- Heteroaryl imidazolone derivatives as jak inhibitors
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New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
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Page/Page column 105-106
(2012/01/06)
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- HETEROARYL IMIDAZOLONE DERIVATIVES AS JAK INHIBITORS
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New heteroaryl imidazolone derivatives having the chemical structure of formula (I) disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
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Page/Page column 172
(2012/01/06)
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- Structure-kinetics relations holding in the amination of six-membered nitrogen-containing heterocyclic compounds
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Relative rates of the amination of 3-X- and 4-X-substituted pyridines (X = H, 3-Me, 4-Me, 3-F3C, 3-CN, 4-CN, 3-Cl, 3-Br, 4-MeO, 4-Me 2N), pyrazine, quinoline, isoquinoline, 2,2′- and 4,4′-bipyridines, and 1,10-phenanthroline with O-
- Borodkin,Vorob'ev,Shubin
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experimental part
p. 897 - 903
(2011/10/04)
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- Concise routes to pyrazolo[1,5-a]pyridin-3-yl pyridazin-3-ones
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Cycloaddition of pyridine N-imine with 6-alkyl-4-oxohex-5-ynoates followed by condensation with hydrazine provides concise access to pharmacologically active 6-(pyrazolo[1,5-a]pyridin-3-yl)pyridazinones. For the first time alkynyl heterocycles are also shown to be effective dipolarophiles for pyridine N-imine, and analogous compounds can be accessed directly in modest yields through the reaction of 6-(alkyn-1-yl)pyridazin-3-one derivatives. The Royal Society of Chemistry 2008.
- Johnston, Karen A.,Allcock, Robert W.,Jiang, Zhong,Collier, Ian D.,Blakli, Haakon,Rosair, Georgina M.,Bailey, Patrick D.,Morgan, Keith M.,Kohno, Yasushi,Adams, David R.
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p. 175 - 186
(2008/09/20)
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- Synthesis of N-benzoylamino-1,2,3,6-tetrahydropyridine derivatives as potential anti-inflammatory agents
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(Chemical Equation Presented) N-Benzoylamino-1,2,3,6-tetrahydropyridines 9a-q were synthesized from 4-substituted pyridines in four steps. Amination of pyridines was carried out to prepare intermediate N-aminopyridinium mesylates using mesytelenesulfonyl hydroxmate (MSH) as aminating agent. N-aminopyridinium mestylates reacted with appropriately substituted acyl chlorides to form N-ylides as stable crystalline solids. Partial reduction of N-ylides with mild reducing agent afforded N-benzoylamino-1,2,3,6-tetrahydropyridines in fair to good yields.
- Mochona, Bereket,Redda, Kinfe K.
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p. 1383 - 1387
(2008/09/18)
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