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US 2020/0369677 A1Published application
Pyranopyrazole and pyrazolopyridine immunomodulators for treatment of autoimmune diseases
AssigneeThe Rockefeller University
InventorsManish P. PONDA, Harold SELNICK, Melissa EGBERTSON, Jan L. BRESLOW
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Abstract
Pyranoyrazoles and pyrazolopyridines of formula I or formula II are disclosed: These compounds inhibit Coagulation Factor XIIa in the presence of thrombin and other coagulation factors. They are useful to treat autoimmune diseases.
Claims32
A compound of formula I or formula II:
- wherein
- R1 is an optionally substituted bicyclic ring system;
- R2 is chosen from hydrogen, halogen, hydroxy, amino, cyano, (C1-C4)alkyl, (C1-alkoxy, (C1-C4)alkylamino, di(C1-C4)alkylamino, (C1-C4)acylamino, (C1-C4)fluoroalkyl, (C1-C4)fluoroalkoxy, and (C1-C6)oxaalkyl;
- one of X1 and X2 is chosen from —O—, and —N(QR5)—, and the other is —CR3R4—;
- Q is chosen from a direct bond, —CH2—, —C(═O)—, —C(═O)O—, —C(═O)NR6—, —SO2—, and —SO2NR6—;
- R3, R4, R6 and R7 are independently chosen from hydrogen and (C1-C6)alkyl;
- and
- R5 is chosen from hydrogen, (C1-C6)alkyl, hydroxy(C2-C6)alkyl, a three- to seven-membered carbocycle, and a three- to seven-membered heterocycle.
5 more elements
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Dependencies are inferred from the claim text.