HIV protease inhibitors useful for the treatment of aids

Claim 2

Compounds of the formula: A-G-B-B-J I, wherein A is 1) wherein R 1 is a) C 1-6 alkyl either unsubstituted or substituted with one or more of i) C I - 4 alkyl; ii) hydroxy; iii) carboxy; iv) halo wherein halo is F, Cl, Br, or I; except no halo on carbon adjacent to carbonyl; v) amino; vi) Ci-3 alkoxycarbonyl; vii) Ci- 3 alkoxy; viii) -CONR 2 R 3 wherein R 2 and R 3 are the same or different and are hydrogen, Ci-5 alkyl or C 1-5 alkoxyalkyl or joined together either directly to form a 5-7 membered heterocycle, or through a heteroatom selected from N, 0, and S, to form a 6-membered heterocycle with the nitrogen to which they are attached; ix) -NR2R 3; X) wherein, R is hydrogen or Ci- 4 alkyl, Pis and R 4 is H, Ci-3 alkyl, C 1-4 alkoxy, or NR 2 R 3 ; xi) C 3 - 7 cycloalkyl or C 6-1 aryl; xii) 5 or 6 membered heterocycle, unsubstituted or substituted with OH, NH or Ci- 4 alkyl; or xiii) aryl of 6-10 carbon atoms, either unsubstituted or substituted with one or more of (a) halo, (b) hydroxy, (c) Ci- 3 alkoxy, (d) C 1-3 alkyl, (e) -NR 2 , wherein R is defined above, (f) (g) (h) -S0 2 NR 2 , (i) -CH 2 NR 2 , (j) or (k) xiv) -OSiR 3 (R 2 ) 2 b) aryl of 6-10 carbon atoms, either unsubstituted or substituted with one or more of i) C 1-4 alkyl, ii) C 1-3 alkoxy, iii) hydroxy, or iv) halo; v) -NR 2 , vi) vii) viii) -S0 2 NR 2 , ix) -CH 2 NR 2 , x) or Xi) c) 5 or 6 membered heterocycle;

Claim 3

2) R 1 -SO 2 -, except R 1 is nor aryl, 3) wherein R 5 is H or C 1-5 alkyl or joined together with R 1 either directly to form 5-7 membered heterocycle, or through a heteroatom selected from N, 0, and S, to form a 6-membered heterocycle with the nitrogen to which they are attached;

Claim 4

2) R 1 -SO 2 -, except R 1 is nor aryl, 3) wherein R 5 is H or C 1-5 alkyl or joined together with R 1 either directly to form 5-7 membered heterocycle, or through a heteroatom selected from N, 0, and S, to form a 6-membered heterocycle with the nitrogen to which they are attached;

Claim 5

4)

Claim 6

4)

Claim 7

5)

Claim 8

5)

