HIV protease inhibitors

A compound selected from:

• 5-Hydroxy-6-methyl-5-[2-(4-methyl-thiazol-5-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3′-oxo-5-(2-thiazol-2-yl-ethyl)-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-thiazol-4-yl-ethyl)-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-thiazol-5-yl-ethyl)-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-5-[2-(5-methyl-thiazol-2-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-5-[2-(4-methyl-thiazol-2-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-5-[2-(2-methyl-thiazol-4-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-5-[2-(5-methyl-thiazol-4-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(2-isopropyl-thiazol-4-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(4-isopropyl-thiazol-5-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(5-isopropyl-thiazol-4-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(4-isopropyl-thiazol-2-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(2-Acetylamino-thiazol-4-yl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-pyridin-2-yl-ethyl)-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-pyridin-4-yl-ethyl)-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-pyridin-3-yl-ethyl)-heptanoic acid methyl ester;
• 5-(2-Furan-2-yl-ethyl)-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-(2-Furan-3-yl-ethyl)-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-[2-(tetrahydro-furan-2-yl)-ethyl]-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-thiophen-3-yl-ethyl)-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-thiophen-2-yl-ethyl)-heptanoic acid methyl ester;
• 5-{2-[2-(tert-Butyl-dimethyl-silanyloxymethyl)-thiophen-3-yl]-ethyl}-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-{2-[5-(tert-Butyl-dimethyl-silanyloxymethyl)-thiophen-3-yl]-ethyl}-5-hydroxy-6-methyl-3′-oxo-heptanoic acid methyl ester;
• 5-{2-[5-(tert-Butyl-dimethyl-silanyloxymethyl)-thiophen-2-yl]-ethyl}-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(5-hydroxymethyl-thiophen-3-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(5-hydroxymethyl-thiophen-2-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(2-hydroxymethyl-thiophen-3-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(3-Fluoro-2-methyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(2-Fluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(4-Fluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-[2-(1-trityl-1H-pyrazol-3-yl)-ethyl]-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-[2-(1H-pyrrol-3-yl)-ethyl]-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(1H-imidazol-4-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-pyrimidin-5-yl-ethyl)-heptanoic acid methyl ester;
• 5-[2-(2-Amino-pyrimidin-5-yl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(4-Cyano-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(2-hydroxymethyl-phenyl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-{2-[2-(tert-Butyl-dimethyl-silanyloxymethyl)-phenyl]-ethyl}-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(1H-indol-5-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-{2-[2-(2,2,2-trifluoro-acetylamino)-thiazol-4-yl]-ethyl}-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-5-[2-(4-methyl-thiophen-3-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-6-methyl-5-[2-(3-methyl-thiophen-2-yl)-ethyl]-3-oxo-heptanoic acid methyl ester;
• 5-{2-[3-(tert-Butyl-dimethyl-silanyloxymethyl)-thiophen-2-yl]-ethyl}-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-Hydroxy-5-[2-(3-hydroxymethyl-thiophen-2-yl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(2.6-Difluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(3,5-Difluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(2,4-Difluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(3,4,5-Trifluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3′-oxo-heptanoic acid methyl ester;
• 5-[2-(5-Fluoro-2-methyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-[2-(2-Ethyl-5-Fluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• 5-{2-[2-(tert-Butyl-dimethyl-silanyloxymethyl)-4-fluoro-phenyl]-ethyl}-5-hydroxy-6-methyl-3-oxo-heptanoic acid methyl ester;
• and
• 5-Hydroxy-5-[2-(4-fluoro-2-hydroxymethyl-phenyl)-ethyl]-6-methyl-3-oxo-heptanoic acid methyl ester.

A compound selected from:

