- Synthesis method of 3-nitro-6- chloroimidazo[1,2-b] pyridazine
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The invention relates to a synthesis method of 3-nitro-6-chloroimidazo[1,2-b] pyridazine. 3-amino-6-chloropyridazine, chloroacetaldehyde water solution and nitric acid are used as raw materials; the mol ratio of the 3-amino-6-chloropyridazine to the 40-percent chloroacetaldehyde water solution is 1:(1.0 to 2.3); the mol ratio of the 3-amino-6-chloropyridazine to the nitric acid is 1:(1.2 to 6.0); in a proper solvent, under the effect of alkali, the reaction is continuously performed at 0 to 90 DEG C for 6 to 12 hours to generate a coarse product of the 3-nitro-6-chloroimidazo[1,2-b] pyridazine; after the purification, a pure product of the 3-nitro-6-chloroimidazo[1,2-b] pyridazine is obtained. The method provided by the invention has the advantages that the raw materials can be easily obtained; the price is reasonable; meanwhile, in the preparation reaction, heavy metal and corrosion gas are not used; the reaction is mild; no special requirements exist on the reaction equipment; the production can be performed by ordinary anti-corrosion equipment; in addition, the reaction conditions of the method are proper.
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Paragraph 0013; 0015; 0017; 0018; 0019; 0020
(2017/08/29)
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- COMPOUNDS AND COMPOSITIONS AS TRK INHIBITORS
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The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.
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Page/Page column 39
(2012/03/27)
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- SUBSTITUTED IMIDAZO[1,2B]PYRIDAZINE COMPOUNDS AS TRK KINASE INHIBITORS
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Compounds of Formula (I): in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.
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Page/Page column 35
(2010/04/25)
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- IMIDAZOPYRIDAZINES FOR USE AS PROTEIN KINASE INHIBITORS
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There is provided compounds of formula (I): wherein Z, M, R1, X, R3, R4 and R5 have meanings given in the description, an pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protei kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, an particularly in the treatment of cancer.
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Page/Page column 113
(2009/06/27)
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- Synthetic studies on condensed-azole derivatives. IV. Synthesis and anti-asthmatic activities of ω-sulfamoylalkyloxyimidazo[1,2-b]pyridazines
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A series of novel (imidazo[1,2-b]pyridazin-6-yl)oxyalkylsulfonamides was synthesized and evaluated for the ability to inhibit platelet activating factor (PAF)-induced bronchoconstriction in guinea pigs. The compounds bearing a gem-dialkyl or a cycloalkylidene group at the 2 position of the sulfamoylpropyloxy group in the side chain were found to have potent activity. Among them, 3-(imidazo[1,2-b]pyridazin-6-yl)oxy-2,2-dimethylpropanesulfonamide (6) showed excellent anti-asthmatic activity and the longest duration of action. The compounds bearing a methyl group at the 7 or 8 position of the imidazo[1,2-b]pyridazine ring were found to have enhanced activity. Among them, 3-(7-methylimidazo[1,2-b]pyridazin-6-yl)oxy-2,2-dimethylpropanesulfonamide (25) showed the most potent inhibitory effect, and its anti-asthmatic effect in an experimental model of allergic asthma was superior to that of theophylline. The structure-activity relationships in this series of compounds are discussed.
- Kuwahara, Masaaki,Kawano, Yasuhiko,Shimazu, Hiroshi,Ashida, Yasuko,Miyake, Akio
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p. 122 - 131
(2007/10/03)
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