1340875-16-2Relevant academic research and scientific papers
METHYLENE LINKED QUINOLINYL MODULATORS OF ROR-GAMMA-T
-
Page/Page column 104; 167, (2015/05/05)
The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt
-
Paragraph 0481; 0482; 0485; 0486, (2014/05/07)
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi
Keenan, Martine,Alexander, Paul W.,Diao, Hugo,Best, Wayne M.,Khong, Andrea,Kerfoot, Maria,Thompson, R. C. Andrew,White, Karen L.,Shackleford, David M.,Ryan, Eileen,Gregg, Alison D.,Charman, Susan A.,Von Geldern, Thomas W.,Scandale, Ivan,Chatelain, Eric
supporting information, p. 1756 - 1763 (2013/05/09)
A scaffold hopping exercise undertaken to expand the structural diversity of the fenarimol series of anti-Trypanosoma cruzi (T. cruzi) compounds led to preparation of simple 1-[phenyl(pyridin-3-yl)methyl]piperazinyl analogues of fenarimol which were investigated for their ability to inhibit T. cruzi in vitro in a whole organism assay. A range of compounds bearing amide, sulfonamide, carbamate/carbonate and aryl moieties exhibited low nM activities and two analogues were further studied for in vivo efficacy in a mouse model of T. cruzi infection. One compound, the citrate salt of 37, was efficacious in a mouse model of acute T. cruzi infection after once daily oral dosing at 20, 50 and 100 mg/kg for 5 days.
