| 摘要 |
<p>A class of non-peptidic biphenylalkyl xanthine compounds is described for use in treatment of cardiovascular disorders. Compounds of particular interest are angiotensin II antagonists of formula (I) wherein each of X?1 and X2¿ is independently selected from oxygen atom and sulfur atom; wherein m is one; wherein each of R?0 and R1¿ is independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, methoxycarbonylmethyl, methoxycarbonylethyl, cyclopropylmethyl, cyclopropylethyl, propenyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, 4-hydroxybutyl, 2-hydroxyethyl and 3-hydroxypropyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neopentyl, 2-cyclohexylethyl, benzyl, 2-phenylethyl, 3-phenylpropyl, cyclohexylmethyl, cyclohexyl, propoxy, butoxy, 1-butenyl, buten-2-yl, 3-butenyl, butyn-1-yl, butyn-2-yl, butyn-3-yl, propylthio and butylthio; wherein each of R3 through R11 is hydrido with the proviso that at lest one of R?5, R6, R8 and R9¿ is an acidic group selected from CO¿2?H, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, NHSO2CH3, NHSO2CF3, NHCOCF3, CONHSO2C6H5, CONHOH, CONHOCH3, CONHSO2CH3 and tetrazole; or a tautomer thereof or a pharmaceutically-acceptable salt thereof. These compounds are particularly useful in treatment or control of hypertension and congestive heart failure.</p> |
