Bio Screening Industry News

Last October, TimTec and Collaborative Drug Discovery (CDD) established a collaboration in which CDD’s web-based data management system would host two TimTec Natural Products libraries on their free community Public Access site.  Through this partnership, researchers would be able to register for a free account with CDD allowing them to chemically mine the contents of these TimTec compound libraries using CDD’s powerful, intuitive web-based database software.

TimTec is now offering three more libraries on the CDD Public Access database:

The TimTec ActiTarg-K Kinase Modulators library contains over 6,000 compounds known to inhibit protein kinase activity:

http://www.timtec.net/actitarg-k-kinase-modulators.html

The TimTec OGT Inhibitors Analogs library contains more than 300 compounds analogous to three known O-GlcNAc Transferase inhibiting molecules:

http://www.timtec.net/o-glcnac-transferase-inhibitors.html

Finally, the TimTec resourceful Diversity Set is a general screening collection of drug-like compounds that present most diversified selection from TimTec stock. This screening library contains 10,000 of the most diverse compounds, all complying with the Lipinski Rule of Five:

http://www.timtec.net/diversity-set-10k.html

TimTec’s five databases join more than 25 other databases containing chemical and biological data hosted on CDD Public Access, including:

• 47,000 Ki values for 20,000 compounds against 699 GPCR targets from the NIMH Psychoactive Drug Screening Program at the University of North Carolina
• Over 15,000 compounds with Malaria assay data from 5 public data sources
• 48,818 compounds from the Distributed Drug Discovery (D3) at Indiana University – Purdue University Indianapolis (IUPUI)
• Almost 7,500 compounds with Tuberculosis antibacterial and cell viability information from 4 public data sets and growing thanks to their collaboration with the Bill & Melinda Gates Foundation

About TimTec, LLC.

TimTec LLC. - http://www.timtec.net - is a privately held company located in NewarkDelaware, USA. It was founded in 1995 and began its work in the areas of acquisition and distribution of synthetic organic and natural compounds, custom synthesis, and laboratory equipment to become a full service partner for drug discovery. TimTec has established a global network of thousands of scientists from research centers around the world. The company has developed strong in-house expertise assembling general and targeted library collections for variety of research purposes. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.

For more information on TimTec library collections, please contact:

Kay Denisova
Business Development
TimTec LLC
Harmony Business Park Building 301-A
Newark, DE 19711
Tel 302 292 8500
Fax 302 292 8520
info(at)timtec.net
http://www.timtec.net

About Collaborative Drug Discovery, Inc.

Collaborative Drug Discovery, Inc. (CDD) - http://www.collaborativedrug.com - provides web-based software that organizes preclinical research data to help scientists advance new drug candidates more effectively. The CDD database enables scientists to “archive, mine, and collaborate”® around preclinical chemical and biological drug discovery data through a web-based interface. The software helps distributed research groups to safely store and intelligently analyze small molecule, enzyme, cell and animal bioactivity data accumulated from both low-throughput and high-throughput screens. Unique collaboration features and CDD’s community-oriented approach help unite globally dispersed humanitarian efforts against neglected infectious diseases. Similar collaborative strategies are also rapidly gaining prominence in the commercial arena. CDD offers its industrial-strength database software at a price affordable to academic laboratories, research foundations, and small companies.

For further information please contact:

Barry Bunin, PhD
President & CEO
Collaborative Drug Discovery (CDD)
1633 Bayshore Hwy, Suite 342
Burlingame, CA 94010
info(at)collaborativedrug.com

Kiev, Ukraine, August 23 - 27, 2009

ASMC09 in Kiev is being prepared by EFMC (European Federation for Medicinal Chemistry) and ChemBridge Corporation, in the series of events which started with ASCMC04 Moscow followed by ASMC07 St. Petersburg.

Prof. Erick Carreira, ETH Zurich, Switzerland and Dr Scott Biller, Novartis Institutes for BioMedical Research, Cambridge, USA, have kindly accepted to be the Chairmen of the Symposium.

The scientific program of the International Symposium on Advances in Synthetic and Medicinal Chemistry will include:

* 28 invited plenary lectures, presented by highly recognized scientists from academia and the pharmaceutical and biotech industry from Europe, USA and former USSR countries.
* 10 short oral communications which will be selected from submitted abstracts
* poster sessions

The scientific program will be complemented by an attractive cultural program in Kiev.

The topics to be covered during this symposium include:

* New Synthetic Methodologies, Total Synthesis of Natural Products and Heterocyclic Chemistry
* Diversity- and Target-Oriented Synthesis and Chemical Biology
* Medicinal Chemistry and Drug Discovery & Development

The program will also include a commercial exhibition and a half-day Business Mini-Symposium “Small Molecule Screening Libraries in Drug Discovery: Experience and Trends”.

