US2009169510A1PendingUtilityA1
Novel macrocyclic inhibitors of hepatitis c virus replication
Est. expiryJul 25, 2025(expired)· nominal 20-yr term from priority
Inventors:Lawrence M. BlattScott D. SeiwertSteven W. AndrewsPierre MartinAndreas SchumacherBradley BarnettC. Todd EaryRobert J. KausTimothy KercherWeidong LiuMichael LyonPaul NicholsBin WangTarek SammakiaApril L. KennedyYutong Jiang
A61P 43/00A61P 31/14A61P 31/12C07K 5/0804C07K 5/0806A61K 38/212A61K 38/217A61P 1/16A61K 38/1793C07D 487/04A61K 38/00A61K 38/55A61K 38/2292C07D 471/04A61K 31/407Y02A50/30
62
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Claims
Abstract
The embodiments provide compounds of the general Formulae I through general Formula VIII, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
Claims
exact text as granted — not AI-modified1 . A compound having the structure of Formula VIII:
or a pharmaceutically acceptable salt thereof wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with C 1-6 alkoxy; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with cyano; C 1-6 alkyl substituted with halo; C 1-6 alkyl substituted with heterocyclyl; C 1-6 alkyl substituted with hydroxy; C 1-6 alkyl substituted with di-(C 1-6 )alkylamino; C 1-6 alkyl substituted with halo(C 1-6 )alkoxy; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
Z is a C 5-7 saturated or unsaturated chain containing one or two heteroatoms selected from O, S, or NR 6 , wherein R 6 is H, C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl;
R 4 is H or C 1-6 alkyl;
R 5 is selected from the group consisting of H; C 1-6 alkyl; C(O)NR 6 R 7 wherein R 6 and R 7 are each independently H or C 1-6 alkyl; C(O)NHR 8 wherein R 8 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl, C 1-6 alkyl substituted with halo, C 3-7 cycloalkyl, or C 6 or 10 aryl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, halo(C 1-6 )alkyl, C 1-6 alkylcyano, or halo(C 1-6 )alkoxy; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; substituted or unsubstituted C 6 or 10 aryl; NR 1a R 1b ; and a substituted or unsubstituted heteroaromatic ring,
or Y is a carboxylic acid;
wherein R 1a and R 1b are each independently H, C 1-6 alkyl, C 1-6 alkyl substituted with aryl, C 1-6 alkyl substituted with halo, C 1-6 alkyl substituted with heterocyclyl, or substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, or C 6 or 10 aryl,
or R 1a and R 1b are each independently H or heterocycle, which is a five-, six-, or seven-membered, saturated or unsaturated heterocyclyl containing from one to four heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur;
V is O;
W is selected from O and NR 15 , wherein R 15 is H; and
the dashed lines represent an optional double bond.
2 . The compound of claim 1 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of substituted or unsubstituted varients of: pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
3 . The compound of claim 1 , wherein Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1.
4 . The compound of claim 1 , wherein Z is a C 5-7 saturated or unsaturated chain containing one or two NR 6 , wherein R 6 is H, C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl.
5 . The compound of claim 1 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
6 . The compound of claim 5 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
7 . The compound of claim 1 , wherein Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of substituted or unsubstituted varients of: pyrazine, pyrimidine, pyridazine, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, quinoline, isoquinoline, quinoxaline, benzothiazole, and benzimidazole; and R 2 is H.
8 . The compound of claim 1 , wherein R 4 is hydrogen.
9 . The compound of claim 1 , wherein R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 and R 7 are each independently H or C 1-6 alkyl; C(O)NHR 8 wherein R 8 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl.
10 . The compound of claim 9 , wherein R 5 is selected from the group consisting of C(O)NHR 8 wherein R 8 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl.
11 . The compound of claim 1 , wherein Z is a C 5-7 saturated or unsaturated chain containing one or two heteroatoms selected from O or NR 6 , wherein R 6 is H, C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl.
12 . The compound of claim 11 , wherein Z is a C 5-7 saturated or unsaturated chain containing one or two heteroatoms selected from O or NR 6 , wherein R 6 is H, C 1-6 alkyl, or C 3-7 cycloalkyl.
