INHIBITORS OF 17Beta-HSD1, 17Beta-HSD3 AND 17Beta-HSD10
AssigneeUniversite Laval
InventorsDonald Poirier, René Maltais, Jenny Roy
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Abstract
The present application discloses 17β hydroxy steroid dehydrogenase (17β HSD) type 1, 3, 10 inhibitors and use thereof (alone and in combination) in the treatment of cancer and other afflictions. 17β HSD1 inhibitors include estradiol derivatives with a nieta-carbamoylbenzyl substituent at C 16. 17β HSD3/HSD10 inhibitors include androsterone derivatives substituted at the C3 position with a sulfonamide piperazine. Also disclosed are compounds that are inhibitors of both 17β HSD1 and 17β HSD3 that have a spiro-morpholine substituent at C20.
Claims47
An inhibitor of 17β-HSD1.
An inhibitor of 17β-HSD3.
An inhibitor of 17β-HSD1 and 17β-HSD3.
An inhibitor of 17β-HSD10.
A radiolabelled compound comprising the structure
- wherein X is I123, I125, I131 or Br76, or a pharmaceutically acceptable salt or tautomer thereof.
A radiolabelled compound comprising the structure
- wherein X is I123, I125, I131 or Br76, or a pharmaceutically acceptable salt or tautomer thereof.
Dependencies are inferred from the claim text.