C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
167/233, 167/251
C07C 225/16 (2006.01) A61K 31/135 (2006.01) A61K 31/275 (2006.01) A61K 31/40 (2006.01) C07C 215/28 (2006.01) C07C 217/48 (2006.01) C07C 255/58 (2006.01) C07D 295/108 (2006.01) C07D 295/112 (2006.01)
Patent
CA 2016738
RAN 4450/52 Abstract The compounds of the general formula Image I wherein R1 and R2 each signify hydrogen, lower alkyl or lower alkenyl or together signify straight- -chain alkylene with 2 to 4 carbon atoms, R3 signifies hydrogen, halogen or lower alkyl, Q signifies alkylene with 2 to 11 carbon atoms and at least 2 carbon atoms between the two free valencies or alkenylene with 4 to 11 carbon atoms and at least 4 carbon atoms between the two free valencies and Y and Y' each signify a direct bond or the group -CH2-, -CH2CH2-, -CH=CH- or -C?C-, the group R1R2N-Q-CH2- is attached to the 3- or 4-position of the ring denoted by A and the symbol R signifies that the ring is unsubstituted or is substituted by halogen, trifluoromethyl, cyano, nitro, lower alkyl or lower alkoxy, and their pharmaceutically acceptable acid addition salts have valuable pharmacological properties. In particular, they have a pronounced antifungal activity and exhibit synergistic effects in combination with known antifungally-active substances which inhibit the sterol biosynthesis such as ketoconazole and terbinafine. The compounds of formula I can accordingly be used as medicaments, especially for the control or prevention of topical or systemic infections which are caused by pathogenic fungi.
Guerry Philippe
Jolidon Synese
Zurfluh Rene
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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