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US 5,212,166 AGranted
Unsaturated 17.beta.-subsituted 3-carboxy steroids
AssigneeFarmitalia Carlo Erba S.p.A.
InventorsAchille Panzeri, Marcella Nesi, Enrico Di Salle
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AssigneeFarmitalia Carlo Erba S.p.A.
InventorsAchille Panzeri, Marcella Nesi, Enrico Di Salle
Estimating the term…
The present invention concerns steroidic 5.alpha.-reductase inhibitors having the following formula (I) ##STR1## wherein Y is oxygen or sulphur; R is a group; a) --OR.sub.4, wherein R.sub.4 is hydrogen or a C.sub.1 -C.sub.6 alkyl group; b) ##STR2## wherein each of R.sub.5 and R.sub.6, independently, is hydrogen or a C.sub.1 -C.sub.6 alkyl group; c) ##STR3## wherein R.sub.7 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and W is a group: (i) ##STR4## wherein R.sub.8 is a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalky group, a C.sub.6 -C.sub.6 cycloalkylalkyl group, a phenyl group or a benzyl group; or (ii) ##STR5## wherein R.sub.9 is a C.sub.1 -C.sub.6 alkyl group or a C.sub.5 -C.sub.6 cycloalkyl group; or (iii) ##STR6## wherein R.sub.5 and R.sub.6 are as defined above; d) ##STR7## wherein each of R.sub.10 and R.sub.11 is, independently, hydrogen or a C.sub.1 -C.sub.6 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; R.sub.1 is hydrogen, a C.sub.1 -C.sub.6 alkyl group, a C.sub.5 -C.sub.6 cycloalkyl group, a C.sub.6 -C.sub.9 cycloalkyalkyl group or an aryl group; each of R.sub.2 and R.sub.3 is, independently, selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.9 cycloalkylalkyl and aryl or R.sub.2 and R.sub.3, 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 doesn't 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.
A compound of the following formula (I) ##STR48## wherein Y is oxygen or sulphur;
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.