| 摘要 |
Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.; |
| 主权项 |
1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein: R1 is H, C1-6 alkyl, C1-6 fluoroalkyl, CycA, AryA, HetA, C1-6 alkyl substituted with CycA, C1-6 alkyl substituted with AryA, or C1-6 alkyl substituted with HetA; R2 is C1-6 alkyl-OH; Ring A is:wherein the asterisks (*) denote the points of attachment to the rest of the compound;
R3A is H, C1-6 alkyl, C1-6 haloalkyl, or CycB; R3B is H or C1-6 alkyl; R4A is:wherein the asterisk (*) denotes the point of attachment to the rest of the compound;
R4B is H or C1-6 alkyl; each XB and each XC are independently halo; m is an integer equal to 0 or 1; n is an integer equal to 0 or 1; R5 is C(O)—RK; RK is O—C1-6 alkyl or AryC; R6 is H or C1-6 alkyl; R7 is AryQ, HetQ, or HetQ; AryQ is an aryl which is independently phenyl, naphthyl, tetrahydronaphthyl, indenyl, or dihydroindenyl, wherein the aryl is optionally substituted with from 1 to 3 XA each of which is independently:
(1) C1-6 haloalkyl,(2) OH(3) halo,(4) NH2,(5) N(H)C(O)O—C1-6 alkyl,(6) C(O)—C1-6 alkyl,(7) C(O)NH2,(8) C1-6 alkyl substituted with:
(a) OH,(b) NH2, or(c) CH(O),(9) C1-6 haloalkyl substituted with OH,(10) HetD(11) C(O)-HetD, or(12) C1-6 alkyl substituted with HetD;with the proviso that no more than 2 XA are HetD, C(O)-HetD or C1-6 alkyl substituted with HetD; HetQ is a heteroaryl which is independently (i) a 5- or 6-membered heteroaromatic ring containing from 1 to 4 heteroatoms independently selected from N, O and S, wherein each N is optionally in the form of an oxide or (ii) a 9- or 10-membered bicyclic, fused ring system containing from 1 to 3 heteroatoms independently selected from N, O and S, and wherein at least one of the rings is aromatic, each N in a ring is optionally in the form of an oxide, and each S is optionally S(O) or S(O)2; and wherein the heteroaryl is optionally substituted with from 1 to 3 substituents selected from halo, NH2 and O—C1-6 alkyl; HetQ′ is independently a dihydro derivative of the heteroaryl defined in HetQ wherein the dihydro derivative is not or does not contain an aromatic ring; and wherein the derivative is optionally substituted with from 1 to 3 oxo substituents; CycA is a C3-7 cycloalkyl which is optionally substituted with from 1 to 3 halo substituents; CycB is a C3-7 cycloalkyl which is optionally substituted with from 1 to 3 substituents each of which is independently halo or C1-6 alkyl; AryA is an aryl which is independently phenyl or naphthyl, wherein the phenyl or naphthyl is optionally substituted with from 1 to 3 halo substituents; AryC is an aryl which is independently phenyl or naphthyl, wherein the phenyl or naphthyl is optionally substituted with from 1 to 3 halo substituents; HetA is a heteroaryl which is independently (i) a 5- or 6-membered heteroaromatic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, or (ii) is a fused, 9- or 10-membered heterobicyclic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, and wherein at least one of the rings is aromatic, each N in a ring is optionally in the form of an oxide, and each S is optionally S(O) or S(O)2; wherein the heteroaromatic ring (i) or the heterobicyclic ring (ii) is optionally substituted with from 1 to 3 YC wherein each YC independently
(1) C1-6 alkyl,(2)O—C1-6 alkyl, or(3) SO2—N(C1-6 alkyl)2; HetC is a heteroaryl which is independently (i) a 5- or 6-membered heteroaromatic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, or (ii) is a fused, 9- or 10-membered heterobicyclic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, and wherein at least one of the rings is aromatic, each N in a ring is optionally in the form of an oxide, and each S is optionally S(O) or S(O)2; wherein the heteroaromatic ring (i) or the heterobicyclic ring (ii) is optionally substituted with from 1 to 3 YD wherein each YD independently is C1-6alkyl or phenyl; and each HetD is independently a 5- or 6-membered heteroaromatic ring containing from 1 to 4 heteroatoms independently selected from N, O and S, wherein the heteroaromatic ring is optionally substituted with from 1 to 3 substituents each of which is independently C1-6 alkyl. |
