C - Chemistry – Metallurgy – 07 – J
Patent
C - Chemistry, Metallurgy
07
J
C07J 41/00 (2006.01) A61K 31/56 (2006.01) C07J 43/00 (2006.01)
Patent
CA 2087953
2087953 9220700 PCTABS00017 The present invention concerns steroidic 5.alpha.-reductase inhibitors having formula (I), wherein Y is oxygen or sulphur; R is a group: a) -OR4, wherein R4 is hydrogen or a C1-C6 alkyl group; b) (1), wherein each of R5 and R6, independently, is hydrogen or a C1-C6 alkyl group; c) (2), wherein R7 is hydrogen or a C1-C6 alkyl group and W is a group: (i) (3), wherein R8 is a C1-C6 alkyl group, a C5-C6 cycloalkyl group, a C6-C9 cycloalkylalkyl group, a phenyl group or a benzyl group; or (ii) (4), wherein R9 is a C1-C6 alkyl group or a C5-C6 cycloalkyl group; or (iii) (5), wherein R5 and R6 are as defined above; (d) (6), wherein each of R10 and R11 is, independently, hydrogen or a C1-C6 alkyl group or taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen, and n is an integer of 2 to 4; R1 is hydrogen, a C1-C6 alkyl group, a C5-C6 cycloalkyl group, a C6-C9 cycloalkylalkyl group or an aryl group; each of R2 and R3 is, independently, selected from the group consisting of hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, C6-C9 cycloalkylalkyl and aryl or R2 and R3, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen; and the symbol (----) represents a single or a double bond provided that when it is a double bond the hydrogen in the 5.alpha. position does not exist and the pharmaceutically acceptable salts thereof. In view of their 5.alpha.-reductase inhibiting activity the compounds of the invention can be useful for the treatment of androgen dependent conditions.
Di Salle Enrico
Nesi Marcella
Panzeri Achille
Farmitalia Carlo Erba S.r.l.
Fetherstonhaugh & Co.
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