Furo- and thieno [3,2-c] pyridines

A technology of -NR5 and -CF3, applied in the field of compounds that inhibit the activity of tyrosine kinases in animals, can solve problems such as affecting cell metabolism, reducing proliferation, and inducing apoptosis
CN102007127AInactive Publication Date: 2011-04-06OSI PHARMA INC
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
OSI PHARMA INC
Publication Date
2011-04-06
Estimated Expiration
Not applicable · inactive patent

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Abstract

Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula (I), and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and / or MET.
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Description

Background technique

[0001] The present invention relates to furo[3,2-c]pyridine and thieno[3,2-c]pyridine compounds, their salts, compositions and therapeutic uses, in particular to inhibition of tyrosine kinase activity in animals (including humans) compounds, thereby preventing and / or treating various diseases and conditions, such as cancer.

[0002] RON (Receptor Tyrosine Kinase) is a receptor tyrosine kinase that is part of the MET proto-oncogene family. RON is activated through the combination of PI3K and MAPK pathways and its natural ligand MSP and signaling. RON can be deregulated in cancer through mechanisms such as receptor overexpression and / or constitutively active splice variants. Inhibition of RON has been shown to result in decreased proliferation, induce apoptosis, and affect cellular metabolism. Overexpression of RON is observed in a variety of human cancers and shows increased expression as the disease progresses.

[0003] MET is a receptor tyrosine kinas...

Claims

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