Archive for the ‘Drug-Like Compounds’ Category
TimTec Launches Division of Organic Synthesis and Medicinal Chemistry Contract Research Services
Last Updated on Saturday, 24 July 2010 04:31 Written by admin Thursday, 8 July 2010 11:39
Newark, DE, July 8, 2010 Press Release – TimTec, LLC is pleased to announce the launching of the new Division that manages Organic Synthesis and Medicinal Chemistry Contract Research Services. The emergence of the division is an evolutionarily progression for TimTecs business development. The company has been known for its expertise in organic chemistry design and supply for drug discovery for 15 years. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.
The Head of Contract Research Services, J. C. Pelletier, PhD., has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist and project Team Leader at large companies and smaller, start-up operations. The TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities. TimTec specialists are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges.
TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. Contract research services include, but are not limited to, flexible contracts, program management, structure-activity relationship evaluation, lead optimization, property optimization for ADME and PK, metabolite synthesis, enabling technologies (parallel synthesis, multistep synthesis, analytical chemistry), mg to kg synthesis capacity, compound distribution, and patent application preparation assistance. The Contract Research Division puts great emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of clients knowledge resources and interests. Dedication to service is matched by exceptionally competitive prices.
Contact Information:
TimTec LLC
Harmony Business Park A-301
Newark DE 19711
Tel 302 292 8500
Fax 302 292 8520
info@timtec.net
http://www.timtec.net/contract-research-services.html
About TimTec
TimTec LLC 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 and collections, 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. International customers include major pharmaceutical, biotech, agricultural, and educational companies and institutions, which use TimTec products for research and development programs.
TimTec’s Contract Research Services
Last Updated on Thursday, 8 July 2010 10:18 Written by Editor Thursday, 8 July 2010 03:22
High Quality Organic Synthesis and Medicinal Chemistry Contract Research Services at an Outstanding Value
TimTec brings 15 years of expertise in organic chemistry design and supply for drug discovery closer to your supplemental bench-top requirements by launching The Organic Synthesis and Medicinal Chemistry Contract Research Services Division. TimTec scientists have a proven track record of providing high quality services and showing outstanding integrity to their clients.
TimTec remains flexible in delivering practical chemistry solutions molded to custom research requirements and budgets. All Contract Research Services are delivered with an emphasis on speed, real-time feedback, ongoing communication, superior compound quality, and the protection of our clients’ knowledge resources and interests. We are dedicated to providing these services at exceptionally competitive prices.
The Head of Contract Research Services has over 20 years of research experience in the US pharmaceutical industry as a hands-on medicinal chemist and project Team Leader at large companies and smaller, start-up operations. We are keenly aware of all the intricate details and chemistry challenges that go into bench-top research before a qualified lead molecule emerges. Your TimTec contract research team consists of experienced, bench level scientists who have access to state of the art synthesis, analytical and quality control facilities.
TimTec Contract Research Services Start with:
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Flexible Contracts
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Program Management
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State of the Art Facilities
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Structure-Activity Relationship Evaluation
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Lead Optimization
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Property Optimization for ADME and PK
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Metabolite Synthesis
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Enabling Technologies – Parallel synthesis, multistep synthesis, analytical chemistry
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Mg to Kg Capacity
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Compound Distribution – Solid or solution, vials or plates
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Patent Application Preparation Assistance
Supplemental Services and Products:
Custom Synthesis
Compound Acquisition
Weighting and Plating
HTS compounds and compound collections – ActiMol Line of products
Posted under ADMET Studies, Drug-Like Compounds, Medicinal Chemistry, New Products, North America, R & D, Research Projects | No Comments
Cellular Dynamics Announces Commercial Launch of iCell(TM) Cardiomyocytes for Drug Candidate Toxicity Screening
Last Updated on Wednesday, 5 May 2010 10:36 Written by Editor Wednesday, 5 May 2010 10:36
Human iCell Cardiomyocytes Provide Alternative to Non-human, Tumor-derived, and Cadaveric Cellular Model Systems to Better Predict Cardiac Toxicity
MADISON, Wis., Dec. 16 /PRNewswire/ — Cellular Dynamics International (CDI) today announced the commercial launch of iCell(TM) Cardiomyocytes for use in testing of new drug candidates by the pharmaceutical industry. These human heart cells are designed to aid drug discovery and improve the predictability of drug compound efficacy and toxicity screens, weeding out ineffective and potentially toxic compounds early in the pharmaceutical pipeline process before significant time and resources have been invested.
iCell Cardiomyocytes are derived from induced pluripotent stem (iPS) cells, spontaneously beat in vitro and exhibit the electrophysiological and biochemical properties of normal human heart cells. Thus, iCell Cardiomyocytes provide significant advances over non-human cell models, which may exhibit a different response than human tissue; tumor-derived cell models, which are genetically different than normal cells; and cadaveric cells, which exhibit batch-to-batch variability, de-differentiate under in vitro conditions, and exhibit non-cardiomyocyte behaviour.
iCell Cardiomyocytes are the first product ever developed from iPS cells, discovered by CDI senior research fellow Junying Yu, Ph.D., then a postdoctoral research associate in the University of Wisconsin-Madison laboratory of James Thomson, V.M.D., Ph.D., in 2007. iCell Cardiomyocytes are produced in-house by CDI from a master cell bank of iPS cells expanded from a single clonal population reprogrammed from fully mature human cells using Dr. Thomson’s patented technology. Based on strong intellectual property and exclusively licensed patents from several universities, CDI has developed a proprietary process to industrialize iCell Cardiomyocytes production so that the cardiomyocytes are manufactured at the high quantity, quality and purity required by pharmaceutical companies. CDI has successfully engaged in pre-launch validation testing with several pharmaceutical customers.
“Drug toxicity testing is an important part of early-stage drug development, said Chris Parker, chief commercial officer of CDI. “The problem our pharmaceutical customers face today is that current cell models to test drugs are inadequate, because they are either non-human, cadaveric, or tumor-derived cells. They miss toxicities that might have manifested themselves in a human cell model. With the launch of iCell Cardiomyocytes, we hope to improve the efficiency and effectiveness of preclinical research studies, so that our pharmaceutical customers are more assured of the safety and efficacy of their drug candidates and a better return on their research investment.”
Robert Palay, chief executive officer of CDI, continued, “Launching iCell Cardiomyocytes to the pharmaceutical industry is an important step for Cellular Dynamics. We have shown that we can manufacture and provide validated human iPS cell-derived terminally differentiated cardiomyocytes in the quantity and quality needed by our customers. We look forward to growing this product with our pharmaceutical customers and developing line extensions of iCell Cardiomyocytes, including panels with multiple iPS starting materials, as well as launching other iPS cell-derived iCell products.”
James Thomson, chief scientific officer of CDI, said, “Rapid application of stem cell technology has been a goal both of my laboratory at the University of Wisconsin and CDI. Utilizing human iPS cells for new drug toxicity testing should improve the drug discovery process in a timeframe that has an effect on human healthcare now, not 10 years from now. Ultimately applications of stem cell technology in drug discovery will provide great utility and enable movement toward a long-term goal of cellular-based therapeutics and personalized medicine.”
About Cellular Dynamics International, Inc.
Cellular Dynamics International, Inc. (CDI) is a leading developer of next-generation stem cell technologies for drug development and personalized medicine applications. CDI harnesses the power of pluripotent stem cells and their ability to differentiate into any cell type for world-class drug development tools. In addition, it is the leader in iPS technology, the production of pluripotent stem cell lines from adult tissue. CDI was founded in 2004 by James Thomson, a pioneer in human embryonic stem cell research at the University of Wisconsin-Madison, and Tactics II Ventures, a Wisconsin-based venture capital fund. CDI’s facilities are located in Madison, Wisconsin. See www.cellulardynamics.com.
SOURCE Cellular Dynamics International (CDI)
Posted under Drug Development, Drug-Like Compounds, Press Releases | No Comments
Alzheimer’s Research Provides Potential Treatment for UTI
Last Updated on Monday, 11 January 2010 06:05 Written by Editor Monday, 11 January 2010 06:05
One element links the disparate areas of research: amyloids, which are fibrous, sticky protein aggregates. Some infectious bacteria use amyloids to attach to host cells and to build biofilms, which are bacterial communities bound together in a film that helps resist antibiotics and immune attacks.
Amyloids also form in the nervous system in Alzheimer’s disease, Parkinson’s disease and many other neurodegenerative disorders.
To probe amyloids’ contributions to neurodegenerative diseases, scientists altered potential UTI-fighting compounds originally selected for their ability to block bacteria’s ability to make amyloids and form biofilms. But when they brought the compounds back to UTI research after the neurology studies, they found the changes had also unexpectedly made them more effective UTI treatments.
“Thanks to this research, we have evidence for the first time that we may be able to use a single compound to impair both the bacteria’s ability to start infections and their ability to defend themselves in biofilms,” said senior author Scott J. Hultgren, Ph.D., the Helen L. Stoever Professor of Molecular Microbiology at Washington University.
The findings were reported online in Nature Chemical Biology.
The National Institutes of Health has estimated that over 80 percent of microbial infections are caused by bacteria growing in a biofilm, according to Hultgren. Scientists in Hultgren’s laboratory have worked for decades to understand the links between biofilms and UTIs.
“UTIs occur mainly in women and cause around $1.6 billion in medical expenses every year in the United States,” said co-lead author Jerome S. Pinkner, laboratory manager for Hultgren.
“We think it’s likely that women who are troubled by recurrent bouts of UTIs are actually being plagued by a single persistent infection that hides in biofilms to elude treatment,” Pinkner added.
Co-lead author Matthew R. Chapman, Ph.D., now associate professor of molecular, cellular and developmental biology at the University of Michigan, was a postdoctoral fellow in Hultgren’s lab in 2002 when he discovered that the same bacterium that causes most UTIs, Escherichia coli, deliberately makes amyloids. The amyloids go into fibers known as curli that are extruded by the bacteria to strengthen the structures of biofilms.
