United States Patent 6,531,479 relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin dependent kinases
(CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukemia, psoriasis and the like.
Paracelsian's patented CDK assays measure the concentration of at least one cyclin dependent kinase
in the blood, plasma or serum of an animal or human, and correlates that concentration to the presence of abnormal cellular proliferation or tumor development in any tissue of the organism from which the sample was obtained.
According to the company, the revenue is a UK grant to progress CYC065, its Cyclin Dependent Kinase
inhibitor, to IND.
Protein kinases include mitogen activated protein kinases and cyclin dependent kinases
. Lipid kinases include sphingosine kinases and phosphatidylinositol kinases.
Milciclib (PHA-848125AC) is a small molecule inhibitor of several cyclin dependent kinases
such as CDK1, CDK4, CDK5 and CDK7.
Several novel agents are now in clinical trials in patients with chemoresistant breast cancer, including rucaparib, an oral small-molecule inhibitor of PARP (poly ADP-ribose polymerase), for triple-negative breast cancer; palbociclib, an oral and selective inhibitor of cyclin dependent kinases
4 and 6, in women with hormone receptor-positive / HER2-negative disease; and trastuzumab emtansine, a conjugate of trastuzum ab and the cytotoxic agent mertansine, in patients with chemoresistant HER2-positive breast cancer, Dr.
Reddy, "Cell cycle control in mammalian cells: role of cyclins, cyclin dependent kinases
(CDKs), growth suppressor genes and cyclin-dependent kinase inhibitors (CKIs)," Oncogene, vol.
Palbociclib is an investigational oral and selective inhibitor of cyclin dependent kinases
(CDK) 4 and 6.