Soft steroids having anti-inflamatory activity

C - Chemistry – Metallurgy – 07 – J

Patent

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260/7, 260/81

C07J 3/00 (2006.01) C07J 31/00 (2006.01) C07J 33/00 (2006.01) C07J 43/00 (2006.01)

Patent

CA 1174667

ABSTRACT OF THE DISCLOSURE The present invention provides compound having anti- flammtory activity selected from the group consisting of: a compound of the formula Image wherein R1 is a C1-C10 alkyl; C1-C10 (monohalo or polyhalo)- alkyl; or -CH2COOR6 wherein R6 is C1-C10 alkyl, or R1 is -CH2-Y-(lower alkyl) wherein Y is -S-, SO, S02 or -O-, or R1 is -CH2-O?R6 wherein R6 is C1-C10 alkyl or phenyl, R2 is C1-C10 alkyl, C3-C8 cycloalkyl, phenyl, benzyl or C1-C10 (monohalo or polyhalo)alkyl, R3 is hydrogen, .alpha.-hydroxy, .beta.-hydroxy, .alpha.-methyl, .beta.-methyl, =CH2, or .alpha.- or .beta.-O?OR2 wherein R2 is identical to R2 as defined hereinabove; R4 is hydrogen, fluoro or chloro; R5 is hydrogen, fluoro, chloro or methyl; X is -O- or -S- Z is carbonyl or .beta.-hydroxymethyl- ene; and the dotted line in ring A indicates that the 1,2 linkage is saturated or unsaturated; and a pharmaceutically acceptable quaternary ammonium salt of the compound represent- ed by said formlula wherein at least one of Rl and R2 is a halo- substituted alkyl group.

381293

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