54287-92-2Relevant academic research and scientific papers
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.
Development of novel 4-aminopyridine derivatives as potential treatments for neurological injury and disease
Smith, Daniel T.,Shi, Riyi,Borgens, Richard B.,McBride, Jennifer M.,Jackson, Kevin,Byrn, Stephen R.
, p. 908 - 917 (2005)
The amine position of the K+ channel blocker 4-aminopyridine was functionalized to form amide, carbamate and urea derivatives in an attempt to identify novel compounds which restore conduction in injured spinal cord. Eight derivatives were tested in vitro, using a double sucrose gap chamber, for the ability to restore conduction in isolated, injured guinea pig spinal cord. The methyl, ethyl and t-butyl carbamates of 4-aminopyridine induced an increase in the post injury compound action potential. The methyl and ethyl carbamates were further tested in an in vivo model of spinal cord injury. These results represent the first time that 4-aminopyridine has been derivatized without losing its ability to restore function in injured spinal cord tissue.
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.
One-pot approach to the synthesis of novel 12H-chromeno[2′,3′:4,5]imidazo[1,2-a]pyridines in aqueous media
Proen?a, M. Fernanda,Costa, Marta
experimental part, p. 4542 - 4550 (2010/07/05)
The chromeno-imidazo[1,2-a]pyridine scaffold was generated in an one pot condensation/cyclization reaction involving a salicylaldehyde and 1-(cyanomethyl)pyridinium chloride, in aqueous sodium carbonate solution. These novel compounds were isolated in 47-71% yield. The reaction pathway was followed by 1H NMR spectroscopy allowing a clear understanding of the side reactions involved in the process. Different mono-substituted pyridinium chlorides were synthesized and reacted with mono-substituted salicylaldehydes and a detailed discussion of the scope of the synthetic method is also presented.
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.
CARBONYL-PIPERAZINYL AND PIPERIDINIL COMPOUNDS WHICH INHIBIT FARNESYL PROTEIN TRANSFERASE
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, (2008/06/13)
Novel carbonyl piperazinyl and piperidinyl compounds of formula (1.0) or (1.1) and pharmaceutical compositions are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel carbonyl piperazinyl or piperidinyl compound to a biological system. In particular, the method inhibits the abnormal growth cells in a mammal such as the human being. A compound of formula (1.0) and (1.1) or a pharmaceutically acceptable salt or solvate thereof, wherein Z is a group which is (i), (ii) or (iii), wherein X1 is CH or N; X2 can be the same or different and can be CH, N, or N-O; b is 0, 1, 2, 3, 4; n and nn independently represent 0, 1, 2, 3, 4 or when X2 is CH, n and nn can be 5; R20 and R21, R1, R2 and R3 are as given in the description.
Tricyclic compounds
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, (2008/06/13)
Novel compounds of Formula STR1 are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
Carbonyl piperazinyl and piperidinyl compounds
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, (2008/06/13)
Novel carbonyl piperazinyl and piperidinyl compounds and pharmaceutical compositions are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering the novel carbonyl piperazinyl or piperidinyl compound to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
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, (2008/06/13)
A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: STR1 to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R20)(R21)(R46), and 5.3, 5.3A and 5.3B, wherein R is --N(R25)(R48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.
Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
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, (2008/06/13)
Novel compounds of Formula (7.0a), (7.0b) or (7.0c): STR1 are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula (7.0a), (7.0b) or (7.0c) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.
