Abstract
Regulating cell function by controlling cell pathways is an important strategy
in the development of agents for the treatment of cancer and numerous other
diseases. Protein kinases are a family of enzymes involved in the regulation
of almost all cell processes. Scientists have identified 518 kinases encoded
by the human genome. By adding phosphate groups to substrate proteins, these
enzymes control the activity, the location, the association of these substrate
proteins with other proteins and their function. Thus kinases play an
essential role in signal transduction and the coordination of complex
functions in particular the cell cycle.
Because alterations in protein phosphorylation are frequently associated with
human disease, investment in the development of pharmacological inhibitors of
protein kinases has grown exponentially. About 30% of existing drug discovery
programs in the pharmaceutical industry target a protein kinase (reviewed in
Cohen, Nature reviews drug discovery, 2002; Fischer & Gianella Borradori, Exp.
Opin. Investig. Drugs, 2005; Grant, Cell. Mol. Life Sci., 2009). Today, dozens
of kinase inhibitors are on the market to treat cancer and the cumulated sales
of the blockbuster drug Gleevec (tyrosine kinase inhibitor, Novartis) was $3.7
billion in 2008 (Novartis annual report 2008). However, no pharmacological
cyclin-dependent kinase inhibitors (CDK, serine/threonine protein kinases), a
key kinase sub-family, have yet reached the market. Although this sub-family
includes 20 members (and 25 cyclins) in humans, a more limited number has been
identified. To constitute active protein kinase complexes (see figure 1), CDKs
are regulated by transient association with a regulatory partner (cyclins), go
through various post-translational modifications (e.g. phosphorylation) and
transient association with a natural inhibitory protein (Cip1, Kip1/2 or
Ink4A-D).
This family is of particular interest because of its essential involvement in
neuronal cell physiology (CDK5), pain signalling (CDK5), apoptosis (CDK1,
CDK2, CDK5), transcription (CDK7, CDK8, CDK9), RNA splicing (CDK11),
differentiation (CDK2, CDK5, CDK6, CDK9) and especially cell cycle control
(CDK1, CDK2, CDK3, CDK4, CDK6, CDK7, CDK10; see figure 2). In addition P.
Nurse, L. Artwell and T. Hunt were awarded the Nobel Prize in
Physiology/Medicine in 2001 for their work in the discovery of the role of
cyclins and CDK in the control of the cell cycle.
Table of Contents
METHODOLOGY
INTRODUCTION
1. BRIEF OUTLINE OF THE PIPELINE
2. PROTECTION STRATEGIES
- 2.1. Evolution of patent filings over time
- 2.2. Priority filings
- 2.3.Extensions
- 2.4. Analysis of industrial patents over time
- 2.5. Study of the granting of US patents
- 2.6. Study of the granting of European patents
- 2.7. Evolution in the number of applicants
3. TOPOLOGY OF PATENTS IN THE SECTOR
- 3.1. Breakdown of patents into classes of CDK inhibitors
- 3.2. Breakdown of patents into types of targeted CDK
