- Matched and mixed cap derivatives in the tetracyclic indole class of HCV NS5A inhibitors
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A matched and mixed capping SAR study was conducted on the tetracyclic indole class of HCV NS5A inhibitors to examine the influence of modifications of this region on the overall HCV virologic resistance profiles.
- Dwyer, Michael P.,Keertikar, Kerry M.,Chen, Lei,Tong, Ling,Selyutin, Oleg,Nair, Anilkumar G.,Yu, Wensheng,Zhou, Guowei,Lavey, Brian J.,Yang, De-Yi,Wong, Michael,Kim, Seong Heon,Coburn, Craig A.,Rosenblum, Stuart B.,Zeng, Qingbei,Jiang, Yueheng,Shankar, Bandarpalle B.,Rizvi, Razia,Nomeir, Amin A.,Liu, Rong,Agrawal, Sony,Xia, Ellen,Kong, Rong,Zhai, Ying,Ingravallo, Paul,Asante-Appiah, Ernest,Kozlowski, Joseph A.
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p. 4106 - 4111
(2016/08/01)
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- SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, D, E, F and L are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
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Page/Page column 63
(2013/03/28)
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- SILYL-CONTAINING HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Silyl-Containing Heterocyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, C, D and R2 are as defined herein. The present invention also relates to compositions comprising at least one Silyl-Containing Heterocyclic Compound, and methods of using the Silyl-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.
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Page/Page column 59
(2013/03/28)
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- TETRACYCLIC INDOLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Tetracyclic Indole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprisingat least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing HCV infection in a patient.
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Page/Page column 72
(2012/04/17)
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- FUSED TETRACYCLE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tetracycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', B, G, R1, U, V, W, W', X, X', Y and Y' are as defined herein. The present invention also relates to compositions comprising at least one Fused Tetracycle Derivative, and methods of using the Fused Tetracycle Derivatives for treating or preventing HCV infection in a patient.
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Page/Page column 71
(2012/05/04)
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- TETRACYCLIC HETEROCYCLE COMPOUNDS FOR TREATING HEPATITIS C VIRAL INFECTION
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Tetracyclic heterocycle compounds of formula (I) and pharmaceutically acceptable salts thereof are provided, wherein A, A', G, R1, R15, U, V, V', W, W, X, X', Y and Y' are as defined in the invention. The pharmaceutical compositions comprising these compounds and the use of the compounds for treating hepatitis C virus (HCV) infection are also provided.
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Page/Page column 65
(2012/04/17)
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- FUSED TETRACYCLIC HETEROCYCLE COMPOUNDS AND METHODS OF USE THEREOF FOR TREATMENT OF VIRAL DISEASES
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The present invention discloses novel Fused Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A', G, R1, R15, U, V, V', W, W', X, X', Y and Y' are as defined herein. The present invention also discloses compositions comprising at least one Fused Tetracyclic Heterocycle Compound, and methods of using the Fused Tetracyclic Heterocycle Compounds for treating or preventing HCV infection in a patient.
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- FUSED TRICYCLIC ARYL COMPOUNDS USEFUL FOR THE TREATMENT OF VIRAL DISEASES
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The present invention relates to novel Fused Tricyclic Aryl Compounds, compositions comprising at least one Fused Tricyclic Aryl Compound, and methods of using the Fused Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient.
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Page/Page column 103
(2010/12/17)
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- Anti-Viral Compounds
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Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection
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Page/Page column 24
(2010/07/08)
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- ANTIVIRAL COMPOUNDS COMPOSED OF THREE LINKED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C
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The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56
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Page/Page column 75-76
(2010/12/26)
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- ANTIVIRAL COMPOUNDS COMPOSED OF THREE ALIGNED ARYL MOIETIES TO TREAT DISEASES SUCH AS HEPATITIS C
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The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
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Page/Page column 40-41
(2010/12/26)
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- Inhibitors of HCV replication
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Compounds having the structure of formula I are described. The compounds can inhibit hepatitis C virus (HCV) replication, and in particular can inhibit the function of the HCV NS5A protein.
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Page/Page column 96
(2010/11/25)
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- Optical Resolution and Asymmetric Transformation of (RS)-N-Alkyl- and (RS)-N,N-Dialkyl-2-phenylglycines
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Optical resolution of (RS)-N-methyl-2-phenylglycine and (RS)-N-ethyl-2-phenylglycine was carried out by using (1S)-10-camphorsulfonic acid as resolving agents, and that of (RS)-N-ethyl-N-methyl-2-phenylglycine by (R)- and (S)-1-phenylethylamine.Racemization rates of optically active Mpg, Epg, Emp, N,N-dimethyl-2-phenylglycine , and six α-amino acids were measured by heating in carboxylic acids.The electron-donating amino acid side chain and N-substituted alkyl group decreased therate to inhibit the formation of intermediary carbanions, whereas the electron-withdrawing side chain increased it.Asymmetric transformation of (RS)-Mpg, (RS)-Epg, and (RS)-Dmp was carried out on the basis of the results of optical resolution and racemization to give the corresponding enantiomers of approximately 100percent optical purities in over 70percent yield based on the sterting racemates.
- Shiraiwa, Tadashi,Baba, Yoshihisa,Miyazaki, Hideya,Sakata, Shinji,Kawamura, Seiko,et al.
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p. 1430 - 1437
(2007/10/02)
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- Chiral β-dimethylaminoalkylphosphines. Highly efficient ligands for a nickel complex catalyzed asymmetric grignard cross-coupling reaction
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Chiral β-dimethylaminoalkylphosphines were prepared starting with amino acids, (S)-alanine, (S)-phenylalanine, (R)-phenylglycine, (S)-valine, and (R)-tert-leucine. The chiral phosphines were found to be highly efficient ligands for a nickel catalyzed asymmetric Grignard cross-coupling reaction (38~94% optical yield).
- Hayashi, Tamio,Fukushima, Motoo,Konishi, Mitsuo,Kumada, Makoto
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