• 4-Hydroxy-6-isopropyl-6-[2-(4-methyl-thiazol-5-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-thiazol-2-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-thiazol-4-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-thiazol-5-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(5-methyl-thiazol-2-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(4-methyl-thiazol-2-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(2-methyl-thiazol-4-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(5-methyl-thiazol-4-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(2-isopropyl-thiazol-4-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(4-isopropyl-thiazol-5-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(5-isopropyl-thiazol-4-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(4-isopropyl-thiazol-2-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• N-{4-[2-(4-Hydroxy-2-isopropyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-ethyl]-thiazol-2-yl}-acetamide;
• 4-Hydroxy-6-isopropyl-6-(2-pyridin-2-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-pyridin-4-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-pyridin-3-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 6-(2-Furan-2-yl-ethyl)-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-(2-Furan-3-yl-ethyl)-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(tetrahydro-furan-2-yl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-thiophen-3-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-thiophen-2-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-[2-(5-hydroxymethyl-thiophen-2-yl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-[2-(5-hydroxymethyl-thiophen-3-yl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-[2-(2-hydroxymethyl-thiophen-3-yl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(3-Fluoro-2-methyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one:
• δ 6-[2-(2-Fluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(4-Fluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(1H-pyrazol-3-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(1H-pyrrol-3-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(1-trityl-1H-imidazol-4-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-pyrimidin-5-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 6-[2-(2-Amino-pyrimidin-5-yl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 4-[2-(4-Hydroxy-2-isopropyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-ethyl]-benzonitrile;
• 4-Hydroxy-6-isopropyl-6-[2-(2-hydroxymethyl-phenyl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-[2-(1H-indol-5-yl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• 2,2,2-Trifluoro-N-{4-[2-(4-hydroxy-2-isopropyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-ethyl]-thiazol-2-yl}-acetamide;
• 4-Hydroxy-6-isopropyl-6-[2-(4-methyl-thiophen-3-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(3-methyl-thiophen-2-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-[2-(3-hydroxymethyl-thiophen-2-yl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(2,6-Difluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(3,5-Difluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(2,4-Difluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(3,4,5-Trifluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(5-Fluoro-2-methyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(2-Ethyl-5-Fluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-{2-[2-(tert-Butyl-dimethyl-silanyloxymethyl)-4-fluoro-phenyl]-ethyl}-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one:
• and
• 6-[2-(4-Fluoro-2-hydroxymethyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one.

A compound selected from:

• (S)-5-Hydroxy-6-methyl-3-oxo-5-(2-thiophen-3-yl-ethyl)-heptanoic acid ethyl ester;
• (R)-5-Hydroxy-6-methyl-3-oxo-5-(2-thiophen-3-yl-ethyl)-heptanoic acid ethyl ester;
• 5-[2-(3-Fluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester, (S) enantiomer;
• (R)-5-[2-(3-Fluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester;
• 5-[2-(3,4-Difluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester (R and S isomers);
• 5-Hydroxy-6-methyl-3-oxo-5-[2-(2-trifluoromethyl-phenyl)-ethyl]-heptanoic acid ethyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-[2 (3-trifluoromethyl-phenyl)-ethyl]-heptanoic acid ethyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-[2-(4-trifluoromethyl-phenyl)-ethyl]-heptanoic acid ethyl ester;
• 5-[2-(3-Fluoro-5-trifluoromethyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester;
• 5-[2-(4-Fluoro-3-trifluoromethyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester;
• (S)-5-Hydroxy-5-[2-(2-hydroxymethyl-phenyl)-ethyl]-6-methyl-3-oxo-heptanoic acid ethyl ester;
• (R)-5-Hydroxy-5-[2-(2-hydroxymethyl-phenyl)-ethyl]-6-methyl-3-oxo-heptanoic acid ethyl ester;
• 5-Hydroxy-6-methyl-3-oxo-5-(2-phenyl-ethyl)-heptanoic acid ethyl ester (R and S isomers);
• 5-[2-(4-Fluoro-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester (S and R isomers);
• 5-{2-[4-(tert-Butyl-dimethyl-silanyloxymethyl)-thiophen-3-yl]-ethyl}-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester;
• (S)-5-Hydroxy-6-methyl-5-[2-(2-methyl-thiophen-3-yl)-ethyl]-3-oxo-heptanoic acid ethyl ester;
• (S)-5-[2-(3-Fluoro-2-methyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester;
• (S)-5-[2-(3,5-Difluoro-2-methyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester;
• and
• (S)-5-[2-(4-Fluoro-2-methyl-phenyl)-ethyl]-5-hydroxy-6-methyl-3-oxo-heptanoic acid ethyl ester.

