SUBSTITUTED AMIDINO COMPOUNDS, AND PHARMACEUTICAL COMPNS. CONTG. THE SAID COMPDS.

摘要

PCT No. PCT/US93/10876 Sec. 371 Date Jul. 25, 1995 Sec. 102(e) Date Jul. 25, 1995 PCT Filed Nov. 12, 1993 PCT Pub. No. WO94/11341 PCT Pub. Date May 26, 1994 (I) The invention relates to the compounds of formula (I) wherein the C(=NH)-NHR3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X1 and X3, independently of one another, are oxygen (-O-) or sulphur (-S-); and X2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical. The compounds are useful as selective LTB4 receptor antagonists in the treatment of conditions or syndromes in mammals which are responsive to LTB4 receptor antagonism.