公开(公告)号：WO2020092950A1

公开(公告)日：2020-05-07

申请号：PCT/US2019/059462

申请日：2019-11-01

Applicant: NORTHWESTERN UNIVERSITY

Inventor： JI, Peng ,  SCHILTZ, Gary, E. ,  MISHRA, Rama, K. ,  JAIN, Atul, D.

IPC: C07D403/06 ,  C07D409/14 ,  A61K31/381 ,  A61K31/404 ,  A61P35/00

Abstract: Disclosed herein are compounds, compositions, and methods for treating cell proliferative diseases and disorders based on present inventors discovery that Pleckstrin-2 (Plek2) can be targeted to treat cell proliferative diseases and disorders. The compositions and methods disclosed herein include or utilize the disclosed compounds as therapeutic agents which inhibit the biological activity or expression of Pleckstrin-2 (Plek2) and collectively may be referred to as "Plek2 inhibitors." Disclosed are small molecule inhibitors of Plek2 biological activity. The compositions and method may be utilized for treating cell proliferative diseases and disorders that are characterized by elevated levels of Plek2 expression and/or by activation of the phosphatidylinositide 3-kinase (PI3K)/Akt pathway. Cell proliferative diseases and disorders that may be treated using the disclosed compositions and methods may include, but not limited to, myeloproliferative neoplasms (MPNs) such as Philadelphia (Ph)-negative MPNs, and cancers such as acute myeloid leukemia (AML) and cancers characterized by solid tumors.

公开(公告)号：WO2020046382A1

公开(公告)日：2020-03-05

申请号：PCT/US2018/049175

申请日：2018-08-31

Applicant: NORTHWESTERN UNIVERSITY

Inventor： SCHILTZ, Gary, E. ,  MISHRA, Rama, K. ,  HAN, Huiying ,  ABDULKADIR, Sarki, A. ,  IZQUIERDO-FERRER, Javier ,  JAIN, Atul, D.

IPC: C07D231/10 ,  C07D239/24 ,  C07D249/06 ,  C07D403/04 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/505 ,  A61P35/00

Abstract: Disclosed are substituted heterocycle compounds including substituted pyrazoles, substituted pyrimidines, and substitute triazoles. The substituted heterocycles disclosed herein are shown to be useful in inhibiting c-MYC and may be utilized as therapeutics for treating cancer and cell proliferative disorders.