Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension

Figures & data

Figure 1. Characteristic symptoms of PAH.

Figure 3. The preparation of compound (1). (a) SOCl₂, toluene, 6 h, 110°C. (b) pyridine, 18 h, 20°C. (c) Cs₂CO_3, PdCl₂(dppf).CH₂Cl₂ dimethoxyethane, H₂O, 7 h, 100°C. (d) iPr₂EtN, HATU, DMF, 90 min, 20°C.

Figure 4. The preparation of compound (2). (a) 2,3,4,6,7,8-hexahydro-1H-pyrimido[1,2-a]pyrimidine, THF, 40 h, 80°C. (b) (4), pyridine, 18 h, 20°C. (c) Cs₂CO_3, PdCl₂(dppf).CH₂Cl₂ dimethoxyethane, H₂O, hν, 1 h, 100°C.

Figure 2. The two compounds that are the subject of the application under discussion.

Figure 5. Known inhibitors of PDGFR kinase.