Pyridinyl ureas and related compounds as alpha7 nicotinic acetylcholine receptor inhibitors and their preparation. Haydar, Simon N.; Ghiron, Chiara; Valacchi, Michela; Zanelli, Ugo. U.S. Pat. Appl. Publ. (2010), US2010016360

Piperidinecarboxamides and related compounds as modulators of alpha7 nicotinic acetylcholine receptors and their preparation and use in the treatment of diseases. Bothmann, Hendrick; Roncarati, Renza; Micco, Iolanda; Nencini, Arianna; Ghiron, Chiara. U.S. Pat. Appl. Publ. (2010), US2010016288

Pyridinyl urea derivatives as alpha7 nicotinic acetylcholine receptor inhibitors and their preparation. Ghiron, Chiara; Valacchi, Michela; Zanelli, Ugo; Haydar, Simon N. U.S. Pat. Appl. Publ. (2010), US2010016343

Pyrazole derivatives as alpha7 nicotinic acetylcholine receptor inhibitors and their preparation. Haydar, Simon N.; Bothmann, Hendrick; Ghiron, Chiara; Maccari, Laura; Micco, Iolanda; Nencini, Arianna; Zanaletti, Riccardo. PCT Int. Appl. (2010), WO2010009290

In 2007 Siena Biotech entered into an R&D collaboration with Roche on small molecule inhibitors of beta-secretase (BACE) as a disease-modifying approach to Alzheimer's Disease. In 2010 Roche exercised its option early to become the lead party for further development, manufacture and commercialization of selected candidates. The most advanced compound from the collaboration with Roche, RG7129, is in Phase I clinical development.
Siena Biotech received an undisclosed initial option exercise fee in 2010, a further undisclosed milestone in July 2011 and is eligible for further success payments upon attainment of certain development and regulatory milestones. Following successful commercialization of any candidate compounds, Siena Biotech will also receive royalties on product sales and retain rights for Orphan indications.

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Preparation of 4,4-diphenyl-4,5-dihydro-oxazol-2-ylamine derivatives as β-secretase inhibitors. Andreini, Matteo; Gabellieri, Emanuele; Guba, Wolfgang; Marconi, Guido; Narquizian, Robert; Power, Eoin; Travagli, Massimiliano; Woltering, Thomas; Wostl, Wolfgang. U.S. Pat. Appl. Publ. (2009), US2009209529

In 2007 Siena Biotech and Elixir Pharmaceuticals entered into an agreement to evaluate Elixir's SIRT1 inhibitors in Huntington's Disease. One of the compounds, SEN196 (EX-527) was found to have cyto- and neuroprotective activity against toxicity induced by mutant huntingtin in vitro and to be effective in a number of HD endpoints in vivo. In January 2010 Siena Biotech obtained Orphan Drug status from both the FDA and the EMEA for SEN196, which will shortly enter Phase II clinical trials.

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In 2010 Siena Biotech signed an alliance with A*STAR, Singapore's Agency for Science, Technology and Research towards new therapies for cancer and bone loss. The first of two arms of the alliance, with the Experimental Therapeutics Centre of A*STAR of is based around the development of small molecule inhibitors of a major signalling pathway involved in brain tumours, gastric cancer and leukaemia. The second part, working with the Singapore Immunology Network involves the development of a novel monoclonal antibody of a specific extracellular component of a signalling pathway for use in bone diseases such as osteoporosis.

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