40741-46-6Relevant articles and documents
Process for Preparation of Sulfonyl Carbamate Bile Acid Derivatives
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Paragraph 0266-0268, (2018/10/30)
The present invention relates to processes for preparing compounds of Formula (I) and compounds of Formula (II): or a pharmaceutically acceptable salt or solvate thereof. These compounds and pharmaceutical compositions are useful as FXR or TGRS modulators. Specifically, the present invention relates to bile acid derivatives and methods for their preparation and use. The present invention relates to a process for the preparation of the compounds of Formula (III), Formula (IV), Formula (V), and Formula (VI), The present invention also relates to a process for the preparation of compounds (VII), (VIII) and (IX),
MTH1 INHIBITORS FOR TREATMENT OF INFLAMMATORY AND AUTOIMMUNE CONDITIONS
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Page/Page column 302; 303, (2016/04/04)
A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.
Discovery of novel HCV inhibitors: Synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B
Zhang, Xiaoyan,Zhang, Nanjing,Chen, Guangming,Turpoff, Anthony,Ren, Hongyu,Takasugi, James,Morrill, Christie,Zhu, Jin,Li, Chunshi,Lennox, William,Paget, Steven,Liu, Yalei,Almstead, Neil,George Njoroge,Gu, Zhengxian,Komatsu, Takashi,Clausen, Valerie,Espiritu, Christine,Graci, Jason,Colacino, Joseph,Lahser, Fred,Risher, Nicole,Weetall, Marla,Nomeir, Amin,Karp, Gary M.
, p. 3947 - 3953 (2013/07/27)
A novel series of 6-(indol-2-yl)pyridine-3-sulfonamides was prepared and evaluated for their ability to inhibit HCV RNA replication in the HCV replicon cell culture assay. Preliminary optimization of this series furnished compounds with low nanomolar potency against the HCV genotype 1b replicon. Among these, compound 8c has identified as a potent HCV replicon inhibitor (EC50 = 4 nM) with a selectivity index with respect to cellular GAPDH of more than 2500. Further, compound 8c had a good pharmacokinetic profile in rats with an IV half-life of 6 h and oral bioavailability (F) of 62%. Selection of HCV replicon resistance identified an amino acid substitution in HCV NS4B that confers resistance to these compounds. These compounds hold promise as a new chemotype with anti-HCV activity mediated through an underexploited viral target.