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US 11,692,005 B2Granted
TLR7 agonists
AssigneePrimmune Therapeutics, Inc.
InventorsStephen E. Webber, James Richard Appleman
Life of this patent
Estimating the term…
Abstract
The present invention relates to TLR7 agonists according to Formula I and their use in the treatment of diseases such as cancer and infectious disease.
Claims20
A compound having the structure of Formula I:
- wherein
- R1 is independently —H, —OH, —O—C(O)—R8 or —F,
- R2 is independently —H, —OH, —O—C(O)—R8 or —F,
- R3 is —OH, or —O—C(O)—R8,
- R4 is —H, —OH, —O—C(O)—R8 or —(C1-C8)alkyl,
- wherein R3 and R4 can be in the form of a carbonyl oxygen (═O),
- R5 is —H, —OH, —O—C(O)—R8, —(C1-C8)alkyl, —O—(C1-C8)alkyl, —NH2 or —NHR8
- wherein R4 and R5 can form a 3-6 membered cycloalkyl ring,
- R6 is —H, —(C1-C8)alkyl, —C(H)═CH2, —C(H)═CH(C1-C8)alkyl), —C(H)═C(C1-C8)alkyl)(C1-C8)alkyl), —C(H)═C═CH2, —C(H)═C═C(C1-C8)alkyl)H, —CH2C≡CH, —OH or —O(C1-C8)alkyl,
- R7 is —H, —OH, —OCH3, —SH or —Cl,
- R8 is independently —(C1-C8)alkyl, aryl, —(CH2)n(aryl), heteroaryl or —(CH2)n(heteroaryl),
- n is an integer 1, 2, 3, 4 or 5,
- wherein at least one R4 or R5 is not —H,
- wherein each alkyl, cycloalkyl, aryl and heteroaryl are independently optionally substituted by one or more of CN, NO2, halogen, (C1-C3)alkyl, (C1-C3)haloalkyl, (C1-C3)cycloalkyl, aryl, heteroaryl, OH, alkenyl, alkynyl, O—(C1-C3)alkyl, O—C(O)—R9, O-(alkylene)aryl, O-(alkylene)heteroaryl, C(O)R9, S(C1-C8)alkyl, S(O)(C1-C8)alkyl, SO2(C1-C8)alkyl, C(O)OR9, C(O)NR9R9, C(O)NR9SO2(C1-C8)alkyl, NR9R9, NR9(CO)OR9, NH(CO)R9, NH(SO2)(C1-C8)alkyl or NH(SO2)NR9R9, and R9 is independently —H, —OH, —(C1-C8)alkyl, cycloalkyl, heterocyclyl, or the two R9's of C(O)NR9R9 or NR9R9 combine together with the nitrogen atom to form a heterocycle;
- or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof.
12 more elements
Dependencies are inferred from the claim text.