Intellectual Property Rights and Pharmaceutical Industry

1. Intellectual Property Rights and Pharmaceutical Industry Drug Development Process and Importance of Intellectual Property Rights for R&D Industry

2. Increasing Challenges in The Pharmaceutical Industry • Increasing R&D costs • High innovation pressure • Many more therapeutic targets to be explored and utilized as drug intervention sites

3. Costs of Drug R&D

4. Number of New Approved Drugs as Compared to Total R&D Expenditureof the Pharmaceutical Industry Inspite of increasing R&D expenditure, the number of new approved drugs remains relatively constant!

5. The Future of Drug Discovery The future of drug discovery depends on understandingthegenetic basis of the disease.

6. Recombinant Drugs Receptors Enzymes Technological Advancements in Pharma Research Genomics Gene Therapy Traditional drugs from plants 1900 1950 1970 1990

7. Classical R&D Approach Known lead structure for symptomatic therapy Optimization of active substance in animal model Clinical trial. Safety and efficacy Registration New R&D Approach Genetic cause of the disease (Genomics) Rational selection of the active substance (molecular genetics) High Throughput Screen Optimization of active substance with recombinant human gene products and combinatorial chemistry Clinical trial. Safety and efficacy Registration The Change of Paradigm in Pharmaceutical R&D

8. Classical NCEs Vaccines bacterial extracts Proteins from animal tissue New NCEs (obtained by using genetic engineering technology) Non-infectious vaccines obtained by genetic engineering NBEs (recombinant human proteins, monoclonal antibodies) Gene Therapy Products of R&D

9. Known Molecular Processes Leading to Cancer

10. Steps in the NCE Discovery Process Late Discovery Early Discovery (exploratory) Lead Optimization Assay Development Lead Identification Target Identification Disease • unmetmedicalneed • commercialopportunity • protein orgeneinvolvedin disease-relatedpathologicalpathways • chemicalstarting point • optimizedcompound • primaryactivityscreens • functionalscreens • in vivo models DevelopmentCandidate

11. Development Candidate Disease Target Assay Lead The New Core Technologies Influence Each Step of The DrugDevelopment Process Gene Technology/Genomics Robotic Screening (HTS) Combinatorial Chemistry Rational Design Information Technology

12. Why patent?

13. Good Reasons for Patenting • Patents prevent others from commercially utilizing an invention. • For the research-based industry, periods of market exclusivity are crucial for the recoupment of R&D expenditure. • Patents encourage financial risk and long-term research. • Patents guarantee the dissemination of information.

14. What is a Patent?Which Rights Does a Patent Confer? • A patent is a limited monopoly granted in respect of an invention. • A patent confers the right to exclude others from making, using or selling the invention. • This right is granted to the inventor (or his/her successor in title) by a national or regional authority. • This right is limited in terms of territory and duration. • The scope of this right is defined by the patent claims.

15. Which Rights Does a Patent Not Confer? • A patent does not confer the "positive" right to use the invention! • The use of an invention, whether patented or not, is subject to other national laws and regulations!

16. The Patent Right is Limited With Regard to Territory and Term • Territorial scope : • National patents - both granting procedure and effect are national • European patents - the granting procedure is European, the effect is national • International patent applications (PCT): the application and examination procedure is international, the granting procedure is European/national, the effect is national • Term • 20 years from filing

17. Product Method Use Broadest protection. It covers all uses of the product, even those not explicitly disclosed. The protection for a method of manufacture also covers the products obtained by that method. Relatively narrow scope of protection - second medical use Categories of Patent Claims

18. Development Candidate Disease Target Assay Lead The New Technologies of the R&D Process are Sources of Inventions Gene Technology/Genomics Robotic Screening (HTS) Combinatorial Chemistry Rational Design Information Technology

19. Patentable Inventions Created During the R&D Process Research Tools target genes screening assays reagents cDNAs, ESTs animal models

20. Patentable Inventions Created During the R&D Process Drug (NCE or NBE) per se method of making formulation combination novel use (second indication) drug delivery system gene therapy

21. Telmisartan - a Boehringer Ingelheim Success Story - Part I 31.1.1992 foreign filings Xmas 1990 Angiotensin receptor antagonist Telmisartan synthesized May 98 European patent for Telmisartan granted* February 1991 Priority patent application *in additon, several manufacturing and processing patent applications filed

22. Telmisartan - a Boehringer Ingelheim Success Story - Part II January 2012 Expiry of European Patent Xmas 1998 Registration of Telmisartan European Market Authorization June 1999 SPC filed Xmas 2013 SPC expiry