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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.


Patent
Plexxikon | Date: 2014-03-14

Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.


Patent
Plexxikon | Date: 2015-09-10

Heterocyclic compounds of formula (I), pharmaceutical compositions containing such a compound and their therapeutic uses.


Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC kinase protein. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of one or more of Fms, Kit, Flt3, TrkA, TrkB and TrkC, including rheumatoid arthiritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimers disease, Parkinsons disease, global ischemia, ulcerative colitis, Crohns disease, immune thrombocytopenic purpura, atherosclerosis, systemic lupus erythematosis, myelopreparation for autologous transplantation, transplant rejection, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, acute myeloid leukemia, melanoma, multiple myeloma, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastoma, neurofibromatosis, osteolytic bone metastases, brain metasteses, gastrointestinal stromal tumors, and giant cell tumors.


Compounds active on the receptor protein tyrosine kinases c-kit and/or c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or conditions and/or c-fms-mediated diseases or conditions, and methods for the use 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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