36725-28-7Relevant articles and documents
ANTIBODY DRUG CONJUGATES (ADCS) WITH NAMPT INHIBITORS
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Page/Page column 329-330, (2021/01/29)
Conjugate of a binder having formula (AA) wherein AB stands for a binder, Z' stands for a linker, D stands for an active component which is a NAMPT inhibitor and its use as pharmaceuticals.
Preparation method of important intermediate of levosimendan
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Paragraph 0059; 0075-0077; 0078; 0094-0096, (2020/03/29)
The invention belongs to the field, of synthesis of intermediates and relates to (R)- 6 - (4 -aminophenyl) - 5 - methyl - 444455-dihydropyridazine - 3333337. acetamide N - (4 - obtained by hydrolyzing)-methylpropionyl, phenyl, acetamide, in N - (4 - (3 - (-propionyl phenyl) - 2 - acetamide as starting material) and then chemical resolution.) yields high-purity,methylpropionyl (R)- N - (4 - (3 - (phenyl) - 2 - acetamide.). The present invention is very suitable for industrial production) by chemically resolving the high yield; dimethylamino,methylpropionyl-methaneanoyl-benzenesulfonamido (R)- N - (4 - (3 - phenylacetamido) obtained by hydrolyzing the intermediates with formaldehyde) dimethylamine. yields a high yield, yields a high yield of intermediate. The present invention relates to a, process for, producing high-chiral purified p-methyl propionylphenyl phenylacetonitrile.
DIHYDROPYRIDAZINONES SUBSTITUTED WITH PHENYLUREAS
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Page/Page column 204, (2018/05/27)
Compounds of formula (I) which are nicotinamide phosphoribosyltransferase (NAMPT) inhibitors and their use for the treatment of hyperproloferative diseases and/or disorders responsive to induction of cell death.
Synthesis and anti-congestive heart failure activity of novel levosimendan analogues
Wang, Lisheng,Zhou, Hongxiang,Yang, Bin,Chen, Zhigang,Yang, Hua
, p. 287 - 292 (2012/06/05)
A series of levosimendan analogues were designed and synthesized, employing the Friedel-Crafts reaction, hydrolysis, and cyclization from the key intermediate compound R(-)-6-(4-aminophenyl)-5-methyl-4, 5-dihydro-3(2H)- pyridazinone, which was obtained from the starting material, acetanilide. These compounds, except 1b, exhibited potent anti-congestive heart failure activities, especially the compounds 1e and 1k, which showed more effective action than levosimendan. Springer Science+Business Media, LLC 2010.
PROCESS FOR PREPARING LEVOSIMENDAN AND INTERMEDIATES FOR USE IN THE PROCESS
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Page/Page column 11, (2011/02/24)
In an embodiment, the present invention provides a process for preparing (-)-6-(4- aminophenyl)-5-methylpyridazin-3-(2H)-one, which process comprises: a) reacting racemic 6-(4-aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone of formula (Il) with a chiral tartaric acid derivative to obtain a diastereomeric salt of (-)-6-(4- aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone and the chiral tartaric acid derivative; and b) reacting the diastereomeric salt with a base to obtain (-)-6-(4- aminophenyl)-4,5-dihydro-5-methyl-3-(2H)-pyridazinone. The (-)-6-(4-aminophenyl)-4,5- dihydro-5-methyl-3-(2H)-pyridazinone may be used to prepare levosimendan.
Synthesis and bioactivity of 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives
Wang, Teng,Dong, Ying,Wang, Li-Chen,Chen, Zhen
, p. 641 - 646 (2008/03/11)
A series of 6-phenyl-4,5-dihydro-3(2H)-pyridazinone derivatives was prepared and examined for cardiotonic activity. The structures of these new pyridazinone derivatives were confirmed by IR, 1H-NMR and mass spectrum. The cardiotonic activities of these compounds were studied on isolated perfused toad heart and compared with the activity of levosimendan (CAS 141505-33-1). Compound 5a emerged as the most interesting compound in this series with potential cardiotonic activity. ECV Editio Cantor Verlag.
Method for obtaining pure enantiomers of a pyridazinone derivative
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, (2008/06/13)
The present invention relates to a method for preparing optically active enantiomers of [[4-(1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl]-hydrazono]propanedinitrile (I), particularly (-) enantiomer of (I). Furthermore, the invention relates to a novel crystalline polymorphic form of the (-) enantiomer.
Studies on agents with vasodilator and β-blocking activities. V. Synthesis and pharmacological activity of the optical isomers of TZC-5665
Seki, Toshimi,Kanada, Arihiro,Nakao, Tomio,Shiraiwa, Masahumi,Asano, Hajime,Miyazawa, Katuhiko,Ishimori, Tsutomu,Minami, Nobuyoshi,Shibata, Kenyu,Yasuda, Kikuo
, p. 84 - 96 (2007/10/03)
Synthesis of the four optical isomers of TZC-5665 (1), a candidate for the treatment of congestive heart failure, was achieved by the reaction of chiral diaminopyridazinone (2) with chiral glycidyl ether (3). The hypotensive and β-blocking activities of 1 and its optical isomers were examined when given intravenously into anesthetized rats. Furthermore these compounds were evaluated for inhibitory activity on cAMP phosphodiesterase III. Among the four optical isomers, R(A),S(B)-one (1c) possessed the essential activities of TZC-5665 (1).
6-(substituted phenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-ones of medicinal interest. The synthesis of SK&F 94836 and SK&F 95654
Burpitt,Crawford,Davies,Mistry,Mitchell,Pancholi,Coates
, p. 1689 - 1695 (2007/10/02)
Two synthetic routes to the dihydropyridazinone-cyanoguanidine 4 (SK&F 94836) are described, both proceeding via the anilino compound 6. An efficient synthesis of the dihydropyridazinone-pyridone 5 (SK&F 95654) is reported. This synthesis proceeds via the fluoro-keto-acid 24, with subsequent displacement of the fluoro substituent by 4-pyridone. The surprising effectiveness of water as a solvent in this reaction has been highlighted.
