7-oxoprostacyclin derivatives and process for the...

C - Chemistry – Metallurgy – 07 – D

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C07D 307/935 (2006.01) C07C 17/08 (2006.01) C07C 57/03 (2006.01) C07C 57/13 (2006.01) C07C 57/52 (2006.01) C07D 307/937 (2006.01) C07D 407/12 (2006.01) C07F 9/40 (2006.01) C07F 9/535 (2006.01)

Patent

CA 1220470

ABSTRACT OF THE DISCLOSURE Prostacyclin, although having a useful dilating effect on blood vessels, is not sufficiently stable to ensure successful use as a hypotensive agent. A 7-oxopro- stacyclin derivative of the general formula Image in which R3 represents a hydrogen atom, a straight-chain or branched-chain alkyl radical having from 1 to 4 carbon atoms, or a C1-C4-alkoxyalkyl radical, W represents a Image group, the hydroxy group of which may be free or substituted by a C1-C4-alkanoyl group or a tetrahydropyranyl group and may be in the ?- or .beta.-position, R2 represents a straight-chain or branched-chain halogen-substituted alkyl group having from 3 to 7 carbon atoms, a straight-chain or branched-chain alkenyl radical having from 3 to 7 carbon atoms which can be substituted by fluoro, chloro or a C1-C4-alkyl group, or a straight-chain or branched-chain alkynyl radical having from 2 to 6 carbon atoms which may be substituted in the 1- position by fluorine or C1-C4-alkyl, and R5 represents a hydroxy group or a tetrahydropyranyl group or a pharmaceu- tically acceptable salt thereof has proved to have not only a hypotensive and bronchodilative action, for example, but also an increased stability over prostacyclin. Advantages in medicinal use over other prostaglandins have also been found.

386074

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