To treat UTIs, Hultgren’s lab has been working with Fredrik Almqvist, Ph.D., a chemist at the University of Umea in Sweden, to develop compounds that block bacteria’s ability to make curli, disrupting their ability to make biofilms and leaving them more vulnerable to antibiotics or immune system attacks.
Almqvist recently suggested altering a group of the most promising curli-blockers to see if they could also block the processes that form amyloids in Alzheimer’s disease.
The alterations worked: In laboratory tests, the new compounds prevented the protein fragment known as amyloid beta from aggregating into amyloid plaques like those found in the brain in Alzheimer’s disease.
When scientists took the new compounds back to a mouse model of UTIs, though, they received a surprise. The altered compounds were better at reducing the virulence of infections, inhibiting not only curli formation but also the formation of a second type of bacterial fibers, the pili.
“Pili aren’t made of amyloids, but they are essential to both biofilms and to the bacteria’s ability to initiate an infection,” Hultgren said.
Hultgren and colleagues are already developing even more potent infection and amyloid fighters, screening a library of thousands of chemicals similar to the most promising compounds from the study.
Chapman cautions that it’s too early to tell which, if any, of the compounds will be helpful in treating neurodegenerative diseases.
“Much neurodegenerative drug development has focused on ways to break up amyloids or prevent them from forming, but because amyloids may also be an important part of normal cellular physiology, we need to identify molecules that will target only the toxic amyloid state,” he said.
Source: farsnews.com
Posted under Compound Screening, Drug Development, Drug-Like Compounds, Press Releases | No Comments
Families of Spinal Muscular Atrophy Funded Program Shows Quinazoline Compounds Give Survival Benefit in a Severe Mouse Model of SMA.
Last Updated on Monday, 28 December 2009 12:06 Written by Editor Monday, 28 December 2009 12:06
This publication, showing data from the testing of Quinazoline derivatives in a Spinal Muscular Atrophy mouse model, has been published in Human Molecular Genetics by lead author Dr. Matthew Butchbach from the laboratory of Dr. Arthur Burghes at the Ohio State University.
The generation of the Quinazoline compounds as a therapeutic drug candidate for Spinal Muscular Atrophy was fully funded by Families of SMA.
The paper explores whether the Quinazoline compounds, which increase the expression of SMN2, are useful as potential therapeutics for SMA. Ultrahigh-throughput screening identified substituted Quinazolines as potent SMN2 inducers. The drug-like properties of the initial screening hits were optimized through directed medicinal chemistry. This resulted in series of C5-Quinazoline derivatives.
Oral administration of three of these compounds (D152344, D153249 and D156844) to neonatal mice resulted in a dose-dependent increase in Smn promoter activity in the central nervous system.  The authors then examined the effect of these compounds on the progression of disease in SMNDelta7 SMA mice. Oral administration of D156844 significantly increased the mean lifespan of SMNDelta7 SMA mice by approximately 21-30% when given prior to motor neuron loss. Overall the authors summarize that the quinazoline derivative D156844 increases SMN expression in neonatal mouse neural tissues, delays motor neuron loss at PND11, and ameliorates the motor phenotype of SMNDelta7 SMA mice.
“This is the first compound series to go from hit-to-preclinical candidate that shows favorable pharmacology in the nervous system and shows benefit to severe SMA mice. This study shows that promising therapies for SMA can be developedâ€, said Matthew Butchbach, Ph.D., who is lead author on this publication.
“Families of SMA is pleased that the first test of this class of compounds in SMA mice shows potential therapeutic benefit. The clinical lead in this series called Quinazoline495, which is a more optimized compound than those tested here, has also been assessed in this animal model with similar results, as well as tested in a slightly less severe mouse model of SMA, in which it showed marked enhancement of survival”, says Jill Jarecki, Ph.D., FSMA research director.
The lead compound Quinazoline495 recently received orphan drug designation from the FDA for the treatment of spinal muscular atrophy. Please click here to read more.
Families of SMA recently licensed this series of compounds to Repligen Corporation for development as a drug treatment for Spinal Muscular Atrophy.
The full reference:
Butchbach ME, Singh J, Thornorsteinsdóttir M, Saieva L, Slominski E, Thurmond J, Andrésson T, Zhang J, Edwards JD, Simard LR, Pellizzoni L, Jarecki J, Burghes AH, Gurney ME. Effects of 2,4-diaminoquinazoline derivatives on SMN expression and phenotype in a mouse model for spinal muscular atrophy. (2009). Human Molecular Genetics, Epub ahead of print.
Source: fsma.org
Posted under Compound Screening, Drug-Like Compounds, Press Releases | No Comments
Tapeworm Drug May Hold Promise For Colon Cancer, Future Research
Last Updated on Tuesday, 15 December 2009 03:22 Written by Editor Tuesday, 15 December 2009 03:22
The findings about this compound, published in the Nov. 3 issue of Biochemistry journal, might prove valuable to patients and clinicians, who may benefit if there is a demonstrated boost to chemotherapy. Researchers also can use the compound to manipulate the receptor to learn more about a common cell replenishing pathway, called the Wnt pathway, which requires the receptor for normal activities and can go wrong in cancer cases.
