HIV integrase inhibitors

A compound of Formula I, or pharmaceutically acceptable salts or solvates thereof

• 2245
• wherein:
• R1 is
• -phenyl substituted with 1-3 R4,
• -naphthyl, furanyl, thienyl, pyridyl, or imidazolyl unsubtituted or substituted with 1-3 R4,
• —C1-C6 alkyl-aryl unsubtituted or substituted with 1-3 R4, or
• —C1-C5 alkyl-O-aryl unsubtituted or substituted with 1-3 R4;
• R2 is
• —H,
• —C1-C6 alkyl,
• -aryl unsubstituted or substituted with 1-3 R4, or
• —C1-C6 alkyl aryl unsubstituted or substituted with 1-3 R4;
• R3 is
• —H,
• —C1-C6 alkyl,
• —C1-C6 alkyl-aryl unsubstituted or substituted with 1-3 R, or
• —OR9;
• R4 is independently selected from
• -halo,
• —CN,
• —C1-C6 alkyl,
• —C3-C6 cycloalkyl,
• —C1-C6 haloalkyl,
• —OR5,
• —CO2R6,
• —N(R7)(R8),
• —CON(R7)(R8),
• —SR5,
• —SOC1-C6alkyl, and
• —SO2C1-C6alkyl;
• R5 and R6 are independently selected from —H and —C1-C6 alkyl;
• R7 and R8 are independently selected from —H and —C1-C6 alkyl, or NR7R8 is a heterocycle selected from pyrrolidine, piperidine,
• 4-hydroxypiperidine, morpholine, thiomorpholine, piperazine, and 4-methylpiperazine;
• R9 is
• —H,
• —C1-C10 alkyl,
• —C1-C6 alkyl-aryl,
• —C2-C10 alkyl-OR5,
• —C1-C10 alkyl-CO2R6,
• —C1-C10 alkyl-N(R7)(R8),
• —C1-C10 alkyl-CON(R7)(R8), or
• —C1-C6 alkyl-heterocycle where the heterocycle is selected from pyrrolidine, piperidine, 4-hydroxypiperidine, morpholine, thiomorpholine, piperazine, 4-methylpiperazine, and thiazinanedioxide;
• B1 is selected from the group consisting of
• 2246
• R10 is
• —H,
• —C1-C6 alkyl,
• -cycloalkyl,
• —C1-C6 alkyl-aryl,
• -phenyl unsubstituted or substituted with 1-3 R12,
• benzofuran, dihydrobenzofuran, benzodioxane, or
• -heteroaryl selected from furan, thiophene, pyrrole, imidazole, oxazole, thiazole, and pyridine;
• R11 is
• —C1-C6 alkyl,
• -cycloalkyl,
• -aryl unsubstituted or substituted with 1-2 R4,
• —C1-C6 alkyl-aryl unsubstituted or substituted with 1-2 R4,
• —C1-C6 alkyl-heteroaryl where the heteroaryl is selected from furan, thiophene, pyrrole, imidazole, oxazole, thiazole, and pyridine,
• —C1-C6 alkyl-NR7R8,
• —C1-C6 alkyl-OR5,
• —C1-C6 alkyl-P(O)(OR6)2,
• —C1-C6 alkyl-CO2R6, or
• —C1-C6 alkyl-C(O)N(R7)(R8);
• R12 is
• halogen,
• —C1-C6 alkyl,
• —C1-C2 haloalkyl,
• —C1-C3 thioalkyl,
• —OR13,
• tetrahydrofuran,
• dihydropyran,
• —NR7R8,
• —CO2R6,
• —CONR7R8, or
• —CONHCH2Ph where Ph is unsubstituted or substituted with 1-2 R4;
• R13 is
• —H,
• —C1-C6 alkyl,
• —C1-C6 fluoroalkyl,
• allyl,
• propargyl,
• phenyl,
• benzyl,
• —COC1-C6alkyl,
• —CH2CO2R6, or
• —CH2CONR7R8.