Bio Screening Industry News

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.

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

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.

ST. LOUIS, Mo.–(BUSINESS WIRE)–Tripos™, a leading provider of drug discovery informatics products and services, today announced an agreement with the European Molecular Biology Laboratory (EMBL), Europe’s leading research institution for molecular biology, to license Tripos’ Themis™ and Surflex-Dock™ software to support their efforts in Chemical Biology. According to Dr. Joe Lewis, Head of the Chemical Biology Core Facility, a collaboration between EMBL, the DKFZ [German Cancer Research Center, Heidelberg] and the University of Heidelberg to provide the infrastructure and expertise to enable small molecule development to research groups at these institutions. “Anytime we can reduce the amount of time it takes to advance our drug discovery efforts, we are very pleased. Tripos’ Surflex-Dock, and new Themis product have enabled us to do exactly that.”

In a benchmark study at EMBL, Surflex-Dock was installed on EMBL’s Linux Grid of 1,400 CPUs. Five million structures of EMBL’s virtual database of commercially available compounds were then docked into a binding site of a project’s receptor structure. The computation was completed in about two days and yielded a promising pool of candidates for experimental testing.

“Virtual screening has become a key technique in Chemical Biology to identify small molecules as tool compounds to help address biological questions. Our testing of Surflex-Dock’s capabilities in this area convinced us that its high speed and accuracy will enable us to quickly find the most promising compounds,” said Dr. Lewis.

Dr. Lewis added, “In first experiments performed at EMBL, Tripos’ Themis already provided interesting new chemical ideas contributing to new drug discovery projects, so in parallel, the Themis technology will enable us to search vast chemical fragment space, as composed and implemented into the Themis database by our medicinal chemists.”

“The decision by the European Molecular Biology Laboratory to select our new Themis technology together with Surflex-Dock is very significant,” said Jim Hopkins, Tripos’ Chief Executive Officer. He added, “The vigorous EMBL study demonstrated that the powerful combination of these two Tripos offerings can effectively enhance the success of discovery efforts.”

Jaidev had joined a leading Pharmaceutical Research Institute in India, for his Ph.D work. He reviewed his research plan thoroughly and also searched patents. Based on discussions with his guide, he formulated a very innovative research plan, pertaining to development of a new screening method for diabetic compounds. He started his work and after nearly 2 years of hard work, came up with very good data. He filed a patent in India and subsequently in the USA. He was confident of grant of patent, since nobody had done the work he had done.

The examination of his patent application started in the USA. He was shocked when his application in the USA was objected owing to a provisional patent filed by a researcher in USA. The provisional application filed by the USA researcher merely discussed theoritically an innovative research plan, very similar to the one proposed by Jaidev. However, there was no follow up after that and the researcher had abandoned the patent application. Mere theoritical discussion on the idea was there, without any data. However, it had been duly published and was in public domain. The US examiner objections were based on the observation, that Jaidev’s idea was not new- it had already been disclosed by someone else. Novelty was destroyed and Jaidev could not get a patent.

Discussion:

The case gives very important lessons for researchers:

1. Don’t wait for research work to be completed before filing a patent- even at initial stage or just when preliminary encouraging results give proof to an innovative concept, file a provisional patent application in India. It is quite cheap- govt. fee is just Rs.1000/- and in case you do it yourself, no further expense. But it protects your idea! After filing, within 12 months, you must file complete patent application, duly accompanied by data and including ‘claims’. In provisional, claims are not there.

2. Filing a provisional patent application can be done for a mere theoritical idea, with due discussion on the scientific and technical logic behind the concept. However, your filing date and hence PRIORITY gets protected from date of filing provisional.

Had Jaidev filed a provisionl application, well in time he might have been able to save his work. It was something very easy and simple, but because he was not aware, he waited to finish his work and lost the race to someone who was smart enough to file a provisional patent. However, the irony in this case is that even the US inventor did not get a patent, since he had not filed a complete patent application within one year. Maybe, he did not get success with experiments or some other problem. Jaidev did succeed in the Lab, but lost the patenting case, since his novelty had been destroyed by the US inventor.

Hence, do not underestimate the VALUE OF PATENTING YOUR IDEAS- THEY ARE PRECIOUS! FILE PROVISIONAL APPLICATIONS AT THE EARLIEST. DO NOT WAIT FOR YOUR RESEARCH TO FINISH.

San Diego, CA (OBBeC) – Researchers at the University of California, San Diego, developed a unique computational approach to identify key compounds that could lead to new drugs to combat African sleeping sickness — a disease spread by the biting tsetse fly and caused by the parasite Trypanosoma brucei.

WuXi PharmaTech (NYSE: WX) has signed a new three-year CRO deal with Pfizer (NYSE: PFE) to collaborate on in vitro ADME (Absorption, Distribution, Metabolism and Excretion) services. Although WuXi has already been providing the services to Pfizer, WuXi said the new agreement “strengthens an already productive relationship.” WuXi also provides Pfizer with synthetic chemistry, parallel medicinal chemistry (PMC), and bioanalytical services.

In partnership with Pfizer, WuXi PharmaTech will establish ADME assays to provide in vitro screening services on compounds WuXi PharmaTech synthesizes for Pfizer. The goal is to improve the pharmacokinetic properties of new compounds.

The announcement did not disclose financial details of the contract.

