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Using drug patent information to synthesize drugs

There is a strong incentive to find out new opportunities for the discovery of new drugs

Annual sales in the pharmaceutical sector have been increasing in the double-digit range for several years. However, the figures are expected to go down significantly in the near future on account of major factors like patent expirations on important products, larger spending on marketing and sales, the increased expenses on research and development, and pressure to cut down healthcare expenditures.

Since the market for the top therapeutic classes of drugs is more than $350 billion annually, there is significant incentive to find out new opportunities for the discovery of new drugs. It’s expected that proteomics, bioinformatics, and genomics will additionally improve the drug discovery process by providing a better comprehension of disease processes and giving insights into innovative opportunities for successful intervention with different medicines.

How Can Patents be Useful?

Drug patent information can assist nations engage with patent owners at an earlier stage in order to explore possibilities for creating drugs, eventually making patent protection more affordable.

In practice, getting accurate and relevant information on drugs, especially in developing nations, comes with high levels of difficulties because of the following reasons:

  • A dearth of references to international non-proprietary names or INNs
  • The technical language of the specification of the patent
  • A particular drug may be covered by multiple patents
  • The information may not be accurate or revised
  • The information cannot easily be obtained from the national patent office, and
  • even if it’s accessible, patent searches may not always reveal all the important patents

Despite the above-mentioned constraints, patent information is now increasingly being made available electronically. There are freely accessible methods and resources that are not heavily technical to help identify if important patents exist on drugs. Even though they are not exhaustive, they can assist procurement agencies and health authorities to recognize pharmaceutical patents at the national level.

As an example, the World Health Organization has assembled "A Methodology for Patent Searches on Essential Medicines in Developing Countries".

A successful pharmaceutical after getting approved by regulators like the EMA in the European Community and the FDA in the US gets exclusive right to sell the drug until its patent expires. Patents in developed nations are normally granted for 20 years; however, the window of sales exclusivity is often less than 10 years since the patents need to be filed well before launch. The company has to recoup the entire R&D expenses of both the medication being sold and of all the other medications that failed during the development phase along with expenses rendered on manufacturing and marketing.


The next section lists new approaches in the synthesis of drugs using patent information along with the challenges faced by the pharmaceutical industry

1. Biological pathways

The growth of information with respect to biological pathways like cell signaling, modulation and regulation, and protein and gene expression ups the challenge of target selection, given the massive effort needed to identify and develop compounds. After the therapeutic target has been picked, associating the target with a specific biological mechanism for the action of the drug paves way for the discovery. In order to accomplish this objective, it’s important to recognize the important biological assays.

A perfect example can be seen in the discovery and development of HIV protease inhibitors to treat HIV. In this case, a cell-free assay where inhibition could be fathomed was used to describe the mechanism of drug action. The active compounds in the assay were then analyzed in cell culture systems subjected to HIV infection. Compounds that acted by this mechanism and could achieve sufficient concentration in the cells were anticipated to restrict viral replication in a manner depending on the concentration. Hence, the information gathered from both the assays provided a handy coupling between drug action mechanism and the predicted response. Data from these assays were used by chemists to create a roadmap right from early lead compounds to effective drugs.

Screening

Leads for the discovery of drugs are often singled out by screening groups of compounds from synthesis or by seclusion from natural sources. High throughput screening techniques and sophisticated equipment have been devised to facilitate the work, considering the fact that there are more than 100,000 compounds to be screened. In many cases, researchers have generated a lead by making some modifications to the structure of a substrate that is being examined.

Two challenges faced by chemists in this aspect are “what to make” and the “process involved in making it.” The knowledge on how to make it is mainly derived from synthetic organic chemistry. Since most medications have a minimum of one stereo center, current major improvements in synthetic techniques that address this issue have turned out to be particularly significant in the case of medicinal chemistry.

There are many factors that are taken into consideration on what to make. A majority of medicinal molecules combine noncovalently with the macromolecular targets and solvation, electronic and steric factors are responsible for the energy created during interaction. Even though designing biologically agile molecules is not pure science, the relationships between structure and activity found from laboratory experiments give an idea on which medication to pursue.

3. Mechanism of drug action

The discovery process has been facilitated by studying the mechanics of drug action. For instance, angiotensin II receptor and Angiotensin converting enzyme (ACE) have tremendously improved treatment for the reversal of hypertension. Regulation of cholesterol biosynthesis by using HMG-CoA reductase inhibitors has cut down the incidence of coronary heart disease by approximately 34%. Bone resorption inhibitors now provide successful therapy for treating osteoporosis. While the therapeutic developments in the last few years have remained impressive, there are many challenges and opportunities that still remain profound.

Organizational relationships and structures that will expedite open sharing of important information and teamwork need to be created and used to achieve success in the complicated world of drug synthesis. The group should have the capacity to work as an interdisciplinary team, comprising of biologists, chemists and scientists, specializing in computational analysis, molecular modeling, drug metabolism, structure determination, safety assessment, pharmaceutics, and all other aspects related to drug discovery. Open access to information is a prerequisite as it encourages boundary crossing in the quest to find innovative solutions in every discovery project.

Structural examination of target macromolecules with the help of NMR spectroscopy and X-ray crystallography has had a great impact on the design of drugs so far. Robust modeling techniques and computational programs have improved the utility of these approaches. While the promise of bioinformatics, genomics and proteomics is yet to be consummated, the potential of these latest techniques to greatly facilitate the discovery of drugs is apparent. The growing advances of analytical chemistry and synthetic organic are also crucial to the pharmaceutical sector. Developments in parallel synthesis can rapidly broaden the plethora of compounds that can be studied as new medications.

The challenge: Access to information

Innovation entails the sharing of information across unique technologies, biological fields and chemistry efforts-data that gets fragmented when spread across tiny biotech companies and academic labs. Dealing with fragmented scientific knowledge is important for future success in the arena of medicine and health. Besides keeping abreast of the latest insights, gaining admittance has become a huge challenge. An easy solution is to place all this information within the public domain (however, safeguarding intellectual property rights very often constrains use or delays disclosure)

The requirement for biotech alliances with huge pharmaceutical firms is unquestioned by tiny private firms-both for financial profits and shared learning, which can be provided only by major partners. A recent revelation found that alliances of universities and small biotech firms are equally significant to bring about biological and chemical innovation into big pharmaceutical companies. On a similar note, collaborations between universities and small biotech companies will gradually become a basis for cross-discipline integration. The present structures of alliances are not so efficient and require new approaches.

Conclusion

The research-based pharmaceutical sector remains beset with problems when it comes to drug synthesis and most of these do not have obvious solutions. Even though patent information can be used to develop new drugs as mentioned above, increasing regulation is resulting in extra expenses and longer development times. The penetration of generics into the market is increasingly rapidly and many are of the view that the current research pharmaceutical model is no longer sustainable.

However, on account of the growing domination of drug development pipelines, we are certain that the next generation of pharmaceuticals will leave a lot of smaller residues than those that result from the use of present drugs.

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2017 DrugPatentWatch pharmaceutical strategic guidance

Deeper Knowledge, Faster

  • Analyze global market entry opportunities
  • Identify first generic entrants
  • Uncover prior art in expired and abandoned patents

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