A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/44 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07D 453/00 (2006.01) C07D 453/02 (2006.01) C07D 453/06 (2006.01) C07D 471/08 (2006.01)
Patent
CA 2043385
T1074Y ABSTRACT USE OF OXADIAZOLES AND THIADIAZOLES FOR TREATMENT OF GLAUCOMA The use of compounds for formula (I): Image ( ¦ ) 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; R1 represents a non-aromatic azacyclic or azabicyclic ring system selected from Image T1074Y wherein the broken line represents an optional chemical bond; the substituents R3 and R4 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 R3 and R4 together represent carbonyl; the group R5 represents hydrogen or C1-4 alkyl; and R2 represents hydrogen, C1-8 alkyl optionally substituted by hydroxy or fluoro, C2-8 alkenyl, OR7. SR7, NR7R8, CN, CO2R7, CONR7R8 OR NHCONHR9 where R9 is C1-4 alkyl; wherein R7 and R8 independently represent hydrogen or saturated or unsaturated C1-4 alkyl provided that, when R7 and R8 in NR7R8 are both hydrogen, at least one of R3 and R4 is C1-4 alkyl, in the treatment of glaucoma, novel compounds having such use, formulations containing them and their synthesis.
Lotti Victor
Showell Graham A.
Goudreau Gage Dubuc
Lotti Victor
Merck Sharp And Dohme Limited
Showell Graham A.
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