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1、 1 Natural Nutraceutical Patent Strategy Case Studies How leading companies are transforming the future nutraceuticals landscape Reference Code: BI00047-008 Publication Date: September 2011 2 About the author Irene Buggle is a consultant and analyst based in London, England with a broad knowledge of
2、 the pharmaceutical and healthcare industries. She had a long career at IMS Health, holding management positions in market research, marketing and editorial areas. She has extensive experience in analyzing markets, writing reports and articles covering a broad range of areas but her latter experienc
3、e has been working in the area of intellectual property. Irene is co-director of a consultancy specializing in pharmaceutical and healthcare commercial intelligence. She has a BSc from Reading University and an MSc in Biochemistry from Kings College, University of London. Disclaimer Copyright 2011 B
4、usiness Insights Ltd This report is published by Business Insights (the Publisher). This report contains information from reputable sources and although reasonable efforts have been made to publish accurate information, you assume sole responsibility for the selection, suitability and use of this re
5、port and acknowledge that the Publisher makes no warranties (either express or implied) as to, nor accepts liability for, the accuracy or fitness for a particular purpose of the information or advice contained herein. The Publisher wishes to make it clear that any views or opinions expressed in this
6、 report by individual authors or contributors are their personal views and opinions and do not necessarily reflect the views/opinions of the Publisher. 3 Table of Contents About the author 2 Disclaimer 2 Executive summary 12 Patenting strategies 12 Innovative company patent strategies 13 Conclusions
7、 14 Chapter 1 Introduction 15 The patents landscape 15 What is this report about? 15 Chapter 2 Patent strategies 17 Introduction 17 What is a patent? 17 Requirement for a therapeutic patent 18 Legal patent frameworks 18 United States 19 European 19 Patent Cooperation Treaty 20 Patenting costs 22 UK
8、patenting fees 22 EPO patenting fees 23 WIPO patenting fees 23 USPTO fees 23 4 Types of patent claims for natural nutraceuticals versus NCEs 23 Product versus composition claims 23 Health claims of natural nutraceuticals often arise from folklore 27 Process patenting strategies for natural nutraceut
9、icals versus drugs 28 Formulation patenting strategies for nutraceutical versus drugs 29 Patent term extensions 30 Differences in NCE and natural nutraceutical patenting 32 New chemical entities 33 Product claims 33 Method of use 33 Composition claims 33 Formulation patent claims 33 Process patent c
10、laims 34 Natural nutraceuticals 34 Characterization of natural active principles and purification claims 34 Composition/formulation patent claims 34 Process patent claims 35 Future patenting strategies 36 Chapter 3 Evgen Limited 38 History, background and management 38 Evgen strategy overview 38 Pro
11、duct portfolio 39 Evgens IP licensing-in strategy 41 PharmAgra 42 Kraft Foods 43 Harnessing gene technology for improved production 44 University of Copenhagen 44 Wider potential for sulforaphane 45 Other companies patenting in this area 46 John Hopkins University 47 Wassen Int Ltd 48 5 Amway Corp 4
12、8 The American Health Foundation 48 Bejo Zaden BV 49 Inventor Gu Hong Park 49 US Department of Agriculture 49 Seoul National Universitys SNU R ES2179640 (T3); FR2778312(B1); ITM1990732(A1); JP4448615 (B2); JP2008200048(A). Mithen and Traka have recently filed a PCT application, WO/2010/001119 entitl
13、ed, Use of Glycosinolates from Cruciferous Plants in Modifying Extracellular Signalling Proteins. The invention relates to methods and compositions for the post-translational modification of extracellular signaling proteins by dietary phytochemicals and related compounds including, one or more of th
14、e following phytochemicals: sulforaphane, erucin, sativin, iberin, beta-phenylethylisothiocyanate (PE-ITC)5 3-methylthiopropyl isothiocyanate. The invention further relates to assays for determining suitable phytochemicals for modifying extracellular signaling proteins. In addition, the use of combi
15、nations of the phytochemicals, isothiocyanates and procyanidins, as well as methods of modifying plants to increase the levels of 3-methylthiopropyl glucosinolate is claimed. 41 Evgens IP licensing-in strategy Table 1: Evgens intellectual property and licensing-in strategy Patent application Patent
16、application title Technology Applicant Licensing status WO9952345 Method for selective increase of the anticarcinogenic glucosinolates in Brassica sp. Improved plant via plant breeding for active principle production Plant Biosciences Ltd Not known WO/2010/001 119 Use of glycosinolates from crucifer
17、ous plants in modifying extracellular signalling proteins Plant Biosciences Ltd Not known US7879822(B 2) Stabilized sulforaphane Cyclodextrin sulforaphane complex to produce stable nutraceutical composition PharmAgra Labs Inc Option agreement with PharmAgra Labs and Lalilab Inc Feb 2010 US200831119
