Carbacyclins, processes for their preparation and their use...

Details Carbacyclins, processes for their preparation and their use... Carbacyclins, processes for their preparation and their use...

C - Chemistry, Metallurgy

07

C

167/205, 260/235

C07C 405/00 (2006.01) C07D 263/14 (2006.01) C07D 309/12 (2006.01)

Patent

CA 1275095

ABSTRACT The invention relates to carbacyclin derivatives of the general formula I: Image (I) where Y1 is the group -CH2-X-(CH2)n-R1 or the group Image n is 1 or 3, R1 is the group - Image , the group - Image . -COCH3, the group COOR2 where R2 is hydrogen or alkyl of 1 to 10 C-atoms optionally substituted by halogen, phenyl, C1-C4-alkoxy or C1-C4-dialkylamino, cycloalkyl, aryl or a heterocyclic group or the group CONHR3, where R3 is hydrogen or an alkanoyl or alkanesulfonyl group in each case with 1 to 10 C-atoms, R9 is the group -(CH2)m-R6 or the group -(CH2)m-o-[Z1-(CH2)m-p]x-[Z2-(CH2)m-q]y-R6 m = 2 to 20 and o, p and q ? 19, x and y = 0, 1 or 2, Z1 is a cis-CH=CH- group, a trans-CH=CH- group or a -C?C- group, in which each of these groups is separated from the C-9 carbon atom of the carbacyclin ring by a methylene group, Z2 is oxygen, sulphur, an NH- or an N-methyl group, R6 is amino, methylamino, hydroxy, carboxy or mercapto, X is an oxygen atom or a methylene group, Y2 is hydrogen or fluorine A is a -CH2-CH2-, trans-CH=CH- or -C?C- group W is a free or functionally modified hydroxymethylene group or a free or functionally modified Image group where the OH group may be in the .alpha. or .beta.-configuration, D is the group Image , a straight-chain saturated alkylene group of 1 to 5 C-atoms, a branched saturated alkylene group or a straight-chain or branched unsaturated alkylene group of 2 to 5 C-atoms which can be substituted by fluorine atoms. o is 1, 2 or 3, E is a direct bond, a -C?C-group or a -CH=CR7 group, where R7 represents a hydrogen atom, an alkyl group of 1 to 5 C-atoms or halogen, R4 is an alkyl group of 1 to 10 C-atoms, a cycloalkyl group of 3 to 10 C-atoms or an optionally substituted aryl group of 6 to 10 C-atoms or a heterocyclic group, and R5 is a free or functionally modified hydroxy group and when R2 is a hydrogen atom, its salts with physiologically acceptable bases, processes for their preparation and pharmaceuticals containing these compounds. 1059I

522586

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