On December 18, 2014, Ikegami, Satoru; Watanabe, Atsushi; Hirano, Kimio; Ohyama, Tadashi published a patent.Application of 386704-04-7 The title of the patent was Preparation of 4-alkynyl imidazole derivatives for the treatment of EP4 receptor-related diseases. And the patent contained the following:
The present invention provides 4-alkynyl imidazole derivatives I [ring A = (un)substituted cycloalkyl, aryl or heteroaryl; ring B = cycloalkyl, aryl or heteroaryl; m = 0-2; n = 1-3; R1 = H, alkyl, alkoxy, etc.; R2 and R3 = independently H, halogen, alkyl or carbocyclic ring when taken together; R4 and R5 = independently H, alkyl or carbocyclic ring when taken together; R6 and R7 = independently H, alkyl, alkoxy, etc.; X = OR8, NR9R10 or halogen; R8 = H, alkyl or haloalkyl; R9 and R10 = independently H, alkyl or heterocycle when taken together; Y = single bond, O or S; E = CO2H, CO2P or biol. equivalent of carboxyl group; CO2P = pharmacol. acceptable ester prodrug] and their pharmaceutically acceptable salts. Thus, compound II (preparation given) was subjected to a coupling reaction with 4-(1-aminocyclopropyl)benzoic acid Me ester followed by O-methylation and hydrolysis to provide compound III. Compound III exhibited antagonistic activity against rat EP4 receptor with an IC50 value of 1.7 nmol/L. The invention compounds have excellent EP4 receptor antagonist effects and are useful as medicines for treating diseases associated with EP4 receptors, for example, anti-inflammatory agents and/or analgesics for inflammatory diseases and diseases associated with various kinds of pain, and also as medicines for treating immune diseases that occur as a result of Th1 cell and/or Th17 cell activation, which causes tissue destruction and gives rise to 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 alkynyl imidazole derivative preparation ep4 receptor antagonist, inflammatory disease pain immune disease treatment antiinflammatory agent, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Application of 386704-04-7
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