54287-92-2Relevant articles and documents
A scalable and facile process for the preparation of N-(pyridin-4-yl) piperazine-1-carboxamide hydrochloride
Wei, Daiyan,Chen, Ligong,Yan, Xilong,Li, Yang,Li, Jianye,Wang, Donghua
, p. 152 - 155 (2016)
A scalable and facile synthetic process for N-(pyridin-4-yl)piperazine-1-carboxamide hydrochloride, a novel Rho kinase inhibitor with an unsymmetrical urea structure currently under investigation for the treatment of central nervous system disorders, was established. After optimisation of the reaction conditions, N-(pyridin-4-yl)piperazine-1-carboxamide hydrochloride was synthesised from 4-aminopyridine and N,N'-carbonyldiimidazole through acylation, deprotection and salt formation. This new procedure affords the product in 53% overall yield with high purity and it can be easily scaled up for production.
Design, Synthesis, and Biological Evaluations of Several Y-26732 Analogues
Wang, Xinran,Chen, Ligong,Li, Hang,Sun, Changhai,Qi, Haofei,Wang, Donghua
, p. 1212 - 1218 (2015/08/06)
A series of pyridine Rho kinase inhibitors were designed and synthesized utilizing the ligand-binding pocket model with Y-26732 as the lead compound. These compounds were evaluated on cell lines for their biological activities.
DOSAGE OF 4-AMINOPYRIDINE DERIVATIVES FOR TREATMENT OF CENTRAL NERVOUS SYSTEM INJURIES
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Page/Page column 12, (2008/06/13)
The invention provides novel pyridines, pharmaceutical compositions comprising such pyridines, and the use of such compositions in treating injured mammalian nerve tissue, including but not limited to an injured spinal cord, in one embodiment, the compounds, compositions, and methods of the instant invention treat a mammalian nerve tissue injury by restoring action potential or nerve impulse conduction through a nerve tissue lesion. Significantly,in vivo application of compounds of the instant invention established, on the basis of SSEP testing, that the compounds provide longer lasting effects at lower concentrations than comparable treatment with the known agent 4-aminopyridine (4 AP).Λ''invention concerne de nouvelles pyridines, des compositions pharmaceutiques comprenant ces pyridines et l''utilisation de ces compositions dans le traitement des lésions du tissu nerveux mammifère, y compris mais non de fa?on limitative, une lésion de la moelle épinière. Dans un mode de réalisation, les composés, les compositions et les méthodes selon l''invention traitent une lésion du tissu nerveux mammifère en rétablissant le potentiel d''action ou la conduction nerveuse à travers une lésion du tissu nerveux. De manière significative, l''application in vivo de composés selon l''invention établit, sur la base d''un test de potentiel évoqué somesthésique, que les composés produisent à de faibles concentrations des effets plus durables qu''un traitement comparable à l''aide de l''agent 4-aminopyridine (4 AP) connu.