The researchers had a choice: to screen libraries of several hundred thousand biochemical compounds or to use a library of about 1,200 FDA approved or biologically active compounds.
“We decided to take the less expensive route of screening FDA approved drugs, and fortunately, we found 26 compounds that seemed to meet our goal, but only one that truly worked with the Frizzled receptor,â€said Wei Chen, Ph.D., Assistant Professor of the Department of Medicine at Duke. “The goal was to drive the Frizzled 1 receptor from the outer membrane to the inside of the cell,†which effectively inactivated the receptor.
The effective compound, niclosamide, is currently approved for use against tapeworm infection. But some colon cancer patients, for example, have a Wnt pathway that is overactivated and may benefit from the “quieting†effects of niclosamide, which blocks the receptor in the Wnt pathway.
“The paper provides a rationale for clinicians to investigate using niclosamide for a new purpose,†Dr. Chen said. “Based on our findings, one oncologist at Duke is writing protocols for a phase 1 (safety) clinical trial to treat colon cancer patients with the intention of bringing our laboratory findings to the patient’s bedside.â€
Chen says he is proud of the work, which is “truly translational science.â€
“I am a basic scientist working with cell receptors, we have a medicinal chemist in our laboratory and one of our collaborators is Dr. H. Kim Lyerly, a professor of surgery, who is a researcher in gene- and immune-based therapies for cancer, as well as director of the Duke Comprehensive Cancer Center,†said Chen. “This type of diverse collaboration lets me shepherd a finding more rapidly from the laboratory to the clinic.â€
Provided by Duke University Medical Center
physorg.com
Zelinsky Institute Inc. announced collaboration with ART-CHEM
Last Updated on Saturday, 10 October 2009 06:10 Written by admin Saturday, 10 October 2009 06:10
Zelinsky Institute Inc. (Newark, DE, August 2009) – Zelinsky Institute Inc. expands its partnership and supplier network with the announcement of collaboration with one of the premier fine chemistry companies – ART-CHEM, which originated from Moscow, Russia, and has started its operations in Berlin, Germany, in 2005. ART-CHEM specializes in synthesis of highly diverse and rich in unique scaffolds HTS compounds and building blocks. The entire line of ART-CHEM product offerings is going to be available via Zelinsky Institute Inc., which is headquartered in and currently operates from Delaware, USA, offices.
ART-CHEM founder, Dr. B. Ugrak, comments, “We are pleased to become a part of Zelinsky Institute, a recognized supplier of specialty chemicals. Together we can provide greater value serving our, now, joined customer base.†Zelinsky Institute CEO, Dr. M. Niazoff, agrees adding, “We are happy to have ART-CHEM high quality fine chemistry products and service capabilities accessible via Zelinsky Institute. Together, we are looking forward to growing our market fueled by ever-evolving research demands.â€
Collaboration aims at making ART-CHEM products and services known and easily accessible for existing and prospective Zelinsky Institute Inc. customers worldwide. September 2009 product databases distributed by Zelinsky Institute Inc. are going to include ART-CHEM’s drug-like and chemically diverse compounds for screening, building blocks, and intermediates. Zelinsky Institute Inc. is going to coordinate procurement, orders, and consolidated delivery of HTS products. Zelinsky Institute Inc. and ART-CHEM collaboration is open to custom projects going beyond the supply of just existing fine organic chemistry. For recently launched databases, products and services, inquiries, orders, and customized solutions please contact \n info@zelinsky.com This e-mail address is being protected from spambots. You need JavaScript enabled to view it .
Zelinsky Institute Inc., located in Delaware, USA, is the official representative of Zelinsky Institute of Organic Chemistry of the Russian Academy of Sciences (ZIOC) in Moscow, Russia. ZIOC is one of the world’s largest scientific centers in the fields of organic chemistry, organic catalysis, and chemistry of biologically active compounds. The Institute was founded on February 23, 1934, following the Decision of the Presidium of the Academy of Sciences of the USSR.
Zelinsky Institute Inc. began its operations in the USA in 1993 to establish the first commercialization bridge in compound supply industry linking Former USSR research centers unique chemistries and R&D service capabilities with Western life-science industries demands. Among Zelinsky Institute Inc. first customers were DuPont, Merck, Johnson&Johnson, and Ely Lilly. Â Zelinsky Institute Inc. has expanded its markets and partnerships and welcomes new global customers and scientific challenges.
Contacts:
ART-CHEM GmbH
Campus Berlin-Buch, Haus B55
Robert-Roessle-Strasse 10
13125 Berlin, Germany
Phone: +49 (0)30 9489-2180
Fax:Â Â Â Â Â +49 (0)30 9489-2181
Zelinsky Institute Inc.
POB 8941, Newark, DE, 19714 USA
For products and services, inquiries, orders, and customized solutions please visit:
Sirona Biochem Says SGLT Test Results Confirm Key ‘Breakthrough’
Last Updated on Friday, 9 October 2009 12:02 Written by Editor Friday, 9 October 2009 12:02
Sirona Biochem Corp. (TSX-V: SBM), an emerging biotech company focused on diabetes and obesity, says results of testing its unique SGLT inhibitor molecules demonstrate a key breakthrough milestone for Sirona Biochem.
