17a, 21-diesters of the pregnane series

C - Chemistry – Metallurgy – 07 – J

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260/18, 260/69

C07J 41/00 (2006.01) C07J 5/00 (2006.01) C07J 43/00 (2006.01)

Patent

CA 1058610

ABSTRACT OF THE DISCLOSURE The specification describes compounds of the general formula:- Image (I) [wherein X represents a .beta.-hydroxy or keto group, Y represents a fluorine or chlorine atom, R1 represents a hydrogen atom or an alkyl group containing 1 - 3 carbon atoms, R2 represents a group of formula -(CH2)nNR3R4 (wherein n is 1, 2 or 3 and R3 and R4, which may be the same or different, each represents an alkyl group containing 1 - 4 carbon atoms or R3 and R4 together with the adjacent nitrogen atom form a saturated substituted or unsubstituted monocyclic 4 to 7 membered, heterocyclic ring, which may, if desired, further contain a sulphur or oxygen atom or another nitrogen atom) or R2 represents a substituted or unsubstituted monocyclic, 6-membered nitrogen- containing heterocyclic ring attached to the adjacent carbonyl group via a carbon atom of the ring, and --- represents a single or double bond] and their acid addition salts. The compounds described in the specification have both topical and systemic anti-inflammatory activity, an especially preferred compound being 9.alpha.-fluoro-11.beta.-hydroxy_ 16.beta.-methyl-21-morpholinoacetoxy-17-propionyloxy-prregna-1,4- diene-3,20-dione. The specification also describes a process for preparing the above compounds as well as pharmaceutical compositions containing such compounds.

232579

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