C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
260/68, 260/9
C07J 5/00 (2006.01) C07J 21/00 (2006.01) C07J 31/00 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01) C07J 71/00 (2006.01)
Patent
CA 1118411
Abstract of the Disclosure: This invention relates to corticoid 17-(alkyl carbonates) of the formula (I) Image wherein A denotes the groupings Image , Image , Image C = O or, if a double bond is present in the 9,11-position, C - H, Y denotes hydrogen, fluorine or chlorine, Z denotes hydrogen, chlorine, fluorine or a methyl group, R1 denotes hydrogen, an acyl radical of the formula II Image (II) wherein R4 denotes hydrogen or a straight-chain or branched aliphatic hydrocarbon radical having 1 - 10 C atoms or a cyclo- aliphatic hydrocarbon radical having 3-8 C atoms and n represents the numbers 0 - 4, or, if n ? 0, R4 represents halogen or a radical of the formula - Image wherein R' and R" are identical or different and denote hydrogen or alkyl radicals having 1 - 4 C atoms, or R' and R" together with the nitrogen atom represent a saturated heterocyclic structure having 5 - 7 members, or R1 denotes a carbonyloxyalkyl radical of the formula III Image (III) wherein n and R4 have the indicated meaning and R4 ? H when n is 0 and can denote only halogen when n is 2 - 4, or an aliphatic or aromatic sulfonic acid ester of the formula IV Image (IV) wherein R5 denotes C1-C4-alkyl, phenyl, methylphenyl, ethyl-phenyl, fluorophenyl, bromophenyl or chlorophenyl, R2 denotes a branched or unbranched alkyl radical having 1 to 8 C atoms and R3 denotes hydrogen, methyl in the .alpha.- or .beta.-position, fluorine or a methyl group which is optionally substituted by one or two fluorine atoms, and in which additional double bonds can be present in at least the 1,2-, 2,3-, 6,7- and 9,11-positions, and in which Image denotes a pyrazole ring which is fused to the 2- and 3-positions of the 3- deoxo-steroid skeleton and can optionally carry a C1-C4-alkyl group or an optionally halogen-substituted phenyl group on one of the two N atoms. The compounds can be used in veterinary therapy and human therapy, in the form of suspensions, ointments, creams, sprays and the like, for the treatment of inflammatory dermatoses of very diverse cause.
308719
Alpermann Hans G.
Fritsch Werner
Stache Ulrich
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Hoechst Aktiengesellschaft
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