18、2(A1) Enteric-coated glucosinolates and beta-thioglucosidases Enteric-coated combination of glucosinolate (glucoraphanin) + beta- thioglucosidase (myrosinase) for improved small intestine delivery of isothiocyanate Kraft Foods Holdings Inc Option agreement with Kraft Foods for composition and delive
19、ry system patents on enteric coated formulation Mar 2010 WO/2009/106 985 Biosynthetic engineering of glucosinolates Gene transfer technology for creating an entire biosynthetic pathway for the manufacture of glucoraphanin University of Copenhagen Licensed patent from University of Copenhagen in 2009
20、 Source: Authors analysis BUSINESS INSIGHTS 42 PharmAgra On 4 February 2010, Evgen announced that it had entered into an option agreement to license, on a worldwide basis, a new pharmaceutical formulation developed by PharmAgra Labs Inc. (North Carolina) and Lalilab Inc. (North Carolina). The licens
21、e rights, which include all pharmaceutical and medical food applications, give Evgen the opportunity to develop its first shelf stable sulforaphane composition for the potential prevention and treatment of a number of conditions, including early stage prostate cancer. It has been impractical to deve
22、lop a clinical candidate to date due to the compounds inherent instability but with PharmAgra and Lalilabs chemistry and manufacturing skills together with Evgens clinical development skills, the companies believe that they have a viable formulation. On 23 September 2010, Evgen, PharmAgra Labs Inc.
23、(US) and Lalilab Inc. (US) announced that the Stabilized Sulforaphane patent application received a notice of allowance and will move to grant in the US. It is also pending in other geographies. The patent contains method and composition claims around the use of cyclodextrins to stabilize sulforapha
24、ne or its analogues. Evgen has an option agreement, on a worldwide exclusive basis, for stabilized sulforaphane (Sulforadex) for medical applications. The initial target is to develop a low cost, long-term use, medicine for patients diagnosed with indolent forms of prostate cancer the objective bein
25、g to significantly reduce the risk of disease progression during an active surveillance program, thereby delaying or removing the requirement for a radical procedure such as a prostectomy. The PCT application, WO2008126030, simply entitled, Stabilized Sulforaphane by the applicant, Pharmagra Labs In
26、c. (US) has entered into the national phase in a number of regions including: US7879822(B2); JP2010516766; EP2120969 (A1); CA2672971 (A1); AU2008209543(A1). The application claimed a method of stabilizing sulforaphane, by forming a complex between sulforaphane and a cyclodextrin. A nutraceutical com
27、position is claimed in which the cyclodextrin is selected from alpha, beta or gamma cyclodextrin or mixtures of these, and the sulforaphane or an analog (such as 6- isothiocyano-2-hexanone; exo-2-acetyl-6-isothiocyanatonorbornane, exo-2-isothiocyanato-6- methylsulfonylnorgomane; 6-isothiocyanato-2-h
28、exanol, 1-isothiocyanato-4-dimethylphosphonylbutane, exo- 2-(1-hydroxyethyl)-5-isothiocyanatonorborane, exo-2-acetyl-5-isothiocyanatonorbornane, 1-isothiocyanato- 5-methylsulfonylpentane, and cis- or trans-3-(methylsulfonyl) cyclohexylmethylisothiocyanate) or mixtures of 43 these. The composition ma
29、y be for oral, topical, parenteral, injectable, buccal, sublingual, intramuscular or intravenous administration. The oral nutraceutical composition is one or more dietary supplement, a food product, a food product supplement or a food additive. Kraft Foods On 2 March 2010, Evgen signed an option agr
30、eement with Kraft Foods to license, on a worldwide exclusive basis, intellectual property related to novel compositions and delivery systems of glucoraphanin combined with the beta-thioglucosidase enzyme, myrosinase which is expected to deliver more consistent levels of sulforaphane. It is anticipat
31、ed that this technology has great potential for supplements and therapeutics as both glucoraphanin and the enzyme are naturally found in foods, have a long history of consumption and are stable. Upon consumption, glucoraphanin is enzymatically converted to a molecule called sulforaphane and it is su
32、lforaphane that shows bioactivity across all stages of cancer development. The enzyme responsible for this conversion is found naturally in plant material (such as broccoli), however it is typically inactivated during processing and cooking. Whilst the enzyme is also found in some gut microbes, the
33、conversion is inefficient and highly variable from person to person. Kraft Food Holdings patent application, (US2008311192) which was filed in June 2007, entitled, Enteric- coated Glucosinolates and Beta-thioglucosidases relates to a particulate composition comprising enteric- coated glucosinolate a
