Compounds useful to treat retroviral infections
First Claim
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1. A compound of the formula I wherein R1 is H—
- ;
wherein R2 isa) C3-C5 alkyl, b) phenyl-(CH2)2—
, c) het-SO2NH—
(CH2)2—
, d) cyclopropyl-(CH2)2—
, e) F-phenyl-(CH2)2—
, f) het-SO2NH-phenyl-, or g) F3C—
(CH2)2—
;
or wherein R1 and R2 taken together are a double bond;
wherein R3 is the moiety of formula X wherein R4 isa) phenyl, b) het, c) cyclopropyl, d) H3C—
[O(CH2)2]2—
, e) het-SO2NH—
, f) Br—
, g) N3—
, or h) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
;
wherein R5 is —
H;
wherein R6 isa) R4—
(CH2)n—
CH(R8)—
, b) H3C—
[O(CH2)2]2—
CH2—
, c) C3-C5 alkyl, d) phenyl-(CH2)2—
, e) het-SO2NH—
(CH2)2—
, f) (HOCH2)3C—
NH—
C(O)—
NH—
(CH2)3—
, g) (HO2C)(H2N)CH—
(CH2)2—
C(O)—
NH—
(CH2)3—
, h) piperazin-1-yl-C(O)—
NH—
(CH2)3, i) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
(CH2)3—
, j) cyclopropyl-(CH2)2—
, k) F-phenyl-(CH2)2—
, l) het-SO2NH-phenyl, or m) F3C—
(CH2)2—
;
wherein n is zero (0), one (1) or two (2);
wherein R7 isa) cyclopropyl, b) CH3—
CH2—
, or c) t-butyl;
wherein R8 isa) —
CH2—
CH3, or b) —
CH2-cyclopropyl;
wherein R9 isa) —
NR12SO2-het, b) —
NR12SO2-phenyl substituted by zero (0) or one (1) R11, c) —
CH2—
SO2-phenyl substituted by zero (0) or one (1) R1 1, or d) —
CH2—
SO2-het;
wherein het is pyridinyl, imidazolyl, benzimidazolyl, quinolinyl, pyrimidinyl, pyrazinyl, pyrazolyl, thiazolyl, purinyl, tetrahydropyranyl or quinazolinyl;
substituted by zero (0) or one (1) R10;
wherein R10 isa) —
CH3, b) —
CN, c) —
OH, d) —
C(O)OC2H5, e) —
CF3, f) —
NH2, or g) —
C(O)—
NH2;
wherein R11 isa) —
CN, b) —
F, c) —
OH, or d) —
NO2;
wherein R12 isa) —
H, or b) —
CH3;
or a pharmaceutically acceptable salt thereof.
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Abstract
The present invention relates to compounds of formula I and II which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.
wherein R10 and R20 taken together are:
-
Citations
12 Claims
-
1. A compound of the formula I
wherein R1 is H— - ;
wherein R2 is a) C3-C5 alkyl, b) phenyl-(CH2)2—
,c) het-SO2NH—
(CH2)2—
,d) cyclopropyl-(CH2)2—
,e) F-phenyl-(CH2)2—
,f) het-SO2NH-phenyl-, or g) F3C—
(CH2)2—
;
or wherein R1 and R2 taken together are a double bond; wherein R3 is the moiety of formula X wherein R4 is a) phenyl, b) het, c) cyclopropyl, d) H3C—
[O(CH2)2]2—
,e) het-SO2NH—
,f) Br—
,g) N3—
, orh) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
;
wherein R5 is —
H;wherein R6 is a) R4—
(CH2)n—
CH(R8)—
,b) H3C—
[O(CH2)2]2—
CH2—
,c) C3-C5 alkyl, d) phenyl-(CH2)2—
,e) het-SO2NH—
(CH2)2—
,f) (HOCH2)3C—
NH—
C(O)—
NH—
(CH2)3—
,g) (HO2C)(H2N)CH—
(CH2)2—
C(O)—
NH—
(CH2)3—
,h) piperazin-1-yl-C(O)—
NH—
(CH2)3,i) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
(CH2)3—
,j) cyclopropyl-(CH2)2—
,k) F-phenyl-(CH2)2—
,l) het-SO2NH-phenyl, or m) F3C—
(CH2)2—
;
wherein n is zero (0), one (1) or two (2); wherein R7 is a) cyclopropyl, b) CH3—
CH2—
, orc) t-butyl;
wherein R8 is a) —
CH2—
CH3, orb) —
CH2-cyclopropyl;
wherein R9 is a) —
NR12SO2-het,b) —
NR12SO2-phenyl substituted by zero (0) or one (1) R11,c) —
CH2—
SO2-phenyl substituted by zero (0) or one (1) R1 1, ord) —
CH2—
SO2-het;
wherein het is pyridinyl, imidazolyl, benzimidazolyl, quinolinyl, pyrimidinyl, pyrazinyl, pyrazolyl, thiazolyl, purinyl, tetrahydropyranyl or quinazolinyl;
substituted by zero (0) or one (1) R10;
wherein R10 is a) —
CH3,b) —
CN,c) —
OH,d) —
C(O)OC2H5,e) —
CF3,f) —
NH2, org) —
C(O)—
NH2;
wherein R11 is a) —
CN,b) —
F,c) —
OH, ord) —
NO2;
wherein R12 is a) —
H, orb) —
CH3;
or a pharmaceutically acceptable salt thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
wherein R1 is H— - ;
wherein R2 is a) C3-C5 alkyl, b) phenyl-(CH2)2—
, orc) het-SO2NH—
(CH2)2—
;
or wherein R1 and R2 taken together are a double bond; wherein R3 is the moiety of formula X wherein R4 is a) phenyl, b) het, c) cyclopropyl, d) H3C—
[O(CH2)2]2—
,e) het-SO2NH—
,f) Br—
,g) N3—
, orh) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
;
wherein R5 is —
H;wherein R6 is a) R4—
(CH2)n—
CH(R8)—
,b) H3C—
[O(CH2)2]2—
CH2—
,c) C3-C5 alkyl, d) phenyl-(CH2)2—
,e) het-SO2NH—
(CH2)2—
,f) (HOCH2)3C—
NH—
C(O)—
NH—
(CH2)3—
,g) (HO2C)(H2N)CH—
(CH2)2—
C(O)—
NH—
(CH2)3—
,h) piperazin-1-yl-C(O)—
NH—
(CH2)3, ori) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
(CH2)3—
;
wherein n is zero (0), one (1) or two (2); wherein R7 is a) cyclopropyl, b) CH3—
CH2—
, orc) t-butyl;
wherein R8 is a) —
CH2—
CH3, orb) —
CH2-cyclopropyl;
wherein R9 is a) —
NR12SO2-het,b) —
NR12SO2-phenyl substituted by zero (0) or one (1) R11,c) —
CH2-SO2-phenyl substituted by zero (0) or one (1) R11, ord) —
CH2—
SO2-het;
wherein het is pyridinyl, imidazolyl, benzimidazolyl, quinolinyl, pyrimidinyl, pyrazinyl, pyrazolyl, thiazolyl, purinyl, tetrahydropyranyl or quinazolinyl;
substituted by zero (0) or one (1) R10;
wherein R10 is a) —
CH3,b) —
CN,c) —
OH, ord) —
C(O)OC2H5;
wherein R11 is a) —
CN,b) —
F,c) —
OH, ord) —
NO2;
wherein R12 is a) —
H, orb) —
CH3;
or a pharmaceutically acceptable salt thereof.
