Triazole derivatives and their use as therapeutic agents

Details Triazole derivatives and their use as therapeutic agents Triazole derivatives and their use as therapeutic agents

1995-09-12

1998-01-20

Morris, Patricia L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546 17, A61K 31445, C07D40106, C07D40114

Patent

active

057101612

ABSTRACT:
The present invention relates to compounds of the formula (I): ##STR1## wherein Ar.sup.1 represents optionally substituted phenyl; Ar.sup.2 represents aryl; benzhydryl; or benzyl; wherein each aryl and heteroaryl and each phenyl moiety of benzyl and benzhydryl may be substituted;
R.sup.1 represents H or a group of the formula Z-R.sup.2 ;
R.sup.2 represents H, CO.sub.2 R.sup.7, CONR.sup.7 R.sup.8, NR.sup.7 R.sup.8, NR.sup.7 COR.sup.9, NR.sup.7 SO.sub.2 R.sup.8, trifluoromethyl, heteroaryl or --O-heteroaryl, each of which heteroaryl groups are as previously defined and may be optionally substituted, or R.sup.2 represents a group selected from phenyl, piperazinyl, piperidinyl, spiro-fused piperidinyl, tetrahydroquinolinyl or tetrahydroisoquinolinyl, each of which may be substituted;
R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each independently represent H or C.sub.1-4 alkyl;
R.sup.7 and R.sup.8 each independently represent H, C.sub.1-6 alkyl, trifluoromethyl, phenyl or benzyl;
Q represents O or S;
X represents a group selected from --CR.sup.3 R.sup.4 CR.sup.5 R.sup.6 -, --CR.sup.3 .dbd.CR.sup.4 --, --C(OH)R.sup.3 CR.sup.4 R.sup.5 -, --CR.sup.3 R.sup.4 C(OH)R.sup.5 -, --C(O)CR.sup.3 R.sup.4 - and --CR.sup.3 R.sup.4 C(O)--;
Y represents a C.sub.1-4 alkylene chain; and
Z represents a straight or branched C.sub.1-6 alkylene or C.sub.3-6 alkenylene chain with the proviso that the alkenylene double bond does not terminate at a carbon atom attached to a nitrogen atom;
and pharmaceutically acceptable salts thereof.
The compounds are of particular use in the treatment or prevention of pain, inflammation, emesis and postherpetic neuralgia.

REFERENCES:
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Malbec, F. et al. "Derivatives of 2,4-dihydro-1, 2,4-triazole-3-thione and 2-amino-1, 3,4-thiadiazole from thiosemicarbazones of esters" Chemical Abstracts, vol. 103, No. 22, Jul. 22, 1985, PG. 571, COL. 1, Abstract No. 22 524w.
Khripak, S. M. et al. "Acylation and iodination of 5-p-phenyl-1,2, 4-triazole-3-thiones" Chemical Abstracts, vol. 101, No. 25, Dec. 17, 1984, p. 761, COL. 1, Abstract No. 230 418 a.
Knysh, E. G. et al. "Synthesis and properties of 5-heteroarylthio-1, 2,-4triazoles" Chemical Abstracts, vol. 105, No. 8, Sep. 1, 1986, p. 17, COL. 1, Abstract No. 72 087t.
Knish, E. G. et al. "Synthesis, properties and biological activity of 5-(acylalkylthio)-1,2,4-triazoles" Chemical Abstracts, vol. 99, No. 8, Aug. 1, 1983, p. 521, COL. 2, Abstract No. 38 421v.
S. I. Ramnarine et al. "Sensory-Efferent Neural Control of Mucus Secretion: Characterization Using Tachykinin Receptor Antagonists in Ferret Trachea in Vitro" Br. J. Pharmacol. (1994) 113, 1183-1190.

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