Patent SG-11201907209Q-A (SG)
Title: Modified relaxin polypeptides comprising a pharmacokinetic enhancer and uses thereof
Inventor: DUBOWCHIK GENE
IPC: C07K14/64
Filed: 2018-02-08
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 16 August 2018 (16.08.2018) WIPO I PCT 0111111010 0111 °nolo DID IH mo mumionio oimIE (10) International Publication Number WO 2018/148419 Al (51) International Patent Classification: (07x14/64 (2006.01) A61K 38/22 (2006.01) (21) International Application Number: PCT/US2018/017436 (22) International Filing Date: 08 February 2018 (08.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/456,161 08 February 2017 (08.02.2017) US 62/627,411 07 February 2018 (07.02.2018) US (71) Applicant: BRISTOL-MYERS SQUIBB COMPANY [US/US]; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). (72) Inventors: DUBOWCHIK, Gene, M.; 5 Research Parkway, Wallingford, Connecticut 06492 (US). GUD- MUNDSSON, Olafur, S.; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). HAN, Xiaojun; 5 Research Parkway, Wallingford, Connecticut 06492 (US). LAWRENCE, R., Michael; 350 Carter Road, Hopewell, New Jersey 08540 (US). LIPOVSEK, Dasa; 100 Beaver Street, Waltham, Massachusetts 02453 (US). MADSEN, Cort, S.; 311 Pennington-Rocky Hill Road, Pennington, New Jersey 08543 (US). MAPELLI, Claudio; 465 Brig- gs Road, Langhorne, Pennsylvania 19047 (US). MORIN, Paul, E.; Route 206 and Province Line Road, Princeton, New Jersey 08543 (US). MYERS, Michael, C.; 350 Carter Road, Hopewell, New Jersey 08540 (US). (74) Agent: TESKIN, Robin, L. et al.; Leclair Ryan, P.C., Intel- lectual Property Department, 2318 Mill Road, Suite 1100, Alexandria, Virginia 22314 (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 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a)) (54) Title: MODIFIED RELAXIN POLYPEPTIDES COMPRISING A PHARMACOKINETIC ENHANCER AND USES THEREOF 1-1 FIG. I 71' WT-RLX A-chain QLYSALANKCCHVGCTKRSLARFC B-chain ASWMEEVIKLCGRELVRAQIAICGMSTWS 1 1' 1 -1 (57) : The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypep- © tides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis. O