University of North Carolina at Chapel Hill

Dehui Zhang

Xiaodong Wang

Dmitri Kireev

Weihe Zhang

Andrew Louis McIver

Henry Shelton Earp, Iii

This invention is in the area of improved therapeutic combinations for and methods of treating selected cancers using selected pyrimidine compounds having pan-TAM or Mer/Axl dual receptor tyrosine kinase inhibitory activity in combination with immune checkpoint inhibitors. In one aspect, an improved treatment for select cancers is disclosed using selected pyrimidine compounds described herein in combination with an immune checkpoint inhibitor, for example, a cytotoxic T-lymphocyte-associated protein 4 (CTLA4) inhibitor, a programmed cell death protein 1 (PD1) inhibitor, or a programmed death-ligand 1 (PDL-1) inhibitor, or combination thereof.

Pan-TAM inhibitors and Mer/Axl dual inhibitors

Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described. 

Growing community of inventors

Chapel Hill, NC, United States of America

Dehui Zhang