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US 6,147,213 AGranted
Diastereomerically pure 3-oxo and 3-thioxo-4-aza-androstan derivatives and the use thereof as antiandrogens
AssigneePolichem SA
InventorsStefano Poli, Roberto Girardello, Vincenzo Olgiati, Ambrogio Magni, Paride Grisenti
Life of this patent
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Abstract
Disclosed are compounds of formula (A) ##STR1## wherein X, R.sub.1 and Y are as defined by the specification. The compounds are useful as antiandrogenic agents.
Claims3
A compound of formula (A):
- ##STR16## wherein:
- the carbon-carbon bond at the 1-2 position is single:
- X is an oxygen or a sulfur atom;
- R.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl residue;
- Y is the residue of an amino acid of formula ##STR17## wherein T is the group CH.sub.2 OH;
- Q represents the branching of .alpha. natural at amino acid of the (L) series or of the (D) series selected from the group consisting of glutamic acid, histidine, aspartic acid, leucine, phenylalanine, tryptophan, valine, asparagine and isoleucine.
3 more elements
A compound of formula (A) ##STR18## wherein:
- the carbon-carbon bond at the 1-2 position is single;
- X is an oxygen or a sulfur atom;
- R.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 alkyl residue;
- Y is the group --NH--M, wherein M is a member selected from the group consisting of .alpha.-methylbenzyl, .alpha.-ethylbenzyl, and .alpha.-propylbenzyl.
1 more element
A compound of formula (A):
- ##STR19## wherein:
- --X.dbd.O, R.sub.1 =CH.sub.3, Y=D(+)-.alpha.-methylbenzylamine, and the carbon atom at the .alpha.-position to the amine function is asymmetric.
Dependencies are inferred from the claim text.