195252-68-7Relevant academic research and scientific papers
On the absolute configuration of 1-cyclopropylethan-1-amine
Perry, Matthew W.D.,Eriksson, Anders,Landergren, Marie Rydén
, p. 1135 - 1138 (2017)
We observed a discrepancy between the reported specific rotation for the enantiomers of 1-cyclopropylethan-1-amine and the values for commercial material. Analyses by VCD of the free amine, by NMR analysis of the derived (S)-O-methylmandelamides and an X-ray crystal structure of one of the mandelamides defined the specific rotation for each enantiomer.
Discovery of 1-amino-5 H-pyrido[4,3-b]indol-4-carboxamide inhibitors of janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders
Lim, Jongwon,Taoka, Brandon,Otte, Ryan D.,Spencer, Kerrie,Dinsmore, Christopher J.,Altman, Michael D.,Chan, Grace,Rosenstein, Craig,Sharma, Sujata,Su, Hua-Poo,Szewczak, Alexander A.,Xu, Lin,Yin, Hong,Zugay-Murphy, Joan,Marshall, C. Gary,Young, Jonathan R.
supporting information; experimental part, p. 7334 - 7349 (2011/12/04)
The JAK-STAT pathway mediates signaling by cytokines, which control survival, proliferation, and differentiation of a variety of cells. In recent years, a single point mutation (V617F) in the tyrosine kinase JAK2 was found to be present with a high incidence in myeloproliferative disorders (MPDs). This mutation led to hyperactivation of JAK2, cytokine-independent signaling, and subsequent activation of downstream signaling networks. The genetic, biological, and physiological evidence suggests that JAK2 inhibitors could be effective in treating MPDs. De novo design efforts of new scaffolds identified 1-amino-5H-pyrido[4,3-b]indol-4-carboxamides as a new viable lead series. Subsequent optimization of cell potency, metabolic stability, and off-target activities of the leads led to the discovery of 7-(2-aminopyrimidin-5-yl)-1- {[(1R)-1-cyclopropyl-2,2,2-trifluoroethyl]amino}-5H-pyrido[4,3-b] indole-4-carboxamide (65). Compound 65 is a potent, orally active inhibitor of JAK2 with excellent selectivity, PK profile, and in vivo efficacy in animal models.
