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US 8,524,702 B2Granted
Substituted benzoazepines as toll-like receptor modulators
AssigneesVentiRx Pharmaceuticals, Inc., Array BioPharma Inc.
InventorsJames Jeffry Howbert, Gregory Dietsch, Robert Hershberg, Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
Life of this patent
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Abstract
Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
Claims20
A compound having the formula I:
- or a tautomer, enantiomer or salt thereof, wherein:
- Y is heteroaryl;
- R2 is selected from OR14 and NR6R7;
- R6 and R7 are each independently selected from H, alkyl, cycloalkyl, heterocycle or benzyl, wherein said alkyl, cycloalkyl, or benzyl is optionally substituted with one or more groups independently selected from —F, —OR8, —NR12SO2R13, —C(═O)NR12R13 or R6 and R7 together with the nitrogen atom to which they are attached form a heterocyclic ring, further wherein said heterocyclic ring is optionally substituted with one or more —OH;
- R8 is selected from hydrogen and alkyl, and
- R12, R13 and R14 are each independently selected from H and alkyl, wherein said alkyl is optionally substituted with —OH.
3 more elements
A compound having the formula III:
- or a tautomer, enantiomer or salt thereof, wherein
- T is CH, CZ, or N;
- U is CH, CZ, or N;
- V is CH, CZ, or N;
- X is CH, CZ, or N;
- W is CH, CZ, or N;
- R2 is selected from OR14 and NR6R7;
- R6 and R7 are each independently selected from H, alkyl, cycloalkyl, heterocycle or benzyl, wherein said alkyl, cycloalkyl, or benzyl is optionally substituted with one or more groups independently selected from —F, —OR8, —NR12SO2R13, —C(═O)NR12R13 or R6 and R7 together with the nitrogen atom to which they are attached form a heterocyclic ring, further wherein said heterocyclic ring is optionally substituted with one or more —OH;
- R8 is selected from hydrogen and alkyl,
- R12, R13 and R14 are each independently selected from H and alkyl, wherein said alkyl is optionally substituted with —OH;
- Z is selected from halogen, —CN, —CONR16R17, —COOR18, —CH═CHCOOR18, and —OR19;
- and
- R16, R17, R18, and a R19 are each independently selected from H, alkyl, and —CH2O(alkyl).
10 more elements
A compound selected from the Group consisting of:
- 132
- 133
- 134
- 135
- 141
- 142
- 143
- 144
- and tautomers, enantiomers and salts thereof.
6 more elements
Dependencies are inferred from the claim text.