Amidino compounds, their manufacture and methods of treatment

Details Amidino compounds, their manufacture and methods of treatment Amidino compounds, their manufacture and methods of treatment

C - Chemistry, Metallurgy

07

C

C07C 257/10 (2006.01) A61K 31/165 (2006.01) A61K 31/27 (2006.01) A61K 31/395 (2006.01) C07C 257/18 (2006.01) C07C 271/64 (2006.01) C07C 311/51 (2006.01) C07C 311/54 (2006.01) C07C 323/45 (2006.01) C07D 213/81 (2006.01) C07D 233/61 (2006.01) C07D 295/192 (2006.01)

Patent

CA 2070795

4-18681/A/CGC 1560 AMIDINO COMPOUNDS,THEIR MANUFACTURE AND METHODS OF TREATMENT Abstract of the Invention The invention relates to the compound of the formula Image and pharmaceutically acceptable salts thereof, in which: Rl 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; R2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, or is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; 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; Xl 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; wherein the phenyl rings of formula I may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical. The compounds are useful as selective LTB-4 receptor antagonists in the treatment of conditions or syndromes in mammals which are responsive to LTB-4 receptor antagonism.

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