- A kind of levosimendan impurity and its preparation and detection method
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The invention discloses a levosimendan impurity, and the impurity is produced in diazotization and condensation reaction in the presence of alcohol (such as ethanol), water and other nucleophiles in the synthesis process of levosimendan. The invention also provides a preparation method of the impurity, the preparation method comprises the steps of preparation of formula III compound by diazotization from 6-(4-amino phenyl)-4, 5-dihydro-5-methyl-3 (2H) - pyridazinone, and preparation of the impurity by reaction of the formula III compound and TOH. The invention also provides a detection method of the impurity and application of the impurity in the study of the quality of levosimendan pharmaceutical raw materials and preparations.
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Paragraph 0045; 0046
(2017/04/27)
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- PYRIDAZINONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1 represents H or C1-6 alkyl, each of R2 and R3 represents H, X, C1-6 alkoxy, Z represents O or S, and A represents AA or BB, wherein AA represents: and BB represents: wherein R4 represents H or C1-6 alkyl, and each of R5 and R6 represents C1-6 alkyl.
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Page/Page column 152
(2010/04/25)
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- PYRAZOLONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT
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It is to provide a novel pyrazolone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1,R2: C1-6 alkyl; R3,R4: H, X, C1-6 alkoxy; Z:O, S; A:AA, BB, wherein AA represents wherein BB represents wherein R5: H, C1-6 alkyl ; R6,R7: C1-6 alkyl.
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Page/Page column 101-102
(2010/04/25)
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- Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: A novel series of potent dual PDE3/PDE4 inhibitory agents
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In this study, the synthesis and in vitro and in vivo pharmacological investigations of a new series of phthalazinone/pyridazinone hybrids with both PDE3 and PDE4 inhibitory activities are described. These compounds combine the pharmacophores of recently discovered 4a,5,8,-8a-tetrahydro-2H-phthalazin-1-one-type inhibitors of PDE4 and the well-known 2H-pyridazin-3-one-type PDE3 inhibitors such as the tetrahydrobenzimidazoles. Most of the synthesized compounds are pharmacologically spoken PDE3/PDE4 hybrids. All hybrids show potent PDE4 inhibitory activity (pIC50 = 7.0-8.7), whereas the pIC50 values for inhibition of PDE3 vary from 5.4 to 7.5. In general, analogues with a 5-methyl-4,5-dihydropyridazinone moiety exhibit the highest PDE3 inhibitory activities. The highest in vivo antiinflammatory activity is displayed by phthalazinones 43 and 44 showing, at a dose of 30μmol/kg po, 46% inhibition of arachidonic acid (AA) induced mouse ear edema. No correlation was found between the in vitro PDE3 and/or PDE4 inhibitory activity and the in vivo antiinflammatory capacity after oral dosing.
- Van der Mey, Margaretha,Bommelé, Kirsten M.,Boss, Hildegard,Hatzelmann, Armin,Van Slingerland, Mike,Sterk, Geert J.,Timmerman, Hendrik
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p. 2008 - 2016
(2007/10/03)
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- Pyridazinones having cardiotonic and beta blocking activities
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Pyridazinones of the following formula (I): STR1 where R1 -R4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
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