Berkeley, CA, United States
Berkeley, CA, United States

Plexxikon is an American drug-discovery company based in Berkeley, California, that was co-founded in 2001 by Joseph Schlessinger of Yale University with Sung-Hou Kim of the University of California, Berkeley.It uses a proprietary structural biology-based platform called Scaffold-Based Drug Discovery to build a pipeline of products in multiple therapeutic areas. This discovery process integrates multiple state-of-the-art technologies, including structural screening as one key component that it hopes will give a significant competitive advantage over other approaches. To date, the company has discovered several clinical and preclinical stage compounds. One of the most advanced drugs under development is an inhibitor of an activated form of the B-Raf kinase. A V600E mutant of the B-Raf kinase is found in approximately 70% of malignant melanomas, a large percentage of colorectal and thyroid cancers and many other tumor types. PLX4032 selectively inhibits this form of the kinase, and is currently in clinical trials. Plexxikon has entered into a partnership with Roche Pharmaceuticals to develop PLX4032 as a targeted anti-cancer therapeutic, which has shown particular promise for treating melanoma. Plexxikon is also collaborating with Wyeth Pharmaceuticals on several products for use in type II diabetes and other metabolic disorders. The most advanced of these agents is PLX204, which is currently in Phase 2 clinical trials for type II diabetes.In April 2011, Plexxikon was acquired by the Japanese pharmaceutical company Daiichi Sankyo for $805 million and an additional $130 m in potential milestone payments. Wikipedia.


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Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.


Compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein A, J, R^(1), R^(2), R^(3), R^(4), R^(5), R^(6), R^(7), R^(9), X, m and n are as described herein, compositions thereof, and methods and uses thereof.


Patent
Plexxikon | Date: 2016-09-19

Provided herein are heterocyclic compounds of Formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses, methods for their preparation, intermediate compounds, pharmaceutical compositions containing such a compound, and their therapeutic uses.


Patent
Plexxikon and Hoffmann-La Roche | Date: 2016-08-19

Provided are solid dispersions, solid molecular complexes, salts and crystalline polymorphs involving propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide.


Patent
Plexxikon | Date: 2016-05-20

The present disclosure provides methods of treating a subject suffering from or at risk of a BRAF V600 mutation or BRAF fusion mutation related disease or condition, without activating the MAPK pathway or inducing expression of MAPK pathway genes in cells harboring wild-type BRAF.


Patent
Plexxikon | Date: 2016-05-05

The present disclosure provides methods of using protein kinase inhibitors for treating diseases and conditions, including diseases and conditions associated with activity of any protein kinase selected from Fms protein kinase including any mutations thereof, Kit protein kinase any mutations thereof, Flt-3 protein kinase any mutations thereof and combinations thereof.


Patent
Plexxikon | Date: 2016-05-20

Solid forms of Compound I (and its S-enantiomer, Compound II), active on protein kinases, were prepared and characterized: Also provided are methods of using the solid forms.


Patent
Plexxikon | Date: 2016-05-20

Provided herein are intermediates and processes useful for facile synthesis of compounds of formula (I): or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein Q, P^(1 )and P^(2 )are as defined in this disclosure.


Compounds of Formula I: or a pharmaceutically acceptable salt, a solvate, a tautomer, an isomer or a deuterated analog thereof, wherein R^(1), R^(2), Q^(1), Q^(2), and Q^(3), are described in this disclosure, compositions thereof, and methods and uses thereof.


Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.

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