10564-83-7

Upstream product

• 931-48-6 2-cyclohexylacetylene 
• 108-24-7 acetic anhydride 
• 64632-96-8 5-Cyclohexyl-2.3-dimethyl-4-pentyn-3-ol 
• 141-78-6 ethyl acetate 
• 64632-88-8 5-Cyclohexyl-2,3-dimethyl-2-penten-4-in 

Downstream Products

• 72001-21-9 4-Cyclohexylidene-but-3-en-2-one 
• 10541-27-2 1-Brom-1-cyclohexyl-buten-⁽¹⁾-on-⁽³⁾ 
• 100385-52-2 4-cyclohexyl-4-semicarbazido-butan-2-one semicarbazone 
• 681432-98-4 (2E)-1-(2-cyclohexylpyrazolo[1,5-b]pyridazin-3-yl)-3-(dimethylamino)prop-2-en-1-one 
• 681432-99-5 1-(2-cyclohexylpyrazolo[1,5-b]pyridazin-3-yl)ethanone 
• 123406-16-6 (Z)-4-cyclohexyl-3-buten-2-one 

Relevant academic research and scientific papers

Phosphane-Catalyzed [3+3] Annulation of C,N-Cyclic Azomethine Imines with Ynones: A Practical Method for Tricyclic Dinitrogen-Fused Heterocycles

A phosphane-catalyzed [3+3] annulation of azomethine imines with ynones has been developed. Under mild reaction conditions, the reaction proceeds smoothly to afford tricyclic dinitrogen-fused heterocyclic compounds in moderate to excellent yields with moderate to excellent stereoselectivies. Using a chiral phosphine as the catalyst, the reaction could work to give the cycloadduct in moderate yield with moderate enantioselectivity. (Figure presented.) .

N-phenyl-4-pyrazolo[1,5-6]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy

Glycogen synthase kinase 3 regulates glycogen synthase, the rate-determining enzyme for glycogen synthesis. Liver and muscle glycogen synthesis is defective in type 2 diabetics, resulting in elevated plasma glucose levels. Inhibition of GSK-3 could potentially be an effective method to control plasma glucose levels in type 2 diabetics. Structure-activity studies on a N-phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine series have led to the identification of potent and selective compounds with good cellular efficacy. Molecular modeling studies have given insights into the mode of binding of these inhibitors. Since the initial leads were also potent inhibitors of CDK-2/CDK-4, an extensive SAR was performed at various positions of the pyrazolo[1,5-b] pyridazin core to afford potent GSK-3 inhibitors that were highly selective over CDK-2. In addition, these inhibitors also exhibited very good cell efficacy and functional response. A representative example was shown to have good oral exposure levels, extending their utility in an in vivo setting. These inhibitors provide a viable lead series in the discovery of new therapies for the treatment of type 2 diabetes.

PYRADAZINE COMPOUNDS AS GSK-3 INHIBITORS

The present invention relates generally to inhibitors of the kinases, such as GSK3, and more particularly to fused pyradazine compounds according to formula (I) and methods of their use.