The official language of the symposium is English.

http://www.ldorganisation.com

BERKELEY, Calif.–(BUSINESS WIRE)–Plexxikon Inc. today announced the issuance of key composition-of-matter patents covering novel compounds discovered through the company’s Scaffold-Based Drug Discovery™ platform. Plexxikon’s pipeline of preclinical and clinical stage product opportunities currently span potential treatments for cardio-renal disease, CNS disorders, inflammation, metabolic disease and oncology. Two of the three recently issued patents (U.S. patents no. 7,498,342 and no. 7,504,509) cover compounds derived from the company’s discovery efforts to target protein kinases for the treatment of multiple indications including oncology and inflammation. The third patent (U.S. patent no. 7,476,746) covers novel compounds from the company’s PPAR (peroxisome proliferator-activated receptor) program yielding novel therapeutic opportunities for metabolic disorders and other diseases.

“We are pleased to be adding these additional patents to our growing and broad intellectual property portfolio,” stated K. Peter Hirth, Ph.D., chief executive officer of Plexxikon. “Plexxikon’s novel approach to drug discovery has enabled the company to advance multiple first-in-class drug candidates which are covered by strong intellectual property, and as a result, to secure significant pharmaceutical industry interest in our programs.”

In contrast to fragment-based approaches, Plexxikon’s platform has generated multiple product opportunities by mining the relatively unexplored chemical space of scaffold-like cores and by utilizing co-crystallography early in the discovery process to guide chemical optimization of these scaffolds. Further, the company has developed methods to make highly selective kinase inhibitors as yet rarely seen. Plexxikon has demonstrated the ability to develop selectivity between two targets with as little as one amino acid difference in their catalytic domains. This capability has created the opportunity for the development of new targeted drugs not only for oncology, but also for chronic disease indications outside oncology where safety hurdles are even higher. To date, Plexxikon’s platform has led to the development of a targeted medicine for the treatment of melanoma, a drug candidate for polycystic kidney disease (PKD), an oral agent for rheumatoid arthritis and a broad spectrum oral diabetic therapeutic, all representing novel agents addressing significant unmet needs.

Dr. Prabha Ibrahim Promoted to Vice President of Chemistry

In other news, Prabha N. Ibrahim, Ph.D., was promoted to the position of vice president of chemistry, bringing over 15 years of experience to her position. As head of chemistry since 2002, she has played a key role in building the company’s synthetic and medicinal chemistry capabilities leading to the discovery of Plexxikon’s novel drug candidates now in the clinic and in preclinical development. Prior to Plexxikon, Dr. Ibrahim was a senior scientist at CV Therapeutics, where she was responsible for the identification and development of preclinical candidates for cardiovascular indications. She also previously worked at Amgen, where she played an integral role in small molecule drug discovery for inflammation therapeutics. Dr. Ibrahim earned her Ph.D. at the University of Victoria, Canada, and was a Welch Foundation Fellow at Rice University in Houston.

Plexxikon Profile

Plexxikon is a leader in the structure-guided discovery and development of novel small molecule pharmaceuticals to treat human disease. The company’s clinical stage programs include PLX4032 for the treatment of melanoma and colorectal cancer, PLX5568 for the treatment of PKD and PLX204 for the treatment of diabetes. Among the company’s preclinical development programs, candidates are being developed for the treatment of rheumatoid arthritis, multiple sclerosis and other autoimmune diseases.

Plexxikon’s proprietary Scaffold-Based Drug Discovery™ platform is being applied to build a pipeline of product opportunities in multiple therapeutic areas. This discovery process integrates multiple state-of-the-art technologies, including structural screening as one key component that provides a significant competitive advantage over other drug discovery approaches. To date, the company has discovered a portfolio of clinical and preclinical stage compounds in varied disease areas addressing significant unmet needs in each therapeutic category.

Plexxikon is seeking pharmaceutical and biotechnology partners for select collaboration opportunities. For more information, please visit www.plexxikon.com.

The Salk Institute says it has formed a new stem cell research partnership with Sanofi-Aventis, the international pharmaceutical giant based in Paris. Financial terms of the five-year alliance were not disclosed, and some details of the deal remain to be worked out, Salk spokesman Mauricio Minotta told me this afternoon.

The Sanofi-Aventis regenerative medicine program will sponsor grants in promising research areas, and is intended to provide long-term, multi-participant collaborations between scientists at San Diego-based Salk and Sanofi-Aventis. “It’s meant to be a true collaboration, it’s not just funding,” says Michael White, who oversees the institute’s office of technology management and development. Sanofi-Aventis has about 16,000 employees in the United States, mostly at its U.S. headquarters in Bridgewater, NJ, and about 100,000 employees worldwide.

The program also will provide unrestricted support for the Salk Institute’s stem cell facility, which was created as a separate laboratory supported by private funding during the years the Bush Administration had placed restrictions on federal stem cell funding.

In a statement, Salk president William Brody says there are no preconditions concerning the collaborative alliance. “Our scientists will continue to freely explore cutting-edge research and publish their work,” Brody says. (That’s important to academic freedom, because companies have been known to try to squelch research findings if they don’t support the company’s marketing message.) Under this deal, Salk will also gain access to “extensive resources” at Sanofi-Aventis, which includes a large-scale facility in Tucson, AZ, for screening compounds with potential to be new drugs.

“That’s something that’s very attractive to us, to be able to screen our targets with their drugs,”White says.

Such industry collaborations could be a sign of the times. In January, San Diego’s Burnham Institute for Medical Research announced a multi-year agreement with Johnson & Johnson’s Pharmaceutical Research and Development unit.

Source: xconomy.com

Thermo Fisher Scientific, the world leader in serving science, announced recently that it has introduced a novel tool to accelerate hit-to-lead programmes in the drug discovery process. Its Maybridge Quick2Lead™ Compound Kits are designed to save time and money by enabling rapid compound library synthesis around bioactive “hits” emerging from screening assays. The kits are made up of pre-weighed, diverse building block selections, facilitating rapid capture of structure-activity (SAR) data from the closely related structural analogues within the library.

Quick2Lead Compound Kits are available as five functionality-based kits, with each one containing 48 carefully selected compounds. This enables the exploration of a wide area of chemical space to maximise credible SAR data acquisition for the successful conversion of an initial hit into a genuine, optimisable lead. Since these compounds are all pre-weighed, the kits are ready to use by simply adding solvent and transferring straight to a synthesiser.

The five functional groups available include: carboxylic acids, sulfonyl chlorides, amines, anilines and boronic acids. Each of these different functional groups is applicable to a wide range of tried and trusted parallel synthesis methodologies. Furthermore, although each kit taps into the hugely diverse Maybridge collection, they all include compounds from the top levels of the relevant Topliss Tree, thereby ensuring quality and rigour in interaction testing.

Each of the pre-selected compounds is supplied as 0.1mMol in a 5mL vial. This saves time and money at several levels — minimising stock, avoiding disposal and reducing storage footprint. The pre-selection process also avoids the “dead time” that can be experienced whilst waiting for multiple building blocks from internal and external sources. Maybridge Quick2Lead Kits arrive as a complete library, delivered rapidly ex-stock.

“Our aim with the Maybridge product range is to help shorten the discovery process, from screening to scale-up, and the introduction of our Quick2Lead Compound Kits is the latest addition to our broad product portfolio of pharmacophorically relevant compounds and services,” said Dr. Mick Durrant, Director of Business Development for Maybridge products at Thermo Fisher Scientific. “We recognise that identifying, sourcing and weighing building blocks to feed the library production process around an initial hit can be time consuming and expensive. Our new Quick2Lead Kits offer a novel approach to drive these costs down by providing pre-weighed, diverse building block selections which are simply ready-to-go.”

About Maybridge
Maybridge, part of Thermo Fisher Scientific, is well known for providing highly innovative drug-like molecules and screening compounds for drug discovery and development. With products available for both lab and development scale, they specialise in producing new heterocyclic and phenyl ring-based chemical building blocks, including a unique and expanding range of reactive intermediates.

About Thermo Fisher Scientific
Thermo Fisher Scientific Inc. is the world leader in serving science, enabling our customers to make the world healthier, cleaner and safer. With annual revenues of $10.5B, we have more than 34,000 employees and serve over 350,000 customers within pharmaceutical and biotech companies, hospitals and clinical diagnostic labs, universities, research institutions and government agencies, as well as environmental and industrial process control settings. Serving customers through two premier brands, Thermo Scientific and Fisher Scientific, we help solve analytical challenges from routine testing to complex research and discovery. Thermo Scientific offers customers a complete range of high-end analytical instruments as well as laboratory equipment, software, services, consumables and reagents to enable integrated laboratory workflow solutions. Fisher Scientific provides a complete portfolio of laboratory equipment, chemicals, supplies and services used in healthcare, scientific research, safety and education. Together, we offer the most convenient purchasing options to customers and continuously advance our technologies to accelerate the pace of scientific discovery, enhance value for customers and fuel growth for shareholders and employees alike.

