C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
260/15, 260/4, 2
C07J 31/00 (2006.01) C07J 51/00 (2006.01) C07J 53/00 (2006.01) C07J 63/00 (2006.01) C07J 71/00 (2006.01) C12P 33/08 (2006.01)
Patent
CA 1127630
ABSTRACT The invention provides corticoid-21-sulphopropionates and their salts, especially physiologically tolerable salts and pharmaceutical preparations containing them. They are distinguished in comparison with free 21- hydroxycorticoids by being readily soluble in water. In comparison with sodium salts of corticoid-21-hemisul- phates, -phosphates and -sulphobenzoates, the corres- ponding 21-(3-sulphopropionate) compounds are split in the body rapidly into the active ingredient, the 21- hydroxycorticoids, and in comparison with sodium salts of corticoid-21-hemisuccinates and -aminoacylates they are more stable in aqueous solution. Preferred compounds have the formula Image (II), in which Image represents a single or double bond, X represents hydrogen, chlorine, fluorine or methyl, Y represents hydrogen, fluorine or chlorine, Z represents oxo or .alpha.-hydrogen and .beta.-hydroxy, -U-V- represents-CH2CH2,-CH=CH- or Image and Image represents Image , Image Image or Image wherein R1 represents hydrogen, hydroxy or (C1-C8)- acyloxy, R2 represents hydrogen or methyl, and R3 and R4 each represent (C1-C4)alkyl, and especially the salts thereof.
336867
Esperling Peter
Kapp Joachim-Friedrich
Laurent Henry
Wiechert Rudolf
Marks & Clerk
Schering Aktiengesellschaft
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