944468-99-9Relevant academic research and scientific papers
THERAPEUTIC PYRIDAZINE COMPOUNDS AND USES THEREOF
-
Page/Page column 131; 162; 163, (2016/09/26)
The present invention relates to compounds of formula (I): (I) and salts thereof, wherein: R1-R4 have any of the values defined in the specification, and compositions and uses thereof. The compounds are useful as inhibitors of BRG1, BRM and/or PB1. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various BRG1-mediated disorders, BRM-mediated disorders and/or PB1-mediated disorders.
Facile synthesis of 4-aryl and alkyl substituted, N6-alkylated pyridazine-3,6-diamines
Wlochal, Joanna,Bailey, Andrew
supporting information, p. 6791 - 6794 (2016/02/05)
Substituted pyridazine-3,6-diamines are attractive but poorly precedented scaffolds in medicinal chemistry and are challenging targets in terms of synthetic tractability. In the following communication we report the use of a Buchwald protocol for the facile synthesis of 4-aryl and alkyl substituted, N6-alkylated pyridazine-3,6-diamines. This approach utilises the unreactive nature of the pyridazine 3-amino group, negating the need for an additional protecting group in the transformation. The relevant precursors were prepared by selective Suzuki or Negishi transformations using commercially available 4-bromo-6-chloro-3-pyridazinamine.
1,2-PYRIDAZINES, 1,6-PYRIDAZINES AND PYRIMIDINES
-
Paragraph 0220; 0234, (2013/10/22)
This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically accep
1,2- PYRIDAZINE, 1,6- PYRIDAZINE OR PYRIMIDINE - BENZAMIDE DERIVATIVES AS GPBAR1 MODULATORS
-
Page/Page column 47; 51, (2013/10/22)
This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula I wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acc
SUBSTITUTED IMIDAZO[1,2-B]PYRIDAZINES
-
, (2013/08/28)
The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia.
Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors
Elagawany, Mohamed,Ibrahim, Mohamed A.,Ali Ahmed, Hany Emary,El-Etrawy, A.Sh.,Ghiaty, Adel,Abdel-Samii, Zakaria K.,El-Feky, Said A.,Bajorath, Juergen
, p. 2007 - 2013 (2013/05/09)
The design and synthesis of pyridazinone and phthalazinone derivatives are described. Newly synthesized compounds were tested on a panel of four kinases in order to evaluate their activity and potential selectivity. In addition, the promising compounds were tested on four cancer cell lines to examine cytotoxic effects. The compounds inhibited DYRK1A and GSK3 with different activity. SAR analysis and docking calculations were carried out to aid in the interpretation of the results. Taken together, our findings suggest that pyridazinone and phthalazinone scaffolds are interesting starting points for design of potent GSK3 and DYRK1A inhibitors.
