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US 10,538,512 B2Granted
Aminoacylindazole immunomodulators for treatment of autoimmune diseases
AssigneeThe Rockefeller University
InventorsManish P. Ponda, Jan L. Breslow, Harold Selnick, Melissa Egbertson
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Abstract
2-Acylindazole compounds of formula I or formula II are disclosed: These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.
Claims18
A compound of formula I or formula II:
- wherein
- R1 is an optionally substituted bicyclic ring system chosen from an optionally substituted indole, isoindole, oxindole, tetrahydroindole, tetralin, indoline, isoindoline, tetrahydroquinoline, tetrahydroisoquinoline, 3,4-dihydro-1H-isochromene, 3,4-dihydro-2H-chromene, benzofuran, dihydrobenzofuran, tetrahydrobenzofuran, benzothiophene, tetrahydrobenzothiophene, indazole, tetrahydroindazole, 2,3-dihydro-1H-indene, naphthalene, tetrahydronaphthalene, and isochroman, said ring system attached to the carbonyl through a carbon, or, when R2 is amino, R1 may additionally be meta- or para-substituted phenyl or an optionally substituted monocyclic heteroaryl ring;
- wherein R1 is optionally substituted with one or more of halogen, hydroxy, amino, cyano, (C1-C8)hydrocarbyl, (C1-C8)hydrocarbyloxy, (C1-C4)alkylamino, di(C1-C4)alkylamino, (C1-C4)acylamino, (C1-C4)alkylsulfonyl, (C1-C4)fluoroalkyl, (C1-C4)fluoroalkoxy, (C1-C6)oxaalkyl, (C3-C6)carbocycle, and (C1-C4)alkenyl;
- R2 is chosen from hydrogen, amino and methyl;
- and
- R3 and R4 are chosen independently from hydrogen, halogen, hydroxy, amino, cyano, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylamino, di(C1-C4)alkylamino, (C1-C7)acylamino, ((C1-C7)hydrocarbyloxy)carbonylamino, (C1-C4)fluoroalkyl, (C1-C4)fluoroalkoxy, and (C1-C6)oxaalkyl, or, taken together, R3 and R4 on adjacent carbons form a double bond.
3 more elements
Dependencies are inferred from the claim text.