16-ALPHA, 17-ALPHA-ACETAL GLUCOCORTICOSTEROID DERIVATIVES AND THEIR APPLICATION

摘要

1. The compound of the formula! ! where R1 represents an oxygen atom; ! R2 represents a hydrogen, fluorine or chlorine atom; ! R3 represents a hydrogen, fluorine or chlorine atom or a methyl group; ! R4 is —C (O) —Y — R7; ! Y represents an oxygen or sulfur atom or a group NR8; ! R5 and R6, together with the carbon atoms to which they are attached, form a 1,3-dioxolanyl group substituted with a 5-10 membered aromatic or heteroaromatic ring system, optionally attached to the 1,3-dioxolanyl group via an alkylene, alkenylene or alkynylene linking group wherein the ring system itself is optionally substituted with one or more substituents independently selected from halogen, cyano, C1-C6 alkyl, C1-C6 alkoxy, trifluoromethyl and trifluoromethoxy; ! R7 represents a C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl group, each of which may optionally be substituted with one or more substituents independently selected from hydroxyl, halogen, cyano, nitro, C1-C6 alkyl, C2-C6 alkenyl, C1 -C6 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylcarbonyl, C1-C6 alkylcarbonyloxy, C1-C6 alkoxycarbonyl, -S (O) mR9, -NHR10 and -NR11; ! m is 0, 1 or 2; ! R8 represents a hydrogen atom, a group R7 or is attached to R7 to form a 3-8 membered, saturated or partially saturated heterocyclic ring, optionally containing an additional ring heteroatom selected from nitrogen, oxygen and sulfur, where the heterocyclic ring is optionally substituted with one or more one substituent independently selected from hydroxyl, halogen, cyano, nitro, C1-C6 alkyl, C2-C6 alkenyl, C1-C6 halogen