Inhibitors of lysyl oxidases
AssigneeUniversity of South Carolina
InventorsOzgur Sahin, Campbell McInnes, Ozge Saatci, Chad Beneker, Abdol-Hossein Rezaeian, Metin Cetin
Life of this patent
Estimating the term…
Abstract
Described herein are compounds that block the activity of LOX family members having good IC50 values, no cellular toxicity below 10 μM, induce sensitization of the cells to doxorubicin, strong activity in a recombinant LOX/LOXL2 activity, and a chemical structure that is drug-like and does not have a PAINS flag, as well as, methods of treatment using the compounds with respect to cancer, organ fibrosis, neurodegenerative and cardiovascular diseases.
Claims17
A method for inhibiting lysyl oxidase comprising:
- administering to a subject in need thereof a therapeutically effective amount of a compound or its pharmaceutically acceptable salt having the following formula:
- wherein:
- R2 is H or NH2;
- R3 is H or CH3;
- and
- R6 is NHCOCH3, NO2, OCH3, OCH2CH3, or OH;
- wherein the compound or its pharmaceutically acceptable salt inhibits lysyl oxidase activity in the subject.
A method for inhibiting lysyl oxidases comprising:
- contacting a cell with an effective amount of a compound or its pharmaceutically acceptable salt having the following formula:
- wherein:
- R2 is H or NH2;
- R3 is H or CH3;
- and
- R6 is NHCOCH3, NO2, OCH3, OCH2CH3, or OH;
- wherein the compound or its pharmaceutically acceptable salt inhibits lysyl oxidase activity in the cell.
A therapeutic composition comprising a pharmaceutically acceptable carrier and a compound or its pharmaceutically acceptable salt having the following formula:
- wherein:
- R2 is H or NH2;
- R3 is H or CH3;
- and
- R6 is NHCOCH3, NO2, OCH3, OCH2CH3, or OH.
A method for forming a therapeutic composition, the method comprising:
- combining a pharmaceutically acceptable carrier with a compound or its pharmaceutically acceptable salt having the following formula:
- wherein:
- R2 is H or NH2;
- R3 is H or CH3;
- and
- R6 is NHCOCH3, NO2, OCH3, OCH2CH3, or OH.
Dependencies are inferred from the claim text.