On May 2, 2013, Bayburt, Erol K.; Clapham, Bruce; Cox, Phil B.; Daanen, Jerome F.; Gomtsyan, Arthur; Kort, Michael E.; Kym, Philip R.; Voight, Eric A.; Schmidt, Robert G.; Dart, Michael J.; Gfesser, Gregory published a patent.Application of 386704-04-7 The title of the patent was Preparation of (cyclobutyl)(pyridinyl)methanol derivatives as TRPV3 modulators. And the patent contained the following:
Title compounds I [each occurrence of Ra and Rb independently = H, (un)substituted alkyl, haloalkyl, halogen, OH, O(alkyl), or phenyl; q = 0-2; X3 = O; X4 = bond or (CH2)m; X5 = (CH2)n; m and n are each 1; each Z1 = alkyl, oxo, halogen, haloalkyl, etc.; p = 1-4; X1 = OH; X2 = H; G1 = (un)substituted aryl, heteroaryl, cycloalkyl, heterocycle, or cycloalkenyl; G2 = aryl, heteroaryl, cycloalkyl, heterocycle, or cycloalkenyl], and their pharmaceutically acceptable salts, are prepared Compounds of the invention were evaluated for ability to antagonize the activation of recombinant human TRPV3 using FLIPR Tetra cellular screening. Thus, e.g., II was prepared in a multi-step synthesis and had IC50 value of 0.19 nM as human TRPV3 antagonist. The invention compounds and combination with other therapeutic agent are useful for treating conditions such as pain and inflammation. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7
The Article related to methanol cyclobutyl pyridinyl preparation trpv3 modulator pain inflammation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Application of 386704-04-7
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