Linomide
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Elimination half-life | 26-42 hours |
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ECHA InfoCard | 100.163.758 |
Chemical and physical data | |
Formula | C18H16N2O3 |
Molar mass | 308.337 g·mol−1 |
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Roquinimex (Linomide) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity. It also inhibits angiogenesis and reduces the secretion of TNF alpha.
Roquinimex has been investigated as a treatment for some cancers (including as adjuvant therapy after bone marrow transplantation in acute leukemia) and autoimmune diseases, such as multiple sclerosis and recent-onset type I diabetes. Several trials have been terminated due to serious cardiovascular toxicity.
Synthesis
![](http://upload.wikimedia.org/wikipedia/commons/thumb/8/84/Roquinimex_synthesis.svg/700px-Roquinimex_synthesis.svg.png)
Ethyl 2-(methylamino)benzoate is condensed with ethyl malonate. Amine-ester interchange of that compound with N-methylaniline results in formation of the amide roquinimex.
References
- ^ E. Eriksoo et al., EP 59698; eidem, U.S. patent 4,738,971 (1982, 1988 both to AB Leo).