On April 12, 2012, Biggadike, Keith; Birault, Veronique; Champigny, Aurelie Cecile; Coe, Diane Mary; Hughes, Owen Rhys; Needham, Deborah; Tape, Daniel Terence published a patent.Synthetic Route of 143803-93-4 The title of the patent was Imidazo[1,2-a]pyridine and pyrazolo[1,5-a]pyridine derivatives as TRPV1 antagonists and their preparation and use for the treatment of TRPV1-mediated diseases. And the patent contained the following:
The invention relates to imidazopyridine and pyrazolopyridine derivatives of formula I, which are TRPV1 antagonists and which are useful in the treatment of TRPV1-mediated diseases. Compounds of formula I wherein A is single bond, CH2 and CH(CH3); X1 is H, F and Me; X2 is H, F, Me and CH2OH; X3 is H, F and Ch2OH; provided that at least two of X1, X2 and X3 are H; Y is C when Z is N, and Y is N when Z is C; R1 is halo, C1-4 alkyl, CF3 and OCF3; R2 and R3 are independently H, halo, C1-4 alkyl, CF3 and OCF3; and pharmaceutically acceptable salts and solvates, are claimed. Example compound II was prepared by a amidation of imidazo[1,2-a]pyridine-3-carboxylic acid with (2-{[4-(1,1-dimethylethyl)phenyl]oxy}ethyl)amine. All the invention compounds were evaluated for their TRPV1 antagonistic activity. From the assay, it was determined that all compounds exhibited a pIC50 value greater than 5.2. The experimental process involved the reaction of 4-Methylpyrazolo[1,5-a]pyridine-3-carboxylic acid(cas: 143803-93-4).Synthetic Route of 143803-93-4
The Article related to imidazopyridine preparation trpv1 antagonist treatment disease, pyrazolopyridine preparation trpv1 antagonist treatment disease, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Synthetic Route of 143803-93-4
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics