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(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 1 1 September 2009 (11.09.2009) (51) International Patent Classification: A61K 38/05 (2006.01) A61K 38/26 (2006.01) A61K 38/22 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: (10) International Publication Number W O 2009/109927 A 3 (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. PCT/IB2009/050890 (22) International Filing Date: 4 March 2009 (04.03.2009) (25) Filing Language: (26) Publication Language: (30) Priority Data: English English US US (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, 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): TEL TM), European (AT, BE, BG, CH, CY, CZ, DE, DK, EE, HASHOMER MEDICAL RESEARCH INFRAS¬ ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, TRUCTURE AND SERVICES LTD. [IL/IL]; The MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR), Chaim Sheba Medical Center Tel Hashomer, 52621 RaOAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, mat Gan (IL). MR, NE, SN, TD, TG). 61/033,9 12 61/033,908 5 March 2008 (05.03.2008) 5 March 2008 (05.03.2008) (72) Inventors; and (75) Inventors/ Applicants (for US only): KARASIK, Avraham [IL/IL]; 32 Habanim Street, 47223 Ramat Hasharon (IL). RUBINEK, Tamar [IL/IL]; 7/32 Hadekel Street, 60407 Or Yehuda (IL). WOLF, Ido [IL/IL]; 7/32 Hadekel Street, 60407 Or Yehuda (IL). KAUFMAN, Bella [IL/IL]; 12 Hameyasdim Street, 55521 Kiryat Ono (IL). (74) Agent: GUR, Erez; Pob 1372, 441 13 Kfar Saba (IL). Published: — — with international search report (Art. 21(3)) before the expiration o the time limit for amending the f claims and to be republished in the event of receipt of amendments (Rule 48.2(h)) with sequence listing part of description (Rule 5 . 2 (a)) — (88) Date of publication of the international search report: 2 5 February 2010 (54) Title: GLP-I RECEPTOR AGONISTS AND RELATED ACTIVE PHARMACEUTICAL INGREDIENTS FOR T REA T MENT OF CANCER Control 500 ng/day Exendin-4 2 µg/day Exendm-4 weeks FIG 12 (57) Abstract: Disclosed are methods and compositions for increasing concentrations of GLP-I receptor agonists in the body for the treatment of cancer, alone or together with other active pharmaceutical ingredients such a s chemotherapeutic agents or h o r mone-regulating agents. nterna ona app cat o n o PCT/IB2009/050890 A . CLASSIFICATION O F SUBJECT MATTER INV. A61K38/05 A61K38/22 A61K38/26 A61P35/00 According Io International Patent Classification (IPC) o r to both national classification and IPC B . FIELDS SEARCHED Minimum documentation searched (classification system followed b y classification symbols) A61K Documentation searched other than minimum documentation to the extent thai such documents are included i n the fields searched Electronic data base consulted during the internalional search (name o f data base and, where practical, search terms used) EPO-Internal, Sequence Search, EMBASE, BIOSIS, WPI Data C . DOCUMENTS CONSIDERED T O BE RELEVANT Category' Citation ol document, with indication, where appropriate, o f the relevant passages Relevant I o claim No P 1X U S 2008/194672 A l (HOVEYDA HAMID [CA] ET AL) 14 August 2008 (2008-08-14) paragraphs , ; claims 32,38,40 WO 2007/127204 A (POINT THERAPEUTICS INC [US]; JESSON MICHAEL I [US]; MCLEAN PAUL A [US]) 8 November 2007 (2007-11-08) page 13, lines 22-26 page 55, line 1 2 - page 69, line 23; claims 2,3,5-7 page 3 , lines 30-32 page 15, line 4 - page 22, line 4 -/-- 1,2,4,5, 15 1,3,4,6, 17-26, 