- ;
-
3. The compound of claim 2 wherein het is the following, substituted by zero (0) or one (1) R10,
a) 2-pyridinyl, b) imidazol-2-yl, c) imidazol-4-yl, d) benzimidazol-2-yl, e) quinolin-8-yl, f) quinolin-2-yl, g) pyrimidin-2-yl, h) quinazolin-2-yl, i) purin-6-yl, j) thiazol-2-yl, k) thiazol-4-yl, l) 2-pyrazolyl, m) 2-pyrazinyl, n) tetrahydropyran-4-yl, or o) tetrahydropyran-3-yl. -
4. The compound of claim 3 of the formula I
wherein R1 is H— - ;
wherein R2 is a) H3C—
(CH2)2—
,b) phenyl-(CH2)2—
,c) (CH3)2CH—
CH2, ord) pentyl;
or wherein R1 and R2 taken together are a double bond; wherein R3 is the moiety of formula X wherein R4 is a) phenyl, b) het, c) cyclopropyl, d) H3C—
[O(CH2)2]2—
,e) het-SO2NH—
,f) Br—
,g) N3—
, orh) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
;
wherein R5 is —
H;wherein R6 is a) R4—
(CH2)n—
CH(R8)—
,b) H3C—
[O(CH2)2]2—
CH2—
,c) H3C—
(CH2)2—
,d) phenyl-(CH2)2—
,e) (CH3)2CH—
CH2—
, orf) pentyl;
wherein n is zero (0), one (1) or two (2); wherein R7 is a) cyclopropyl, or b) CH3—
CH2—
;
wherein R8 is a) —
CH2—
CH3, orb) —
CH2-cyclopropyl;
wherein R9 is a) —
NHSO2-het, orb) —
NHSO2-phenyl substituted by zero (0) or one (1) R11;
wherein het is the following, substituted by zero (0) or one (1) R10, a) 2-pyridinyl, b) imidazol-2-yl, c) imidazol-4-yl, d) quinolin-8-yl, e) tetrahydropyran-4-yl, f) tetrahydropyran-3-yl, or g) benzimidazol-2-yl;
wherein R10 is a) —
CH3;
wherein R11 is a) —
CN,b) —
F orc) —
NO2;
or a pharmaceutically acceptable salt thereof.
- ;
-
5. The compound of claim 4 of the formula VI
wherein R2 is a) H3C— - (CH2)2—
,b) phenyl-(CH2)2—
,c) (CH3)2CH—
CH2—
, ord) pentyl;
wherein R3 is the moiety of formula X wherein R6 is a) H3C—
(CH2)2—
,b) phenyl-(CH2)2—
,c) (CH3)2CH—
CH2—
, ord) pentyl;
wherein R7 is a) CH3—
CH2—
, orb) cyclopropyl;
wherein R9 is a) —
NHSO2-phenyl substituted by one (1) R11, orb) —
NHSO2-het;
wherein het is the following, substituted by zero (0) or one (1) R10, a) imidazol-4-yl, or b) quinolin-8-yl;
wherein R10 is —
CH3;wherein R11 is a) —
CN, orb) —
F.
- (CH2)2—
-
6. The compound of claim 4 of the formula VII
wherein R3 is the moiety of formula X wherein R4 is a) phenyl, b) het, c) cyclopropyl, d) H3C— - [O(CH2)2]2—
,e) het-SO2NH—
,f) Br—
,g) N3—
, orh) HO3S(CH2)2—
N(CH3)—
C(O)—
(CH2)6—
C(O)—
NH—
;
wherein R6 is a) R4—
(CH2)n—
CH(R,)—
, orb) H3C—
[O(CH2)2]2—
CH2—
;
wherein R7 is cyclopropyl; wherein R8 is a) —
CH2—
CH3, orb) —
CH2-cyclopropyl;
wherein R9 is a) —
NHSO2-het, orb) —
NHSO2-phenyl substituted by one (1) R11;
wherein n is zero (0), one (1) or two (2); wherein het is the following, substituted by zero (0) or one (1) R10, a) imidazol-4-yl, b) imidazol-2-yl, c) quinolin-8-yl, d) tetrahydropyran-3-yl, e) tetrahydropyran-4-yl, f) 2-pyridinyl, or g) benzimidazol-2-yl;
wherein R10 is —
CH3;wherein R11 is a) —
NO2,b) —
F, orc) —
CN;
or a pharmaceutically acceptable salt thereof.