TimTec LLC., the international distributor of synthetic organic and natural compounds, and Collaborative Drug Discovery, Inc. (CDD), the community based research information management enterprise, announced today that the CDD web-based software now hosts TimTec’s Natural Product Library and Natural Derivatives Library. The TimTec natural product and derivative compounds are now available as a structure searchable database in the CDD Web2.0 collaborative research information system.

The CDD-TimTec Natural Products Library (NPL-480) and Natural Derivatives Library (NDL-3000) databases comprise almost 3,500 compounds available from TimTec. NPL-480 is a new library of 480 natural compounds composed of pure natural products as lead identifying materials. NDL-3000 elaborates on structural variety of pure natural compounds and includes synthetic compounds and synthetically modified pure natural compounds including, but not limited to, alkaloids, natural phenols, nucleoside analogs, carbohydrates, purines, pyrimidines, flavonoids, steroidal compounds and natural amino acids.

“The growing number of research institutions world-wide now investigating natural products will buoy the discovery of novel chemistry leading to a wealth of therapeutic breakthroughs,” said Dr. Barry Bunin, President of Collaborative Drug Discovery. “It’s natural that TimTec’s laboratories complement CDD’s academic partners in natural products research with a unique commercial source of natural products and diverse derivatives.”

“Beyond our successful compounds libraries, chemical software and drug discovery services, TimTec immediately appreciates the unique advantage and elegance of the CDD system to share our natural product compounds with the growing CDD community,” said Dr. Murat Niyazymbetov founder and President of TimTec.

The TimTec databases join 14 other publicly available data sources in the CDD system with chemical and biological data for over 42,000 agents including:

* 1,700 FDA approved drugs with indications and sponsors
* Over 15,000 compounds with Malaria assay data from 5 public data sources
* More than 850 compounds with Tuberculosis antibacterial activity information
* Over 47,000 Ki values against 699 GPCR targets from the NIMH Psychoactive Drug Screening Program (PDSP) Database
* 25,000 plus compounds available for purchase

About TimTec LLC.
TimTec LLC. - http://www.timtec.net - is a privately held company located in Newark Delaware, 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 further information please contact:

Barry Bunin, Ph.D.
President & CEO
Collaborative Drug Discovery (CDD)
1818 Gilbreth Road, Suite 220
Burlingame, CA 94010
650-204-3084
info(at)collaborativedrug.com

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

September 4th, 2008 - Tocris Bioscience announced today the signing of an exclusive deal with AstraZeneca to supply Gefitinib (also known as Iressa  and ZD1839) to preclinical researchers working on the mechanisms underlying cancer development. For the first time, scientists will be able to buy authentic, fully licensed, non-formulated Gefitinib as an off-the shelf product for use in biological research.

In recent years pharmaceutical companies have developed a number of small molecule drugs that are clinically effective against certain types of cancer. Tyrosine kinase inhibitors (TKIs) such as Gefitinib are at the forefront of this new generation of targeted anticancer agents.

Gefitinib is an EGFR-TKI (epidermal growth factor tyrosine kinase inhibitor), which targets and blocks the activity of the EGFR-TK, an enzyme that regulates intracellular signalling pathways implicated in cancer cell proliferation and survival. Growth factor signalling has been identified as a key driver of tumour growth and spread in a wide range of cancers. For clinical use, Gefitinib has been approved for the treatment of advanced Non Small Cell Lung Cancer (NSCLC) in 36 countries.

This molecule has been licensed to Tocris for use as a preclinical research compound only. Strict conditions have been imposed by AstraZeneca to ensure that it is not used in human studies.

Duncan Crawford, Tocris’ Chief Scientific Officer, said, “We know that there is a great deal of interest in Gefitinib from the global research community. By making fully licensed Gefitinib available through our catalogue, we hope to promote new and exciting research in the fundamental processes that drive cancer development. For Tocris this important new product perfectly compliments our comprehensive and expanding range of high purity compounds, which are in use worldwide to further biomedical research. We are delighted that our excellent relationship with AstraZeneca has allowed us to make this compound available to scientists working on the fundamental mechanisms of cancer cell biology”

About Tocris Bioscience
Tocris Bioscience is a leading supplier of high performance chemicals, peptides and antibodies, with customers in virtually all of the world’s major pharmaceutical companies, universities and research institutes. The Company is committed to making new life science discoveries possible by providing the highest performing and most innovative range of research reagents.

Tocris Bioscience products are used by scientists carrying out non-clinical research in fields such as cancer, stroke, Alzheimer’s disease and obesity. The Company’s product range of over 2,000 reagents represents a unique collection of novel, exclusive and licensed research tools. A major source of key signal transduction reagents and arguably the world leader in the supply of neuroscience reagents, the Company won the Queen’s Award for Enterprise (International Business) in 2002.

Tocris Bioscience is the trading name for the companies in the Tocris Cookson Group. Formed from the 1994 merger of Tocris Neuramin and Cookson Chemicals, Tocris Cookson Ltd is privately held and headquartered in Bristol, UK. Its US subsidiary, Tocris Cookson Inc, is located in St. Louis, Missouri, USA. There are approximately 50 employees in the Group worldwide, operating out of two sites in the UK and one in the US.

About AstraZeneca
AstraZeneca is a major international healthcare business engaged in the research, development, manufacturing and marketing of meaningful prescription medicines and supplier for healthcare services. AstraZeneca is one of the world’s leading pharmaceutical companies with healthcare sales of $29.55 billion and is a leader in gastrointestinal, cardiovascular, neuroscience, respiratory, oncology and infectious disease medicines. For more information about AstraZeneca, please visit: www.astrazeneca.com