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US 12,735,402 B2Granted
PAI-1 inhibitors and uses thereof
AssigneeThe Cleveland Clinic Foundation
InventorsVara Prasad Josyula, Thaddeus Stappenbeck
Life of this patent
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Abstract
Disclosed herein are compounds, pharmaceutical compositions comprising the compounds, methods of inhibiting PAI-1 using the compounds, and methods of treating IBDs using the compounds.
Claims8
A compound of formula (Ia):
- or a pharmaceutically acceptable salt thereof, wherein:
- R2 is H, halo, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, C1-C4 alkoxy, C1-C4 haloalkyl, or C1-C4 haloalkoxy;
- R3 is H, halo, or C1-C4 alkyl;
- wherein R2 and R3 are optionally taken together with the carbon atoms to which they are attached to form a 5-or 6-membered ring optionally substituted with 1 or 2 substituents independently selected from C1-C4 alkyl, halo, and oxo;
- X6 is CR6 or N;
- R6 is H, halo, or C1-C4 alkyl;
- and
- R8 is a group of formula:
- wherein Rx is —(CH2)n—Y or a monocyclic heterocyclyl having 1 or 2 heteroatoms independently selected from O and N, wherein the monocyclic heterocyclyl is unsubstituted or substituted with 1 C1-C4 alkyl group, wherein n is 1 or 2, and Y is selected from —COORg and —NRhRi, wherein Rg, Rh, and Ri are each independently selected from H and C1-C4 alkyl.
6 more elements
A compound:
- 4-chloro-2-[[3-(1-tetrahydropyran-4-ylpyrazol-4-yl)benzoyl]amino]benzoic acid,
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.