SOURCE: Thermo Scientific Brand Products, Part of Thermo Fisher

A meeting in Colorado, USA has brought together chemists, biologists, pharmacologists, and clinicians in an attempt accelerate the discovery of new drugs for diseases caused by protozoan parasites. These include some of the major infectious diseases of poverty – malaria, leishmaniasis, human African trypanosomiasis and Chagas’ disease.

The organizers of the meeting, “Drug Discovery for Protozoan Parasites” held 22-26 March, point out that recent years have seen the welcome development of public-private research partnerships focused on diseases caused by protozoa – in most cases on malaria. However, these partnerships have mainly been concerned with translational research. As a result, several drugs have been advanced into clinical evaluation but, in the meantime, development of several apparently promising new drugs has not proved successful, “…thus leaving a sparse pipeline of new chemical entities that have potential for registration in the next few years”.

The objectives of the meeting were to discuss current methods to identify and validate new drug targets and to screen libraries of compounds to discover novel chemotypes; assess the potential for chemical biology and medicinal chemistry to optimize compounds that are specific and avoid resistance mechanisms; and identify critical paths for compound progression and to discuss the utility of key models for assessing preclinical drug leads.

Key problems addressed included identification and validation of new targets, chemical biology and medicinal chemistry approaches to characterize new compounds, novel screening techniques to identify new chemotypes, mechanisms of drug resistance, and cutting edge strategies to progress new drug candidates into clinical trials.

Several potentially important findings were reported. To give just one example, oral administration of an amphotericin B formulation, iCo-009, has been shown to have significant efficacy with no evidence of toxicity in mice infected with Leishmania donovani. Manufacturers iCo Therapeutics Inc, claim that “iCo-009 has overcome amphotericin B’s significant physicochemical barriers to absorption and holds promise for the development of a self-administered oral therapy for the treatment of visceral leishmaniasis”.

The meeting was supported by the Bill & Melinda Gates Foundation.

HOPKINTON, Mass., March 19 /PRNewswire-FirstCall/ — Caliper Life Sciences, Inc. (NASDAQ: CALP) , a leading provider of tools and services for drug discovery and life sciences research, today announced that the United States Environmental Protection Agency (EPA) presented initial analyses of Phase I data generated by Caliper Discovery Alliances and Services (CDAS) under the EPA’s ToxCast(TM) screening program at the annual meeting of the Society of Toxicology (SOT) held this week in Baltimore, MD. Separately, the EPA notified Caliper that it has exercised the first additional option year under Caliper’s ToxCast contract with the EPA. Task orders under this contract have already generated approximately $3.5 million in total revenues for Caliper since the initiation of the contract in April, 2007, $1.2 million of which was recognized in 2008.

“We are pleased with the preliminary findings presented by the EPA,” said Kevin Hrusovsky, President and CEO of Caliper Life Sciences. “These results, coupled with the EPA’s third year option exercise, reinforce the likelihood for Phase II efforts to begin at Caliper in the third quarter of this year, which supports our expectation of receiving approximately $3 million of service task orders under this contract in 2009.”

Caliper works with the EPA under its ToxCast initiative to develop new in vitro (laboratory) approaches to identify chemicals that are potentially toxic to the environment. The initial phase of the EPA ToxCast program was aimed at creating a database of in vitro assay data on a broad set of compounds for which in vivo (animal) safety data already existed. Key goals for this phase were to assess overall data quality and establish that the database was predictive of in vivo toxicity profiles. Initial analyses of the data generated at CDAS indicate that the goals for high quality data and potential predictive power have been met. For the 11 replicate controls included in the initial 320 compound set, there was greater than 99% concordance in the screening results across 240 assays tested, and more than 200 correlations between the in vitro results generated at CDAS and in vivo toxicity parameters have already been identified. In addition, 75% of the assays tested showed activity for one or more compounds, reinforcing the need for broad in vitro profiling.

“We believe this data presentation validates the importance of in vitro profiling as a tool for predicting potential toxicity liabilities of compounds and highlights the high quality data generated by Caliper,” said David Manyak, Ph.D., Executive Vice President of Discovery Services at Caliper Life Sciences. “Our access to the entire Phase I ToxCast database makes Caliper an ideal partner for collaborative data mining projects. We also believe that the assay screening panel employed by Caliper for the ToxCast initiative will be broadly applicable for product development programs within the agricultural chemical and pharmaceutical industries.”