A compound of Formula IA

• 490
• wherein
• R4, R5, and R6 are independently H, a straight or branched alkyl of 1-6 carbons, a cycloalkyl of 3-6 carbons, (CR′2)nOR, (CR′2)nN(R)2, F, Cl, Br, CN, CF3, ═O, (CR′2)pNR′COR, (CR′2)pSOpR, (CR′2)pR, (CR′2)pOCOR, O(CR′2)mOR, NR(CR′2)mOR, (CR′2)pNR′CON(R)2, (CR′2)pOCON(R)2, (CR′2)pNR′CO2R, (CR′2)pCOR, (CR′2)pCO2R, (CR′2)pCON(R)2, (CR′2)pNR′SO2R, (CR′2)pSO2N(R)2, (CR′2)pNR′SO2OR, (CR′2)pOSO2N(R)2 (CR′2)pNR′SO2N(R)2, (CR′2)pC(NR′)N(R)2, (CR′2)pNR′C(NR′)N(R)2, (CR′2)pHet;
• any two of R4-R6 may together form a ring of 5-6 total atoms which may contain 0-3 heteroatoms;
• n is an integer of from 0 to 3;
• p is an integer from 0 to 2;
• R7 is a straight or branched alkyl of 1-6 carbons or a carbocycle of 3-6 carbons;
• R is independently H, a straight or branched alkyl of 1-4 carbons, (CH2)nPh, or a (CH2)nheterocycle of 5-6 atoms containing 1-2 heteroatoms and wherein the (R)2 in N(R)2 may form a heterocycle containing the nitrogen, all optionally substituted by F, Cl, Br, OR′, CN, CO2R′, N(R′)2, NR′COR′, CF3, or ═O;
• R′ is independently H, a straight or branched alkyl of 1-4 carbons, or phenyl;
• R″ is independently H, a straight or branched alkyl of 1-4 carbons, F, Cl, Br, OR′, or N(R′)2;
• Ar2 is phenyl or Het wherein Het is a heterocycle of from 5-6 atoms having from 1-4 heteroatoms.

A compound selected from:

• 2-Amino-5-tert-butyl-benzothiazole-6-thiol;
• 2-Amino-5-isopropyl-benzothiazole-6-thiol;
• 5-Isopropyl-benzothiazole-6-thiol;
• 2-Amino-7-isopropyl-4-methyl-benzothiazole-6-thiol;
• 2-Amino-6-tert-butyl-benzothiazole-4-thiol:
• 2-(Methyloxycarbonyl)amino-4-isopropyl-7-methyl-benzothiazole-6-thiol;
• 3-tert-Butyl-2-mercapto-benzo[b]thiophene:
• 5-(tert-Butyl-dimethyl-silanyloxymethyl)-2-isopropyl-3-mercapto-thiophene;
• (5-tert-Butyl-4-mercapto-5-methyl-phenyl)methanol;
• (3-tert-Butyl-4-mercapto-phenyl)methanol;
• and
• 2-(5-tert-Butyl-4-mercapto-2-methyl-phenyl)-ethanol.

A compound selected from:

• Toluene-4-thiosulfonic acid S-(2-amino-5-tert-butyl-benzothiazol-6-yl)ester;
• Toluene-4-thiosulfonic acid S-(2-amino-5-isopropyl-benzothiazol-6-yl)ester;
• Toluene-4-thiosulfonic acid S-(5-isopropyl-benzothiazol-6-yl)ester;
• Toluene-4-thiosulfonic acid S-(2-amino-7-isopropyl-4-methyl-benzothiazol-6-yl)ester;
• Toluene-4-thiosulfonic acid S-(4-isopropyl-2-methoxycarbonylamino-7-methyl-benzothiazol-6-yl)ester;
• Toluene-4-thiosulfonic acid S-(2-amino-6-tert-butyl-benzothiazol-4-yl)ester;
• Toluene-4-thiosulfonic acid S-(3-tert-butyl-benzo[b]thiophen-2-yl)ester;
• Toluene-4-thiosulfonic acid S-[5-(tert-butyl-silanyloxymethyl)-2-isopropyl-thiophen-3-yl]ester;
• Toluene-4-thiosulfonic acid S-(2-tert-butyl-4-hydroxymethyl-phenyl)ester;
• Toluene-4-thiosulfonic acid S-[2-tert-butyl-4-(2-hydroxy-ethyl)-5-methyl-phenyl]ester;
• Benzenesulfonothioic acid, 4-methyl-, S-[2-(1,1-dimethylethyl)-5-methyl-4-[[[[(5-trifluoromethyl)-2-pyridinyl]sulfonyl]amino]phenyl]ester;
• 6-tert-Butyl-5-(toluene-4-sulfonylsulfanyl)-indole-1-carboxylic acid tert-butyl ester;
• 6-tert-Butyl-5-(toluene-4-sulfonylsulfanyl)-2,3-dihydro-indole-1-carboxylic acid tert-butyl ester;
• Toluene-4-thiosulfonic acid S-[6-tert-butyl-1-(4-cyanobenzenesulfonyl)-2,3-dihydro-1H-indol-5-yl] ester;
• Toluene-4-thiosulfonic acid S-(6-isopropyl-3H-benzoimidazol-5-yl) ester;
• Toluene-4-thiosulfonic acid S-(6-tert-butyl-3H-benzoimidzol-5-yl) ester;
• Toluene-4-thiosulfonic acid S-(6-tert-butyl-2-oxo-2,3-dihydro-1H-benzoimidzol-5-yl) ester;
• 6-tert-Butyl-5-(toluene-4-sulfonylsulfanyl)-1H-indole-2-carboxylic acid ethyl ester;
• Toluene-4-thiosulfonic acid S-(7-tert-butyl-2,3-dioxo-1,2,3,4-tetrahydro-quinoxalin-6-yl) ester;
• Toluene-4-thiosulfonic acid S-[5-tert-butyl-2-(4-cyanobenzenesulfonyl-amino)-benzothiazol-6-yl)] ester;
• Toluene-4-thiosulfonic acid S-(6-tert-butyl-2-methanesulfonylamino-benzothiazol-6-yl) ester;
• Toluene-4-thiosulfonic acid S-(2-acetylamino-5-tert-butyl-benzothiazol-6-yl) ester;
• and
• Toluene-4-thiosulfonic acid S-(6-isopropyl-2-oxo-2,3-dihydro-1H-benzimidazol-5-yl) ester.

