Patent ID: 6489320
Filing Date: 2002-12-03
Classification: A61P,C07D

Abstract:
A method of treating HIV infection which comprises administering, in combination, to a host in need thereof a therapeutically effective amount of:(a) a compound of formula (I): â€ƒor a stereoisomer or pharmaceutically acceptable salt form thereof, wherein: A is O or S; W is N or CR3; X is N or CR4; Y is N or CR5; Z is N or CR6; provided that if two of W, X, Y, and Z are N, then the remaining are other than N; Ra is selected from H, CF3CF2H, C1-4 alkyl, C3-5 cycloalkyl, C2-4 alkenyl, C2-4 alkynyl, and phenyl substituted with 0-2 R10; Rb is selected from H, CF3, CF2H, C1-4 alkyl, C3-5 cycloalky, C2-4 alkenyl, C2-4 alkynyl, and phenyl substituted with 0-2 R10; alternatively, Ra and Rb together form â€”(CH2)nâ€”; R1 is selected from CF3, CF2H, C1-4 alkyl, C3-5 cycloalkyl, C2-4 alkenyl, and C2-4 alkynyl; R2 is selected from â€”Câ‰¡Câ€”R8, â€”CH&boxH;CR7R8, â€”(CH2)pCHR7R8, â€”CHR7Câ‰¡Câ€”R8, â€”CHR7CH&boxH;CHR8, and CH&boxH;CHCHR7R8; provided that when either of Ra or Rb is phenyl, then R1 is other than C1-4 alkyl and C3-5 cycloalkyl and R2 is other than â€”(CH2)pCHR7R8; R3 is selected from H, F, Cl, Br, I, C1-3 alkoxy, and C1-3 alkyl; R4 is selected from H, F, Cl, Br, I, C1-3 alkyl substituted with 0-3 R11, C2-3 alkenyl, C2-3 alkynyl, C1-3 alkoxy, OCF3, â€”CN, NO2, CHO, C(O)CH3, C(O)CF3, C(O)NH2, C(O)NHCH3, NR7R7a, NR7C(O)OR7b, C(O)OR7, S(O)pR7, SO2NHR7, NR7SO2R7b, phenyl substituted with 0-2 R10, and 5-6 membered aromatic heterocycle system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-2 R10; alternatively, R3 and R4 together form â€”OCH2Oâ€”; R5 is selected from H, F, Cl, Br, and I; alternatively, R4 and R5 together form a â€”OCH2Oâ€” or a fused benzo ring; R6 is selected from H, OH, C1-3 alkoxy, â€”CN, F, Cl, Br, I, NO2, CF3, CHO, C1-3 alkyl, and C(O)NH2; R7, at each occurrence, is selected from H and C1-3 alkyl; R7a, at each occurrence, is selected from H and C1-3 alkyl; R7b, at each occurrence, is C1-3 alkyl; R8, at each occurrence, is selected from H, C1-6 alkyl substituted with 0-3 R11, CH(â€”OCH2CH2Oâ€”), C2-6 alkenyl, C3-7 cycloalkyl substituted with 0-2 R9, phenyl substituted with 0-2 R10, and 5-6 membered aromatic heterocycle system containing from 1-4 heteroatoms selected from the group consisting of N, O, and S and substituted with 0-2 R10; R9, at each occurrence, is selected from D (2H), OH, C1-3 alkoxy, C1-3 alkyl, and F; R10, at each occurrence, is selected from OH, C1-3 alkyl, C1-3 alkoxy, F, Cl, Br, I, CN, NR7R7a, and C(O)CH3; R11, and each occurrence, is selected from OR7, CN, F, Cl, Br, I, NO2, NR7R7a, CHO, C(O)CH3, C(O)NH2; n, at each occurrence, is selected from 1, 2, 3, 4, and 5; and, p, at each occurrence, is selected from 0, 1, and 2; and (b) at least one compound selected from the group consisting of HIV reverse transcriptase inhibitors and HIV protease inhibitors.