494799-18-7Relevant articles and documents
HEPATITIS B CORE PROTEIN MODULATORS
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, (2018/04/13)
The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound of formula:
The First Kilogram Synthesis of Beclabuvir, an HCV NS5B Polymerase Inhibitor
Bien, Jeffrey,Davulcu, Akin,Delmonte, Albert J.,Fraunhoffer, Kenneth J.,Gao, Zhinong,Hang, Chao,Hsiao, Yi,Hu, Wenhao,Katipally, Kishta,Littke, Adam,Pedro, Aghogho,Qiu, Yuping,Sandoval, Maria,Schild, Richard,Soltani, Michelle,Tedesco, Anthony,Vanyo, Dale,Vemishetti, Purushotham,Waltermire, Robert E.
, p. 1393 - 1408 (2018/09/06)
The process development and kilogram-scale synthesis of beclabuvir (BMS-791325, 1) is described. The convergent synthesis features the use of asymmetric catalysis to generate a chiral cyclopropane fragment and coupling with an indole fragment via an alkyl
Bronsted acid ionic liquid-catalyzed reductive Friedel-Crafts alkylation of indoles and cyclic ketones without using an external reductant
Taheri, Amir,Lai, Bingbing,Cheng, Cheng,Gu, Yanlong
supporting information, p. 812 - 816 (2015/03/04)
In the absence of an external reductant, C3-cycloalkylated indole could be synthesized through reductive alkylation of indole with cyclic ketone using a sulfonyl-functionalized Bronsted acid ionic liquid as a catalyst. Water generated in the initial stage of the reaction played a key role in rendering the reductive coupling possible. The reaction proceeds most likely in a radical way.
An efficient process for the large-scale synthesis of a 2,3,6-trisubstituted indole
Alorati, Anthony D.,Gibb, Andrew D.,Mullens, Peter R.,Stewart, Gavin W.
, p. 1947 - 1952 (2013/03/14)
The efficient synthesis of a key trisubstituted indole intermediate 1 is described. The synthetic route required the use of an aryl Grignard reagent which was not commercially available, and the large-scale formation of this fragment and the thermal evalu
The synthesis of novel heteroaryl-fused 7,8,9,10-tetrahydro-6H-azepino[1,2- a]indoles, 4-oxo-2,3-dihydro-1H-[1,4]diazepino[1,7-a]indoles and 1,2,4,5-tetrahydro-[1,4]oxazepino[4,5-a]indoles. Effective inhibitors of HCV NS5B polymerase
Ding, Min,He, Feng,Poss, Michael A.,Rigat, Karen L.,Wang, Ying-Kai,Roberts, Susan B.,Qiu, Dike,Fridell, Robert A.,Gao, Min,Gentles, Robert G.
scheme or table, p. 6654 - 6662 (2011/11/06)
Three synthetic approaches have been developed that allow efficient access to novel heteroaryl fused indole ring systems, including: 7,8,9,10-tetrahydro- 6H-azepino[1,2-a]indoles, 4-oxo-2,3-dihydro-1H-[1,4]diazepino[1,7-a]indoles and 1,2,4,5-tetrahydro-[1,4]oxazepino[4,5-a]indoles. Each strategy is fully exemplified and the relative merits and limitations of the approaches are discussed. The hepatitis C virus (HCV) non-structural 5B (NS5B) polymerase inhibitory activities of select examples from each molecular class are briefly presented.
CARBOXYL SUBSTITUTED INDOLES FOR USE AS PPAR ALPHA MODULATORS
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Page/Page column 67-68, (2009/12/28)
There is provided according to the invention novel compounds of formula (I) or pharmaceutically acceptable salts or solvates thereof wherein one of R1 and R2 is H and the other is COOH. The compounds are useful as PPAR modulators.
Compounds for the Treatment of Hepatitis C
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, (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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, (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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, (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 175, (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.