- [O(CH2)2]2—
-
7. The compound of claim 2 selected from the group consisting of:
-
3-[cyclopropyl[3-[(4-cyanophenylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-(2-phenylethyl)-6-(1-propyl)-5,6-dihydro-2H-pyran-2-one;
3-[cyclopropyl[3-[(2-pyridinylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-(2-phenylethyl)-6-(1-propyl)-5,6-dihydro-2H-pyran-2-one;
3-[cyclopropyl[3-[(1-methyl-4-imidazolylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-(2-phenylethyl)-6-(1-propyl)-5,6-dihydro-2H-pyran-2-one;
3-[cyclopropyl[3-[(5-cyano-2-pyridinylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-(2-phenylethyl)-6-(1-propyl)-5,6-dihydro-2H-pyran-2-one;
3-[cyclopropyl[3-[(2-benzimidazolylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-(2-phenylethyl)-6-(1-propyl)-5,6-dihydro-2H-pyran-2-one;
3-[cyclopropyl[3-[(2-quinolinylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-(2-phenylethyl)-6-(1-propyl)-5,6-dihydro-2H-pyran-2-one;
4-Cyano-N-[3-[1-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-8-quinolinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-8-quinolinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5 ,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazolesulfonamide;
4-Fluoro-N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
4-Cyano-N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
N-[3-[1-(4-hydroxy-6,6-diisobutyl-2-oxo-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-cyclo-propylmethyl]-phenyl]-1-methyl-1H-imidazolesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-cyclo-propylmethyl]-phenyl]-8-quinolinesulfonamide;
4-Cyano-N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-benzenesulfonamide;
4-Fluoro-N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-benzenesulfonamide;
(R or S)-N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-8-quinolinesulfonamide;
(R or S)-N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
(S or R)-N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-8-quinolinesulfonamide;
(S or R)-N-[3-[1-(4-hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
(R or S)-N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
(S or R)-N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipropyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
4-Cyano-N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-benzenesulfonamide;
4-Fluoro-N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-benzenesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-8-quinolinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-cyclopropylmethyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipentyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
4-Cyano-N-[3-[1-(4-Hydroxy-2-oxo-6,6-dipentyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
N-[3-[1(R or S)-(6(R or S)-4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1(R or S)-(6(S or R)-4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1(S or R)-(6(R or S)-4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1(S or R)-(6(S or R)-4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[t-Butyl-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-methyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
4-Cyano-N-[3-[t-butyl-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-methyl]-phenyl]-benzenesulfonamide;
4-Fluoro-N-[3-[t-butyl-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-methyl]-phenyl]-benzenesulfonamide;
N-[3-[t-Butyl-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-methyl]-phenyl]-8-quinolinesulfonamide;
N-[3-[1-(6-(2-(1-Methyl-1H-imidazole-4-sulfonylamino)-ethyl)-4-hydroxy-2-oxo-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-pyridinesulfonamide;
4-Cyano-N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-pyridinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-quinolinesulfonamide;
2-Hydroxy-N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-pyrimidinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-quinazolinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-7H-purine-6-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1H-imidazole-2-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1H-benzimidazole-2-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-thiazole-4-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-pyridinesulfonamide;
4-Cyano-N-[3-[1-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-pyridinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-quinolinesulfonamide;
2-Hydroxy-N-[3-[1-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-pyrimidinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-2-quinazolinesulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-7H-purine-6-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1H-imidazole-2-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-1H-benzimidazole-2-sulfonamide;
N-[3-[1-(4-Hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-thiazole-4-sulfonamide;
4-Fluoro-N-[3-[1-(4-hydroxy-2-oxo-6-phenethyl-6-propyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-benzenesulfonamide;
5-cyano-N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-pyridinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-quinolinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-imidazolesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-pyrimidinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-benzimidazolesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-quinazolinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-5 phenyl]-N-methyl-6-purinesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-4-thiazolesulfonamide;
N-[3-[1-(4-hydroxy-2-oxo-6,6-diphenethyl-5,6-dihydro-2H-pyran-3-yl)-propyl]-phenyl]-N-methyl-2-pyridinesulfonamide;
N-[3-(1-[5,6-Dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-(1(S)-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-(1(R)-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-(1(S)-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-(1(R)-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide;
5-Cyano-N-[3-(1-[5,6-dihydro-4-hydoxy-2-oxo-6-(2-phenethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide; and
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide.