13 . The compound of claim 1 , wherein:
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, halo(C 1-6 )alkyl, C 1-6 alkylcyano, or halo(C 1-6 )alkoxy; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; substituted or unsubstituted C 6 or 10 aryl; NR 1a R 1b ; and a substituted or unsubstituted heteroaromatic ring, wherein R 1a and R 1b are each independently H, C 1-6 alkyl, or substituted or unsubstituted varients of: C 3-7 cycloalkyl or C 4-10 cycloalkyl-alkyl.
14 . The compound of claim 13 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, NR 1a R 1b , and a substituted or unsubstituted heteroaromatic ring, wherein R 1a and R 1b are each independently H or C 1-6 alkyl.
15 . The compound of claim 1 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
Z is a C 6-7 saturated or unsaturated chain containing one or two heteroatoms selected from O or NR 6 , wherein R 6 is H, C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl;
R 4 is H;
R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 and R 7 are each independently H or C 1-6 alkyl, C(O)NHR 8 wherein R 8 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, or cyano; substituted or unsubstituted C 4-10 cycloalkyl-alkyl, substituted or unsubstituted C 6 or 10 aryl; NR 1a R 1b ; and a substituted or unsubstituted heteroaromatic ring; and
W is O.
16 . The compound of claim 15 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 5 is selected from the group consisting of C(O)NHR 8 wherein R 8 is C 1-6 alkyl, C(O)R 8 wherein R 8 is C 1-6 alkyl, and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Z is a C 7 saturated or unsaturated chain containing one heteroatom selected from O or NR 6 , wherein R 6 is H, C 1-6 alkyl, or C 3-7 cycloalkyl; and
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, NR 1a R 1b , and a substituted or unsubstituted heteroaromatic ring, wherein R 1a and R 1b are each independently H or C 1-6 alkyl.
17 . The compound of claim 16 , wherein R 9 is C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy.
18 . A compound having the structure of Formula VIII:
or a pharmaceutically acceptable salt thereof wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
Z is a C 5-7 saturated or unsaturated chain containing one NR 6 , wherein R 6 is H, C 1-6 alkyl, or C 3-7 cycloalkyl;
R 4 is H;
R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 and R 7 are each C 1-6 alkyl; C(O)NHR 8 wherein R 8 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl or C 6 or C 10 aryl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, halo(C 1-6 )alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, mono(C 1-6 )alkylamino carbonyl, di(C 1-6 )alkylamino carbonyl, or C 3-6 cycloalkyl(C 1-6 alkyl); substituted or unsubstituted substituted or unsubstituted C 6 or 10 aryl; NR 1a R 1b ; and a substituted or unsubstituted heteroaromatic ring,
or Y is a carboxylic acid;
wherein R 1a and R 1b are each independently H, C 1-6 alkyl, C 1-6 alkyl substituted with aryl, C 1-6 alkyl substituted with halo, C 1-6 alkyl substituted with heterocyclyl, or substituted or unsubstituted varients of: C 3-7 cycloalkyl or C 6 or 10 aryl;
V is O;
W is selected from O and NR 15 , wherein R 15 is H; and
the dashed lines represent an optional double bond.
19 . The compound of claim 18 , wherein Z is a chain selected from:
20 . The compound of claim 18 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of substituted or unsubstituted varients of: phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
21 . The compound of claim 18 , wherein R 9 is C 3-7 cycloalkyl.
22 . The compound of claim 18 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 5 is selected from the group consisting of C(O)NHR 8 wherein R 8 is C 1-6 alkyl, C(O)R 8 wherein R 8 is C 1-6 alkyl, and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, NR 1a R 1b , and a substituted or unsubstituted heteroaromatic ring, wherein R 1a and R 1b are each independently H or C 1-6 alkyl; and
W is O.
