945686-02-2Relevant academic research and scientific papers
A practical and efficient synthesis of 6-carboalkoxy-13-cycloalkyl-5H- indolo[2,1-a][2]benzazepine-10-carboxylic acid derivatives
Hewawasam, Piyasena,Tu, Yong,Hudyma, Thomas W.,Zhang, Xiaofan,Gentles, Robert G.,Kadow, John F.,Meanwell, Nicholas A.
supporting information, p. 1148 - 1153 (2014/02/14)
A convenient and practical synthesis of 6-carboalkoxy-13-cycloalkyl-5H- indolo[2,1-a][2]benzazepine-10-carboxylic acid derivatives (6) has been developed. The key step in the synthesis utilizes an intramolecular tandem reaction sequence of a Michael addition followed by a Horner-Wadsworth-Emmons (HWE) olefination reaction between hemi-aminal 11 and methyl 2-(dimethoxyphosphoryl)acrylate 12. The ring construction occurred efficiently and purification of the products 6 was straightforward. The C-10 methyl ester of 6a was hydrolyzed selectively to the carboxylic acid 13 while the olefin of 6d was converted to the cyclopropane 14 using trimethylsulfoxonium iodide in DMSO in the presence of NaH.
Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055
Vendeville, Sandrine,Lin, Tse-I.,Hu, Lili,Tahri, Abdellah,McGowan, David,Cummings, Maxwell D.,Amssoms, Katie,Canard, Maxime,Last, Stefaan,Van Den Steen, Iris,Devogelaere, Benoit,Rouan, Marie-Claude,Vijgen, Leen,Berke, Jan Martin,Dehertogh, Pascale,Fransen, Els,Cleiren, Erna,Van Der Helm, Liesbet,Fanning, Gregory,Van Emelen, Kristof,Nyanguile, Origène,Simmen, Kenny,Raboisson, Pierre
scheme or table, p. 4437 - 4443 (2012/07/17)
Optimization of a novel series of macrocyclic indole-based inhibitors of the HCV NS5b polymerase targeting the finger loop domain led to the discovery of lead compounds exhibiting improved potency in cellular assays and superior pharmacokinetic profile. F
MACROCYCLIC INDOLE DERIVATIVES USEFUL AS HEPATITIS C VIRUS INHIBITORS
-
Page/Page column 63, (2010/04/03)
Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
Compounds for the Treatment of Hepatitis C
-
, (2009/05/28)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Compounds for the Treatment of Hepatitis C
-
Page/Page column 35-36, (2009/05/28)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Compounds for the Treatment of Hepatitis C
-
, (2008/12/07)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Compounds for the Treatment of Hepatitis C
-
, (2008/12/07)
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Compounds for the Treatment of Hepatitis C
-
, (2008/12/07)
The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Compounds for the Treatment of Hepatitis C
-
Page/Page column 39, (2008/12/07)
The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