Sirona Biochem CEO, Dr. Howard Verrico, said, “There are two vital steps in the early stage of drug testing: validation of concept i.e. a molecule is able to hit the desired target and secondly its in vivo effectiveness. This first round of testing has shown a key breakthrough milestone in the process of validating this concept.”
“The test results now mean we can proceed to find out whether the molecules are selective, safe and robust enough to have potential to be effective when they reach the parts of the body where the re-uptake of glucose needs to be limited.”
Dr. Bertrand Plouvier, Chief Scientist, said, “The results from the first round of screening are indeed very encouraging and Sirona Biochem will use the next following months to further study the molecules through specific assays to demonstrate their effectiveness and drug likeness.”
Dr. Verrico said management of sugar metabolism is a primary medical challenge associated with treating diabetes and obesity and that is why SGLT inhibitors show such promise in this regard. “At present SGLT2 inhibitors have demonstrated their ability to limit the re-uptake of glucose back into the blood stream from urine. However, they have been notoriously lacking in ability to resist being rapidly metabolized by the body, thus rendering them largely ineffective.
“What we have now done is show that our molecules, with their unique GlycoMim® technology, can inhibit the glucose transporter SGLT2. The next challenge, and an exciting one, is to show that our molecules are selective, safe and have the potential to have an increased efficacy compared to the current molecules undergoing clinical development.”
Sirona Biochem owns the worldwide product rights to a library of unique sodium glucose transporter (SGLT) inhibitors to treat diabetes and obesity. SGLT inhibitors, as previously stated, block the re-uptake of excess sugars from urine, which can then reduce high blood sugar towards normal levels.
Sirona Biochem has entered into a strategic partnership with TFChem, a drug discovery company based in Rouen, France. TFChem licenses its technology of fluorinated carbohydrate mimics: GlycoMim®, and products in development to biotech companies. This strategic partnership was completed by a detailed research and licence agreement signed on September 29, 2008.
23.6 million people, or 7.8% of the population of the United States, have diabetes. (February 2009 DACG.ORG)
Market Trends
In 2007, the prevention and treatment of diabetes and its complications was estimated to cost US$ 232 billion according to the International Diabetes Federation. By 2025, this is likely to increase to more than US$ 302.5 billion.
The diabetes drug market reached US$18 billion in 2005, and is expected to increase to $21-25 billion in 2011. With many new products yet to realise their full potential and the high incidence of T2DM expected in emerging markets, prospects for the sector look strong. Some of the fastest growing markets for diabetes are in emerging economies. India, China and Indonesia are in the top 5 for disease prevalence. The impact for both branded and generic drugs is considerable.
Furthermore, in recent years, obesity has become a major health problem for many post-industrial societies, so much so that in 2004, the United States Health and Human Services declared obesity to be a disease. The World Health Organization (WHO) projects that globally in 2005, 1.6 billion adults were overweight with at least 400 million adults obese. By 2015, approximately 2.3 billion adults will be overweight and 700 million will be obese. Obesity poses a major health risk because it greatly increases the risk of co-morbidities such as diabetes, cardiovascular diseases, arthritis, and cancer. Recognizing the potential for a new blockbuster market, major pharmaceutical companies have increasingly focused on obesity and its causes and, in the process, seeking to identify many potential targets and pathways that could be exploited to create novel therapies.
Sirona Biochem’s website is at: www.sironabiochem.com where we feature the most recent information about the company and its activities. Alternatively, investors are able to e-mail all questions and correspondence to info@sironabiochem.com where they can also request to be added to the investor e-mail list to receive all future press releases and updates or call John Dougherty, Corporate Development at 604-641-4466.
About Sirona Biochem
Sirona Biochem Corp. (TSX-V: SBM) is an emerging biotech company dedicated to the discovery and development of novel drug compounds. The current focus is on treatments for Type II diabetes and obesity. Sirona has entered into a license agreement with TFChem S.A.R.L., a drug discovery company based in Rouen, France. TFChem licenses its technology of fluorinated carbohydrate mimics: GlycoMim®, and products in development to biotech companies. The license agreement with TFChem provides for research and development of new compounds known as SGLT Inhibitors. SGLT inhibitors are a new and exciting class of compounds that have great promise and potential to treat both diabetes and obesity.
Mark Senner President and Director
Neither the TSX Venture Exchange nor its Regulation Services Provider (as that term is defined in the policies of the TSX Venture Exchange) accepts responsibility for the adequacy or accuracy of this release.
