Apoptosis Inhibitors
Unique chemistry and stability under physiological conditions. Potent compounds active in nanomolar range with an IC50 several fold lower than other apoptosis inhibitors such as pifithrin. Demonstrated efficacy in animal models.
Wide range of clinical treatments where suppression of apoptosis of normal cells is desirable such as radiation and chemotherapy for human cancers to prevent side effects that include mucositis, hair loss, myelosuppression and diarrhea. Protection from apoptosis in heart and brain ischemia, peripheral limb protection in vascular disease and prevention of shock resulting from viral or bacterial infections, or burns.
Researchers at the University of California have developed novel heterocyclic compounds that protect normal cells from apoptosis. These compounds are active in vitro in the nanomolar range and prevent apoptosis in cells treated with glucocorticoids or ionizing radiation. In addition, the compounds also significantly increase survival rates of mice irradiated with gamma rays with no observable toxicity.
Patent Number: US6696441B1
Application Number: US2000637531A
Inventor: Cottam, Howard B. | Leoni, Lorenzo M. | Carson, Dennis A.
Priority Date: 11 Aug 2000
Priority Number: US6696441B1
Application Date: 11 Aug 2000
Publication Date: 24 Feb 2004
IPC Current: A61K0031519 | C07D048704 | C07D051304
US Class: 5142332 | 514322 | 514368 | 514375 | 544115 | 546199 | 5462704 | 5462731 | 5462741 | 548151 | 548218 | 548368
Assignee Applicant: The Regents of the University of California
Title: Inhibition of p53-induced stress response
Usefulness: Inhibition of p53-induced stress response
Summary: In the manufacture of medicament useful to prevent detrimental effect upon cells due to DNA damage such as caused by chemotherapy, radiation, ischemic event e.g. stroke, infarct, ischemia reperfusion injury and organ transplantation, environmental pollution or contamination, etc; for study of the physiological processes associated with intracellular DNA damage; to prevent growth of microorganisms; to inhibit cancer or sensitize cancer cells to chemotherapeutic agents, radiation or other cancer treatments.
Novelty: New polycyclic imidazole derivatives useful for preventing detrimental effects of e.g. stroke
Disease Diagnostic/Treatment
Cancer/Tumor
State Of Development Synthesized product was formulated as a topical ointment, which was efficacious, in vivo (mouse), for healing of irradiation-induced skin damage (see Related Materials). Research interests can be found at: http://cancer.ucsd.edu/Research/summaries/dcarson.asp Related Materials Additional Technologies by these Inventors Tech ID/UC Case 22359/2005-E50-0 Related Cases 2005-E50-0, 2000-E70-0
USA
