- Synthesis and biological evaluation of 2-benzylamino-4(5)-(6-methylpyridin- 2-yl)-5(4)-([1,2,4]triazolo[1,5-a]-pyridin-6-yl)thiazoles as transforming growth factor-β type 1 receptor kinase inhibitors
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A series of 2-benzylamino-4(5)-(6-methylpyridin-2-yl)-5(4)-([1,2,4] triazolo[1,5-a]pyridin-6-yl)thiazoles 12a-ab, 13a, 13b, and 18a-d has been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. The N-(3-fluorobenzyl)-4-(6- methylpyridin-2-yl)-5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)thiazol-2-amine (12b) inhibited ALK5 phosphorylation with an IC50 value of 7.01 nM and showed 61% inhibition at 30 nM in a luciferase reporter assay using HaCaT cells permanently transfected with p3TP-luc reporter construct.
- Krishnaiah, Maddeboina,Jin, Cheng Hua,Sreenu, Domalapally,Subrahmanyam, Vura Bala,Rao, Kota Sudhakar,Son, Do-Hyun,Park, Hyun-Ju,Kim, Seung Won,Sheen, Yhun Yhong,Kim, Dae-Kee
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- 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors
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This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors.
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- Synthesis and biological evaluation of 1-substituted-3-(6-methylpyridin-2- yl)-4-([1,2,4triazolo[1,5-apyridin-6-yl)pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors
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A series of 1-substituted-3-(6-methylpyridin-2-yl)-4-([1,2,4triazolo[1,5- apyridin-6-yl)pyrazoles 14a-ae, 16a, 16b, and 21a-c has been prepared and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter ass
- Jin, Cheng Hua,Krishnaiah, Maddeboina,Sreenu, Domalapally,Subrahmanyam, Vura Bala,Rao, Kota Sudhakar,Mohan, Annaji Venkata Nagendra,Park, Chul-Yong,Son, Jee-Yeon,Sheen, Yhun Yhong,Kim, Dae-Kee
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scheme or table
p. 6049 - 6053
(2011/10/18)
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- Tri-substituted heteroaryls and methods of making and using the same
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Compounds of formula (I) possess unexpectedly high affinity for Alk 5 and/or Alk 4, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including fibrotic disorders. In one embodiment, the invention features a compound of the general formula (I).
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Page/Page column 17
(2008/06/13)
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