-
-
8. The compound of claim 2 selected from the group consisting of:
-
3-[cyclopropyl[3-[(4-cyanophenylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-[1-(phenylmethyl)propyl]-2H-pyran-2-one;
3-[cyclopropyl[3-[(2-pyridinylsulfonyl)methylphenylmethyl]-4-hydroxy-6-[1-(phenylmethyl)propyl]-2H-pyran-2-one;
3-[cyclopropyl[3-[(1-methyl-4-imidazolylsulfonyl)methyl]phenyl]methyl)-4-hydroxy-6-[1-(phenylmethyl)propyl]-2H-pyran-2-one;
3-[cyclopropyl[3-[(5-cyano-2-pyridinylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-[1-(phenylmethyl)propyl]-2H-pyran-2-one;
3-[cyclopropyl[3-[(2-benzimidazolylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-[1-(phenylmethyl)propyl]-2H-pyran-2-one;
3-[cyclopropyl[3-[(2-quinolinylsulfonyl)methyl]phenyl]methyl]-4-hydroxy-6-[1-(phenylmethyl)propyl]-2H-pyran-2-one;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-fluoro-benzenesulfonamide;
4-Cyano-N-(3-{cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzenesulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-8-quinolinesulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl]-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
(R or S)-N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl]-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
(R or S)-N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl]-phenyl)-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-benzoimidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(2-cyclopropyl-1-cyclopropylmethyl-ethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-quinolinesulfonamide;
N-(3-{(Cyclopropyl-[4-hydroxy-6-(3-{2-methoxy-ethoxy}-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethyl-3-{2-methoxy-ethoxy}-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
4-Cyano-N-(3-{cyclopropyl-[6-(1-ethyl-3-{2-methoxy-ethoxy}-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzenesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethyl-3-{1-methyl-1H-imidazole-4-sulfonylamino}-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl-methyl}-phenyl)-1-methyl-H-imidazole-4-sulfonamide;
N-(3-{[6-(3-Bromo-1-ethyl-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-cyclopropyl-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{[6-(3-Azido-1-ethyl-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-cyclopropyl-methyl)-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
2-[[8-[[3-[3-[Cyclopropyl[3-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]aminolphenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]pentyl]amino]-1,8-dioxooctyl]methylamino]-ethane sulfonic acid, monosodium salt;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-[(2-hydroxy-1,1-bisfhydroxymethyl}-ethyl)-amino]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzenesulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[(2-hydroxy-1,1-bis{hydroxymethyl}-ethyl)-amino]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{(2-hydroxy-1,1-bisthydroxymethyl}-ethyl)-amino-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-2-sulfonamide;
N-(3-Cyclopropyl-[4-hydroxy-6-(3-{[(2-hydroxy-1,1-bis{hydroxymethyl}-ethyl)-amino]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-benzoimidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[(2-hydroxy-1,1-bis{hydroxymethyl}-ethyl)-amino]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[(2-hydroxy-1,1-bis{hydroxymethyl}-ethyl)-amino]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{γ
-L-glutamyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzenesulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{γ
-L-glutamyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{γ
-L-glutamyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{γ
-L-glutamyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-benzoimidazole-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{γ
-L-glutamyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{γ
-L-glutamyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[piperazin-1-yl]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzenesulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[piperazin-1-yl]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[piperazin-1-yl]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[piperazin-1-yl]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-benzoimidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[piperazin-1-yl]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[4-hydroxy-6-(3-{[piperazin-1-yl]-carbonyl}-amino-propyl)-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
2-[[8-[[3-[3-[Cyclopropyl[3-[[phenylsulfonyl]amino]phenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]propyl]amino]-1,8-dioxooctyl]methylamino]-ethanesulfonic acid, monosodium salt;
