Med.Chem.Cool

FDA Grants TransTech Pharma Inc. Fast Track Designation for TTP488 for the Treatment of Alzheimer’s Disease

 BusinessWire · Mar. 18, 2013 | Last Updated: Mar. 18, 2013 6:00 PM ET

TransTech Pharma Inc. announced today that the U.S. Food and Drug Administration (FDA) has granted Fast Track designation for TTP488, a new small-molecule chemical compound being developed for the treatment of Alzheimer’s disease. TTP488 prevents the interaction of amyloid beta (Aβ), a material found in the cells of Alzheimer’s patients, and a member of the immunoglobulin supergene family of molecules known as the Receptor for Advanced Glycation Endproducts (RAGE). TTP488 is the first drug related to RAGE, a relatively new biological target in Alzheimer’s disease research, with demonstrated success in multiple clinical trials. TransTech Pharma discovered, developed and owns the rights to this drug candidate.

The FDA’s Fast Track designation is granted to development products intended for the treatment…

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Discovery of an HIV integrase inhibitor with an excellent resistance profile

Discovery of an HIV integrase inhibitor with an excellent resistance profile

Med. Chem. Commun., 2013, Advance Article
DOI: 10.1039/C3MD00014A, Concise Article
David C. Pryde, Rob Webster, Scott L. Butler, Edward J. Murray, Kevin Whitby, Chris Pickford, Mike Westby, Michael J. Palmer, David J. Bull, Hannah Vuong, David C. Blakemore, Darren Stead, Christopher Ashcroft, Iain Gardner, Claire Bru, Wai-Yee Cheung, Ieuan O. Roberts, Jennifer Morton, Richard A. Bissell
PFIZER GLOBAL, KENT, UK
Structure-activity relationship studies within a series of N-hydroxy-dihydronaphthyridinone HIV integrase inhibitors led to a candidate compound, of high potency and with an excellent resistance profile.

In the present article, we describe SAR studies within a series of N-hydroxy-dihydronaphthyridinone HIV integrase inhibitors that led to a candidate compound, PF-4776548, of high potency and with an excellent resistance profile. Uncertainties around the human pharmacokinetic predictions for PF-4776548 led to the compound being taken into a human microdose study to confirm its human pharmacokinetics, the results of which are described herein.

Graphical abstract: Discovery of an HIV integrase inhibitor with an excellent resistance profile
DOI: 10.1039/C3MD00014A

Identification of 4,6-diaryl-1,4-dihydropyridines as a new class of neuroprotective agents

Identification of 4,6-diaryl-1,4-dihydropyridines as a new class of neuroprotective agents

Med. Chem. Commun., 2013, 4,590-594
DOI: 10.1039/C3MD20345J, Concise Article
Giammarco Tenti, Javier Egea, Mercedes Villarroya, Rafael Leon, Jose Carlos Fernandez, Juan Fernando Padin, Vellaisamy Sridharan, M a Teresa Ramos, J. Carlos Menendez
MADRID SPAIN
4,6-Diaryl-1,4-dihydropyridines, lacking the structural features needed for vascular activity, were found to prevent calcium overload and behave as neuroprotective agents.

A library of 4,6-diaryl-1,4-dihydropyridines was synthesized using a CAN-catalyzed, Hantzsch-related three component reaction starting from ammonium acetate, β-dicarbonyl compounds and a variety of α,β-unsaturated ketones including chalcones, their vinylogs and heteroanalogues. These compounds lack the structural features needed for vascular activity and were found to prevent calcium overload and behave as neuroprotective agents. One of the compounds, bearing a 2-thienyl substituent at C-4, showed the highest neuroprotective activity and was also a moderate antioxidant, being a good lead compound for further studies in this area.

Graphical abstract: Identification of 4,6-diaryl-1,4-dihydropyridines as a new class of neuroprotective agents

ORGANIC CHEMISTRY SELECT

There are a lot of chemicals racing around your brain and body when you’re in love. Researchers are gradually learning more and more about the roles they play both when we are falling in love and when we’re in long-term relationships. Of course, estrogen and testosterone play a role in the sex drive area . Without them, we might never venture into the “real love” arena.

That initial giddiness that comes when we’re first falling in love includes a racing heart, flushed skin and sweaty palms. Researchers say this is due to the dopamine, norepinephrine and phenylethylamine we’re releasing. Dopamine is thought to be the “pleasure chemical,” producing a feeling of bliss. Norepinephrine is similar to adrenaline and produces the racing heart and excitement. According to Helen Fisher, anthropologist and well-known love researcher from Rutgers University, together these two chemicals produce elation, intense energy, sleeplessness, craving, loss of appetite and…

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SRxA's Word on Health

Few topics inspire more heated discussion among drug developers and pharmaceutical industry watchers than the regulation of new products.  For those unfamiliar with the debate, the two sides of the argument can be summarized as follows.

Industry veterans feel that excessively conservative regulators squelch innovation in a desire to cover their own behinds, while industry critics contend that regulators aren’t strict enough, and that pharmaceutical companies should be held to an even higher standard and warrant even greater supervision.

In the meantime, patients wonder why modern science hasn’t produced the medicines they so desperately need.

Now it seems there may be an answer that could satisfy everyone.  Susan Desmond-Hellmann, Chancellor of the University of California, San Francisco (UCSF) and former Genentech executive, suggests turning drug approvals from a discrete yes or no variable into a continuous moving target.

The fundamental problem with the current system, Desmond-Hellmann observes, is that…

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