272-14-0Relevant articles and documents
Design, synthesis, and antifibrosis evaluation of 4-(benzo-[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methyl- pyridin-2-yl)pyrazole and 3(5)-(6-methylpyridin- 2-yl)-4-(thieno-[3,2,-c]pyridin-2-yl)pyrazole derivatives
Zhu, Wen-Jing,Cui, Ben-Wen,Wang, Hui Min,Nan, Ji-Xing,Piao, Hu-Ri,Lian, Li-Hua,Jin, Cheng Hua
, p. 15 - 27 (2019)
Six series of 4-(benzo[c][1,2,5]thiadiazol-5-yl)-3(5)-(6-methylpyridin-2-yl)- pyrazoles 18a–d, 19a–d, 22a–d and 3(5)-(6-methylpyridin-2-yl)-4-(thieno[3,2,-c]- pyridin-2-yl)pyrazoles 20a–d, 21a–d, 23c, 23d have been synthesized and evaluated for their activin receptor-like kinase 5 (ALK5) and p38α mitogen activated protein (MAP) kinase inhibitory activities in enzymatic assays. Among these compounds, the most active compound, 22c, inhibited ALK5 phosphorylation with an IC50 value of 0.030 μM in the enzymatic assay. Compound 22c showed four-fold more potent activity against ALK5 kinase than the clinical candidate, compound LY-2157299. The selectivity index of 22c against p38α MAP kinase is 235, which is much higher than that of LY-2157299 (4) and equally selective to that of EW-7197 (218). Compound 22c effectively suppressed protein and mRNA expression of collagen I and α-SMA in TGF-β-induced LX-2 human hepatic stellate cell (HSC), this result shows that compound 22c has the ability to inhibit the activation of HSC. Compound 22c is expected to be a preclinical candidate for the treatment of hepatic fibrosis.
Preparation method of thienopyridine heterocyclic compound and derivatives thereof
-
Paragraph 0009-0010, (2019/06/30)
The invention discloses a preparation method of a thienopyridine heterocyclic compound and derivatives thereof. The provided preparation method is different from reported methods. According to the preparation method, 4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrochloride is taken as the raw material and is cheap and easily available; the reaction conditions of all steps are mild; the operation of post treatment is simple; the reaction yield is high, and the requirements of industrial production are met. The thienopyridine heterocyclic compound and derivatives thereof have a wide application value in fields such as ionic liquid, ionic liquid crystal, organic semiconductor materials, and the like.
Rho-kinase inhibitors
-
, (2010/02/05)
Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds of the present invention are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.