thereof. And the patent contained the following:
The invention relates to new pyridinyl sulfonamide derivatives of the formula I [ring A = azetidin-1-yl, pyrrolidin-1-yl, 3-azabicyclo[3.1.0]hexan-3-yl, or piperidin-4-yl; R1 = H, F, Ci, Br, cyano, OH, or each (un)substituted C1-4-alkyl, C1-4-alkyloxy, (CH2)m-CO2H, (CH2)m-C(O)O-(C1-4-alkyl), (CH2)m-C(O)-heterocyclyl, (CH2)m-C(O)NH2, (CH2)m-C(O)NH-(C1-4-alkyl), (CH2)m-C(O)-N-(C1-4-alkyl)2, C(O)-NH-C3-6-cycloalkyl, C(O)-NH-heterocyclyl, (CH2)m-NH-C(O)(C1-3-alkyl), N-(C1-3-alkyl)-C(O)-(C1-4-alkyl), N-(C1-3-alkyl)-C(O)NH2, NH-C(O)NH-(C1-4-alkyl), heterocyclyl, or Ph; wherein multiple R1 may be identical or different, if n = 2; n = 1 or 2; m = 0, 1, or 2] or salts thereof. The compounds I or salts thereof are selective inhibitors of AOC3 (amine oxidase, copper containing 3; vascular adhesion protein 1) and are useful for the treatment of cancer, NASH (non-alc. steatohepatitis), pulmonary fibrosis, retinopathy, nephropathy, or stroke. Thus, a solution of 0.19 mmol 1-[1-(6-chloropyridine-3-sulfonyl)piperidin-4-yl]-3-methylimidazolidin-2-one in NMP and Et3N was cooled in an ice bath, treated with a solution of 0.19 mmol tert-butyl-N-[2-(fluoromethylidene)-3-hydroxypropyl]carbamate in 0.5 mL THF and 390μL 2 M sodium tert-butoxide/THF, and stirred at room temperature for 2 h to give 1-[1-[6-((Z)-2-(tert-butoxycarbonylamino)methyl-3-fluoroallyloxy)pyridine-3-sulfonyl]piperidin-4-yl]-3-methylimidazolidin-2-one (isolated as trifluoroacetate salt) which was stirred with CF3CO2H in CH2Cl2 at room temperature for 2 h to give 1-[1-[6-((Z)-2-aminomethyl-3-fluoroallyloxy)pyridine-3-sulfonyl]piperidin-4-yl]-3-methylimidazolidin-2-one trifluoroacetate (II). II showed IC50 of 7, 120, 15,265 nM, and >50.0μM against AOC3, AOC2, AOC1, and monoamine oxidase-A (MAO-A), resp. The experimental process involved the reaction of tert-Butyl 3-(piperidin-4-yl)azetidine-1-carboxylate(cas: 1251006-64-0).Recommanded Product: 1251006-64-0
The Article related to pyridinesulfonamide preparation aoc3 inhibitor, amine oxidase copper containing 3 aoc3 inhibitor, vascular adhesion protein 1 inhibitor, azetidinylsulfonylpyridine pyrrolidinylsulfonylpyridine preparation aoc3 inhibitor, azabicyclohexanylsulfonylpyridine piperidinylsulfonylpyridine preparation aoc3 inhibitor and other aspects.Recommanded Product: 1251006-64-0
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem