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US 2021/0196665 A1Published application
CCL5 Inhibitors
AssigneeAfecta Pharmaceuticals, 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.
Claims24
-32. (canceled)
A compound according to Formula 1 or a tautomer thereof
- wherein:
- n and p are independently selected from 0 or 1;
- R1 and R2 are independently selected from H, OH, F, Cl, Br, I, (halogen)alkyl, 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, CH2C(O)-aryl, CH2C(O)-optionally substituted aryl, O-(halogen)alkyl, C(O)-optionally substituted aryl, wherein the optional substituent of the aryl is selected from oxo, fluorine, bromine, iodine, —CN, —NH2, —OH, —NH(CH3), —N(CH3)2, alkyl (including straight chain, branched and/or unsaturated alkyl), substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, fluoroalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted alkoxy, fluoroalkoxy, —S-alkyl, —S(O)2-alkyl, —CONH((substituted or unsubstituted alkyl) or (substituted or unsubstituted phenyl)), —CON(H or alkyl)2, —OCON(substituted or unsubstituted alkyl)2, —NHCONH((substituted or unsubstituted alkyl) or (substituted or unsubstituted phenyl)), —NHCOalkyl, —N(substituted or unsubstituted alkyl)CO(substituted or unsubstituted alkyl), —NHCOO(substituted or unsubstituted alkyl), —C(OH)(substituted or unsubstituted alkyl)2, and —C(NH2)(substituted or unsubstituted alkyl)2;
- R3, 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, optionally substituted alkylheteroaryl, and wherein 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 COOH, COO-straight or branched chain alkyl;
- or a pharmaceutically acceptable salt, ester or prodrug form thereof with the proviso that when n and p are both 0, R1 is H, R3 is methyl, R4 is methyl, and R9 is COOH, COOCH3, or COOC2H5, then R2 cannot be Cl, and when n and p are both 0, R2 is H, R3 is methyl, R4 is methyl, and R9 COOH, COOCH3, or COOC2H5, then R1 cannot be Cl.
3 more elements
Dependencies are inferred from the claim text.