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Tranzyme
Pharma Announces Issuance of European Patent Protecting
Company’s Novel Macrocyclic Chemistry


RESEARCH TRIANGLE PARK, N.C. and
SHERBROOKE, Québec (December 13, 2006) -Tranzyme Pharma, a
leading biopharmaceutical company developing novel
mechanism-based therapeutics for the treatment of
gastrointestinal (GI) and metabolic disorders, announced today
the issuance of a European patent (EP 1 218 403) entitled
“Combinatorial Synthesis of Libraries of Macrocyclic Compounds
Useful in Drug Discovery.” The patent protects key aspects of
the Company’s core drug discovery technology, Macrocyclic
Template Chemistry (MATCH™). MATCH™ is based on the synthesis of
specific types of low-molecular weight, drug-like compounds
called macrocycles. This European patent, together with the
notice of allowance for the corresponding U.S. patent received
earlier this year, provides substantial protection for the
Company’s novel chemistry technology. Tranzyme currently has
approximately 40 patent applications covering MATCH™ as well as
its unique drug candidates for GI and metabolic diseases.
Tranzyme has leveraged MATCH™ to develop first-in-class drug
candidates that have shown to be well tolerated in man and have
demonstrated oral bioavailability, in vivo efficacy, and high
potency and selectivity against multiple types of
pharmaceutically important targets. Tranzyme has developed the
first synthetic library of these macrocyclic compounds which
contains 25,000 unique structures. The MATCH™ library exhibits
excellent chemical and conformational diversity to provide broad
target applicability in modulating G-protein coupled receptors,
protein kinases, protein-protein interactions and ion channels.
“MATCH™ enables Tranzyme to design its macrocyclic compounds to
exhibit highly specific recognition of a pharmacological target,
which leads to greatly reduced safety issues during
development,” said Helmut Thomas, Ph.D., DABT, Senior Vice
President of Research & Preclinical Development for Tranzyme
Pharma. “We are able to achieve excellent fit for a biological
target by combining recognition elements for multiple
pharmacophores in a compact structure.”
“We are very excited with the significant progress that we have
made in demonstrating the ability of our chemistry to produce a
pipeline of high-quality drug candidates,” added Vipin K. Garg,
Ph.D., President & CEO of Tranzyme Pharma. “Our strategy is to
further leverage this technology in joint drug discovery and
development alliances across multiple therapeutic areas.”
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