Inhibitors of the farnesoid X receptor and uses in medicine
AssigneesThe United States of America, as represented by the Secretary, Department of Health and Human Services, The Penn State Research Foundation
InventorsFrank J. Gonzalez, Changtao Jiang, Cen Xie, Andrew D. Patterson, Fei Li, James B. Mitchell
Life of this patent
Estimating the term…
Abstract
Disclosed are inhibitors of the farnesoid X receptor, for example of formula (I), wherein R1, R2, R4, X, Y, Z, m, and n are as defined herein, which are useful in treating or preventing obesity, type 2 diabetes/insulin resistance and non alcoholic fatty liver disease in a mammal in need thereof. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least Cone compound of the invention, a method of method of inhibiting a farnesoid X receptor in a mammal, and a method of treating or preventing obesity in a mammal.
Claims9
A method of treating a disease or disorder selected from obesity, type 2 diabetes, insulin resistance, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and alcoholic liver disease in a mammal in need thereof, comprising administering to the mammal an effective amount of a compound of formula (I):
- wherein R1 and R2 are independently selected from hydrogen, alkyl, and C(═O)R3,
- R4 is selected from hydrogen, alkyl, and C(═O)R3,
- X is selected from C═O and CH2,
- Y is selected from CH2, NR5, O, S, SO, SO2, and Se,
- or X and Y taken together form C═C,
- Z is selected from COOR6, SO3R7, P(═O)(OR8)2 and NR9R10,
- R3, R5, R6, R7, R8 R9, and R10 are independently selected from hydrogen, alkyl, and aryl,
- in is an integer of 1 to 6, and
- n is an integer of 1 to 6,
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.