SAN DIEGO, Nov. 12, 2013 /PRNewswire-iReach/ -- SignalRX Pharmaceuticals Inc., focused on developing more effective oncology drugs through molecular design imparting multiple target inhibition, today announced the issuance of U.S. Patent No. 8,557,807 entitled "Thienopyranones as kinase inhibitors" by the U.S. Patent and Trademark Office claiming composition of matter for a broad generic molecular scaffold (TP) of compounds that possess novel kinase inhibition profiles aimed at imparting maximum anticancer efficacy. This U.S. patent grants coverage of the TP scaffold compounds into the year 2029 and is complemented by additional U.S. applications as well as by corresponding patent applications pending in other major markets throughout the world.
The compounds covered in the patent inhibit PI3 kinase and several other key cancer target kinases such as mTORC1, mTORC2, DNA-PK, PLK1 and PIM1. Further mechanisms of action include induction of oxidative stress and demonstrated anti-cancer stem cell activity. Furthermore, certain of these compounds can be molecularly manipulated to maintain their PI3 kinase inhibitory activity while simultaneously also inhibiting certain other key cancer targets providing dual inhibition from a single molecule, in line with the CRIMP (Control Resulting from Inhibition of Multiple Pathways) platform which is focused on the development of more effective cancer treatments. Additionally, other diseases besides cancer such as, age-related macular degeneration and autoimmune diseases along with various inflammatory diseases all potentially can be treated by the kinase inhibition properties of these compounds.
"This patent is a key member of our growing intellectual property portfolio as it provides protection for the cutting edge efforts to deliberately design molecules having multiple mechanisms of action to overcome the devastating ability of cancer cells to shrug off treatments or to develop resistance or re-establish itself via cancer stem cells," said Donald L. Durden, MD, PhD, SignalRx President and Chief Executive Officer. "We are among a select group of cancer researchers who are actively developing anticancer drugs with dual inhibitory properties including PI3K/MEK, PI3K/BRAF, PI3K/HDAC, PI3K/PARP, and PI3K/BET bromodomain setting the stage for the most efficacious smart combination anticancer treatments based on evolving cancer biology and personalized oncology paradigms. In addition, these dual inhibitory drugs solve the problem of early stage clinical trial evaluation of multiple combinations by consolidating at least two of the combination partners into one drug. Moreover, one molecule hitting two targets in the same cell is the only way to ensure that desired simultaneous blockage of both signaling pathways is achieved in vivo because two separate drugs will always suffer from differing cell penetration, metabolism, pharmacokinetics, etc., which promotes tumor cell resistance by diminishing the time and likelihood that useful dual blockage is achieved."
Additional information about these compounds was recently published in the Journal of Medicinal Chemistry (February 14th 2013 issue, volume 56, pages 1922-1939).
About SignalRx Pharmaceuticals Inc.
SignalRx is a privately held corporation developing small molecule inhibitors of key signaling pathways used by cancer and cancer stem cells to evade treatments. Such key signaling pathways include major cell survival mechanisms, epigenetic regulation processes, and DNA repair actions encompassing critical targets such as PI3K, MEK, BRAF, Wnt, HDAC, DNMT, BET bromodomains, and PARP. SignalRx is leveraging its expertise in PI3K pathway inhibition to be the leader in developing single molecule therapeutics that selectively inhibit synergistic critical cancer pathways. These designed multi-action therapeutics are expected to exhibit enhanced anticancer effects and are the result of an effort to be both efficacious and cost effective in an evolving price sensitive oncology environment relying increasingly on prohibitively expensive combination treatments.
Media Contact: Joseph Garlich, SignalRx Pharmaceuticals Inc., 317-418-8246, garlich@signalRx.com
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|SOURCE SignalRx Pharmaceuticals Inc.|
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