157141-56-5Relevant academic research and scientific papers
AMINO-SUBSTITUTED HETEROCYCLIC DERIVATIVES AS SODIUM CHANNEL INHIBITORS
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Page/Page column 59; 60, (2016/11/17)
The present invention relates to novel aminoindazolyl derivative compounds of Formula(I), the use of said compounds in treating diseases mediated by modulation of voltage-gated sodium channels in particular Nav1.7 AND to compositions containing said derivatives.
Synthesis of N-substituted γ-methylene γ-lactams
Adhikari, Raju,Jones, Dionne A.,Liepa, Andris J.,Nearn, Roland H.
, p. 882 - 890 (2007/10/03)
N-Substituted cyanoacetamides 1 were condensed with 1,2-diketones 2 under base catalysis to form ?-hydroxy ?-lactams 3. Treatment of 3 with acids gave novel fungicidal ?-methylene ?-lactams 4. The exocyclic double bond of 4b reacted reversibly with 4-toluene sulfinate. CSIRO 2005.
Synthesis, structure-activity relationships, and pharmacokinetic properties of dihydroorotate dehydrogenase inhibitors: 2-cyano-3-cyclopropyl- 3-hydroxy. N-[3'-methyl-4'-(trifluoromethyl)phenyl]propenamide and related compounds
Kuo, Elizabeth A.,Hambleton, Philip T.,Kay, David P.,Evans, Phillip L.,Matharu, Saroop S.,Little, Edward,McDowall, Neil,Jones, C. Beth,Hedgecock, Charles J. R.,Yea, Christopher M.,Chan, A. W. Edith,Hairsine, Peter W.,Ager, Ian R.,Tully, W. Roger,Williamson, Richard A.,Westwood, Robert
, p. 4608 - 4621 (2007/10/03)
The active metabolite (2) of the novel immunosuppressive agent leflunomide (1) has been shown to inhibit the enzyme dihydroorotate dehydrogenase (DHODH). This enzyme catalyzes the fourth step in de novo pyrimidine biosynthesis. A series of analogues of the active metabolite 2 have been synthesized. Their in vivo biological activity determined in rat and mouse delayed type hypersensitivity has been found to correlate well with their in vitro DHODH potency. The most promising compound (3) has shown activity in rat and mouse collagen (II)-induced arthritis models (ED50 = 2 and 31 mg/kg, respectively) and has shown a shorter half-life in man when compared with leflunomide. Clinical studies in rheumatoid arthritis are in progress.
2-cyano-3-hydroxy-(n-pyridyl)-propenamide compounds
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, (2008/06/13)
A compound selected from the group consisting of a compound of the formula STR1 wherein A, B and E are individually selected from the group consisting of =CH-- and =N-- with at least one being =N--, R is selected from the group consisting of cycloalkyl of 3 to 6 carbon atoms, and alkenyl and alkynyl of 2 to 6 carbon atoms, R1 is hydrogen or alkyl of 1 to 3 carbon atoms, R2 and R3 together are --O--CH2 --O-- or are individually selected from the group consisting of hydrogen, halogen, --NO2, --CN, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR4, --(CH2)m --CX3, --O--(CH2)m --CX3, --S--(CH2)m --CX3, --O--(CX2)m --CX3 and --S--(CX2)m --CX3, R4 is hydrogen or alkyl or cycloalkyl of up to 6 carbon atoms, X is halogen and m is 0, 1, 2 or 3 and their addition salts with a non-toxic, pharmaceutically acceptable base having anti-flammatory and immulodulatory activity and their preparation.
