Compound 1 is a PDE4 inhibitor and is expected to improve memory impairment. In addition to the mechanism of action, 1 enhances BDNF signal transduction and induces NXF, a brain specific transcription factor, in the presence of low concentrations of BDNF. NXF induction is expected to lead to nerve regeneration and neuroprotective efficacy.

US88290352014-09-09Agent for treatment or prevention of diseases associated with activity of neurotrophic factors

 

Example 11
5- (benzoxazol-2-yl) -2-methyl -1-(tetrahydropyran-4-yl) benzimidazole 　eggplant flask (100 mL), 2- methyl-1- (tetrahydropyran – 4-yl) reference benzimidazole-5-carboxylic acid (example 4-3) (0.64 g, 2.46 mmol ), 2- amino-phenol (0.32 g, 2.95 mmol), and polyphosphoric acid (about 18 g) put, heated to 160 ℃, and the mixture was stirred for 17 hours. After cooling, ice was added, and the mixture was about pH 9 the liquid with concentrated aqueous ammonia (28%). Extraction with chloroform (about 50 mL X 3 times), dried over anhydrous magnesium sulfate, the crude product obtained by distilling off the solvent (0.08 g) PTLC (CHCl ₃ by weight deploy _{purified), the title compound ( 0.002 g, 0.2% yield) was obtained as a yellow-brown semi-solid.} ¹H-NMR (CDCl ₃ ) Deruta (Ppm): 1.88-1.92 (M, 2 H), 2.58-2.68 (M, 2 H), 2.70 (S, 3 H), 3.57-3.64 (M , 2 H), 4.21-4.25 (m , 2 H), 4.43-4.49 (m, 1 H), 7.29 (d, 1H, J = 9.2 Hz), 7.33-7.35 (m, 2 H ), 7.59-7.62 (m, 1 H ), 7.76-7.78 (m, 1 H), 8.18 (dd, 1 H, J = 8.6, 1.6 Hz), 8.57 (d, 1 H, J = 1.4 Hz).