950-789 west pender street
vancouver, b.c., v6c 1h2
Direct: 604-641-4466
Fax: 604-608-5471
info@sironabiochem.com
Source: Marketwire
Agilux Laboratories Hires New Associate Director to Lead In Vitro ADMET Services Division
Last Updated on Thursday, 8 October 2009 12:22 Written by Editor Thursday, 8 October 2009 12:22
- Adrian Sheldon, Ph.D., Positions Contract Research Organization for Growth - WORCESTER, Mass.--(Business Wire)-- Agilux Laboratories, Inc., a Contract Research Organization (CRO) that provides bioanalytical and in vitro Absorption Distribution Metabolism Excretion Toxicology (ADMET) services for the biotechnology and pharmaceutical industries, has appointed Dr. Adrian Sheldon as associate director of In Vitro ADMET Services. In this role, Dr. Sheldon will build the In Vitro ADMET Services division offering testing services that allow biotechnology and pharmaceutical companies to screen drug candidates for desirable ADMET properties. Dr. Sheldon will leverage more than 17 years of industry experience, including establishing new business units for In Vitro ADMET and Immunochemistry within an established CRO. He will extend Agilux`s emphasis on customer service, rapid turnaround and exceptional data quality to the company`s newly formed In Vitro ADMET Services Testing Division. "We are excited to have someone with Adrian`s expertise, successful track record and demonstrated abilities at Agilux," said Jim Jersey, president and CEO at Agilux. "Adrian brings the right balance of scientific expertise and customer focus, which is consistent with Agilux`s mission of delivering high quality data at unprecedented speeds. We are confident that both the Agilux team and our clients will benefit from his unique skill set." Prior to Agilux, Dr. Sheldon served as associate director of In Vitro ADMET at Charles River Laboratories. Prior to Charles River Laboratories, Dr. Sheldon was group leader in Assay Development/HTS/In Vitro ADMET at ArQule where he co-managed a team responsible for screening compounds generated by the industry-leading combinatorial chemistry laboratory. He received his Ph.D. from Boston University and his A.B. from Harvard University. Dr. Sheldon has authored numerous scientific publications and holds two patents. "I am very pleased about joining the team at Agilux," stated Dr. Sheldon. "We have an incredible opportunity to change the way early stage development services are delivered and I am confident that I will be able to contribute to Agilux`s continuing success." About Agilux Laboratories, Inc. Agilux Laboratories, Inc. is a privately held contract research organization (CRO) focused on bioanlaytical and PK/PD testing services for the biotech and pharmaceutical industries. Leveraging industry and contract research experience of its management team, the company delivers high quality bioanlaytical chemistry and PK/PD data more rapidly. Agilux helps clients make better decisions during drug discovery and development by providing quality data earlier in the research process by using technologies and systems that increase turnaround speed well beyond industry standards. Founded in 2007 by industry experts Jim Jersey, Steve Guyan and Peter Glick, Agilux is headquartered in Worcester, MA and is funded by private equity firm, Ampersand Ventures. For more information, call 508-753-5000 or email sguyan@agiliuxlabs.com. Online at www.agiluxlabs.com. Agilux Laboratories, Inc. Steve Guyan Vice President, Sales and Marketing 508-762-4402 sguyan@agiluxlabs.com
Source: Reuters
Evotec Announces Research Agreement With Biogen Idec
Last Updated on Thursday, 8 October 2009 12:14 Written by Editor Thursday, 8 October 2009 12:14
HAMBURG, Germany and OXFORD, UK, Sept. 9, 2009 (GLOBE NEWSWIRE) -- Evotec AG (Frankfurt:EVT) (Nasdaq:EVTC), a leading provider in the discovery and development of novel small molecule drugs, today announced that it has entered into a research agreement with Biogen Idec (Nasdaq:BIIB), a leading biopharmaceutical company headquartered in Cambridge, Mass., USA. Evotec will use its expertise and technologies in protein production, assay development and high throughput screening to identify hit molecules for Biogen Idec. Under the research agreement Evotec will screen a target selected by Biogen Idec with the option to add further targets as agreed. Evotec will provide Biogen Idec with access to its full range of screening technologies and diverse library of high quality compounds and will use its expertise in protein production and assay development to develop new assays for the target. Dr. Mark Ashton, Evotec's EVP, Business Development commented: "We believe that the quality of future drug candidates is very much dependent on the identification of high quality starting points. To this end we have established a platform of screening technologies that have been proven to identify high-class hit molecules. We are looking forward to working with Biogen Idec and identifying interesting hit compounds for them." Evotec has built a comprehensive platform of hit finding technologies that allow it to screen challenging targets and identify new classes of hit compounds that can be progressed towards new treatments for various diseases. These proven screening technologies coupled with Evotec's high quality screening library have been shown to unlock numerous biological targets and identify excellent start points for subsequent optimization. No financial details are disclosed. About Evotec AG Evotec is a leader in the discovery and development of novel small molecule drugs. The Company has built substantial drug discovery expertise and an industrialized platform that can drive new innovative small molecule compounds into the clinic. In addition, Evotec has built a deep internal knowledge base in the treatment of diseases related to neuroscience, pain, and inflammation. Leveraging these skills and expertise the Company intends to develop best-in-class differentiated therapeutics and deliver superior science-driven discovery alliances with pharmaceutical and biotechnology companies. Evotec has long-term discovery alliances with partners including Boehringer Ingelheim, CHDI, Novartis, Ono Pharmaceutical and Roche. The Company has a P2X7 antagonist for the treatment of inflammatory diseases in clinical development and a