A SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVE, PHARMACEUTICAL COMPOSITIONS MADE THEREFROM

摘要

1. 7-(1, 1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine. 2. Polymorph A of 7-(1, 1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine as characterised herein. 3. A pharmaceutical composition comprising 7-(1,1dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)1,2,4-triazolo [4,3-b] pyridazine in association with a pharmaceutically acceptable carrier. 4. The use of 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine for the manufacture of a medicament for the treatment and/or prevention of anxiety. 5. A process for the preparation of 7-(1,1-dimethylethyl)-6-(2ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1, 2, 4-triazolo [4,3-b] pyridazine, which comprises reacting a compound of formula III with the compound of formula IV: wherein L<1> represents a suitable leaving group. 6. A process for manufacturing 7-(1, 1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine, which comprises reacting a compound of formula XI (or tautomer thereof 1, 2, 4-triazolo [4,3-b] pyridazine-6-one) with the compound of formula XII: wherein L<3> represents a suitable leaving group 7. A process for manufacturing 7-(1, 1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine, which comprises reacting trimethylacetic acid with the compound of formula XIII: in the presence of silver nitrate and ammonium persulfate. 8. A process for manufacturing 7-(1, 1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine, which comprises reacting the compound of formula XIV with the compound of formula XV: wherein M represents -B(OH)2 or -Sn(Alk)3, where Alk is C1-6 alkyl group, and L<4> represents a suitable leaving group in the presence of a catalyst based on a transition metal. 9. A process as claimed in claim 5 wherein reaction (A) is carried out in 1-methyl-2-pyrrolidinone, in the presence of sodium hydroxide, at a temperature in the region of 0 degree C. 10. A method for the treatment and/or prevention of anxiety which comprises administering to a patient in need of such treatment an effective amount of 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo [4,3-b] pyridazine.