39-50 Further documents are listed in the continuation o l Box C * See patent family annex Special categories o f cited documents "A' document defining ihe general stale o f the art which is nol considered to be ol particular relevance "E' earlier document but published on o r after the international filing dale "L" document which may throw doubts o n priority cla ιm(s) o r which is cued Io establish the publication date o l another citation o r other special reason (as specilied) "O" document relernng I o a n oral disclosure, use exhibition o r other means "P" document published prior t o Ihe international filing date but later than Ihe priority date claimed Dale o f Ihe actual completion o l the international search "T" later documenl published after Ihe international filing dale o r pno πl y dale and nol in conflict with Ihe application but cited to understand the principle o r theory underlying the invention "X" document o l particular relevance, the claimed invention cannot be considered novel o r cannot be considered I o involve a n inventive step when the document is taken alone "Y" document o l particular relevance, the claimed invention cannot be considered to involve a n inventive step when the document is combined with one o r more olher such docu¬ ments, such combination being obvious Io a person skilled i n Ihe art '&" document member o l Ihe same patent family Dale o l mailing o l Ihe international search report 2 9 December 2009 Name and mailing address o l Ihe ISA/ European Patent Office, P B 5818 Pat βntlaan 2 N L - 2280 HV RlJSWijk TeI (+31-70) 340-2040, Fax (+31-70) 340-3016 Form PCT/ISA/210 (second sheet) (Ap πl 2005) 11/01/2010 Authonzed oflicer Greif, Gabriel a n erna ona app ca o n o PCT/IB2009/050890 C(Conti πuat ιon). Category' Cilalion DOCUMENTS CONSIDERED T O B E RELEVANT o l document, with indication, where appropriate Ot the relevant passages Relevanl to claim N o X WICKI ANDREAS ET AL: " [Lys40(Ahx-DTPA-lllIn )NH2]-Exendin-4 is a highly effici ent radiotherapeutic for g l ucagon-l i k e peptide-1 receptor-targeted therapy for insul i noma . " CLINICAL CANCER RESEARCH : A N OFFICIAL JOURNAL OF THE AMERICAN ASSOCIATION FOR CANCER RESEARCH 1 5 JUN 2007, vol . 13, no. 12, 1 5 June 2007 (2007-06-15) , pages 3696-3705, XP002561708 ISSN: 1078-0432 abstract page 3704, l eft-hand col umn, paragraph 3page 3705, right-hand col umn, paragraph 1 BAGGIO L L ET A L : "Gl ucagon-l ike peptide-1 and glucagon-l ike peptide-2" BAILLIERE' S BEST PRACTICE AND RESEARCH . CLINICAL ENDOCRINOLOGYAND METABOLISM, BAILLIERE TINDALL , LONDON, GB, vol . 18, no. 4 , 1 December 2004 (2004-12-01 ) , pages 531-554 , XP004631153 ISSN: 1521-690X the whol e document 27-32 A 1-50 A 98/08871 A (NOVONORDISK A S [DK] ; KNUDSEN LISELOTTE BJERRE [DK] ; SOERENSEN PER OLAF ) 5 March 1998 ( 1998-03-05) WO 1 ,2,4,5 7-16, 18-38 , cited i n the appl ication the whol e document A WO 00/09666 A (US HEALTH [US] ; EGAN JOSEPHINE [US] ; PERFETTI RICCARDO [IT] ; PASSANITI ) 2 4 February 2000 (2000-02-24) cited i n the appl ication the whol e document E P 1 629 849 A (AMYLIN PHARMACEUTICALS INC 1 , 2 ,4,5 , 7-16 , 18-38 A [US] ) 1 March 2006 (2006-03-01 the A whol e document "Bi o l ogy of ) 1 ,2,4,5 7-16, 18-38 , BAGGIO ET A L : Incretins : 1-50 GLP-I and GIP" GASTROENTEROLOGY, ELSEVIER , PHILADELPHIA, PA, vol . 