A compound selected from:

• 3-Hydroxy-4-methyl-3-(2-thiophen-3-yl-ethyl)-pentanoic acid tert-butyl ester;
• 5-(3-Fluoro-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• 5-(3,4-Difluoro-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• 3-Hydroxy-3-isopropyl-5-(2-trifluoromethyl-phenyl)-pent-4-enoic acid benzyl ester;
• 3-Hydroxy-3-isopropyl-5-(3-trifluoromethyl-phenyl)-pent-4-enoic acid benzyl ester;
• 3-Hydroxy-3-isopropyl-5-(4-trifluoromethyl-phenyl)-pent-4-enoic acid benzyl ester;
• 5-(3-Fluoro-5-trifluoromethyl-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• 5-(4-Fluoro-3-trifluoromethyl-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• 3-Hydroxy-3-[2-(2-hydroxymethyl-phenyl)-ethyl]-4-methyl-pentanoic acid tert-butyl ester;
• 3-Hydroxy-4-methyl-3-(2-phenyl-ethyl)-pentanoic acid tert-butyl ester;
• 3-Hydroxy-3-isopropyl-5-phenyl-3′-pent-4-enoic acid benzyl ester;
• 5-(4-Fluoro-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• 3-{2-[4-(tert-Butyl-dimethyl-silanyloxymethyl)-thiophen-3-yl]-ethyl}-3-hydroxy-4-methyl-pentanoic acid ethyl ester;
• 3-Hydroxy-4-methyl-3-[2-(2-methyl-thiophen-3-yl)-ethyl]-pentanoic acid tert-butyl ester;
• 5-(3-Fluoro-2-methyl-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• 5-(3,5-Difluoro-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid benzyl ester;
• and
• 5-(4-Fluoro-2-methyl-phenyl)-3-hydroxy-3-isopropyl-pent-4-enoic acid tert-butyl ester.

A compound selected from:

• (S)-3-Hydroxy-4-methyl-3-(2-thiophen-3-yl-ethyl)-pentanoic acid;
• (R)-3-Hydroxy-4-methyl-3-(2-thiophen-3-yl-ethyl)-pentanoic acid;
• (+/−)-3-Hydroxy-4-methyl-3-(2-thiophen-3-yl-ethyl)-pentanoic acid;
• 3-[2-(3-Fluoro-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• 3-[2-(3,4-Difluoro-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• 3-Hydroxy-4-methyl-3-[2-(2-trifluoromethyl-phenyl)-ethyl]-pentanoic acid;
• 3-Hydroxy-4-methyl-3-[2-(3-trifluoromethyl-phenyl)-ethyl]-pentanoic acid;
• 3-Hydroxy-4-methyl-3-[2-(4-trifluoromethyl-phenyl)-ethyl]-pentanoic acid;
• 3-[2-(3-Fluoro-5-trifluoromethyl-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• 3-[2-(4-Fluoro-3-trifluoromethyl-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• (S)-3-Hydroxy-3-[2-(2-hydroxymethyl-phenyl)-ethyl]-4-methyl-pentanoic acid;
• (R)-3-Hydroxy-3-[2-(2-hydroxymethyl-phenyl)-ethyl]-4-methyl-pentanoic acid;
• 3-Hydroxy-4-methyl-3-(2-phenyl-ethyl)-pentanoic acid;
• 3-[2-(4-Fluoro-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• 3-{2-[4-(tert-Butyl-dimethyl-silanyloxy-methyl)-thiophen-3-yl]-ethyl}-3-hydroxy-4-methyl-pentanoic acid;
• 3-Hydroxy-4-methyl-3-[2-(2-methyl-thiophen-3-yl)-ethyl]-pentanoic acid;
• 3-[2-(3-Fluoro-2-methyl-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• 3-[2-(3,5-Difluoro-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid;
• and
• 3-[2-(4-Fluoro-2-methyl-phenyl)-ethyl]-3-hydroxy-4-methyl-pentanoic acid.

