Substituted 5-alkynyl pyrimidines having neurotrophic activity

Patent Number: 7,205,297

This patent discloses a series of companies that are substituted 5-alkynyl pyrimidines with nerve growth factor-like (NGF) activity for treatment of neurological disorders.

Essentially, the data the inventors disclosed in the patent is that these compounds they generated can induce promotion of neurite outgrowth and elevation of choline acetyltransferase in the PC12 cell line.

The patent's issued claims cover specific compositions of matter, pharmaceutical compositions and methods of treatment. Some claims cover reatment of diseases such as Alzheimer's disease, peripheral neuropathy, senile dementia, seizure disorders,
Huntington's disease, and Parkinson's disease.

This patent will be interesting to use in combination with various stem cell therapies since NGF activities are not only specific to neurons but are active other stem cells such as hematopoietic stem cells (Bracci-Laudiero et al. CD34-positive cells in human umbilical cord blood express nerve growth factor and its specific receptor TrkA. J Neuroimmunol. 2003 Mar;136(1-2):130-9).

The assignee of the patent, Krenitsky Pharmaceuticals, Inc. from Durham, North Carolina seems to be in the business of preclinically developing small molecule candidates and licensing to others for clinical trials. It seems that their candidate KP544 is described in the current patent.

KP544 is in preclinical development, it is orally available, relatively easy to synthesize, and has activity against taxol-induced peripheral neuropathy and intrastriatal quinolinic acid induced cognitive dysfunction.

For more information about this, Krenitsky Pharmaceuticals has a website at www.kpi-pharmadotcom

View this patent on the USPTO website.