23 . The compound of claim 22 , wherein Z is a chain selected from:
24 . A compound having the structure of Formula VIII:
or a pharmaceutically acceptable salt thereof wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with C 1-6 alkoxy; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with cyano; C 1-6 alkyl substituted with halo; C 1-6 alkyl substituted with heterocyclyl; C 1-6 alkyl substituted with hydroxy; C 1-6 alkyl substituted with di-(C 1-6 )alkylamino; C 1-6 alkyl substituted with halo(C 1-6 )alkoxy; and substituted or unsubstituted varients of C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
Z is a C 5-7 saturated or unsaturated chain containing one O;
R 4 is H;
R 5 is selected from the group consisting of H; C 1-6 alkyl; C(O)NR 6 R 7 wherein R 6 and R 7 are each H or are each C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, C 6 or C 10 aryl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl, C 1-6 alkyl substituted with halo, C 3-7 cycloalkyl, or C 6 or 10 aryl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, halo(C 1-6 )alkyl, cyano(C 1-6 )alkyl, aryl(C 1-6 )alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, di-(C 1-6 )alkylaminocarbonyl, mono-(C 1-6 )alkylaminocarbonyl, arylcarbonyl, C 3-6 cycloalkyl(C 1-6 )alkyl, or heteroaryl(C 1-6 )alkyl; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; substituted or unsubstituted C 6 or 10 aryl; NR 1a R 1b ; and a substituted or unsubstituted heteroaromatic ring,
or Y is a carboxylic acid;
wherein R 1a and R 1b are each independently H, C 1-6 alkyl, C 1-6 alkyl substituted with aryl, C 1-6 alkyl substituted with halo, C 1-6 alkyl substituted with heterocyclyl, or substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, or C 6 or 10 aryl,
or R 1a and R 1b are each independently H or heterocycle, which is a five-, six-, or seven-membered, saturated or unsaturated heterocyclyl containing from one to four heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur;
V is O;
W is selected from O and NR 15 , wherein R 15 is H; and
the dashed lines represent an optional double bond.
25 . The compound of claim 24 , wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
26 . The compound of claim 24 , wherein Z is a chain selected from:
27 . A compound having the structure of Formula VIII:
or a pharmaceutically acceptable salt thereof wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
Z is a C 5-7 saturated or unsaturated chain containing one O;
R 4 is H;
R 5 is selected from the group consisting of C(O)NHR 8 wherein R 8 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, NR 1a R 1b , and a substituted or unsubstituted heteroaromatic ring, wherein R 1a and R 1b are each independently H or C 1-6 alkyl;
V is O;
W is O; and
the dashed lines represent an optional double bond.
28 . The compound of claim 27 , wherein Z is a chain selected from:
29 . A composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.
30 . The composition according to the claim 29 further comprising at least one of an interferon and ribavirin.
31 . The composition according to claim 29 further comprising a second compound having anti-HCV activity.
32 . The composition according to claim 31 wherein the second compound having anti-HCV activity is an interferon.
33 . The composition according to claim 32 wherein the interferon is selected from interferon alpha, pegylated interferon alpha, and consensus interferon.
34 . The composition according to claim 31 wherein the second compound having anti-HCV activity is selected from ribavirin and an inosine monophosphate dehydrogenase inhibitor.
35 . The composition according to claim 31 wherein the second compound having anti-HCV activity is effective to inhibit the function of a target selected from HCV serine protease, HCV polymerase, and HCV helicase for the treatment of an HCV infection.
36 . A method of inhibiting the function of HCV serine protease comprising contacting the HCV serine protease with the compound of claim 1 .
37 . A method of treating an HCV infection in a patient, comprising administering to the patient a therapeutically effective amount of the compound of claim 1 .
38 . The method of claim 37 wherein the compound is effective to inhibit the function of the HCV serine protease.
39 . The method of claim 37 further comprising administering a second compound having anti-HCV activity prior to, after, or simultaneously with the compound of claim 1 .
40 . The method of claim 39 wherein the second compound having anti-HCV activity is an interferon.
41 . The method of claim 40 wherein the interferon is selected from interferon alpha, pegylated interferon alpha, and consensus interferon.
42 . The method of claim 39 wherein the second compound having anti-HCV activity is selected from ribavirin and an inosine monophosphate dehydrogenase inhibitor.
43 . The method of claim 39 wherein the second compound having anti-HCV activity is effective to inhibit the function of a target selected from HCV serine protease, HCV polymerase, and HCV helicase for the treatment of an HCV infection.
