- TLR7/8 ANTAGONISTS AND USES THEREOF
-
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.
- -
-
Paragraph 00229; 00249
(2020/02/23)
-
- Synthesis of 2- and 3-trifluoromethylmorpholines: Useful building blocks for drug discovery
-
2- and 3-Trifluoromethylmorpholines were prepared in racemic and optically active forms. The synthesis commenced from the commercially available 2-trifluoromethyloxirane. The elaborated procedures were scalable, and the products were obtained in multigram quantities. The obtained compounds were comprehensively characterized by crystallographic analysis, fluorescence measurements, solubility, pKa, logD parameters, and clearance rate. The potential of the synthesized amines as the building blocks for drug discovery is thus demonstrated.
- Shcherbatiuk, Andriy V.,Shyshlyk, Oleg S.,Yarmoliuk, Dmytro V.,Shishkin, Oleg V.,Shishkina, Svitlana V.,Starova, Viktoriia S.,Zaporozhets, Olga A.,Zozulya, Sergey,Moriev, Roman,Kravchuk, Olga,Manoilenko, Olga,Tolmachev, Andrey A.,Mykhailiuk, Pavel K.
-
p. 3796 - 3804
(2013/07/05)
-
- TRICYCLIC TETRAHYDROQUINOLINE ANTIBACTERIAL AGENTS
-
The invention includes tetrahydroquinoline and related compounds of formula (I), and pharmaceutical compositions thereof, that exhibit useful antibacterial activity against a wide range of human and veterinary pathogens.
- -
-
-
- The synthesis of fluorine-containing pterins
-
The synthesis of some 7,7-difluoro-7,8-dihydropterins and pterins with fluoroalkyl substituents at the 6 or 7 positions from fluorine-containing aliphatic precursors and suitably substituted pyrimidines is described. The fluorine-containing pterins were found to be very insoluble and also stable to nucleophiles and bases in dilute aqueous solution.
- Dunn, Caroline,Gibson, Colin L.,Suckling, Colin J.
-
p. 13017 - 13026
(2007/10/03)
-