Method of using 5-arylheteroarylalkyl-1,3 5-trisubstituted-1,24-

Details Method of using 5-arylheteroarylalkyl-1,3 5-trisubstituted-1,24- Method of using 5-arylheteroarylalkyl-1,3 5-trisubstituted-1,24-

1993-12-21

1995-09-19

Ivy, C. Warren

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514338, 514339, 514340, 514341, 514824, A61K 3144

Patent

active

054515912

ABSTRACT:
A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein m is one; wherein R.sup.1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R.sup.2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.11 is hydrido and R.sup.5 is selected from COOH, SH, PO.sub.3 H.sub.2, SO.sub.3 H, CONHNH.sub.2, CONHNHSO.sub.2 CF.sub.3, OH, ##STR3## wherein each of R.sup.42 and R.sup.43 is independently selected from chromo, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.

REFERENCES:
patent: 4816463 (1989-03-01), Blankley et al.
patent: 4880804 (1989-11-01), Carini et al.
P. C. Wong et al, J. Pharmacol. Exp. Ther., 247(1), 1-7 (1988).
A. T. Chiu et al, European J. Pharmacol., 157, 13-21 (1988).
A. T. Chiu et al J. Pharmacol. Exp. Ther., 250(3), 867-874 (1989).

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