44 . The method of claim 39 wherein the second compound having anti-HCV activity is effective to inhibit the function of target in the HCV life cycle other than the HCV serine protease.
45 . A compound having the general Formula VIIIb:
or a pharmaceutically acceptable salt thereof wherein:
R 1 and R 2 are each independently H, halo, cyano, hydroxy, C 1-3 alkyl, or C 1-3 alkoxy;
R 5 is H; C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 5-6 cycloalkyl; or C(O)NHR 8 wherein R 8 is C 1-6 alkyl;
R 9 is C 1-3 alkyl, C 3-5 cycloalkyl, or phenyl which is optionally substituted by up to two halo, cyano, hydroxy, C 1-3 alkyl, or C 1-3 alkoxy;
W is selected from O or NH;
Z is a C 5-7 saturated or unsaturated chain containing one or two heteroatoms selected from O, S, or NR 6 ; and
R 6 is H, C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl.
46 . The compound of claim 45 , wherein:
R 1 and R 2 are each independently H or halo; R 5 is C(O)OR 8 wherein R 8 is C 1-6 alkyl; R 9 is C 3-5 cycloalkyl; W is O; Z is a C 5-7 saturated or unsaturated chain containing one NR 6 ; and R 6 is C 3-7 cycloalkyl.
47 . The compound of claim 45 having the structure:
48 . A compound having the Formula VIIIa:
or a pharmaceutically acceptable salt thereof wherein:
Q is a unsubstituted or substituted core ring
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with C 1-6 alkoxy; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with cyano; C 1-6 alkyl substituted with halo; C 1-6 alkyl substituted with heterocyclyl; C 1-6 alkyl substituted with hydroxy; C 1-6 alkyl substituted with di-(C 1-6 )alkylamino; C 1-6 alkyl substituted with halo(C 1-6 )alkoxy; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 4 is H or C 1-6 alkyl;
R 5 is selected from the group consisting of H; C 1-6 alkyl; C(O)NR 6 R 7 wherein R 6 and R 7 are each independently H or C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl, C 1-6 alkyl substituted with halo, C 3-7 cycloalkyl, or C 6 or 10 aryl;
V is O;
W is selected from O and NH; and
Y is an acyl sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, halo(C 1-6 )alkyl, C 1-6 alkylcyano, or halo(C 1-6 )alkoxy; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; substituted or unsubstituted C 6 or 10 aryl; and a substituted or unsubstituted heteroaromatic ring; and
the dashed line represents an optional double bond.
49 . The compound of claim 48 , wherein:
Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with C 1-6 alkoxy; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with cyano; C 1-6 alkyl substituted with halo; C 1-6 alkyl substituted with heterocyclyl; C 1-6 alkyl substituted with hydroxy; C 1-6 alkyl substituted with di-(C 1-6 )alkylamino; C 1-6 alkyl substituted with halo(C 1-6 )alkoxy; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
50 . The compound of claim 48 , wherein Q is a unsubstituted or substituted core ring
where p is 0 or 1.
51 . The compound of claim 48 , wherein:
Q is a unsubstituted or substituted core ring
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
52 . The compound of claim 51 , wherein:
Q is a unsubstituted or substituted core ring
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
53 . The compound of claim 48 , wherein Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of substituted or unsubstituted varients of: pyrazine, pyrimidine, pyridazine, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, quinoline, isoquinoline, quinoxaline, benzothiazole, and benzimidazole; and R 2 is H.
54 . The compound of claim 48 , wherein R 4 is hydrogen.
55 . The compound of claim 48 , wherein R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 and R 7 are each independently H or C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl.
56 . The compound of claim 55 , wherein R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 is H and R 7 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl.
57 . The compound of claim 48 , wherein:
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, or halo(C 1-6 )alkyl; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; and a substituted or unsubstituted heteroaromatic ring.
58 . The compound of claim 57 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, and a substituted or unsubstituted heteroaromatic ring.
59 . The compound of claim 48 , wherein:
Q is a unsubstituted or substituted core ring
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 4 is H;
R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 and R 7 are each independently H or C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Y is an acyl sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, or halo(C 1-6 )alkyl; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; substituted or unsubstituted C 6 or 10 aryl; and a substituted or unsubstituted heteroaromatic ring; and
W is O.
