Dea-steroids

Details Dea-steroids Dea-steroids

C - Chemistry, Metallurgy

07

C

260/362, 260/517

C07C 49/737 (2006.01) C07C 45/67 (2006.01) C07C 51/41 (2006.01) C07C 59/215 (2006.01) C07C 59/90 (2006.01) C07C 62/38 (2006.01) C07D 307/94 (2006.01) C07D 317/72 (2006.01) C07D 493/10 (2006.01)

Patent

CA 1195997

ABSTRACT Novel deA-steroids of the formula Image i , wherein R1 and R2 each represent a hydrogen atom or a lower alkyl group; R3 represents a hydrogen or halogen atom or a methyl group; R4 represents a hydrogen atom or, where R3 represents a methyl group, a hydrogen atom or a methyl group; R5 represents a hydrogen atom or a cyano, lower alkoxy or aryl-(lower alkoxy) group or a group of the formula SR7; or R3 and R5 together represent a methylene group; R6 represents a hydrogen atom or an acyl- thio group; R7 represents an acyl, alkyl or aralkyl group; X represents an oxo or methylene group; Y represents a hydrogen atom; Z represents a hydroxymethyl group or a group of the formula -COA; A represents a hydroxy group; or Y and A together represent a O-C bond; n stands for zero or 1 and the dotted bonds within the rings are optio..al; whereby each ring contains at most one double bond; the B-ring is 9(10)-unsaturated when the C-ring is 11(12)-unsaturated; at least one of R5 and R6 represents a hydrogen atom; R5 represents a hydrogen atom when R4 represents a methyl group; R5 represents a hydrogen atom or R3 and R5 together represent a methylene group and R6 represents a hydrogen atom when Z represents a carboxy group; R3 represents a hydrogen or halogen atom or a methyl group and R4 is absent when a 6(7)- or 7(8)-double bond is present; the 6(7)- and 11(12)-bonds are saturated when R6 represents an acylthio group; R1 is absent when a 9(10)-double bond is present; and the total of carbon atoms in R1 and R2 is at least 2, when simultaneously the B ring is saturated or 9(10)-unsaturated, the C and D rings are saturated, n stands for zero, Z represents a group of the formula -COA and R6 is hydrogen and sal's of said compounds in which Z represents a carboxy group, have aldosterone-antagonistic activity and can accordingly be used as medicaments. The novel deA-steroids can be manufactured by subjecting known deA-steroids to molecular transformations according to various methods.

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