Tetrazole derivatives

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 257/06 (2006.01) A61K 31/41 (2006.01) A61P 25/00 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2415673

The present invention is concerned with 2H-tetrazole-5-yl-amide derivatives of general formula (I) wherein R1 signifies hydrogen, lower alkyl, -(CH2)n-CF3, - (CH2)n-CHF2, -(CH2)n-CN, -(CH2)n-cycloalkyl, -(CH2)n-O-lower alkyl, -(CH2)n-O- cycloalkyl or -(CH2)n-C(O)O-lower alkyl; R2 signifies hydrogen, lower alkyl, lower alkoxy, halogen, -C(O)-lower alkyl, -C(O)OH, -C(O)O-lower alkyl, -NR3R4 or -C(O)-NR3R4 and wherein R3 and R4 may be independently from each other hydrogen or lower alkyl; X signifies -O-, -S-, -CH2, -OCH2- or two hydrogen atoms not forming a bridge; and n signifies 0, 1, 2, 3 or 4; as well as with their pharmaceutically acceptable salts. It has been found that the compounds of general formula (I) are group 1 metabotropic glutamate receptor agonists (mGluR) and are therefore useful in the treatment of corresponding CNS- disorders.

La présente invention concerne des dérivés de 2H-tétrazole-5-yl-amide présentant la formule générale (I) dans laquelle R?1¿ représente de l'hydrogène, de l'alkyle inférieur, -(CH¿2?)¿n?-CF¿3?, -(CH¿2?)¿n?-CHF¿2?, -(CH¿2?)¿n?-CN, -(CH¿2?)¿n?-cycloalkyle, -(CH¿2?)¿n?-O-alkyle inférieur, -(CH¿2?)¿n?-O-cycloalkyle ou -(CH¿2?)¿n?-C(O)O- alkyle inférieur; R?2¿ représente de l'hydrogène, de l'alkyle inférieur, de l'alcoxy inférieur, halogène, -C(O)-alkyle inférieur, -C(O)OH, -C(O)O-alkyle inférieur, -NR?3¿R?4¿ ou -C(O)-NR?3¿R?4¿ et où R?3¿ et R?4¿ peuvent, indépendamment l'un de l'autre, représenter de l'hydrogène ou de l'alkyle inférieur; X signifie -O-, -S-, -CH¿2?, -OCH¿2?- ou deux atomes d'hydrogène ne formant pas un pont; et n représente 0, 1, 2, 3 ou 4; ainsi que leurs sels pharmaceutiquement acceptables. On a observé que les composés présentant la formule générale (I) sont des agonistes du récepteur de glutamate métabotropique du groupe 1 (mGluR) et présentent par conséquent une grande utilité dans le traitement des troubles correspondants du SNC.

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