TRYPANOSOMIASIS / MALARIA

Human African Trypanosomiasis (HAT) is a disease caused by a blood-borne parasite and transmitted by
tsetse fly bites to humans and cattle in central Africa. Infection rates vary, but estimates during epidemic
periods have ranged as high as 500,000 cases per year, resulting in tens of thousands of deaths as the
parasite passes into the brain of patients, causing neurological disorders and - if left untreated - death.
Treatment options are limited, not readily available and generally not well tolerated.

Since 2011, we have partnered with scientists at the Center for World Health and Medicine / St. Louis
University (CWHM / SLU) in St. Louis, MO, to discover and evaluate novel treatments for HAT. Using our
knowledge and experience in the design and devolpment of CNS targeted drugs, we have identified
several distinct chemical templates which can be exploited to create safer and more efficacious
medications, especially for Stage 2 HAT patients. CWHM/SLU is collaborating with MediSynergics to
assess the potency of these compounds against a number of
Trypanosoma brucei strains in an effort
to select the best compounds for development and human efficacy studies.

In April 2016 we were awarded a 2-year, SBIR Phase 1 grant, totaling $600,000, by the National Institute
for Allergy and Infectious Diseases (NIAID), part of the National Institutes of Health (NIH). With this
generous grant we have significantly increased our efforts into finding better treatment options for HAT.  
During the first year we will prepare a number of chemically similar compounds(analogs) for in vitro
assessment at SLU.  The second year will focus upon optimization of potency in an animal model of HAT
and determination of the mechanism of action for our lead compound(s).  In vivo studies will be directed
by Dr. Kojo Mensa-Wilmot of the University of Georgia in Athens, GA (UGA).

We also were recently selected as participants in the Technology Incubator Program (TIP) sponsored by the
University of Connecticut. We have moved into new, state-of-the-art labs in the Cell and Genome Sciences
building located at 400 Farmington Avenue in Farmington, CT.

During our previous careers at Pfizer Inc. our primary focus was on the discovery and development of
novel therapeutic agents to treat a variety of CNS disorders. Our experience with Geodon / Zeldox (TM)
during the R&D stages has enabled us to design and evaluate new chemical matter that may eventually
lead to new therapies for depression, Alzheimer's disease and other related human disorders.

Screening of our compounds in this area is offered through the Psychotherapeutic Drug Screening
Program (PDSP) at the University of North Carolina, Chapel Hill. With funding provided by the National
Institutes of Mental Health (NIMH), Dr. Bryan Roth and his colleagues test each compound in a variety of
receptor and enzyme assays. Recently, we have identified compounds that have high affinity for Kappa and
Delta Opioid receptors in the CNS. We are currently exploring additional examples from this class to
identify the optimal compound(s) for advanced testing with the goal of selecting a candidate for study
in animal models of depression and/or mania.

                   INTELLECTUAL PROPERTY (IP)

MediSynergics, LLC has filed numerous patent applications with the United States Patent and Trademark
Office (USPTO) for the use of our novel compounds in the treatment of patients with CNS and parasitic
diseases.  To date, nine US Patents have been assigned to MediSynergics and others are pending approval.

Simarro PP1, Cecchi G, Paone M, et al.  "The Atlas of human African
trypanosomiasis: a contribution to global mapping of neglected tropical
diseases."  Int. J. Health Geogr. 2010 Nov 1;9:57.
doi: 10.1186/1476-072X-9-57.
Photomicrograph of T. brucei
parasite in human blood sample.
Tsetse fly