artCy {in CDR) y-region mAb constant region peptide---N () INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 03 May 2018 (03.05.2018) WIP0 I PCT omit °nolo omm im °mono lio iflo oimIE (10) International Publication Number WO 2018/081370 Al (51) International Patent Classification: C07K 14/47 (2006.01) A61K 38/04 (2006.01) (21) International Application Number: PCT/US2017/058455 (22) International Filing Date: 26 October 2017 (26.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/413,586 27 October 2016 (27.10.2016) US 62/413,613 27 October 2016 (27.10.2016) US (71) Applicant: JANSSEN PHARMACEUTICA NV [BE/BE]; Turnhoutseweg 30, B-2340 Beerse (BE). (72) Inventor; and (71) Applicant (for US only): MACIELAG, Mark [US/US]; 1400 McKean Road, Spring House, PA 19477 (US). (72) Inventors: MACIELAG, Mark; 1400 McKean Road, Spring House, PA 19477 (US). PATCH, Raymond, J.; 1400 McKean Road, Spring House, PA 19477 (US). ZHANG, Rui; 1400 McKean Road, Spring House, PA 19477 (US). CASE, Martin, A.; 3210 Merryfield Row, San Diego, CA 92121 (US). RANGWALA, Shamina, M.; 1400 McKean Road, Spring House, PA 19477 (US). LEONARD, James, N.; 1400 McKean Road, Spring House, PA 19477 (US). CAMACHO, Raul, C.; 1400 McKean Road, Spring House, PA 19477 (US). HUNTER, Michael, J.; 3210 Merryfield Row, San Diego, CA 92121 (US). D'AQUINO, Katharine, E.; 1400 McKean Road, Spring House, PA 19477 (US). EDWARDS, Wilson; 3210 Merryfield Row, San Diego, CA 92121 (US). SWANSON, Ronald, V.; 3210 Merryfield Row, San Diego, CA 92121 (US). MAN, Wenying; 1400 McKean Road, Spring House, PA 19477 (US). ZHANG, Yue-Mei; 1400 McKean Road, Spring House, PA 19477 (US). WALL, Mark; 1400 McK- ean Road, Spring House, PA 19477 (US). CHI, Ellen; 3210 Merryfield Row, San Diego, CA 92121 (US). (74) Agent: BARANIAK, Andrew, P. et al.; Panitch Schwarze Belisario & Nadel LLP, Two Commerce Square, 2001 Mar- ket Street, Suite 2800, Philadelphia, PA 19103 (US). (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, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) = (54) Title: ANTIBODY-COUPLED CYCLIC PEPTIDE TYROSINE TYROSINE COMPOUNDS AS MODULATORS OF NEU- = ROPEPTIDE Y RECEPTORS Fig. I O (57) : The present invention comprises conjugates comprising a monoclonal antibody conjugated to a cyclic PYY peptide. \' The invention also relates to pharmaceutical compositions and methods for use thereof. The novel conjugates are useful for preventing, C treating or ameliorating diseases and disorders disclosed herein. [Continued on next page] 1-1 O N 1-1 00 WO 2018/081370 Al MIDEDIMOHNOIREIEREIMMENHOMMEHOIS Published: with international search report (Art. 21(3)) before the expiration of the time limit for amending the 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))
ANTIBODY-COUPLED CYCLIC PEPTIDE TYROSINE TYROSINE COMPOUNDS AS MODULATORS OF NEUROPEPTIDE Y RECEPTORS