79472-17-6

Upstream product

• 78157-26-3 6-(pyridin-4-yl)pyridazin-3(2H)-one 
• 141-30-0 3,6-dichlorpyridazine 
• 1692-15-5 4-pyridylboronic acid 

Downstream Products

• 78157-26-3 6-(pyridin-4-yl)pyridazin-3(2H)-one 

Relevant academic research and scientific papers

HERBICIDAL COMPOUNDS

Compounds of the formula (I) wherein the substituents are as defined in claim 1, useful as a pesticides, especially as herbicides.

Towards dual inhibitors of the MET kinase and WNT signaling pathway; Design, synthesis and biological evaluation

Both the kinase MET and the WNT signaling pathway are attractive targets in cancer therapy, and synergistic effects have previously been observed in animal models upon simultaneous inhibition. A strategy towards a designed multiple ligand of MET and WNT signaling is pursued based on the two hetero biaryl systems present in both the MET inhibitor tepotinib and WNT signaling inhibitor TC-E 5001. Initial screening was conducted to find the most suitable ring systems for further optimization, whereas a second screen explored modifications towards pyridazinones and triazolo pyridazines. Up to 54% reduction of WNT signaling activity at 10 μM concentration was achieved, however, only low affinities towards MET were observed. Overall, the thiophene substituted pyridazinone 40 was the best dual MET and WNT signaling inhibitor, with a 17% and 19% reduction of activity, respectively. Although further optimizations are needed to achieve more potent dual inhibitors, the strategy presented herein can be valuable towards the development of a dual inhibitor of MET and WNT signaling.

Novel Triazolo Pyridazine Derivatives and Use Thereof

The present invention relates to a novel triazolo pyridazine derivative or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition for inhibiting c-Met tyrosine kinase activity and a pharmaceutical composition for preventing or treating an abnormal proliferation disorder (hyperproliferative disorder) comprising same as an active ingredient, and to a method for preventing or treating an abnormal proliferation disorder (hyperproliferative disorder) comprising a step of administering a pharmaceutically effective amount of the pharmaceutical composition to a subject in need thereof. The present invention can advantageously be used as a therapeutic agent for various abnormal proliferation disorders such as cancer, psoriasis, rheumatoid arthritis and diabetic retinopathy which are associated with excessive cell proliferation and growth due to irregular kinase activity by effectively suppressing the activity of c-Met tyrosine kinase.

Discovery of substituted pyrazol-4-yl pyridazinone derivatives as novel c-Met kinase inhibitors

A series of pyridazin-3-one substituted with morpholino-pyrimidine derivatives was synthesized and evaluated as tyrosine kinase inhibitors against c-Met enzyme, and anti-proliferative activities of Hs746T human gastric cancer cell line. Most of compounds exhibited good biological activity, while compound 10, 12a, 14a displayed excellent c-Met enzyme inhibitory activities and Hs746T cell-based activities.

Novel pyridazinone derivatives as inhibitors of CDK2

The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R1 and R2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2)

PYRIDAZINONE DERIVATIVES, METHODS FOR PRODUCING THEM AND THEIR USE AS PHARMACEUTICALS

The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R1 and R2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. Formula (I) These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK-15 30 (glycogen synthase kinase-3?).

3-Hydrazino-6-(pyridinyl) pyridazines and cardiotonic use thereof

3-Hydrazino-6-PY-pyridazine or pharmaceutically-acceptable acid-addition salt thereof is useful as a cardiotonic agent, where PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substitutents. 6-PY-3-pyridazinol is prepared by reacting 6-PY-3-pyridazinol with a chlorinating agent to produce 3-chloro-6-PY-pyridazine and reacting said 3-chloro compound with hydrazine to produce said 3-hydrazino compound. 3-Hydrazino-6-PY-pyridazine or pharmaceutically-acceptable acid-addition salt thereof is disclosed as the active component in cardiotonic compositions for increasing cardiac contractility and in the method for increasing cardiac contractility in a patient requiring such treatment. The novel intermediate 3-chloro-6-PY-pyridazine is prepared as noted above.