132, no. 6 , 1 0 May 2007 (2007-05-10) , pages 2131-2157 , XP022072503 ISSN : 0016-5085 abstract figures 2-4 page 2148, l eft-hand col umn, paragraph 2page 2149, right-hand col umn, paragraph 1 Form PCT/ISA/210 (conlmualion o l second sheet) (April 2005) nterna ona app ca o n o PCT/IB2009/050890 C(Co πtinuation). Category" DOCUMENTS CONSIDERED T O B E RELEVANT Citation ol document, with indication, where approp πate. ol the relevant passages Relevant to claim No GADSBY ET AL: "New treatments for type 2 diabetes-The DPP4 inhibitors" 20071203, vol . 1 , no. 4 , 3 December 2007 (2007-12-03), pages 209-211, XP022384653 the whole document WO 99/47152 A (SLOAN KETTERING INST CANCER [US]; HOUGHTON ALAN N [US]; WESLEY UMADEVI) 2 3 September 1999 (1999-09-23) the whole document P ,A 1,3, 17-26, 39-50 1,3, 17-26, 39-50 JIN ET AL: "Why diabetes patients are more prone t o the development o f colon cancer?" MEDICAL HYPOTHESES, EDEN PRESS, PENRITH, US, vol . 71, no. 2 , 1-50 1 August 2008 (2008-08-01), pages 241-244, XP022776269 ISSN: 0306-9877 [retrieved o n 2008-05-05] the whole document Form PCT/ISA/210 (conlinuation ol second sheet) (April 2005) I nternational application No Information o n patent family members PCT/IB2009/050890 Patent family member(s) Publication date Patent document cited in search report Publication date US 2008194672 Al 14-08-2008 AU CA EP WO 2008241532 2677399 2118080 2008130464 Al Al Al Al 30-10-2008 30-10-2008 18-11-2009 30-10-2008 WO 2007127204 9808871 A A 08-11-2007 05-03-1998 NONE WO AT AU AU BR CA CN CZ DE DK EP ES HU JP JP JP JP KR NO NO PL PT RU WO 356830 732957 3847897 9711437 2264243 1232470 9900629 69737479 0944648 0944648 2283025 9903714 2000500505 3149958 2001011095 2006348038 20000035964 990950 2009027 331896 944648 2214419 445006 776514 5552499 2339326 2028269 1105460 2002522068 2007209348 2007041951 7056734 T B2 A A Al A A3 T2 T3 Al T3 A2 T B2 A A A A Il Al E C2 15-04-2007 03-05-2001 19-03-1998 18-01-2000 05-03-1998 20-10-1999 14-07-1999 29-11-2007 02-07-2007 29-09-1999 16-10-2007 28-03-2000 18-01-2000 26-03-2001 16-01-2001 28-12-2006 26-06-2000 28-04-1999 30-11-2009 16-08-1999 26-06-2007 20-10-2003 15-10-2009 09-09-2004 06-03-2000 24-02-2000 25-02-2009 13-06-2001 23-07-2002 23-08-2007 22-02-2007 06-06-2006 0009666 A 24-02-2000 AT AU AU CA EP EP T B2 A Al Al A2 JP JP US US EP WO T A Al Bl 1629849 9947152 A A 01-03-2006 23-09-1999 NONE AU 3357299 A 11-10-1999 Form PCT ΛSA/210 (patent lamily a πnax) (April 2005) International application No INTERNATIONAL SEARCH REPORT Box No. I 1 PCT/IB2009/050890 Nucleotide and/or amino acid sequence(s) (Continuation of item 1.b of the first sheet) With regard t o any nucleotide and/or amino acid sequence disclosed in the international application and necessary to the claimed invention, the international search was carried out o n the basis o f a type of material I I b I I a sequence listing table(s) related to the sequence listing format o f material I I c I I o n paper in electronic form time o f filing/furnishing IX I IX J I 2 J contained in the international application a s filed filed together with the international application in electronic form furnished subsequently t o this Authonty for the purpose o f search In addition in the case that more than one version o r copy of a sequence listing and/or table relating thereto has been filed o r furnished, the required statements that the information in the subsequent o r additional copies is identical to that in the application a s filed o r does not go beyond th θ application a s filed, a s appropriate, were furnished 3 Additional comments Form PCT/ISA/210 (continuation of first sheet (1)) (April 2005)