Publication number: 20220213026
Abstract: Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Type:
Application
Filed:
February 14, 2020
Publication date:
July 7, 2022
Inventors:
Dean A. Wacker, Susheel Jethanand Nara, Srinivas Cheruku, Kandhasamy Sarkunam, Firoz Ali Jaipuri, Soodamani Thangavel, Rishikesh Narayan, Subba Reddy Bandreddy, Srinivas Jogi, Pavan Kalyan Kathi
Publication number: 20220081430
Abstract: Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, when Q is: (i) halo, cyano, hydroxyl, NRxRx, C(O)OH, C(O)NH2, C1-6 alkyl substiuted with zero to 6 R1a, or P(O)R1cR1c, or (ii) L R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R1a, R1c, R2, R3a, R3b, Rx, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Type:
Application
Filed:
February 14, 2020
Publication date:
March 17, 2022
Inventors:
Dean A. Wacker, Susheel Jethanand Nara, Srinivas Cheruku, Kandhasamy Sarkunam, Firoz Ali Jaipuri, Soodamani Thangavel, Rishikesh Narayan, Srinivas Jogi, Pavan Kalyan Kathi