On December 3, 2009, Matsukawa, Tatsuya; Masuzaki, Kazuhiro; Kawasaki, Akiko; Akasaka, Akiko; Kawai, Yosuke published a patent.Computed Properties of 86239-00-1 The title of the patent was Preparation of benzene or thiophene compounds as VAP-1 inhibitors for disease treatment. And the patent contained the following:
The present invention provides a novel benzene derivative or thiophene derivative of general formula I (wherein A1 is a residue derived from benzene or a heterocycle containing at least one nitrogen atom or sulfur atom; A2 is a divalent residue derived from optionally substituted benzene or optionally substituted thiophene; B1 is H, OH, halo, etc.; B2 is H or a functional group containing at least one nitrogen atom; or B1 and B2 together form a cyclic structure; Y is J-L-M; J is a bond, lower alkylene, etc.; L is a bond, O, etc.; M is a bond, lower alkylene, etc.; X is -(CH2)m-, -(CH2)m-O-, etc.; m is 0-6; D is -NR3-; R3 is H, lower alkyl, etc.; and E is optionally substituted amino) useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like. Synthetic procedures for preparing I are exemplified. Example compound II-2HCl, prepared in a multistep synthesis using 4-(5-bromopyridin-2-yl)morpholine as a starting material, had IC50 values of 20.8 and 1.1 nM in radiochem. enzyme assays that measured inhibitory effect on human and rat VAP-1 enzymes, resp. The experimental process involved the reaction of Ethyl 3-fluoro-4-methylbenzoate(cas: 86239-00-1).Computed Properties of 86239-00-1
The Article related to benzene thiophene compound preparation therapeutic vap1 inhibitor, Heterocyclic Compounds (One Hetero Atom): Thiophenes and other aspects.Computed Properties of 86239-00-1
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