Intellectual Property Rights and Pharmaceutical Industry BISansCond 10 Intellectual Property Rights and Pharmaceutical Industry Drug Development Process and Importance of Intellectual Property Rights for R&D Industry

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

Costs of Drug R&D

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

The Future of Drug Discovery The future of drug discovery depends on understanding the genetic basis of the disease.

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

The Change of Paradigm in Pharmaceutical R&D BISansCond 10 The Change of Paradigm in Pharmaceutical R&D 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

Products of R&D Classical New NCEs BISansCond 10 Products of R&D 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

Known Molecular Processes Leading to Cancer

Steps in the NCE Discovery Process BISansCond 10 Steps in the NCE Discovery Process Early Discovery (exploratory) Late Discovery Lead Optimization Target Identification Assay Development Lead Identification Disease unmet medical need commercial opportunity protein or gene involved in disease- related pathological pathways primary activity screens functional screens in vivo models chemical starting point optimized compound Development Candidate 3

Robotic Screening (HTS) Information Technology BISansCond 10 The New Core Technologies Influence Each Step of The Drug Development Process Disease Target Assay Lead Development Candidate Gene Technology/Genomics Robotic Screening (HTS) Combinatorial Chemistry Rational Design Information Technology 4

Why patent?

Good Reasons for Patenting BISansCond 10 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.

What is a Patent? Which Rights Does a Patent Confer? BISansCond 10 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.

Which Rights Does a Patent Not Confer? BISansCond 10 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!

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

Categories of Patent Claims 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

Robotic Screening (HTS) Information Technology BISansCond 10 The New Technologies of the R&D Process are Sources of Inventions Disease Target Assay Lead Development Candidate Gene Technology/Genomics Robotic Screening (HTS) Combinatorial Chemistry Rational Design Information Technology 4

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

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

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

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