Claim 9

6) (R 1 ) q wherein q is 1 or 2; Gis wherein Z is 0, S, or HH, and R 9 is independently 1) hydrogen; 2) 3) -OR, wherein R is H, or C 1-4 alkyl 4) -NR 2 , 5) -C 1-4 alkylene-R 11 ; wherein n is 0-5 and R 10 is independently a) hydrogen, b) hydroxy, or c) C 1-4 -alkyl; R 11 is a) hydrogen, b) aryl, unsubstituted or substituted with one or more of i) halo, ii) hydroxy, iii) -NH 2 , -N0 2 , -NHR, or -NR 2 , wherein R is H, or Ci-4 alkyl, iv) C 1 - 4 alkyl, v) Ci-3 alkoxy, vi) -COOR, vii) viii) -CH 2 NR 2 , ix) x) CN, xi) CF 3 , xii) xiii) aryl C 1-3 alkoxy, xiv) aryl, xv) -NRS0 2 R, xvi) -OP(O)(ORx) 2 wherein R x is H or aryl, or xvii) alkyl substituted with one or more of amine or quaternary amine; c) 5 or 6 membered heterocycle including up to 3 heteroatoms selected from N, 0, and S, any of which heterocycle may be unsubstituted or substituted with one or more of i) halo, ii) hydroxy, iii) -NH 2 , -NHR, -NR 2 , iv) C 1-4 alkyl, v) Ci- 3 alkoxy, vi) -COOR, vii) viii) -CH 2 NR 2 , ix) x) -CN, xi) CF 3 , xii) -NHS0 2 R, xiii) -OP(O)(OR x ) 2 wherein R x is H or aryl, or alkyl substituted with one or more of amine or quaternary amine; d) Ci- 6 alkyl or C 1-6 alkenyl, unsubstituted or substituted with one or more of i)hydroxy, ii) Cy 1-4 alkyl, iii) -NH 2 , -NHR, -NR 2 , iv) v) vi) -COOH, vii) viii) -SR or arylthio, ix) -S0 2 NHR, x) Ci-4 alkyl sulfonyl amino or aryl sulfonyl amino, xi) -CONHR, xii) xiii) -OR xiv) aryl C 1-3 alkoxy, or, xv) aryl; e) C 3 - 7 cycloalkyl unsubstituted or substituted with one or more of i) hydroxy, ii) Ci- 4 alkyl, iii) -NH 2 , -NHR, -NHR 2 , iv) v) vi) -COOH, vii) viii) -SR, ix) -S0 2 NH 2 , x) alkyl sulfonylamino or aryl sulfonylamino, xi) -CONHR, or xii) f) a 5- to 7-membered carbocyclic or 7- to 10-membered bicyclic carbocyclic ring which is either saturated or unsaturated, said carbocyclic ring being unsubstituted or substituted with one or more of i) halo ii) -OR, wherein R is H or C 1-4 alkyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 or -S(O)y R wherein y is 0,1, or 2; vii) -NR 2 , viii) ix) Ci- 4 alkyl, x) phenyl, xi) -CF 3 , or xii) g) benzofuryl; indolyl; azabicyclo C 7 - 11 cycloalkyl; or benzopiperidinyl; R 12 is-OH or-NHR13, wherein R 13 is -H, alkyl or-COOR; and Ⓗ is 1) C 3-7 cycloalkyl either unsubstituted or substituted with one or more of a) C 1-4 alkyl, b) hydroxy, c) -NR 2 , d) -COOR, e) CONHR, f) -NHSO 2 R, g) h) aryl, i) aryl substituted with Ci- 4 alkyl, j) heterocycle, or k) heterocycle substituted with Ci-4 alkyl; 2) phenyl, either unsubstituted or substituted with one or more of a) hydroxy, b) -OR, c) -NHR 13 , d) -COOR, e) or f) or

Claim 10

6) (R 1 ) q wherein q is 1 or 2; Gis wherein Z is 0, S, or HH, and R 9 is independently 1) hydrogen; 2) 3) -OR, wherein R is H, or C 1-4 alkyl 4) -NR 2 , 5) -C 1-4 alkylene-R 11 ; wherein n is 0-5 and R 10 is independently a) hydrogen, b) hydroxy, or c) C 1-4 -alkyl; R 11 is a) hydrogen, b) aryl, unsubstituted or substituted with one or more of i) halo, ii) hydroxy, iii) -NH 2 , -N0 2 , -NHR, or -NR 2 , wherein R is H, or Ci-4 alkyl, iv) C 1 - 4 alkyl, v) Ci-3 alkoxy, vi) -COOR, vii) viii) -CH 2 NR 2 , ix) x) CN, xi) CF 3 , xii) xiii) aryl C 1-3 alkoxy, xiv) aryl, xv) -NRS0 2 R, xvi) -OP(O)(ORx) 2 wherein R x is H or aryl, or xvii) alkyl substituted with one or more of amine or quaternary amine; c) 5 or 6 membered heterocycle including up to 3 heteroatoms selected from N, 0, and S, any of which heterocycle may be unsubstituted or substituted with one or more of i) halo, ii) hydroxy, iii) -NH 2 , -NHR, -NR 2 , iv) C 1-4 alkyl, v) Ci- 3 alkoxy, vi) -COOR, vii) viii) -CH 2 NR 2 , ix) x) -CN, xi) CF 3 , xii) -NHS0 2 R, xiii) -OP(O)(OR x ) 2 wherein R x is H or aryl, or alkyl substituted with one or more of amine or quaternary amine; d) Ci- 6 alkyl or C 1-6 alkenyl, unsubstituted or substituted with one or more of i)hydroxy, ii) Cy 1-4 alkyl, iii) -NH 2 , -NHR, -NR 2 , iv) v) vi) -COOH, vii) viii) -SR or arylthio, ix) -S0 2 NHR, x) Ci-4 alkyl sulfonyl amino or aryl sulfonyl amino, xi) -CONHR, xii) xiii) -OR xiv) aryl C 1-3 alkoxy, or, xv) aryl; e) C 3 - 7 cycloalkyl unsubstituted or substituted with one or more of i) hydroxy, ii) Ci- 4 alkyl, iii) -NH 2 , -NHR, -NHR 2 , iv) v) vi) -COOH, vii) viii) -SR, ix) -S0 2 NH 2 , x) alkyl sulfonylamino or aryl sulfonylamino, xi) -CONHR, or xii) f) a 5- to 7-membered carbocyclic or 7- to 10-membered bicyclic carbocyclic ring which is either saturated or unsaturated, said carbocyclic ring being unsubstituted or substituted with one or more of i) halo ii) -OR, wherein R is H or C 1-4 alkyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 or -S(O)y R wherein y is 0,1, or 2; vii) -NR 2 , viii) ix) Ci- 4 alkyl, x) phenyl, xi) -CF 3 , or xii) g) benzofuryl; indolyl; azabicyclo C 7 - 11 cycloalkyl; or benzopiperidinyl; R 12 is-OH or-NHR13, wherein R 13 is -H, alkyl or-COOR; and Ⓗ is 1) C 3-7 cycloalkyl either unsubstituted or substituted with one or more of a) C 1-4 alkyl, b) hydroxy, c) -NR 2 , d) -COOR, e) CONHR, f) -NHSO 2 R, g) h) aryl, i) aryl substituted with Ci- 4 alkyl, j) heterocycle, or k) heterocycle substituted with Ci-4 alkyl; 2) phenyl, either unsubstituted or substituted with one or more of a) hydroxy, b) -OR, c) -NHR 13 , d) -COOR, e) or f) or

