Substituted oxadiazoles and thiadiazoles for use in the treatment of glaucoma and novel compounds having such use.

摘要

The use of compounds for formula (I): <CHEM> or a salt or prodrug thereof; wherein one of X, Y, or Z is an oxygen or sulphur atom and the other two are nitrogen atoms, and the dotted circle represents two double bonds thus forming a 1,3,4-oxadiazole, 1,2,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-thiadiazole nucleus; R<1> represents a non-aromatic azacyclic or azabicyclic ring system selected from <CHEM> wherein the broken line represents an optional chemical bond; the substituents R<3> and R<4> may be present at any position, including the point of attachment to the oxa- or thia-diazole ring, and independently represent hydrogen, C1-4 alkyl, halo, C1-4 alkoxy, hydroxy or carboxy, or R<3> and R<4> together represent carbonyl; the group R<5> represents hydrogen or C1-4 alkyl; and R<2> represents hydrogen, C1-8 alkyl optionally substituted by hydroxy or fluoro, C2-8 alkenyl, OR<7>, SR<7>, NR<7>R<8>, CN, CO2R<7>, CONR<7>R<8> OR NHCONHR<9> where R<9> is C1-4 alkyl; wherein R<7> and R<8> independently represent hydrogen or saturated or unsaturated C1-4 alkyl provided that, when R<7> and R<8> in NR<7>R<8> are both hydrogen, at least one of R<3> and R<4> is C1-4 alkyl, in the treatment of glaucoma, novel compounds having such use, formulations containing them and their synthesis.