2-[[8-[[3-[3-[Cyclopropyl[3-[[(2-pyridyl)sulfonyl]amino]phenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]propyl]amino]-1,8-dioxooctyl]methylamino]-ethane sulfonic acid, monosodium salt;
2-[[8-[[3-[3-[Cyclopropyl[3-[[(1H-benzimidazol-2-yl)sulfonyl]amino]phenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]propyl]amino]-1,8-dioxooctyl]methyl amino]-ethanesulfonic acid, monosodium salt;
2-[[8-[[3-[3-[Cyclopropyl[3-[[(1H-imidazol-2-yl)sulfonyl]amino]phenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]propyl]amino]-1,8-dioxooctyl]methylamino]-ethane sulfonic acid, monosodium salt;
2-[[8-[[3-[3-[Cyclopropyl[3-[[(1-methyl-1H-imidazol-4-yl)sulfonyl]amino]phenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]propyl]amino]-1,8-dioxooctyl]methylamino]-ethanesulfonic acid, monosodium salt;
2-[[8-[[3-[3-[Cyclopropyl[3-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl]methyl]-4-hydroxy-2-oxo-2H-pyran-6-yl]propyl]amino]-1,8-dioxooctyl]methylamino]-ethane sulfonic acid, monosodium salt;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(S)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(S)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1-methyl-1H-imidazole-2-sulfonamide;
N-(3-[Cyclopropyl[4-hydroxy-2-oxo-6-[1-[(tetrahydro-2H-pyran-3-yl)methyl]propyl]-2H-pyran-3-yl]methyl]phenyl]-8-quinolinesulfonamide;
N-(3-[Cyclopropyl[4-hydroxy-2-oxo-6-[1-[(tetrahydro-2H-pyran-3-yl)methyl]propyl]-2H-pyran-3-yl]methyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzimidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-2-sulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-cyanobenzenesulfonamide;
N-(3-(R or S)-{Cyclopropyl-[6-(1-(R)-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-cyanobenzenesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-nitrobenzenesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-cyano-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-quinolinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-hydroxybenzenesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyrazolesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-quinazolinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-7H-purine-6-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzimidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-thiazole-4-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-ethoxycarbonyl-1H-imidazole-2-sulfaonamide;
N-(3-{Cyclopropyl-[6-(1-(tetrahydropyran-4-ylmethyl)-propyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-3-hydroxy-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-cyano-2-pyridinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-quinolinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-2-hydroxybenzenesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-ethyl}-phenyl)-2-pyrazolesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-ethyl}-phenyl)-2-quinazolinesulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-ethyl}-phenyl)-7H-purine-6-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-1H-imidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-benzimidazole-2-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-thiazole-4-sulfonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-4-ethoxycarbonyl-1H-imidazole-2-sulfaonamide;
N-(3-{Cyclopropyl-[6-(1-ethylphenethyl)-4-hydroxy-2-oxo-2H-pyran-3-yl]-methyl}-phenyl)-3-hydroxy-2-pyridinesulfonamide;
5-cyano-N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-2-pyridinesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyronel-N-methyl-2-quinolinesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-2-imidazolesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-2-pyrimidinesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-2-benzimidazolesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyronel-N-methyl-2-quinazolinesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-6-purinesulfonamide;
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-4-thiazolesulfonamide; and
N-[6-(1′
-benzylpropyl)-4-hydroxy-3-(1′
-cyclopropylmethylphenyl)-2-pyrone]-N-methyl-2-pyridinesulfonamide.
-
-
9. The compound of claim 1 of the formula VI
wherein R2 is a) H3C— - CH2—
,b) H3C—
(CH2)2—
,c) cyclopropyl-(CH2)2—
,d) F-phenyl-(CH2)2—
,e) het-SO2NH-phenyl-, f) (H3C)2HC—
CH2,g) phenyl-(CH2)2—
, orh) F3C—
(CH2)2—
;
wherein R3 is the moiety of formula X wherein R6 is a) H3C—
CH2—
,b) H3C—
(CH2)2—
,c) cyclopropyl-(CH2)2—
,d) F-phenyl-(CH2)2—
,e) het-SO2NH-phenyl, f) (H3C)2HC—
CH2,g) phenyl-(CH2)2—
, orh) F3C—
(CH2)2—
;
wherein R7 is a) H3C—
CH2—
,b) t-butyl, or c) cyclopropyl wherein R9 is a) —
NHSO2-het, orb) —
NHSO2-phenyl substituted by one (1) R1l;
wherein het is the following, substituted by zero (0) or one (1) R10, a) imidazol-4-yl, b) 2-pyridinyl, or c) quinolin-8-yl;
wherein R10 is, a) —
CH3,b) —
CN,c) —
CF3,d) —
NH2, ore) —
C(O)—
NH2;
wherein R11 is CN.