60 . The compound of claim 59 , wherein:
Q is a unsubstituted or substituted core ring
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 is H and R 7 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl; and
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, and a substituted or unsubstituted heteroaromatic ring.
61 . The compound of claim 60 , wherein R 9 is C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy.
62 . The compound of claim 48 , wherein:
Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of substituted or unsubstituted varients of: phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H; R 4 is H; R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 is H and R 7 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl; W is O; and Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, and a substituted or unsubstituted heteroaromatic ring.
63 . A compound having the Formula VIIIa:
or a pharmaceutically acceptable salt thereof wherein:
Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with C 1-6 alkoxy; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with cyano; C 1-6 alkyl substituted with halo; C 1-6 alkyl substituted with heterocyclyl; C 1-6 alkyl substituted with hydroxy; C 1-6 alkyl substituted with di-(C 1-6 )alkylamino; C 1-6 alkyl substituted with halo(C 1-6 )alkoxy; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 4 is H;
R 5 is selected from the group consisting of H; C 1-6 alkyl; C(O)NR 6 R 7 wherein R 6 and R 7 are each H or are each C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; C 6 or C 10 aryl, tetrahydrofuran ring, or tetrahydropyran ring; and C(O)OR 8 wherein R 8 is C 1-6 alkyl, C 1-6 alkyl substituted with halo, C 3-7 cycloalkyl, or C 6 or 10 aryl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 1-6 alkyl; C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl, C 1-6 alkoxy, halo, cyano, halo(C 1-6 )alkyl, cyano(C 1-6 )alkyl, aryl(C 1-6 )alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, di-(C 1-6 )alkylaminocarbonyl, mono-(C 1-6 )alkylaminocarbonyl, arylcarbonyl, C 3-6 cycloalkyl(C 1-6 )alkyl, or heteroaryl(C 1-6 )alkyl; substituted or unsubstituted C 4-10 cycloalkyl-alkyl; substituted or unsubstituted C 6 or 10 aryl; and a substituted or unsubstituted heteroaromatic ring,
V is O;
W is selected from O and NH; and
the dashed lines represent an optional double bond.
64 . The compound of claim 63 , wherein:
Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of C 1-6 alkyl; C 1-6 alkyl substituted with aryl; C 1-6 alkyl substituted with heterocyclyl; and substituted or unsubstituted varients of: C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H.
65 . A compound having the Formula VIIIa:
or a pharmaceutically acceptable salt thereof wherein:
Q is R 1 -R 2 , wherein R 1 is selected from the group consisting of phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is H;
R 4 is H;
R 5 is selected from the group consisting of C(O)NR 6 R 7 wherein R 6 is H and R 7 is C 1-6 alkyl; C(O)R 8 wherein R 8 is C 1-6 alkyl; and C(O)OR 8 wherein R 8 is C 1-6 alkyl or C 3-7 cycloalkyl;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is selected from the group consisting of C 3-7 cycloalkyl optionally substituted with C 1-6 alkyl or C 1-6 alkoxy, and a substituted or unsubstituted heteroaromatic ring,
V is O;
W is O; and
the dashed lines represent an optional double bond.
