NOVEL COMPOSITIONS USEFUL FOR INHIBITING HIV-1 INFECTION AND METHODS USING SAME

摘要

The present invention includes novel compounds, and compositions comprising same, useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, comprising administering to the subject an effective amount of a compound and/or composition of the invention. In certain embodiments, the subject is further administered at least one additional therapeutic agent.

主权项

1. A compound of formula (I), or a salt or solvate thereof:wherein:
R1 is selected from the group consisting of ring A is selected from the group consisting of: wherein the atom labeled with A is linked to ring R1; linker L is selected from the group consisting of: wherein the atom labeled with B is linked to ring B; ring B is selected from the group consisting of: wherein rings C, D, and E are each independently absent or a monocyclic aryl or monocyclic heteroaryl ring optionally substituted; each occurrence of R2 and R3 is independently selected from the group consisting of —(C1-C6)alkyl, —(C1-C6)fluoroalkyl, —(C1-C6)heteroalkyl, —F, —Cl, —Br, —I, —CN, —NO2, —OR7, —SR7, —S(═O)R7, —S(═O)2R7, —NHS(═O)2R7, —C(═O)R7, —OC(═O)R7, —CO2R7, —OCO2R7, —CH(R7)2, —N(R7)2, —C(═O)N(R7)2, —OC(═O)N(R7)2, —NHC(═O)NH(R7), —NHC(═O)R7, —NHC(═O)OR7, —C(OH)(R7)2, and —C(NH2)(R7)2; R4 and R5 are each selected from the group consisting of —(C1-C6)alkyl, —(C1-C6)fluoroalkyl, —(C1-C6)heteroalkyl, —F, —Cl, —Br, —I, —CN, —NO2, —OR7, —SR7, —S(═O)R7, —S(═O)2R7, —NHS(═O)2R7, —C(═O)R7, —OC(═O)R7, —CO2R7, —OCO2R7, —CH(R7)2, —N(R7)2, —C(═O)N(R7)2, —OC(═O)N(R7)2, —NHC(═O)NH(R7), —NHC(═O)R7, —NHC(═O)OR7, —C(OH)(R7)2, and —C(NH2)(R7)2, heterocycloalkyl, aryl, and heteroaryl, wherein the heterocycloalkyl, aryl or heteroaryl may be optionally substituted; R6 is H or F; each occurrence of R7 is independently selected from the group consisting of H, —(C1-C6)alkyl, —(C1-C6)heteroalkyl, —(C1-C3)alkyl-(C3-C6)cycloalkyl, —(C4-C10)heterocyclyl, —(C1-C3)alkyl-(C4-C10)heterocyclyl, —(C6-C10)aryl, —(C1-C3)alkyl-(C6-C10)aryl, —(C5-C10)heteroaryl, and —(C1-C3)alkyl-(C5-C10)heteroaryl, wherein the alkyl, heteroalkyl, cycloalkyl, heterocycle, aryl, or heteroaryl group is optionally substituted; R8 is O or S; X and Y are independently CH or N; x is an integer from 0-5; y is an integer from 0-4; each occurrence of n is independently 0 or 1; wherein the compound is not (4-benzoylpiperazin-1-yl)(1,2-dihydroacenaphthylen-5-yl)methanone (SC03).