- CH2—
-
10. The compound of claim 9 selected from the group consisting of:
-
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-(4-fluorophenyl)ethyl)-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-(4-fluorophenyl)ethyl)-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-(4-fluorophenyl)ethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-(4-fluorophenyl)ethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-(l-[6,6-Bis-(2-cyclopropyl-ethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-(1-[6,6-Bis-(2-cyclopropyl-ethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-5-cyano-2-pyridinesulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-(3-[1-(6-Ethyl-5,6-dihydro-4-hydroxy-6-[3-([(l-methyl-1H-imidazol-4-yl)sulfonyl]amino)phenyl]-2-2H-pyran-3-yl)propyl]phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
5-Cyano-N-(3-[1-(6-[3-([(5-cyano-2-pyridinyl)sulfonyl]amino)phenyl]-6-ethyl-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl)propyl]phenyl)-2-pyridinesulfonamide;
N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-(1-[6,6-Bis-(2-cyclopropyl-ethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethyl-propyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-(1-[6,6-Bis-(2-cyclopropyl-ethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethyl-propyl)phenyl]-5-cyano-2-pyridinesulfonamide, 5-cyano-N-[3-(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R or S)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-cyano-N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-cyano-N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(S)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-cyano-N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(S)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-cyano-N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, N-[3-(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(R or S)-(2-phenethyl)-6-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(R)-(2-phenethyl)-6-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(S)-(2-phenethyl)-6-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(S)-(2-phenethyl)-6-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(R)-(2-phenethyl)-6-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, 5-amino-N-[3-(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R or S)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-amino-N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-amino-N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(S)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-amino-N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R)-(3,3,3-trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-amino-N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(S)-(3,3,3trifluoropropyl)-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, N-[3-(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-[6-(R or S)-propyl]-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R)-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, N-[3-(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(S)-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(R)-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, N-[3-(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-(S)-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]1-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]1-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-phenethyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-phenethyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-phenethyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-phenethyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-phenethyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-phenethyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenethyl)-6-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenethyl)-6(R or S)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenethyl)-6(R or S)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 4-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenethyl)-6(R or S)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridine sulfonamide, 5-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3-(1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(R or S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridine-sulfonamide, 5-Cyano-N-[3(R)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(R)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3-(1-[5,6-dihydro-6,6-diisobutyl-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-2-pyridinesulfonamide, N-[3-(1-[5,6-Dihydro-6,6-diisobutyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, 5-Cyano-N-[3-(1-[5,6-dihydro-6,6-diisobutyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, N-[3(R or S)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(R or S)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(R)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(R)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(R)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(S)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(S)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(R)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(S)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(S)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, 5-Cyano-N-[3-(1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]cyclopropylmethyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R or S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridine-sulfonamide, 5-Amino-N-[3(R)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R or S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R)-(-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R or S)-(1-[6(R or S)-(2-[4-fluorophenyl]ethyl)-5,6-dihydro-4-hydroxy-2-oxo-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridine-sulfonamide, 5-Amino-N-[3(R)-(1-[6(R)-(2-[4-fluorophenyl]ethyl)-5,6-dihydro-4-hydroxy-2oxo-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R)-(1-[6(S)-(2-[4-fluorophenyl]ethyl)-5,6-dihydro-4-hydroxy-2-oxo-6-propyl-2H-pyran-3-yl-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[6(R)-(2-[4-fluorophenyl]ethyl)-5,6-dihydro-4-hydroxy-2-oxo-6-propyl-2H-pyran-3-yl-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[6(S)-(2-[4-fluorophenyl]ethyl)-5,6-dihydro-4-hydroxy-2-oxo-6-propyl-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, N-[3(R or S)-(1-[5,6-Dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(R)-(-[5,6-Dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(S)-(-[5,6-Dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, 5-Amino-N-[3(R or