Inhibitors of 17β-HSD1, 17β-HSD3 and 17β-HSD10
AssigneeUniversite Laval
InventorsDonald Poirier, Jenny Roy, Rene Maltais
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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.
Claims6
An inhibitor of 17β-HSD1, wherein the inhibitor is of the structure:
- wherein R is halo, —NH2, alkyl, —OCH2CH2Br, aralkyl, carboxy, —CH2-heterocyclyl, heterocyclyloyl, —C(O)N(R′)(R″) or —B(OH)2,
- wherein R′ and R″ are independently or simultaneously H or alkyl, or R′ and R″ are joined together, along with the nitrogen atom to which they are attached, to form a heterocyclic ring,
- or a pharmaceutically acceptable salt or tautomer thereof.
An inhibitor of 17β-HSD1, wherein the inhibitor is of the structure:
- or a pharmaceutically acceptable salt thereof.
A radiolabeled compound of 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.