68549-22-4Relevant academic research and scientific papers
MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN
-
Paragraph 0732; 0822, (2017/11/16)
The present invention provides for compounds of formula (I) wherein R1, m, Z, G1, R2, and R3 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sj?gren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).
A direct and efficient synthetic method for nitriles from ketones
Kloubert, Stephane,Mathe-Allainmat, Monique,Andrieux, Jean,Langlois, Michel
, p. 2873 - 2887 (2007/10/03)
Cyclic cyano derivatives 3 were obtained by the reaction of Me3SiCN / ZnI2 with the cyclic ketones 2 which gave the trimethylsilyloxy nitriles 4. They were directly transformed to cyano derivatives 3 (70-80% yield) by the reductive reagent Me3SiCl-NaI in acetonitrile in the presence of H2O.
Synthesis of benzocycloalkane derivatives as new conformationally restricted ligands for melatonin receptors
Kloubert,Mathe-Allainmat,Andrieux,Sicsic,Langlois
, p. 3325 - 3330 (2007/10/03)
Benzocycloalkane derivatives 1-4 were synthesized as new conformationally restricted melatoninergic ligands. They were prepared by the reaction of the ketones 5 with diethylcyanophosphonate and the reduction of the corresponding cyano compounds or by the Wittig reaction and Curtius degradation to obtain the amines 8. The 1-Cyanobenzocyclobutane derivative was obtained by the benzyne cyclisation reaction. The amines 8 were acylated with acetyl, propionyl or butyryl groups. The affinity of the compounds for chicken brain melatonin receptors was evaluated using 2-[125I]- iodomelatonin as the radioligand. The indanyl (2b, c), tetralin (3a-c) and benzocyeloheptane (4c) derivatives were potent compounds with nanomolar affinity and an important enantioselectivity of the receptor was observed with the (+) enantiomers 2b and 3b.
