MARKUSH FOR PATENT ANALYSIS Steve Hajkowski ChemAxon UGM Budapest 2013
THOMSON REUTERS MARKUSH DATA Indexing for 2.4 million patent families 1.6m Markush structures, re-drawn & stored in Thomson Reuters vmn file format 1.98m specific compounds plus the corresponding DWPI records 28 patent issuing authorities covered backfile from 1978 for US, EP and WO patents covers pharmaceutical, agrochemical and general chemistry patents Indexed as part of the editorial process that creates Derwent World Patents Index (DWPI) Informative English language titles & abstracts from worldwide patents Patent family listing, patent assignees
COVERAGE START DATES Austria 1987 Korea 2008 Australia 1987 Malaysia 2010 Belgium 1987 Netherlands 1987 Brazil 2010 New Zealand 1987 Canada 1987 PCT/WO 1978 (Pharma); 1982 (Agro + Gen. Chem.) China 2008 Poland 2011 European Patents 1978 (Pharma); 1982 (Agro + Russia Gen. Chem.) 1993-1998 and 2010 to date France 1961-1976 (FR-M); 1978 (Pharma); 1982 (Agro + Gen South Africa 1987 Chem) 1980 (Pharma); 1983-84 and Germany 1987 to date (Agro + Gen. Spain 2010 Chem.) Great Britain 1980 (Pharma); 1983-84 and 1987 to date (Agro + Gen. Sweden 1987 Chem.) Gulf Cooperation Council 2008 Switzerland 1987 India 2000 Thailand 2010 Ireland 1987 United States 1978 (Pharma); 1982 (Agro + Gen. Chem.) Japan 1987 Vietnam 2010
MARKUSH DATA ACCESS Markush structure data available alongside corresponding specific compounds & DWPI records Load into ChemAxon s JChem database tools Resulting solution gives access to full chemistry & patents dataset data can be searched, enumerated & integrated into the customer s own systems & workflows 4
JCHEM MARKUSH BENEFITS Structure data displayed alongside high quality patent summaries from DWPI includes abstract, patent assignee, patent family, activities & mechanisms of action Time saving visualisation and enumeration capabilities enable fast relevance analysis of hit structures/patents Enumerated structures are in standard format allowing easy integration with other chemistry datasets/tools
USE CASES Novelty searching by IP departments Easy assessment of structural proximity of query structure to hit Markush Screening of new structures against existing IP Potential use in white-space identification, patent busting etc. Creation of libraries of specifics for use in other systems
MARKUSH PATENT ANALYSIS What can analysis of Markush and DWPI patent data tell us about global patenting trends in 2012? > 8000 patents claiming new pharmaceutical Markush structures > 3700 patents claiming new non-pharma Markush structures
MARKUSH PHARMA PATENTING COMPANIES 2012 Number of patents Company 129 MERCK & CO 119 ROCHE 82 BAYER AG 60 ABBOTT 59 GLAXOSMITHKLINE 57 NOVARTIS 57 CENTRE NATIONAL RECHERCHE SCIENTIFIQUE 55 BOEHRINGER INGELHEIM 54 SANOFI AVENTIS 52 BRISTOL-MYERS SQUIBB 51 MERCK PATENT GMBH 42 JOHNSON & JOHNSON 41 ALLERGAN 39 TAKEDA PHARMA 37 PFIZER 30 COUNCIL SCI&IND RES INDIA 27 SHIONOGI 26 DAIICHI SANKYO 25 UNIV CALIFORNIA
MARKUSH PHARMA PATENTING TERRITORIES IN 2012
MARKUSH CHEMICAL PATENTING COMPANIES 2012 Number of patents Company 164 SUMITOMO CHEMICAL CO 90 BAYER CROPSCIENCE 82 BASF 65 MERCK PATENT GMBH 61 FUJI FILM CO 42 SEMICONDUCTOR ENERGY LAB 40 SYNGENTA 39 ROHM&HAAS ELECTRONIC MATERIALS KOREA 38 CANON KK 38 OCEANS KING LIGHTING SCI&TECHNOLOGY CO 37 IDEMITSU KOSAN CO LTD 36 DU PONT 34 HAIYANGWANG LIGHTING TECHNOLOGY CO LTD 34 NIPPON KAYAKU KK 34 POLITECHNIKA WROCLAWSKA 30 JNC CORP 28 KOREA RES INST CHEM TECHNOLOGY 27 TOSOH CORP 26 TIANJIN DEKAI CHEM LTD
MARKUSH CHEMICAL PATENTING TERRITORIES IN 2012
MARKUSH CASE STUDY Analysis of all Markush patents claiming new molecules containing the structure fragment below look at companies, timeframes, activities, inventors
SEARCH RESULTS A structure search of the Thomson Reuters data generates hits from 122 patents, with hits found back to 1988
SAMPLE HITS New heterocyclic derivatives useful for treating cardiovascular diseases,hypertension, ischemic heart disease, atherosclerosis and metabolic syndrome CTG PHARMA SRL WO2008122356A1 20081016 Novel benzyloxymethyl-4-chloro-imidazol methyl-biphenyl-tetrazole group containing compound useful for treating diseases associated withperoxisome proliferator-activated receptor-gamma, e.g. diabetes and angiocardiopathy SHANGHAI AILISI MEDICINE SCI & TECHNOLOGY WO2008110062A1 20080918
SAMPLE HITS New 2-butyl-4-chloro-imidazol-5-yl-methyl ester compound used for preparing drugs for prophylaxis and/or treating high blood pressure or correlative diseases including pulmonary arterial hypertension, coronary heart disease and/or migraine WANG J CN101475565A 20090708 Forming biphenyltetrazole derivatives useful to treat e.g. stroke involves reacting 2-(trimethylsilyl)ethoxymethyl protected biphenyltetrazole compounds with nucleophilic reagent and subsequent deprotection ofprotecting group SIMS SOC ITAL MEDICINALI SCANDICCI SRL WO--2008012852A1
TOP 10 COMPANIES Number of patents Company 17 MERCK & CO INC 8 NICOX SA 7 DU PONT DE NEMOURS & CO 7 KOTOBUKI SEIYAKU CO LTD 6 MERCK PATENT GMBH 4 NITROMED INC 4 TANABE SEIYAKU CO 4 THERAVANCE INC 3 DIPHARMA SPA 3 SANKYO CO LTD
TOP PATENT COUNTRIES
PATENTING TIMELINE
DRUG ACTIVITIES CLAIMED % of Patents Activity 88 Hypotensive 64 Cardioactive 47 Renal active 43 Anti-cholesterol 43 Eye preparations 34 Circulatory active 32 Antipsychotic 30 Coronary dilator 28 Antimetabolite 27 Antiinflammatory 25 Enzyme inhibitor
TOP INVENTORS AT MERCK Number of patents Inventor 9 LO M M 8 ALI A 6 ALMIRANTE N 5 STEFANINI S 4 BIONDI S 4 CHAKRAVARTY P K 4 FRANKLIN C 4 GREENLEE W J 4 NARGUND R P 4 PATCHETT A A 4 SEBHAT I K
SUMMARY Markush analysis allows us to view the chemistry patent lansdcape broad view of trends for companies, countries etc narrower view for particular structure types shows which companies are active, trends over time, top inventors, drug activities etc.
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