The ultimate goal of the ToxCast program is to develop a set of predictive in vitro assays that can supplement or replace in vivo tests currently used for regulatory approval of new environmental chemicals. If successful, the ToxCast initiative will reduce the cost and improve the speed of regulatory approval of new environmental chemicals. More extensive data analysis from the EPA is expected in mid-May of this year.

About Caliper Life Sciences

Caliper Life Sciences is a premier provider of cutting-edge technologies enabling researchers in the life sciences industry to create life-saving and enhancing medicines and diagnostic tests more quickly and efficiently. Caliper is aggressively innovating new technology to bridge the gap between in vitro assays and in vivo results and then translating those results into cures for human disease. Caliper’s portfolio of offerings includes state-of-the-art microfluidics, lab automation & liquid handling, optical imaging technologies, and discovery & development outsourcing solutions. For more information please visit www.caliperLS.com.

SAN DIEGO–(BUSINESS WIRE)–Ligand Pharmaceuticals Incorporated (NASDAQ:LGND - News) and Trevena Inc. today announced the initiation of a joint research and license alliance to screen targets using Trevena’s novel biological platform against Ligand’s combinatorial library of compounds, to identify active compounds with potential for development as novel G-protein coupled receptor (GPCR) therapeutics.

Under the terms of the agreement, Trevena has been granted exclusive worldwide rights to sublicense active compounds resulting from the collaboration. Ligand expects to screen 24 targets over two years and receive payments triggered by a tiered screening paradigm for each target.

“We are delighted to enter into this collaboration that allows us to generate cash flow from the combinatorial chemistry technology we gained through our acquisition of Pharmacopeia,” said John L. Higgins, President and Chief Executive Officer of Ligand. “Working closely with the Trevena team, we hope to rapidly identify and advance novel drug candidates using their unique insight into GPCR signaling pathways.”

Maxine Gowen, President and CEO of Trevena said, “We are excited to work with these exceptional scientists and get access to this proven chemistry platform. We believe that this collaboration will accelerate our drug discovery efforts and the validation of our biological platform.”

About Trevena, Inc.

Trevena, Inc. is a Philadelphia-based drug discovery company focused on developing pharmaceutical products targeting GPCRs. Pharmaceutical products that target GPCRs represent up to 40% of marketed drugs today. Trevena’s drug discovery platform, licensed from Duke University Medical Center, is based on extensive research from the laboratories of scientists Robert J. Lefkowitz, M.D. and Howard A. Rockman, M.D. The company’s drug discovery portfolio is currently focused on programs for cardiovascular and CNS indications. Trevena, Inc. is privately held. (www.trevenainc.com)

About Ligand Pharmaceuticals

Ligand discovers and develops new drugs that address critical unmet medical needs of patients with muscle wasting, frailty, hormone-related diseases, osteoporosis, inflammatory diseases and anemia. Ligand’s proprietary drug discovery and development programs are based on its leadership position in gene transcription technology. In December 2008, we acquired Pharmacopeia in a transaction that provides Ligand rights to numerous collaborations with pharmaceutical companies, pipeline programs and the world’s largest combinatorial chemistry library.

Mechelen, Belgium; 18 November 2008 – Galapagos NV (Euronext: GLPG) announced today new collaboration agreements with Merck Serono, a division of Merck KGaA, Darmstadt, Germany. Total value of the contracts for Galapagos is €1.1 million over one year.

Galapagos’ service division BioFocus DPI will provide SoftFocus© compounds for use in Merck Serono’s drug discovery programs. In a separate agreement, BioFocus DPI will perform medicinal chemistry services on an undisclosed Merck Serono program; this represents an extension of a long running collaboration which was last expanded in 2005.

“BioFocus DPI has a long relationship with Merck Serono in medicinal chemistry, which we are pleased to extend again this year,” said Onno van de Stolpe, CEO of Galapagos. “The purchase of BioFocus DPI’s SoftFocus libraries underscores our ability to grow business with clients.”

About Galapagos and BioFocus DPI

Galapagos (Euronext Brussels: GLPG; Euronext Amsterdam: GLPGA; OTC: GLPYY) is a drug discovery company with pre-clinical programs in bone and joint diseases and bone metastasis. Its BioFocus DPI division offers a full suite of target-to-drug discovery products and services to pharmaceutical and biotech companies, encompassing target discovery and validation, screening and drug discovery through to delivery of pre-clinical candidates. BioFocus DPI also provides adenoviral reagents for rapid identification and validation of novel drug targets, compound libraries for drug screening as well as ADMET database products to select compounds. Galapagos currently employs about 460 people and operates facilities in six countries, with global headquarters in Mechelen, Belgium. More information about Galapagos and BioFocus DPI can be found at www.glpg.com and www.biofocusdpi.com.