Pyrrolo[2,3-d]pyrimidines as inhibitors of pp60c-src

Abstract

Over the past decade, a great deal of progress has been made towards elucidating the molecular basis of intercellular and intracellular communication. Phosphorylation of intracellular substrates by protein tyrosine kinases is now known to play a pivotal role in normal cell growth and is often dysregulated in a number of proliferative diseases. In this patent, Ciba-Geigy discloses a series of novel pyrrolo[2,3-d]pyrimidines, 178 in total, which inhibit the activity of the protein tyrosine kinase pp60_c-src. Potencies for the inhibition of purified enzyme range from 1 nM to 10 <μ>m</μ>M and activity is also claimed in both in vitro and in vivo models for osteoporosis. Compounds in the series are also reported to be inhibitors of other non-receptor and receptor protein tyrosine kinases. It is possible that these compounds may prove useful in a range of therapeutic areas, including cancer, osteoporosis, thrombosis and immune disorders.