Claim 11

3) 5 to 7-membered heterocycle, any of which heterocycle may be unsubstituted or substituted with one or more of i) halo, ii) hydroxy, iii) NR 2 , or iv) C 1-4 alkyl; Qis wherein R 9 and R 13 are defined above; X is 0, S, or NH; and Wis 1) OH, 2) NH 2 , 3) OR, or 4) NHR; B is, independently, absent, or J is 1) YR14 wherein: Y is O or NH, and R 14 is a) H; b) C 1-6 alkyl, unsubstituted or substituted with one or more of i) , ii) -OR, iii) -NHSO 2 C 1-4 alkyl, iv) -NHS02 aryl, or-NHS02 (dialkylaminoaryl), v) -CH 2 0R, vi) -C 1-4 alkyl, vii) viii) - NR2, ix) X) xi) xii) xiii) -NR 3 ⊕A⊖ wherein A⊖ is a counterion, xiv) -NR 15 R 16 wherein R 15 and R 16 are the same or different and are C 1-5 alkyl joined together directly to form a 5-7 membered heterocycle, xv) aryl, xvi) -CHO, xvii) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xviii) alkyl substituted with one or more of amine or quaternary amine; c) -(CH 2 CH 2 0)CH 3 or-(CH 2 CH 2 0)nH; 2) -N(R 14 ) 2 ; 3) -NR 15 R 16 wherein R 15 and R 16 are defined above; 4) wherein: Y, R 14 , and n are defined above, and R 17 is a) hydrogen; b) aryl unsubstituted or substituted with one or more of i) halo, ii) -OR, wherein R is H or C 1-4 alkyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 , vii) , viii) ix) Ci-4 alkyl, x) phenyl, xi) -CF 3 , xii) xiii) -C 1 - 4 alkyl-NR 2 , xiv) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xv) alkyl substituted with one or more of amine or quaternary amine; c) heterocycle, unsubstituted or substituted with one or more of i) halo, ii) -OR, wherein R is H, C 1-4 alkyl, or C 1-4 alkenyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 , vii) -NR 2 , viii) ix) C 1 - 4 alkyl, x) phenyl, xi) -CF 3 , xii) xiii) phenyl C 1-4 alkyl, xiv) xv) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xvi) alkyl substituted with one or more amine or quaternary amine; d) A 5- to 7-membered carbocyclic or 7- to 10-membered bicyclic carbocyclic ring which is either saturated or unsaturated, the carbocyclic ring being unsubstituted or substituted with one or more of i) halo, ii) -OR, wherein R is H or Ci- 4 alkyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 , vii) -NR 2 , viii) ix) C 1-4 alkyl, x) phenyl, xi) -CF 3 , xii) xiii) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xiv) alkyl substituted with one or more of amine or quaternary amine; or pharmaceutically acceptable salts thereof.

