1445856-13-2Relevant articles and documents
2 Tyrosine kinase mediated signal transduction inhibitors
-
Paragraph 0526; 0527; 0528, (2019/09/17)
Disclosed herein are compounds of Formula (), and pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, X, X, X, X, X, and n are as defined herein, pharmaceutical compositions comprising same, and methods of preparation and use.
Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors
Lee, Wendy,Crawford, James J.,Aliagas, Ignacio,Murray, Lesley J.,Tay, Suzanne,Wang, Weiru,Heise, Christopher E.,Hoeflich, Klaus P.,La, Hank,Mathieu, Simon,Mintzer, Robert,Ramaswamy, Sreemathy,Rouge, Lionel,Rudolph, Joachim
supporting information, p. 3518 - 3524 (2016/07/21)
A series of 4-azaindole-containing p21-activated kinase-1 (PAK1) inhibitors was prepared with the goal of improving physicochemical properties relative to an indole starting point. Indole 1 represented an attractive, non-basic scaffold with good PAK1 affinity and cellular potency but was compromised by high lipophilicity (c log D = 4.4). Azaindole 5 was designed as an indole surrogate with the goal of lowering log D and resulted in equipotent PAK1 inhibition with a 2-fold improvement in cellular potency over 1. Structure–activity relationship studies around 5 identified additional 4-azaindole analogs with superior PAK1 biochemical activity (Kia 20-fold decrease in unbound clearance in mouse PK studies for azaindole 5 relative to indole 1.
2, 4-DIAMINE-PYRIMIDINE DERIVATIVE AS SERINE/THREONINE KINASE INHIBITORS
-
Page/Page column 41; 45, (2013/07/05)
Compounds having the formula I wherein A, Rla, Rlb, R2, R3, R4, R5, R6, R7, Rs, Ra, Rb, X1, X2, X3 and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders
