Tetralones with pharmacological activity, compositions...

C - Chemistry – Metallurgy – 07 – D

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Details

C07D 213/89 (2006.01) A61K 31/44 (2006.01) A61K 31/695 (2006.01) C07D 213/30 (2006.01) C07D 213/50 (2006.01) C07D 213/57 (2006.01) C07D 405/04 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2097045

ABSTRACT The present invention relates to new tetralones having the formula I: Image I wherein R1 and R2 independently represent hydrogen, C1-4 alkyl, hydroxy, C1-4 alkoxy, formyl, C1-4 alkylcarbonyl, C1-4 alkylthiocarbonyl, carboxyl, C1-4 alkoxycarbonyl, C1-4 alkoxythiocarbonyl, C1-4 alkylcarbonyloxy, C1-4 alkylthiocarbonyloxy, hydroxy-(C1-4) alkyl, mercapto-(C1-4) alkyl, perfluoro-(C1-4) alkyl, nitro, amino, cyano, halogen, trifluoromethoxy, ethynyl, trimethylsilylethynyl, C1-4 alkylsulfinyl, arylsulfinyl, C1-4 alkylsulfonyl, arylsulfonyl, C1-4 alkoxysulfinyl, C1-4 alkoxysulfonyl, C1-4 alkylcarbonylamino, C1-4 alkoxycarbonylamino, aminosulfinyl, aminosulfonyl, aminocarbonyl, aminothiocarbonyl, C1-4 alkylsulfinylamino, C1-4 alkylsulfonylamino, C1-4 alkoxysulfinylamino, C1-4 alkoxysulfonylamino, (C1-4 alkyl)carbonyl(C1-4 alkyl), nitro-(C1-4 alkyl), cyano-(C1-4 alkyl), (C1-4 alkyl)C(=NOH), (C1-4 alkyl)C(=NNH2) or (C1-4 alkoxy)C(=NH), the above amino groups, if required, being substituted by one or two C1-4 alkyl groups; R3 and R4 are the same or different and independently represent a C1-4 alkyl group, or R3 and R4 together form a C2-5 polymethylene chain; R5 is hydrogen and then R6 represents hydrogen, hydroxy or C1-4 alkoxy, or R5 is hydroxy and then R6 is hydrogen, or else R5 and R6 together with the ring carbons form a bond or a group of formula: Image R7 is a 2-, 3- or 4-pyridyl radical unsubstituted or substituted by a hydroxy group or whose nitrogen atom is in the form of the N- oxide; or a pharmaceutically acceptable salt or pharmaceutically acceptable solvate thereof. The invention also relates to processes for their preparation, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments. These compounds are antihypertensive and bronchodilator agents.

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