52240-10-5

Upstream product

• 36725-37-8 6-(4-bromophenyl)-4,5-dihydropyridazin-3(2H)-one 
• 36725-21-0 4-(6-oxo-1,4,5,6-tetrahydropyridazin-3-yl)benzonitrile 
• 1443-80-7 4-cyanophenyl methyl ketone 
• 298-12-4 Glyoxilic acid 
• 50636-57-2 6-(4-bromophenyl)-3(2H)-pyridazin-3-one 

Downstream Products

• 832735-48-5 2-(1-t-butoxycarbonylpiperidin-4-yloxy)-5-(4-cyanophenyl)pyridazine 
• 1087379-64-3 ethyl {3-[6-oxo-3-(4-cyanophenyl)-6H-pyridazin-1-ylmethyl]phenyl}carbamate 
• 1087379-79-0 N-hydroxy-4-(6-oxo-1,6-dihydropyridazin-3-yl)benzamidine 
• 67820-75-1 N'-[6-(4-cyano-phenyl)-pyridazin-3-yl]-hydrazinecarboxylic acid ethyl ester 
• 67821-02-7 4-[4-methyl-6-(N-methyl-hydrazino)-pyridazin-3-yl]-benzonitrile 
• 67820-85-3 N'-[6-(4-cyano-phenyl)-5-methyl-pyridazin-3-yl]-hydrazinecarboxylic acid tert-butyl ester 
• 66548-54-7 3-chloro-6-(4-cyano-phenyl)-pyridazine 

Relevant academic research and scientific papers

Synthesis and Bioevaluation of 3,6-Diaryl-[1,2,4]triazolo[4,3-b] Pyridazines as Antitubulin Agents

A series of 3,6-diaryl-[1,2,4]triazolo[4,3-b]pyridazines were designed as a class of vinylogous CA-4 analogues. The easily isomerized (Z,E)-butadiene linker of vinylogous CA-4 was replaced by a rigid [1,2,4]triazolo[4,3-b]pyridazine scaffold. Twenty-one target compounds were synthesized and exhibited moderate to potent antiproliferative activity. The compound 4q with a 3-amino-4-methoxyphenyl moiety as the B-ring, comparable to CA-4 (IC50 = 0.009-0.012 μM), displayed the highly active antiproliferative activity against SGC-7901, A549, and HT-1080 cell lines with IC50 values of 0.014, 0.008, and 0.012 μM, respectively. Tubulin polymerization experiments indicated that 4q effectively inhibited tubulin polymerization, and immunostaining assay revealed that 4q significantly disrupted tubulin microtubule dynamics. Moreover, cell cycle studies revealed that compound 4q dramatically arrested cell cycle progression at G2/M phase in A549 cells. Molecular modeling studies showed that 4q could bind to the colchicine binding site on microtubules.

Copper-catalyzed aerobic dehydrogenation of C-C to C=C bonds in the synthesis of pyridazinones

A simple and efficient procedure for the synthesis of pyridazin-3(2H)-ones through copper-catalyzed dehydrogenation of a single C-C bond of 4,5-dihydropyridazin-3(2H)-ones to a C=C bond with oxygen as the terminal oxidant is described. Functional groups including hydroxy, carboxylic, bromo, chloro, cyano, nitro and alkoxy were all tolerated under the reaction conditions. Moreover, this methodology was applied to the preparation of a series of structurally similar N-substituted 6-phenylpyridazinone compounds containing fluorine. The dehydrogenation reactions exhibit good yields and selectivity. Copper-catalyzed dehydrogenation of a C-C bond of 4,5-dihydropyridazinones to a C=C bond with oxygen as the terminal oxidant is described. Various functional groups were tolerated under the reaction conditions. The method was also applied to the preparation of a series of N-substituted 6-phenylpyridazinones containing fluoride. The dehydrogenation reactions exhibit good yields and selectivity.

PYRIDAZINONE DERIVATIVES

Compounds of the formula (I), in which R1, R2, R3, W and D have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.

PYRIDAZINONE DERIVATIVES

Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.

Heterobiarly derivatives and pharmaceutical compositions thereof

Heterobiaryl derivatives of the formula wherein R1, X1 to X3 and Y1 to Y4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologica

2-pyrrolidinones, pharmaceutical compositions containing these compounds and processes for preparing them

The invention relates to cyclic imino derivatives of general formula wherein A, B, E, X2 to X5 and Y are defined as in claim 1, the stereoisomers, tautomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions which contain these compounds and processes for preparing them.

Hypotensive alkyl-3-[6-(aryl)-3-pyridazinyl]-carbazates

This disclosure describes novel alkyl 3-[6-(aryl)-3-pyridazinyl]-carbazates useful as hypotensive agents in mammals. SP CROSS REFERENCE TO RELATED APPLICATIONS This application is a continuation of our copending application Ser. No. 692,254, filed June 3, 1976 now abandoned, which in turn is a continuation-in-part of our abandoned application Ser. No. 552,024, filed Feb. 24, 1975 now abandoned.