Wo 2009/053857 A3
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(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date 30 April 2009 (30.04.2009) WO 2009/053857 A3 (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, A61K 36/48 (2006.01) A61P 13/08 (2006.01) CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (21) International Application Number: HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, PCT/IB2008/05 1330 KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, (22) International Filing Date: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, ; April 2008 (08.04.2008) NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, (25) Filing Language: English US, UZ, VC, VN, ZA, ZM, ZW. (26) Publication Language: English (84) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of regional protection available): ARIPO (BW, GH, 2007/09260 26 October 2007 (26.10.2007) ZA GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, (71) Applicant (for all designated States except US): CSIR TM), European (AT, BE, BG, CH, CY, CZ, DE, DK, EE, [ZAIZA]; Scientia, 0002 Pretoria (ZA). ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR), OAPI (72) Inventors; and (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, (75) Inventors/Applicants (for US only): FOUCHE, Gerda NE, SN, TD, TG). [ZAIZA]; 485 Mulberry Street, Moreleta Park, 0044 Pre toria (ZA). MAHARAJ, Vinesh, Jaichand [ZA/ZA]; 25 Declarations under Rule 4.17: Naaldehout Street, Heuweloord, 0149 Pretoria (ZA). — of inventorship (Rule 4.1 7(iv)) MTHEMBU, Xolani [ZA/ZA]; House No. 644, ACD, Makwena Street, Ext. 1, 0064 Mahube Valley (ZA). Published: ACKERMAN, Louis [ZA/ZA]; 87B Dadelpalm Lane, — with international search report (Art. 21(3)) Wonderboom, 0182 Pretoria (ZA). VAN DER MERWE, Marina [ZA/ZA]; #40 Waterkloof 101, 170 Johan Rissik, — before the expiration of the time limit for amending the Drive, Waterkloof Ridge, 0181 Pretoria (ZA). claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) (74) Agents: FORBES, Craig, Paul et al; Adams & Adams, Adams & Adams, Place, 1140 Prospect Street, Hatfield, (88) Date of publication of the international search report: PO, Box 1014, 0001 Pretoria (ZA). 27 August 2009 (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (54) Title: MANAGEMENT AND TREATMENT OF BENIGN PROSTATIC HYPERPLASIA (57) Abstract: The invention provides the use of an extract of a plant of the genus Elephantorrhiza and at least one compound se lected from quercitin-3'-O-glucoside, trans-3-O-galloyl-3,3',5,5',7-pentahydroxyflavan, taxifolin-3'-O-glucoside, catechin and epi- catechin in the preparation of a medicament for the treatment of benign prostatic hyperplasia (BPH). The mode of action is by a route selected from blocking the conversion of testosterone to dihydrotestosterone by inhibiting the 5α-reductase enzyme or by re ducing oxidative stress or both. International application No PCT/IB2008/051330 A CLASSIFICATION OF SUBJECT MATTER INV. A61K36/48 A61P13/08 According to International Patent Classification (IPC) orto both national classification and IPC B. RELDS SEARCHED Minimum documentation searched (classification systam followed by classification symbols) A61K A61P Documentation searched other than minimum documentation to the extent that such documents are included in the fields searched Electronic data base consulted during the international search (name of data base and, where practical search terms used) EPO-Internal , WPI Data, BIOSIS, EMBASE, CHEM ABS Data C DOCUMENTS CONSIDERED TO BE RELEVANT Category * Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No WO 2006/013420 A (GENPROFILER S R L [IT]; 1-17 BETTUZZI SAVERIO [IT]; CORTI ARNALDO [IT]; COR) 9 February 2006 (2006-02-09) page U , line 5 - page 12, line 10; claims LIAO S : "THE MEDICINAL ACTION OF 1-17 ANDROGENS AND GREEN TEA EPIGALLOCATECHIN GALLATE" HONG KONG MEDICAL JOURNAL, XX, HK, vol . 7 , no. 4 , 1 December 2001 (2001-12-01), pages 369-374, XP009033309 ISSN: 1024-2708 figures 1,2 _ / Further documents are listed in the continuation of Box C See patent family annex * Special categories of cited documents 'T' later document published after the international filing date or pnonty date and not in conflict with the application but 'A' document defining the general state of the art which is not cited to understand the principle or theory underlying the considered to be of particular relevance invention 1 E" earlier document but published on or after the international 'X' document of particular relevance, the claimed invention filing date cannot be considered novel or cannot be considered to 1L" document which may throw doubts on pnonty claιm(s) or involve an inventive step when the document is taken alone which is cited to establish the publication date of another "Y" document of particular relevance, the claimed invention citation or other special reason (as specified) cannot be considered to involve an inventive step when the 'O" document referring to an oral disclosure, use exhibition or document is combined with one or more other such docu¬ other means ments such combination being obvious to a person skilled 1P' document published prior to the international filing date but in the art later than the pnonty date claimed '&' document member of the same patent family Date of the actual completion of the international search Date of mailing of the international search report 2 July 2009 15/07/2009 Name and mailing address of the ISA/ Authorized officer European Patent Office P B 5818 Patentlaan 2 NL - 2280 HV Rl|SWI|k TeI (+31-70) 340-2040 Friederich , Martin Fax (+31-70) 340-3016 Form PCT/ISA/210 (second sheet) (April 200S) C(Continuation). DOCUMENTS CONSIDERED TO BE RELEVANT Category * Citation of document, with indication, where appropriate, of the relevant passages Relevant to claim No. HIIPAKKA R A ET AL: "Structure-activity 1-17 relationships for inhibition of human 5[alpha]-reductases by polyphenols" BIOCHEMICAL PHARMACOLOGY 20020315 US, vol. 63, no. 6 , 15 March 2002 (2002-03-15), pages 1165-1176, XP002534993 ISSN: 0006-2952 figures 2,4; tables 1,4 WANJALA C C ET AL: "A new stilbene glycoside from Elephantorrhiza goetzei." FITOTERAPIA AUG 2001, vol. 72, no. 6 , August 2001 (2001-08), pages 649-655, XP002534994 ISSN: 0367-326X the whole document MOYO FORTUNE ET AL: "A new flavan from Elephantorrhiza goetzei" FITOTERAPIA, vol. 70, no. 4 , August 1999 (1999-08), pages 412-416, XP002534995 ISSN: 0367-326X the whole document A ,P BISSON J-F ET AL: "Preventive effects of ACTICOA powder, a cocoa polyphenol ic extract, on experimentally induced prostate hyperplasia in W istar-Unilever rats" JOURNAL OF MEDICINAL FOOD, MARY ANN LIEBERT, LARCHMONT, NY, US, vol. 10, no. 4 , 1 December 2007 (2007-12-01), pages 622-627, XP009119186 ISSN: 1096-620X page 623, paragraph 2 ; table 3 Form PCT/ISA/210 (continuation oi second sheet) (April 2005) ca on o Information on patent family members PCT/IB2008/051330 Patent document Publication Patent family Publication cited in search report date member(s) date WO 2006013420 09-02-2006 CA 2612149 A l 09-02-2006 EP 1781375 A2 09-05-2007 JP 2008508252 T 21-03-2008 US 2008194675 Al 14-08-2008 Form PCT/ISA/210 (patent family annex) (April 2005).