877269-51-7Relevant academic research and scientific papers
Discovery and preclinical characterization of the cyclopropylindolobenzazepine BMS-791325, a potent allosteric inhibitor of the hepatitis C virus NS5B polymerase
Gentles, Robert G.,Ding, Min,Bender, John A.,Bergstrom, Carl P.,Grant-Young, Katharine,Hewawasam, Piyasena,Hudyma, Thomas,Martin, Scott,Nickel, Andrew,Regueiro-Ren, Alicia,Tu, Yong,Yang, Zhong,Yeung, Kap-Sun,Zheng, Xiaofan,Chao, Sam,Sun, Jung-Hui,Beno, Brett R.,Camac, Daniel M.,Chang, Chong-Hwan,Gao, Mian,Morin, Paul E.,Sheriff, Steven,Tredup, Jeff,Wan, John,Witmer, Mark R.,Xie, Dianlin,Hanumegowda, Umesh,Knipe, Jay,Mosure, Kathy,Santone, Kenneth S.,Parker, Dawn D.,Zhuo, Xiaoliang,Lemm, Julie,Liu, Mengping,Pelosi, Lenore,Rigat, Karen,Voss, Stacey,Wang, Yi,Wang, Ying-Kai,Colonno, Richard J.,Gao, Min,Roberts, Susan B.,Gao, Qi,Ng, Alicia,Meanwell, Nicholas A,Kadow, John F.
, p. 1855 - 1879 (2014/04/03)
Described herein are structure-activity relationship studies that resulted in the optimization of the activity of members of a class of cyclopropyl-fused indolobenzazepine HCV NS5B polymerase inhibitors. Subsequent iterations of analogue design and synthe
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.
Compounds for the Treatment of Hepatitis C
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Page/Page column 34, (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
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Page/Page column 25, (2008/12/06)
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
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Page/Page column 37, (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.
Indolobenzazepine HCV NS5B inhibitors
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Page/Page column 176, (2008/06/13)
The invention encompasses compounds and salts of Formulas I, II, III, and IV 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.
Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
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Page/Page column 72, (2008/06/13)
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.
INHIBITORS OF HCV REPLICATION
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Page/Page column 143, (2010/11/28)
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of
Inhibitors of HCV replication
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Page/Page column 140-141, (2010/10/20)
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.
