Lipoxygenase inhibitors
AssigneeSRI International
InventorLing Jong
Life of this patent
Estimating the term…
Abstract
The disclosure provides bisindole suitable for inhibiting lipoxygenases or Aβ-formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation.
Claims13
A method of inhibiting a lipoxygenase selected from the group consisting of:
- 5-lipoxygenase, 12-lipoxygenase, 15-lipoxygenase, and a combination thereof in cells determined to be in need thereof, comprising contacting the cells with a bisindole of a formula selected from:
- or a salt thereof.
A method of treating a person for a neurodegenerative disease selected from Alzheimer's disease, dementia and amyloid beta (Aβ) associated disease by inhibiting lipoxygenase activity, comprising-inhibiting lipoxygenase in cells of the person, the lipoxygenase selected from the group consisting of:
- 5-lipoxygenase, 12-lipoxygenase, 15-lipoxygenase, and a combination thereof, by contacting the cells with a composition comprising a bisindole of a formula selected from:
- or a salt thereof.
A method of inhibiting a lipoxygenase selected from the group consisting of:
- 5-lipoxygenase, 12-lipoxygenase, 15-lipoxygenase, and a combination thereof in cells determined to be in need thereof, comprising contacting the cells with a bisindole of formula (I):
- wherein:
- R1, R3, R4, R5, R7, and R8 are hydrogen;
- R2 and R6 are fluorine;
- R9 are substituents independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C5-C10 aryl, C6-C10 alkaryl, C6-C10 aralkyl, halo, hydroxyl, sulfhydryl, C1-C10 alkoxy, C2-C10 alkenyloxy, C2-C10 alkynyloxy, C5-C10 aryloxy, C2-C10 alkoxycarbonyl, C6-C10 aryloxycarbonyl, C2-C10 alkylcarbonyl, C6-C10 arylcarbonyl, halocarbonyl, C2-C10 alkylcarbonato, C6-C10 arylcarbonato, carboxy, carboxylato, carbamoyl, mono-(C1-C10 alkyl)-substituted carbamoyl, di-(C1-C10 alkyl)-substituted carbamoyl, thiocarbamoyl, carbamido, cyano, isocyano, cyanato, isocyanato, di-(C1-C10)-alkoxyboryl, isothiocyanato, azido, amino, mono- and di-(C1-C10 alkyl)-substituted amino, mono- and di-(C5-C10 aryl)-substituted amino, C2-C10 alkylamido, imino, alkylimino, nitro, sulfo, sulfonato, C1-C10 alkylsulfanyl, C1-C10 alkylsulfinyl, C1-C10 alkylsulfonyl, C5-C10 arylsulfonyl and combinations thereof;
- and
- R11 and R12 are hydrogen or methyl;
- and
- R10 is:
- or a salt of the bisindole.
Dependencies are inferred from the claim text.