series of preclinical compounds and development partnerships, including a strategic alliance with Roche for EVT 101, a subtype selective NMDA receptor antagonist, for use in treatment-resistant depression. For additional information please go to www.evotec.com Forward-looking statements Information set forth in this press release contains forward-looking statements, which involve a number of risks and uncertainties. Such forward-looking statements include, but are not limited to, statements about our expectations and assumptions concerning regulatory, clinical and business strategies, the progress of our clinical development programs and timing of the results of our clinical trials, strategic collaborations and management's plans, objectives and strategies. These statements are neither promises nor guarantees, but are subject to a variety of risks and uncertainties, many of which are beyond our control, and which could cause actual results to differ materially from those contemplated in these forward-looking statements. In particular, the risks and uncertainties include, among other things: risks that the Company may be unable to reduce its cash burn through recent restructuring and cost containment measures and may not recognize the results of such measures within the expected timeframe; risks that product candidates may fail in the clinic or may not be successfully marketed or manufactured; the risk that we will not achieve the anticipated benefits of our collaborations, partnerships and acquisitions in the timeframes expected, or at all; risks relating to our ability to advance the development of product candidates currently in the pipeline or in clinical trials; our inability to further identify, develop and achieve commercial success for new products and technologies; the risk that competing products may be more successful; our inability to interest potential partners in our technologies and products; our inability to achieve commercial success for our products and technologies; our inability to protect our intellectual property and the cost of enforcing or defending our intellectual property rights; our failure to comply with regulations relating to our products and product candidates, including FDA requirements; the risk that the FDA may interpret the results of our studies differently than we have; the risk that clinical trials may not result in marketable products; the risk that we may be unable to successfully secure regulatory approval of and market our drug candidates; and risks of new, changing and competitive technologies and regulations in the U.S. and internationally. The list of risks above is not exhaustive. Our most recent Annual Report on Form 20-F, filed with the Securities and Exchange Commission, and other documents filed with, or furnished to the Securities and Exchange Commission, contain additional factors that could impact our businesses and financial performance. We expressly disclaim any obligation or undertaking to release publicly any updates or revisions to any such statements to reflect any change in our expectations or any change in events, conditions or circumstance on which any such statement is based.
Source: Reuters
KINAXO launches KinAffinity® services for efficient profiling of kinase inhibitors in cells or tissue
Last Updated on Thursday, 8 October 2009 10:53 Written by Editor Thursday, 8 October 2009 10:53
Martinsried, Germany, October 01, 2009 / b3c newswire / - KINAXO Biotechnologies GmbH announced today that it added KinAffinity® to its service portfolio. KinAffinity® provides invaluable information about a kinase inhibitor’s selectivity in a cell or tissue of interest. It simultaneously determines affinities for native kinases expressed within a cellular proteome and thus overcomes the limitations of traditional biochemical assays that only use recombinant proteins.
Kinase inhibitors with favorable pharmaceutical properties are extensively pursued as therapeutics in numerous oncological, neurological and inflammatory indications. However, their development faces significant challenges such as target specificity for the disease-relevant target proteins. Here, KinAffinity® provides critical information to select the right lead compound for clinical development.
KinAffinity® combines proprietary chemical proteomics methods with state-of-the-art quantitative mass spectrometry (see Sharma et al., Nature Methods 2009). Endogenously expressed, post-translationally modified kinases are enriched by a ready-to-use affinity matrix in the presence of native binding partners and competed with the kinase inhibitor of interest. Subsequently, bioinformatic methods are used to reveal the inhibitor’s quantitative cellular target profile. The inhibitor’s targets are ranked by their affinities and reported to the customer.
KinAffinity® is applicable for type I and type II kinase inhibitors. It facilitates selectivity analysis on an organism level that accounts for differences in protein expression between different cells, as well as their mutational and modification status that might affect drug binding.
Link to the news release
About KINAXO – www.kinaxo.com
KINAXO Biotechnologies GmbH is a privately-held biotechnology company based in Munich/Martinsried, Germany. As a spin-off of the Max Planck Institute of Biochemistry in Martinsried, we closely cooperate with several of the Institute’s most outstanding scientists in the field of chemical proteomics and quantitative mass spectrometry, namely Dr. Henrik Daub, Prof. Jesper Olsen and Dr. Jürgen Cox. KINAXO’s technology portfolio delivers direct insights into a compound’s cellular interactions and its mode of action and is routinely applied to decrease drug development times and improve therapeutic strategies. To expand its KinAffinity® platform, KINAXO recently received financial funding from the Bavarian Ministry of Economics. The underlying technology was licensed from the Max Planck Society and co-developed by scientists of the Max Planck Institute of Biochemistry and KINAXO’s scientists.
KINAXO has several ongoing collaborations with major pharmaceutical and biotechnology companies such as Boehringer Ingelheim, Johnson & Johnson and Bayer, and is financed by European investors BioM, High-Tech Gründerfonds, KfW, the Max Planck Society, and Mountain Partners.