66 . A compound having the structure of Formula VIII:
or a pharmaceutically acceptable salt, prodrug, or ester thereof wherein:
Q is an unsubstituted or substituted core ring selected from:
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole; and R 2 is a substituted or unsubstituted group selected from H, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole;
Z is a C 5-7 saturated or unsaturated chain containing one or two heteroatoms selected from O, S, or NR 6 ;
R 4 is H, C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;
R 5 is H, C 1-6 alkyl, C(O)NR 6 R 7 , C(O)NHR 8 , C(S)NR 6 R 7 , C(O)R 8 , C(O)OR 8 , S(O) 2 R 8 , or (CO)CHR 21 NH(CO)R 22 ;
R 6 and R 7 are each independently H, C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, or substituted or unsubstituted phenyl; or R 6 and R 7 are taken together with the nitrogen to which they are attached to form indolinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl;
R 8 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, C 6 or 10 aryl, C 1-6 alkyl, tetrahydrofuran ring, tetrahydropyran ring;
Y is a sulfonimide of the formula —C(O)NHS(O) 2 R 9 , wherein R 9 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl, C 6 or 10 aryl, C 1-6 alkyl, NR 6 R 7 , NR 1a R 1b , and a heteroaromatic ring,
or Y is a carboxylic acid or pharmaceutically acceptable salt, solvate, or prodrug thereof;
wherein R 1a and R 1b are each independently H or a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, and C 6 or 10 aryl,
or R 1a and R 1b are each independently H, heterocycle, which is a five-, six-, or seven-membered, saturated or unsaturated heterocyclic molecule, containing from one to four heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur,
or NR 1a R 1b is a three- to six-membered optionally substituted alkyl cyclic secondary amine,
or NR 1a R 1b is a heteroaryl selected from the group consisting of:
wherein R 1c is H, halo, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 3-6 cycloalkoxy, NO 2 , N(R 1d ) 2 , NH(CO)R 1d , or NH(CO)NHR 1d , wherein each R 1d is independently H, C 1-6 alkyl, or C 3-6 cycloalkyl,
or R 1c is NH(CO)OR 1e , wherein R 1e is C 1-6 alkyl or C 3-6 cycloalkyl; p=0 or 1;
V is selected from O, S, and NH;
W is selected from O, NR 15 , and CHR 15 , wherein R 15 is H, C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, and substituted or unsubstituted C 1-6 alkyl;
the dashed lines represent an optional double bond;
R 21 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, C 6 or 10 aryl, pyridyl, pyrimidyl, pyrazinyl, thienyl, furanyl, thiazolyl, oxazolyl, phenoxy, and thiophenoxy; and
R 22 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl, and phenyl.
67 . A compound having the Formula VIIIa:
or a pharmaceutically acceptable salt, prodrug, or ester thereof wherein:
Q is a unsubstituted or substituted core ring
where p is 0 or 1,
or Q is R 1 -R 2 , wherein R 1 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, or benzimidazole; and R 2 is a substituted or unsubstituted group selected from H, phenyl, pyridine, pyrazine, pyrimidine, pyridazine, pyrrole, furan, thiophene, thiazole, oxazole, imidazole, isoxazole, pyrazole, isothiazole, naphthyl, quinoline, isoquinoline, quinoxaline, benzothiazole, benzothiophene, benzofuran, indole, and benzimidazole;
R 4 is selected from H, C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, substituted or unsubstituted phenyl, and substituted or unsubstituted benzyl;
R 5 is H, C 1-6 alkyl, C(O)NR 6 R 7 , C(S)NR 6 R 7 , C(O)R 8 , C(O)OR 8 , S(O) 2 R 8 , or (CO)CHR 21 NH(CO)R 22 ;
R 6 and R 7 are each independently H, C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, or substituted or unsubstituted phenyl, or R 6 and R 7 are taken together with the nitrogen to which they are attached to form indolinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl;
R 8 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, C 6 or 10 aryl, C 1-6 alkoxy, C 1-6 alkyl, tetrahydrofuran ring, and tetrahydropyran ring;
V is selected from O, S, and NH;
W is selected from O, NH, and CH 2 ;
Y is an amide of the formula —C(O)NHR 9 , wherein R 9 is a substituted or unsubstituted group selected from C 1-6 alkyl, phenyl, cyano, C 3-7 cycloalkyl, or C 4-10 cycloalkyl-alkyl, C 5-10 arylalkyl, and heteroarylalkyl;
or Y is an acyl sulfonimide of the formula —C(O)NHS(O)R 9 , wherein R 9 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, C 5-10 arylalkyl, C 6 or 10 aryl, and heteroaromatic ring;
the dashed line represents an optional double bond;
R 21 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, phenyl, C 6 or 10 aryl, pyridyl, pyrimidyl, pyrazinyl, thienyl, furanyl, thiazolyl, oxazolyl, phenoxy, and thiophenoxy; and
R 22 is a substituted or unsubstituted group selected from C 1-6 alkyl, C 3-7 cycloalkyl, C 4-10 cycloalkyl-alkyl, and phenyl.Join the waitlist — get patent alerts
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