| abstract |
A method of forming analogs of CDD- 0304, i.e., tetra(ethyleneglycol) (4-methoxy- 1,2,5-thiadiazol-3 -yl)[3 -(1 -methyl- 1.2,4,5-tetrahydropyrid-3 -yl)-1,2,5-thiadiazol-4-yl]ether hydrochloride includes one or more of the following steps: a) replacing the tetrahydropyridine moiety with one of the following heterocyclic rings, including quinuclidine, [2.2.1]-exo-azabicycloheptane, [2.2.1]-endo-azabicycloheptane and terahydropyrimidine; b) varying the length of the linking group by replacing the tetra (ethylene) glycol moiety with one of: ethylene glycol, di(ethylene) glycol, penta(ethylene) glycol, or diether diol; and/or, c) replacing the 1,2,5-thiadiazole moiety with an ester isostere. Also, a method for an asymmetric analog CCD-0304 includes replacing at least one moiety with an ester isostere and at least a second moiety with an ammonium isostere. Also, such analogs compounds and their uses are disclosed. |