- 3.3. Cross analysis of the categories "classes of CDK inhibitors" and
"types of targeted CDK"
4. ANALYSIS OF THE MAIN APPLICANTS
- 4.1. Main applicants
- 4.2. Filings by main applicants over time
- 4.3. Focus on the global strategy of the major industrial applicants
- 4.4. Topics protected
- 4.5.Collaborations
- 4.6. Citations between applicants
- 4.7. Emerging applicants
5. ANALYSIS OF THE MAIN INVENTORS
- 5.1. Main inventors
- 5.2. Topics protected
- 5.3. Research teams
- 5.4. Experts
- 5.5. Emerging inventors
CONCLUSION
APPENDIX 1: APPLICANTS WITH ACTIVE CLINICAL TRIALS AND THEIR NUMBER OF PATENT FILINGS
APPENDIX 2: PATENT FILINGS OF APPLICANTS BY MAIN TOPICS
APPENDIX 3: NUMBER OF PATENT FILINGS PER APPLICANTS
List of Figures
- FIGURE 1 - SCHEMATIC REGULATION OF THE CDK-CYCLIN COMPLEX
- FIGURE 2 - THE CELL CYCLE AND ITS REGULATION BY CDK
- FIGURE 3 - CDK INHIBITORS UNDER DEVELOPMENT BY CLASS OF COMPOUNDS (AUGUST
2009)
- FIGURE 4 - EVOLUTION IN PATENT FILINGS
- FIGURE 5 - GEOGRAPHIC DISTRIBUTION OF PRIORITY FILINGS
- FIGURE 6 - GEOGRAPHIC DISTRIBUTION OF EXTENSIONS
- FIGURE 7 - EVOLUTION OF THE BREAKDOWN OF INDUSTRIAL PATENTS
- FIGURE 8 - EVOLUTION OF AVERAGE GRANT TIME FOR US PATENTS
- FIGURE 9 - EVOLUTION OF THE GRANTING OF US PATENTS
- FIGURE 10 - EVOLUTION OF AVERAGE GRANT TIME FOR EUROPEAN PATENTS
- FIGURE 11 - EVOLUTION OF AVERAGE GRANT TIME FOR EUROPEAN PATENTS
- FIGURE 12 - EVOLUTION OF THE NUMBER OF APPLICANTS
- FIGURE 13 - BREAKDOWN OF THE PORTFOLIO BY CLASSES OF COMPOUNDS
- FIGURE 14 - BREAKDOWN OF THE PORTFOLIO BY TYPES OF TARGETED CDK
- FIGURE 15 - CROSS-ANALYSIS OF THE CATEGORIES "CLASSES OF CDK INHIBITORS"
AND "TYPES OF TARGETED CDK"
- FIGURE 16 - MAIN APPLICANTS IN THE ENTIRE PORTFOLIO
- FIGURE 17 - BREAKDOWN OF THE MAIN PATENT PORTFOLIOS
- FIGURE 18 - EXTENSION POLICY FOR THE FIVE MAJOR INDUSTRIAL PLAYERS
- FIGURE 19 - CLASSES OF CDK INHIBITORS BY MAIN APPLICANTS
- FIGURE 20 - TYPES OF TARGETED CDK BY MAIN APPLICANTS
- FIGURE 21 - MAIN PLAYERS POSITIONED ON THE DEVELOPMENT OF SCREENING
METHODS, COMBINATIONS AND OLIGONUCLEOTIDES (>3 FILINGS)
- FIGURE 22 - MAJOR COLLABORATIONS AND JOINT-FILINGS
- FIGURE 23 - MAP OF CITATIONS BETWEEN APPLICANTS
- FIGURE 24 - CLASSES OF CDK INHIBITORS BY MAIN INVENTORS
- FIGURE 25 - TYPES OF TARGETED CDK BY MAIN INVENTORS
- FIGURE 26 - MAIN RESEARCH TEAM
- FIGURE 27 - LIST OF EXPERT
List of Tables
- TABLE 1 - CYCLIN DEPENDENT KINASES INVOLVED IN DISEASES OR REPRODUCTION
- TABLE 2 - EVOLUTION OF PRIORITY FILINGS
- TABLE 3 - EVOLUTION OF EXTENSIONS
- TABLE 4 - DESCRIPTION OF THE CLASSES OF COMPOUNDS USED TO BREAK DOWN THE
PORTFOLIO
- TABLE 5 - BREAKDOWN BY CLASSES OF CDK INHIBITORS OVER TIME
- TABLE 6 - BREAKDOWN BY SCREENING METHODS, COMBINATIONS AND
OLIGONUCLEOTIDES OVER TIME
- TABLE 7 - BREAKDOWN BY CLASSES OF CDK INHIBITORS OVER TIME
- TABLE 8 - BREAKDOWN OF FILINGS BY MAIN APPLICANTS OVER TIME
- TABLE 9 - EMERGING APPLICANTS
- TABLE 10 -LIST OF THE MAIN INVENTORS
- TABLE 11 -EMERGING INVENTORS
