University of Texas System

Novartis Ag

Gsf-international Research Institute for Environment and Health

Moshe Talpaz

Nicholas J Donato

Alexander Levitzki

Waldemar Priebe

Izabela Fokt

Slawomir Szymanski

Paul William Manley

Michael Hallek

Markus Warmuth

Doriano Fabbro

Ji Wu

Bryant G Darnay

Janet E Price

Ann Poblenz

The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.

Compounds for treatment of cell proliferative diseases

The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.

Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia

The present invention include methods and compositions for treating bone-resorbing diseases or bone resorption related to a pathologic condition generally, including, but not limited to osteoporosis, arthritis, rheumatoid arthritis, cancer metastases to the bone, bone cancer, hypercalcemia, osteolytic lesions with orthopedic implants, Paget's disease, and bone loss associated with hyperparathyroidism. Representative cancers include, but are not limited to breast cancer, prostrate cancer, colon cancer, endometrial cancer, multiple myeloma, renal cell carcinoma, heck and neck cancers, and cervical carcinoma. Arthritic conditions include, but are not limited to adjuvant-, collagen-, bacterial- and antigen-induced arthritis, particularly rheumatoid arthritis.

Inhibition of osteolytic lesions by SRC kinase inhibitors

Growing community of inventors

Houston, TX, United States of America

Moshe Talpaz