- Synthesis, structure-activity relationships and stereochemical investigations of new tricyclic pyridazinone derivatives as potential STAT3 inhibitors
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Through a cell-based biological screening, the benzocinnolinone derivative (±)-2c was identified as a promising STAT3 inhibitor. Since SAR studies on a series of compounds structurally related to (±)-2c (1c, 2a-p, 3c, 4c, 6) showed that the latter had the
- Masciocchi, Daniela,Gelain, Arianna,Porta, Federica,Meneghetti, Fiorella,Pedretti, Alessandro,Celentano, Giuseppe,Barlocco, Daniela,Legnani, Laura,Toma, Lucio,Kwon, Byoung-Mog,Asai, Akira,Villa, Stefania
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p. 1181 - 1188
(2013/08/23)
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- SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
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Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
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Page/Page column 145
(2008/12/07)
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- PYRIDAZINE COMPOUNDS AND METHODS
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The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of
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Page/Page column 8; 55; 1/7
(2008/06/13)
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- Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound
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Excessive glial activation, with overproduction of cytokines and oxidative stress products, is detrimental and a hallmark of neurodegenerative disease pathology. Suppression of glial activation is a potential therapeutic approach, and protein kinases are targets of some antiinflammatory drugs. To address an unmet need for selective inhibitors of glial activation, we developed a novel 3-amino-6-phenylpyridazine derivative that selectively blocks increased IL-1β, iNOS, and NO production by activated glia, without inhibition of potentially beneficial glial functions.
- Mirzoeva, Salida,Sawkar, Anu,Zasadzki, Magdalena,Guo, Ling,Velentza, Anastasia V.,Dunlap, Vincent,Bourguignonl, Jean-Jacques,Ramstrom, Helena,Haiech, Jacques,Van Eldik, Linda J.,Watterson
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p. 563 - 566
(2007/10/03)
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- Simple synthesis of ring-fused pyridazin-3-ones
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Bicyclic and tricyclic pyridazin-3-ones, 6,7-dihydro-5H-cyclopenta[e]-2H-pyridazin-3-one (5), 5,6,7,8-tetrahydrobenzo[e]-2H-pyridazin-3-one (6), 9,10-dihydronaphtho[1,2-e]-2H-pyridazin-3-one (15) and 9,10-dihydronaphtho[1,2-e]-2-methylpyridazin-3-one (21) were prepared in a one-pot procedure by reacting, hydrazine hydrate with a corresponding ketocarboxylic acid.
- Suzuki, Koichi,Senoh, Akihiro,Ueno, Kazunori
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p. 723 - 731
(2007/10/03)
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- Efficient aromatization of 4,5-dihydro-3(2H)-pyridazinones substituted at 5 position by using anhydrous copper (II) chloride
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An efficient conversion of 5-substituted-4,5-dihydro-3(2H)-pyridazinones into their corresponding dehydrogenated derivatives was achieved by treatment with anhydrous copper(II) chloride in acetonitrile.
- Sotelo, Eddy,Ravina, Enrique
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- Behavior of 5,6-dihydrobenzo[h]cinnolinones towards hydrazine. Synthesis of benzo[h]cinnolinones and of 4-aminobenzo[h]cinnolinones
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Dehydrogenation and amination of 4,4a,5,6-tetrahydro and 5,6- dihydrobenzocinnolinones in refluxing hydrazine hydrate to give new benzo[h]cinnolinones and 4-aminobenzo[h]cinnolinones are reported, and reaction mechanisms proposed. Experiments were also extended to 4,4a-dihydro- 5H-indenopyridazinone which underwent hydrazine induced dehydrogenation to 5H-indenopyridazin-3-one but not subsequent amination.
- Villa, Stefania,Evoli, Giacomo Luca,Cignarella, Giorgio,Curzu, Michela M.,Pinna, Gerard A.
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p. 485 - 492
(2007/10/03)
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- Synthesis, hypotensive and diuretic activities of several 3-hydrazino-5,6-dihydrobenzo[h]cinnolines. Part 10: Pyridazine derivatives
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New 3-hydrazino-5,6-dihydrobenzo[h]cinnolines were prepared, and their effects on arterial pressure, diuresis and Na+ and K+ excretion in conscious normotensive rats were studied.
- Ravina,Fueyo,Teran,Cid,Garcia Mera,Orallo,Bardan
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p. 574 - 577
(2007/10/02)
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- Tricyclic pyridazinone compounds
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This invention relates to tricyclic pyridazinone compounds, pharmaceutical compositions containing the compounds, and a method of stimulating cardiac activity in a mammal by administering an effective amount of the compound. A compound of the invention is
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