S)-(1-[5,6-dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(R)-(1-[5,6-dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Amino-N-[3(S)-(1-[5,6-dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(R or S)-(1-[5,6-dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(R)-(1-[5,6-dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, 5-Cyano-N-[3(S)-(1-[5,6-dihydro-6,6-dipropyl-4-hydroxy-2-oxo-2H-pyran-3-yl]-2,2-dimethylpropyl)phenyl]-2-pyridinesulfonamide, N-[3(R or S)-(1-[6,6-Bis(2-phenylethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(R)-(1-[6,6-Bis(2-phenylethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(S)-(1-[6,6-Bis(2-phenylethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3(R or S)-(1-[6,6-Bis(2-phenylethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-5-cyano-2-pyridinesulfonamide, N-[3(R)-(1-[6,6-Bis(2-phenyl-ethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-5-cyano-2-pyridinesulfonamide, N-[3(S)-(1-[6,6-Bis(2-phenyl-ethyl)-5,6-dihydro-4-hydroxy-2-oxo-2H-pyran-3-yl]propyl)phenyl]-5-cyano-2-pyridinesulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-4-cyanobenzenesulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-8-quinolinesulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)propyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-carbamoylpyridine-2-sulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-(4-fluorophenyl)ethyl)-2H-pyran-3-yl)propyl}phenyl]-5-carbamoylpyridine-2-sulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)propyl}phenyl]-5-carbamoylpyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-phenethyl-6-propyl-2H-pyran-3-yl)propyl]phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl,phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-bis(2-phenylethyl)-2H-pyran-3-yl)-2,2-dimethylpropyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl}-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-1-methyl-1H-imidazole-4-sulfonamide, N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-(2-(4-fluorophenyl)ethyl)-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-(2-(4-fluorophenyl)ethyl)-6-5 propyl-2H-pyran-3-yl)propyl}phenyl]-5-aminopyridine-2-sulfonamide, N-[3-[1-(S)-[5,6,-Dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(triflouromethyl)-2-pyridinesulfonamide (3S,6R)-N-[3-[1-[5,6,-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(triflouromethyl)-2-pyridinesulfonamide (3S)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6,6-dipropyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (3R)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6,6-dipropyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (3R)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6-propyl-6-phenethyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (3R,6S)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6-propyl-6-phenethyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (3S,6S)-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(triflouromethyl)-2-pyridinesulfonamide.
-
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11. The compound of claim 9
wherein R2 is a) H3C— - (CH2)2—
, orb) phenyl-(CH2)2—
;
wherein R3 is the moiety of formula X; wherein R6 is a) H3C—
(CH2)2—
, orb) phenyl-(CH2)2—
;
wherein R7 is a) H3C—
CH2—
, orb) t-butyl;
wherein R9 is —
NHSO2-het;wherein het is the following, substituted by one (1) R10, a) imidazol-4-yl, or b) 2-pyridinyl;
wherein R10 is, a) —
CH3,b) —
CN, orc) —
CF3.
- (CH2)2—
-
12. The compound of claim 11 selected from the group consisting of:
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5-Trifluoromethyl-N-[3-(R or S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
5-Trifluoromethyl-N-[3-(R)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
or (3R)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6,6-dipropyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide5-Trifluoromethyl-N-[3-(S)-[1-[4-hydroxy-2-oxo-6,6-di-n-propyl-5,6-dihydro-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
or (3S)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6,6-dipropyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide5-Trifluoromethyl-N-[3(R or S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R or S)-(2-phenethyl)-6(R or S)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridine sulfonamide;
5-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
5-Trifluoromethyl-N-[3(R)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
or (3R,6S)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6-propyl-6-phenethyl-2H-pyran-3-yl)propy]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide5-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(R)-(2-phenethyl)-6(R)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
or (3S,6R)-N-[3-[1-[5,6,-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(triflouromethyl)-2-pyridinesulfonamide5-Trifluoromethyl-N-[3(S)-[1-[5,6-dihydro-4-hydroxy-2-oxo-6(S)-(2-phenethyl)-6(S)-n-propyl-2H-pyran-3-yl]-propyl]-phenyl]-2-pyridinesulfonamide;
or (3S,6S)-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(triflouromethyl)-2-pyridinesulfonamideN-[3-[1-(S)-[5,6,-Dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(triflouromethyl)-2-pyridinesulfonamide (3R)-N-[3-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6-propyl-6-phenethyl-2H-pyran-3-yl)propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide N-[3(R or S)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(R or S)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl)-1-methyl-1H-imidazole-4-sulfonamide;
N-[3(R)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(R)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3(R)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(S)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3(S)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(R)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3(S)-[1-(5,6-Dihydro-4-hydroxy-2-oxo-6(S)-[2-phenylethyl]-6-propyl-2H-pyran-3-yl)-2,2-dimethylpropyl]phenyl]-1-methyl-1H-imidazole-4-sulfonamide;
N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6,6-dipropyl-2H-pyran-3-yl)-propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1(R or S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R or S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1(R)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide;
N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(R)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide; and
N-[3-{1(S)-(4-Hydroxy-5,6-dihydro-2-oxo-6(S)-phenethyl-6-propyl-2H-pyran-3-yl)propyl}phenyl]-5-cyanopyridine-2-sulfonamide.
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Specification