C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 403/10 (2006.01) A61K 31/41 (2006.01) A61K 31/44 (2006.01) A61K 31/675 (2006.01) C07D 249/08 (2006.01) C07D 249/10 (2006.01) C07D 401/14 (2006.01) C07D 405/00 (2006.01) C07D 409/14 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 521/00 (2006.01) C07F 9/547 (2006.01)
Patent
CA 2082074
A class of 1H-substituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders, especially cardiovascular disorders. Compounds of interest are angiotensin II antagonists of formula Image wherein R1 is selected from hydroxy, formyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, n-hexyl, n-heptyl, n-octyl, n-nonyl, carboxyethyl, phenyl, benzyl, phenethyl, cyclopentyl, cyclohexyl, cyclopentylmethyl, cyclohexylmethyl, cyclohexylethyl, cyclohexylpropyl, adamantyl, adamantylmethyl, 1-oxoethyl, 1- oxopropyl, 1-oxobutyl, 1-oxopentyl, dimethoxymethyl, diethoxymethyl, 1,1-dimethoxypropyl, 1,1-dimethoxybutyl, 1,1-dimethoxypentyl, hydroxypropyl, halo, monofluorormethyl, difluoromethyl, 1,1- difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1- difluoropentyl, pentafluoroethyl, heptafluoropropyl, phenylacetyl, phenyldifluoroethyl, aminomethyl, aminoethyl, aminopropyl, acetyl- aminomethyl, t-butoxycarbonylaminoethyl, glutamic acid methyl ester and glutamic acid ethyl ester; wherein R2 is selected from carboxyethyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl and neopentyl; wherein each of R3 through R11 is hydrido with the proviso that at least one of R5 and R9 must be selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH Image wherein each of R40 and R41 is independently selected from chloro, cyano, nitro, trifluoro-methyl, methoxycarbonyl and trifluoromethylsulfonyl. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.
G.d. Searle & Co.
Osler Hoskin & Harcourt Llp
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