A compound selected from:

• (S)-4-Hydroxy-6-isopropyl-6-(2-thiophen-3-yl-ethyl)-5,6-dihydro-pyran-2-one;
• (R)4-Hydroxy-6-isopropyl-6-(2-thiophen-3-yl-ethyl)-5,6-dihydro-pyran-2-one;
• 6-[2-(3-Fluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one (R and S isomers);
• 6-[2-(3,4-Difluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one (R and S isomers);
• 4-Hydroxy-6-isopropyl-6-[2-(2-trifluoromethyl-phenyl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(3-trifluoromethyl-phenyl)-ethyl]-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-[2-(4-trifluoromethyl-phenyl)-ethyl]-5,6-dihydro-pyran-2-one;
• 6-[2-(3-Fluoro-5-trifluoromethyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• 6-[2-(4-Fluoro-3-trifluoromethyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• (S)-4-Hydroxy-6-[2-(2-hydroxymethyl-phenyl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• (R)-4-Hydroxy-6-[2-(2-hydroxymethyl-phenyl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• 4-Hydroxy-6-isopropyl-6-(2-phenyl-ethyl)-5,6-dihydro-pyran-2-one (R and S isomers);
• 6-[2-(4-Fluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one (R and S isomers);
• 4-Hydroxy-6-[2-(4-hydroxymethyl-thiophen-3-yl)-ethyl]-6-isopropyl-5,6-dihydro-pyran-2-one;
• (S)-4-Hydroxy-6-isopropyl-6-[2-(2-methyl-thiophen-3-yl)-ethyl]-5,6-dihydro-pyran-2-one;
• (S)-6-[2-(3-Fluoro-2-methyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• (S)-6-[2-(3,5-Difluoro-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one;
• and
• (S)-6-[2-(4-Fluoro-2-methyl-phenyl)-ethyl]-4-hydroxy-6-isopropyl-5,6-dihydro-pyran-2-one.

A compound and the R and S isomer thereof selected from:

• 3-[2-(3-Fluoro-phenyl)-ethyl]-3-hydroxy-1-imidazol-1-yl-4-methyl-pentan-1-one;
• 3-Hydroxy-1-imidazol-1-yl-4-methyl-3-phenethyl-pentan-1-one;
• 3-[2-(3,4-Difluoro-phenyl)-ethyl]-3-hydroxy-1-imidazol-1-yl-4-methyl-pentan-1-one;
• 3-Hydroxy-1-imidazol-1-yl-4-methyl-3-[2-(2-trifluoromethyl-phenyl)-ethyl]-pentan-1-one;
• 3-[2-(4-Fluoro-3-trifluoromethyl-phenyl)-ethyl]-3-hydroxy-1-imidazol-1-yl-4-methyl-pentan-1-one;
• 3-Hydroxy-1-imidazol-1-yl-4-methyl-3-[2-(3-trifluoromethyl-phenyl)-ethyl]-pentan-1-one;
• 3-[2-(4-Fluoro-2-trifluoromethyl-phenyl)-ethyl]-3-hydroxy-1-imidazol-1-yl-4-methyl-pentan-1-one;
• 3-Hydroxy-1-imidazol-1-yl-4-methyl-3-[2-(4-trifluoromethyl-phenyl)-ethyl]-pentan-1-one;
• 3-[2-(4-Fluoro-phenyl)-ethyl]-3-hydroxy-1-imidazol-1-yl-4-methyl-pentan-1-one;
• 3-Hydroxy-1-imidazol-1-yl-4-methyl-3-[2-thiophen-3-yl-ethyl)-pentan-1-one;
• and
• 3-Hydroxy-3-[2-(2-hydroxymethyl-phenyl)-ethyl]-1-imidazol-1-yl-4-methyl-pentan-1-one.