873050-48-7Relevant academic research and scientific papers
PROCESS FOR THE SYNTHESIS OF IVACAFTOR AND RELATED COMPOUNDS
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Paragraph 062-063; 069, (2016/12/01)
The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R1, R2, R3, R4, R5, R6, R7 and Ar1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.
Breaking and Making of Rings: A Method for the Preparation of 4-Quinolone-3-carboxylic Acid Amides and the Expensive Drug Ivacaftor
Vasudevan,Jachak, Gorakhnath R.,Reddy, D. Srinivasa
supporting information, p. 7433 - 7437 (2016/01/25)
A simple and convenient method to access 4-quinolone-3-carboxylic acid amides from indole-3-acetic acid amides through one-pot oxidative cleavage of the indole ring followed by condensation (Witkop-Winterfeldt type oxidation) was explored. The scope of the method was confirmed with more than 20 examples and was successfully applied to the synthesis of the drug Ivacaftor, the most expensive drug on the market.
Synthesis, cytotoxicity and mechanistic evaluation of 4-oxoquinoline-3- carboxamide derivatives: Finding new potential anticancer drugs
Forezi, Luana Da S. M.,Tolentino, Nathalia M. C.,De Souza, Alessandra M. T.,Castro, Helena C.,Montenegro, Raquel C.,Dantas, Rafael F.,Oliveira, Maria E. I. M.,Silva Jr., Floriano P.,Barreto, Leilane H.,Burbano, Rommel M. R.,Abrahim-Vieira, Barbara,De Oliveira, Riethe,Ferreira, Vitor F.,Cunha, Anna C.,Boechat, Fernanda Da C. S.,De Souza, Maria Cecilia B. V.
, p. 6651 - 6670 (2014/06/10)
As part of a continuing search for new potential anticancer candidates, we describe the synthesis, cytotoxicity and mechanistic evaluation of a series of 4-oxoquinoline-3-carboxamide derivatives as novel anticancer agents. The inhibitory activity of compounds 10-18 was determined against three cancer cell lines using the MTT colorimetric assay. The screening revealed that derivatives 16b and 17b exhibited significant cytotoxic activity against the gastric cancer cell line but was not active against a normal cell line, in contrast to doxorubicin, a standard chemotherapeutic drug in clinical use. Interestingly, no hemolytical activity was observed when the toxicity of 16b and 17b was tested against blood cells. The in silico and in vitro mechanistic evaluation indicated the potential of 16b as a lead for the development of novel anticancer agents against gastric cancer cells.
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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Page/Page column 119; 169, (2012/12/14)
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
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Page/Page column 230, (2008/06/13)
The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
