Aromatase inhibitors
AssigneeEndorecherche, Inc.
InventorsFernand Labrie, Yves Merand
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Abstract
Novel aromatase inhibitors are disclosed for use in therapeutic preparations for treatment of estrogen-dependent diseases. The compounds are specified 7.alpha.-substituted androstanedione and androstenedione derivatives which show a strong inhibitory activity towards aromatase. The invention includes synthesis and pharmaceutical compositions of said compounds.
Claims35
An aromatase-inhibiting compound represented by the following molecular structure:
- ##STR14## wherein the dotted line represents an optional double bond;
- wherein R.sub.7 is selected from the group consisting of alkenyl and alkynyl.
The compound 7.alpha.-allyl 4-androsten-3,17-dione:
- "EM 173" ##STR15##
The compound 7.alpha.-allyl-5.beta.-androstan-3,17-dione:
- "EM 176" ##STR16##
The compound 7.alpha.-allyl-5.alpha.-androstan-3,17-dione:
- "EM 198" ##STR17##
The compound 7.alpha.-propyl-5.alpha.-androstan-3,17-dione:
- "EM 199" ##STR18##
An aromatase-inhibiting compound having the following molecular structure:
- ##STR19## wherein B is methyl or ethyl;
- wherein the dotted line represents an optional double bond;
- and
- wherein R.sub.7 is selected from the group consisting of alkenyl and alkynyl.
The compound 7.alpha.-(2-propynyl)-4-androsten-3,17-dione:
- "EM-235" ##STR20##
Dependencies are inferred from the claim text.