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US 11,628,154 B2Granted
CCL5 inhibitors
AssigneeLapko Inc
InventorBruce Kovacs
Life of this patent
Estimating the term…
Abstract
Compounds, pharmaceutically acceptable salts, esters, prodrugs, and pharmaceutical compositions thereof are disclosed that are useful for inhibition of the biological activity of CCL5 on mammalian cells, as well as methods of treatment for diseases involving the increased biological activity of CCL5.
Claims10
A compound according to Formula 1 or a tautomer thereof
- wherein:
- n is 0;
- p is 1;
- R1 and R2 are independently selected from H, OH, dichloroalkyl, trichloroalkyl, diidioalkyl, triidioalkyl, difluoroalkyl, C1-C8 straight or branched chain alkyl, C1-C8 cycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, optionally substituted C1-C8 alkenyl, optionally substituted C1-C8 alkynyl, optionally substituted aryl, optionally substituted alkylaryl, optionally substituted heteroaryl, optionally substituted alkylheteroaryl, O-alkyl, O-cycloalkyl, O-alkylcycloalkyl, O-aryl, O-optionally substituted aryl, alkyl-O-aryl, alkyl-O-optionally substituted aryl, C(O)-aryl, C(O)-optionally substituted aryl, CH2C(O)-aryl, CH2C(O)-optionally substituted aryl, O-(halogen)alkyl;
- R3, if present, is selected from C1-C2 straight or branched chain alkyl, C1-C8 cycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, optionally substituted C1-C2 alkenyl, optionally substituted C1-C2 alkynyl, optionally substituted aryl, optionally substituted alkylaryl, optionally substituted heteroaryl, or optionally substituted alkylheteroaryl;
- R4, R5, R6, R7, and R8, if present, are independently selected from H, C1-C8 straight or branched chain alkyl, C1-C8 cycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, optionally substituted C1-C8 alkenyl, optionally substituted C1-C8 alkynyl, optionally substituted aryl, optionally substituted alkylaryl, optionally substituted heteroaryl, or optionally substituted alkylheteroaryl, and/or adjacent substituents R1 and R2, R3 and R4, R5 and R6, R7 and R8, if present, may form a saturated or unsaturated 3-7 membered carbocyclic or heterocyclic ring;
- R9 is selected from B(OH)2, B(OR10)(OR11);
- R10 and R11, if present, are independently selected from optionally substituted alkyl, cycloalkyl, alkylcycloalkyl, and/or when R10 and R11 are present and adjacent to each other can together from an alkyl bridged 5 or 6 membered heterocyclic ring, or a pharmaceutically acceptable salt, ester or prodrug form thereof.
5 more elements
Dependencies are inferred from the claim text.