34、nd beta-thioglucosidase particles. The invention provides a method of converting glucosinolates to isothiocyanate in the small intestine following the oral administration of an enteric-coated chemoprotectant precursor composition comprising enteric-coated glucosinolate and beta-thioglucosidase parti
35、cles. In another aspect of the application, uncoated glucosinolate and beta-thioglucosinodase particles are provided in an enteric-coated capsule. The preferred composition is that the glucosinolate is glucoraphanin and the beta-thioglucosidase enzyme is myrosinase. The enteric coating facilitates r
36、elease of the composition in the small intestine where beta-thioglucosinodase enzyme converts glucosinolate to the chemoprotectant, isothiocyanate. Kraft Foods also has a patent, US7744937B1, entitled Chemoprotectants from Crucifer Seeds and Sprouts filed in August 2005, covering chemoprotectant pre
37、cursor compositions provided from crucifer seeds and 44 sprouts by treating aqueous extracts with adsorbents which substantially increases the ratio of certain highly chemoprotectant precursor compounds (alkyl glucosinolates such as glucoraphanin, a. k. a. sulforaphane glucosinolate) to undesirable
38、compounds such as indole glucosinolates (for example 4- hydroxyglucobrassicin). The extract has improved color and odor, and may be dried or used directly as an additive in a variety of foodstuffs. Harnessing gene technology for improved production University of Copenhagen Evgen also holds a researc
39、h collaboration with the University of Copenhagen. On 14 December 2010, this academic body announced that it had been successful in securing a grant for E1.8m from the Danish Strategic Research Council in order to develop a novel manufacturing platform designed to yield a rich source of pure glucora
40、phanin. The program will also complete safety studies and culminate in a human trial on the product. Glucoraphanin has to date, been too difficult to manufacture by chemical synthesis and too costly to purify from plant material. To get around these barriers, a research team from the University of C
41、openhagen is aiming to use its patented gene technology to recreate the entire biosynthetic pathway in a strain of yeast, using the 14 essential genes naturally used by broccoli plants. When the work is completed, it will be possible to manufacture glucoraphanin by simple fermentation at a cost that
42、 will enable its widespread use in foods and dietary supplements. The grant will fund the development program, called NAT4LIFE, led by Professor Barbara Halkier in collaboration with the human nutritionist, Professor Richard Mithen, Institute of Food Research (Norwich, UK), the yeast expert, Dr Uffe
43、 Mortensen of Denmarks Technical University and the health coach and communicator, Chris McDonald. Barbara Halkier is an expert in glucosinolate biosynthesis and was the first to successfully move this biosynthetic pathway to a plant that would not normally produce these molecules. The University of
44、 Copenhagens PCT application which has a priority date of February 2008, WO/2009/106985 entitled, Biosynthetic Engineering of Glucosinolates, by the inventors: Fernando Geu- Flores; Morten Thrane Nielsen; Michael Dalgaard Mikkelsen; Barbara Ann Halkier; and Morten Emil Moldrup 45 has already entered
45、 the national phase as EP2257630(A2), which was published on 08.12.2010 and US2011016582 which was published on 20.01.2011. The invention relates to methods and materials, such as newly characterized genes, and novel processes, for converting a host from a phenotype whereby the host is unable to car
46、ry out glucosinolate (GSL) biosynthesis or chain elongation from an amino acid GSL-precursor to a phenotype whereby the host carries out biosynthesis or elongation. Wider potential for sulforaphane In addition to reduction of risk of specific cancers, sulforaphane has been linked to eradication of H
47、. pylori, delaying age-related macular degeneration (AMD), reversal of diabetic heart damage and reduction of risk of cardiovascular disease; suggesting even wider potential for sulforaphane. 46 Other companies patenting in this area Table 2: Additional patenting in the area of Brassica isothiocyana
48、tes Patent application Patent application title Applicant/Inventor Priority date WO9419948 Chemoprotective isothiocyanates University John Hopkins 12/03/1993 WO/2000/001222 Development of novel, highly chemoprotectant crucifer germplasm University John Hopkins 01/07/1998 WO/2006/065736 Method of ext
49、raction of isothiocyanates in oil from Glucosinolate-containing plants University John Hopkins 14/12/2004 WO2006118941 Methods of suppressing UV light- induced skin carcinogenesis University John Hopkins 29/04/2005 WO/0045829 Brassica extracts or sulforaphane combination with resveratrol as antitumor agents Wassen International 20/02/1999 US5686108 Brassica vegetable supplement and process for manufacture Amway Corp 27/09/1995 US6433011(B1) Method for inhibition or treatment of colon tumorigenesis The American Health Foundation 08/03/2000 WO/2004/089065