247092-10-0Relevant articles and documents
NOVEL INHIBITORS OF MAP4K1
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Page/Page column 63; 64, (2018/12/13)
The invention relates to novel inhibitors of MAP4K1 (HPK1) useful for the treatment of diseases or disorders characterised by dysregulation of the signal transduction pathways associated with MAPK activation, including hyperproliferative diseases, diseases of immune system dysfunction, inflammatory disorders, neurological diseases, and cardiovascular diseases. The invention further relates to pharmaceutical compositions comprising the same and methods of treatment of said diseases and disorders. The inhibitors are of formula (I) wherein the definitions for A, D, E, F, R5, R6, R7, Z, ring Q, n, x and y are as given in the application.
Rapid Access to Orthogonally Functionalized Naphthalenes: Application to the Total Synthesis of the Anticancer Agent Chartarin
Unzner, Teresa A.,Grossmann, Adriana S.,Magauer, Thomas
supporting information, p. 9763 - 9767 (2016/08/10)
We report the synthesis of orthogonally functionalized naphthalenes from simple, commercially available indanones in four steps. The developed method proceeds through a two-step process that features a thermally induced fragmentation of a cyclopropane indanone with simultaneous 1,2-chloride shift. Migration of the chloride substituent occurs in a regioselective manner to preferentially afford the para-chloronaphthol substitution pattern. The obtained naphthols are versatile building blocks that can be selectively modified and used for the efficient construction of biologically active molecules. This has enabled the total synthesis of the potent anticancer natural product chartarin through a highly convergent retrosynthetic bond disconnection.
Structure-based design of a potent, selective, and brain penetrating PDE2 inhibitor with demonstrated target engagement
Buijnsters, Peter,De Angelis, Meri,Langlois, Xavier,Rombouts, Frederik J. R.,Sanderson, Wendy,Tresadern, Gary,Ritchie, Alison,Trabanco, Andrs A.,Vanhoof, Greet,Roosbroeck, Yves Van,Andrs, Jos-Ignacio
, p. 1049 - 1053 (2014/12/10)
Structure-guided design led to the identification of the novel, potent, and selective phosphodiesterase 2 (PDE2) inhibitor 12. Compound 12 demonstrated a >210-fold selectivity versus PDE10 and PDE11 and was inactive against all other PDE family members up