Claim 12

3) 5 to 7-membered heterocycle, any of which heterocycle may be unsubstituted or substituted with one or more of i) halo, ii) hydroxy, iii) NR 2 , or iv) C 1-4 alkyl; Qis wherein R 9 and R 13 are defined above; X is 0, S, or NH; and Wis 1) OH, 2) NH 2 , 3) OR, or 4) NHR; B is, independently, absent, or J is 1) YR14 wherein: Y is O or NH, and R 14 is a) H; b) C 1-6 alkyl, unsubstituted or substituted with one or more of i) , ii) -OR, iii) -NHSO 2 C 1-4 alkyl, iv) -NHS02 aryl, or-NHS02 (dialkylaminoaryl), v) -CH 2 0R, vi) -C 1-4 alkyl, vii) viii) - NR2, ix) X) xi) xii) xiii) -NR 3 ⊕A⊖ wherein A⊖ is a counterion, xiv) -NR 15 R 16 wherein R 15 and R 16 are the same or different and are C 1-5 alkyl joined together directly to form a 5-7 membered heterocycle, xv) aryl, xvi) -CHO, xvii) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xviii) alkyl substituted with one or more of amine or quaternary amine; c) -(CH 2 CH 2 0)CH 3 or-(CH 2 CH 2 0)nH; 2) -N(R 14 ) 2 ; 3) -NR 15 R 16 wherein R 15 and R 16 are defined above; 4) wherein: Y, R 14 , and n are defined above, and R 17 is a) hydrogen; b) aryl unsubstituted or substituted with one or more of i) halo, ii) -OR, wherein R is H or C 1-4 alkyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 , vii) , viii) ix) Ci-4 alkyl, x) phenyl, xi) -CF 3 , xii) xiii) -C 1 - 4 alkyl-NR 2 , xiv) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xv) alkyl substituted with one or more of amine or quaternary amine; c) heterocycle, unsubstituted or substituted with one or more of i) halo, ii) -OR, wherein R is H, C 1-4 alkyl, or C 1-4 alkenyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 , vii) -NR 2 , viii) ix) C 1 - 4 alkyl, x) phenyl, xi) -CF 3 , xii) xiii) phenyl C 1-4 alkyl, xiv) xv) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xvi) alkyl substituted with one or more amine or quaternary amine; d) A 5- to 7-membered carbocyclic or 7- to 10-membered bicyclic carbocyclic ring which is either saturated or unsaturated, the carbocyclic ring being unsubstituted or substituted with one or more of i) halo, ii) -OR, wherein R is H or Ci- 4 alkyl, iii) iv) v) -CH 2 NR 2 , vi) -S0 2 NR 2 , vii) -NR 2 , viii) ix) C 1-4 alkyl, x) phenyl, xi) -CF 3 , xii) xiii) -OP(O)(OR x ) 2 wherein R x is H or aryl, or xiv) alkyl substituted with one or more of amine or quaternary amine; or pharmaceutically acceptable salts thereof.

Claim 13

The compounds of Claim 1 wherein B is independently present twice and Z is O.

Claim 14

The compounds of Claim 2 wherein J is NH 2 , and Q is

Claim 15

The compounds of Claim 2 wherein J is NH 2 , and Q is

Claim 16

The compounds of Claim 2 wherein J is NH 2 , and Q is

Claim 17

The compounds of Claim 1 wherein B is present once and Z is O.

Claim 18

The compounds of Claim 6 wherein Q is

Claim 19

The compounds of Claim 6 wherein Q is

Claim 20

The compounds of Claim 6 wherein Q is

Claim 21

The compounds of Claim 1 wherein B is always absent.

Claim 22

The compounds of Claim 10 wherein Q is

Claim 23

The compounds of Claim 10 wherein Q is

Claim 24

The compounds of Claim 10 wherein Q is

Claim 25

The compounds of Claim 1 wherein G is:

Claim 26

Compounds of Claim 1 wherein G is: and B is absent or present once.

Claim 27

Compounds of Claim 1 wherein G is

Claim 28

B is absent or present once; and

Claim 29

B is absent or present once; and

Claim 30

Compounds of Claim 1 wherein: A is , with the proviso that R 1 is not aryl when attached to S; B is absent or present once; and

Claim 31

N'-(1,1-dimethylethylaminocarbonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl-phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 32

N'-(1,1-dimethylethylaminocarbonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl-phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 33

19 N'-(2,2-dimethylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl- phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 34

19 N'-(2,2-dimethylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl- phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 35

N'-(2-thienoyl)-5(S)amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl-phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 36

N'-(2-thienoyl)-5(S)amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl-phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 37

N'-(3,3-dimethylbutanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl- phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 38

N'-(3,3-dimethylbutanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl- phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 39

N'-(3-phenylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl- phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 40

N'-(3-phenylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-leucyl- phenylalanylamide, or pharmaceutically acceptable salt thereof.