Source:Â B3C Newswire
Posted under Drug Development, Drug-Like Compounds, Industry News, Press Releases, R & D | No Comments
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 27 March 2009 10:00 Written by admin Friday, 27 March 2009 10:00
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 Discoveryâ„¢ 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.â€
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 Accelerates Drug Discovery Process With New Maybridge Quick2Leadâ„¢ Compound Kits
Last Updated on Friday, 27 March 2009 09:32 Written by admin Friday, 27 March 2009 09:32
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 Quick2Leadâ„¢ 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
Posted under Compound Libraries, Diversity Libraries, Drug-Like Compounds, Europe, New Products, Press Releases | No Comments
Plexxikon Receives Key Patents on Novel Compounds for Multiple Programs
Last Updated on Friday, 20 March 2009 04:54 Written by Editor Friday, 20 March 2009 04:54
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 Discoveryâ„¢ 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.â€
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.
European Molecular Biology Laboratory (EMBL) Signs Agreement to License Themis and Surflex-Dock Technologies from Tripos
Last Updated on Wednesday, 18 February 2009 04:13 Written by Editor Wednesday, 18 February 2009 04:13
ST. LOUIS, Mo.–(BUSINESS WIRE)–Triposâ„¢, 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’ Themisâ„¢ and Surflex-Dockâ„¢ 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.â€
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.â€
“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.â€
ZINC Database – emolecule repository
Last Updated on Monday, 12 January 2009 03:52 Written by Editor Monday, 12 January 2009 03:52
Why is it needed? Compounds that are available today can become unavailable in six months because of unavailability of the underlying reagents. For most vendors, the list of available compounds is significantly smaller than the list of compounds they have made in the past. If you are doing virtual HTS you are probably interested in a quick verification of predicted hits. So, it makes sense to know which compounds can be ordered quickly i.e turn-around time of 30 days or less.
Why is this a difficult task? Typically, this means maintaining databases of compounds and updating them on regular basis. In my experience, I have received updates from vendors as frequently as a dozen times an year to none at all. Staying up-to-date with chemical vendor catalogs can quickly become a daunting challenge for small labs and organizations who don’t have dedicated people for this purpose.
How does ZINC help? They stay up-to-date with vendors. At any time, you can download the original 2D vendor catalog from ZINC. They have grown significantly in size and use in the last 5 years. More consumers typically means lesser bugs and better updated catalogs.
Of course, ZINC allows you to download the 3D formats as well. I have not found any documentation on their 2D to 3D pipeline. It may be available upon request. Going from 2D to 3D is a whole bag of tricks. One could potentially glue together applications provided by software vendors such as Open Eye or Molecular Networks to create a 2D to 3D pipeline. While it is great to have your own pipeline as it enables greater control on bugs and issues, it is significant amount of algorithmic work. Therefore, for some organizations, having a ready to dock 3D format is a considerable time saving.
Any Gotchas? I have not found any useful information or discussion at the ZINC forums. Ideally, it would be good to know the quality of vendors. Are these vendor lists as up-to-date as they claim to be? What is the typical ordering time? Quality of drug like compounds is also an issue.
In ZINC’s 3D formatted database, the compounds are renamed using ZINC ID and any information about the original vendor catalog ID is lost. This can be tricky when ordering compounds from vendors. The vendor catalog ID can be retrieved by going to the original vendor catalog and matching the compound but this translates to extra algorithmic work.
Nutshell? Nevertheless this is the best free resource on the web that allows user to download latest vendor compounds for virtual screening. The closest competition, emolecules charges upwards of $20K for doing the same.
Source: biotechnorati.wordpress.com
Other online searchable by structure databases:
Compounds and Compound Libraries from TimTec
Posted under ChemInformatics, Compound Libraries, Drug-Like Compounds, New Products, North America, Press Releases | No Comments
IPR story 12- Patenting a mere idea
Last Updated on Wednesday, 26 November 2008 02:14 Written by Editor Wednesday, 26 November 2008 02:14
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.
Virtual Screening Gives Drug Design a Boost
Last Updated on Wednesday, 19 November 2008 05:07 Written by Editor Wednesday, 19 November 2008 05:07
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.
The approach developed by McCammon’s group uses a combination of several computational tools. It starts with a detailed model of the biological target –REL1 in this case — derived from X-ray crystallography. It then uses biophysical principles to find all the ways in which the protein can twist, turn, and wiggle.
McCammon’s computational method has already proven its utility for designing other important drugs. His group used it to develop a model for a new class of drugs to treat AIDS that led to raltegravir, which the Food and Drug Administration approved in 2007. McCammon’s team also used the method to identify promising drug candidates for treating H5N1 avian flu.
WuXi PharmaTech Inks New Three-year Deal with Pfizer
Last Updated on Tuesday, 11 November 2008 02:55 Written by admin Tuesday, 11 November 2008 02:55
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 and Collaborative Drug Discovery Team Up to Provide Chemically Searchable Natural Products and Derivatives Available to the Scientific Community
Last Updated on Wednesday, 22 October 2008 04:52 Written by admin Wednesday, 22 October 2008 04:50
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.â€
“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
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