Claim 41

N-benzyl-N'-(succinoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl isoleucyl amide; N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(succinoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide; N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(methanesulfonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide; N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(5-oxo-2(S)-tetrahydrofurancarbonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide, N'-(2,2-dimethylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl) hexanoyl-Leu-Phe- amide, N'-(1,1-dimethylethylaminocarbonyl)-5(S)-amino-4(S)-hydroxy-2(R)-phenylmethyl-hexanoyl -Leucyl-Phenylalanyl-amide, N'-(3-phenylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(Phenylmethyl)-hexanoyl-Leucyl-Phenylalanyl-amide, N'-(Succinoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-N-(phenylmethyl)-Ile- amide, N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(4-t-butyldimethylsilyloxybutanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide, N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(methanesulfonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl) hexanamide, N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(4-hydroxybutanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-phenylmethyl hexanamide, N'-(methanesulfonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-N-[2,3-dihydroxypropyl]-Val-amide, or N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(2-(2-[2-methoxyethoxy]ethoxy)ethoxycarbonyl]-5(S)-amino-2(R)-benzyl-4(S)-hydroxy-6-phenyl hexanamide, or pharmaceutically acceptable salts thereof.

Claim 42

N-benzyl-N'-(succinoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl isoleucyl amide; N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(succinoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide; N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(methanesulfonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide; N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(5-oxo-2(S)-tetrahydrofurancarbonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide, N'-(2,2-dimethylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl) hexanoyl-Leu-Phe- amide, N'-(1,1-dimethylethylaminocarbonyl)-5(S)-amino-4(S)-hydroxy-2(R)-phenylmethyl-hexanoyl -Leucyl-Phenylalanyl-amide, N'-(3-phenylpropanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(Phenylmethyl)-hexanoyl-Leucyl-Phenylalanyl-amide, N'-(Succinoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-N-(phenylmethyl)-Ile- amide, N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(4-t-butyldimethylsilyloxybutanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanamide, N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(methanesulfonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl) hexanamide, N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(4-hydroxybutanoyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-phenylmethyl hexanamide, N'-(methanesulfonyl)-5(S)-amino-4(S)-hydroxy-6-phenyl-2(R)-(phenylmethyl)hexanoyl-N-[2,3-dihydroxypropyl]-Val-amide, or N-(2(R)-hydroxy-1 (S)-indanyl)-N'-(2-(2-[2-methoxyethoxy]ethoxy)ethoxycarbonyl]-5(S)-amino-2(R)-benzyl-4(S)-hydroxy-6-phenyl hexanamide, or pharmaceutically acceptable salts thereof.

Claim 43

The compounds of Claims 1-23, in combination with any of the antivirals, immunomodulators, antibiotics or vaccines of Table VI.

Claim 44

A pharmaceutical composition comprising the compounds of Claims 1-23, and a pharmaceutically acceptable carrier.

Claim 45

A pharmaceutical composition comprising the compound in combination according to Claim 24, and a pharmaceutically acceptable carrier.

Claim 46

The pharmaceutical composition of Claim 25, for use in the treatment of AIDS, in the prevention of infection by HIV, in the treatment of infection by HIV, or in the inhibition of HIV protease.

Claim 47

The pharmaceutical composition of Claim 26, for use in the treatment of AIDS, in the prevention of infection by HIV, in the treatment of infection by HIV, or in the inhibition of HIV protease.

Claim 48

The use of a compound of any one of Claims 1-23, for the preparation of a medicament useful for treating AIDS.

Claim 49

The use of a combination according to Claim 24, for the preparation of a medicament useful for treating AIDS.

Claim 50

The use of a compound as claimed in any one of Claims 1-23, for the preparation of a medicament useful for preventing infection by HIV.

Claim 51

The use of the combination as claimed in Claim 24 for the preparation of a medicament useful for preventing infection by HIV.

Claim 52

The use of a compound as claimed in any one of claims 1-23 for the preparation of a medicament useful for treating infection by HIV.

Claim 53

The use of the combination as claimed in Claim 24 for the preparation of a medicament useful for treating infection by HIV.

Claim 54

The use of a compound as claimed in any one of claims 1-23 for the preparation of a medicament useful for inhibiting HIV protease.

Claim 55

The use of the combination as claimed in Claim 24 for the preparation of a medicament useful for inhibiting HIV protease.