Patent SG-11201811062X-A (SG)
Title: Cysteine engineered fibronectin type iii domain binding molecules
Inventor: ANDERSON MARK
IPC: A61K38/00
Filed: 2017-06-21
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) -., (19) World Intellectual Property 1111111011110111011111111010111110011111111111111110111111111111ffinill Organization International Bureau (10) International Publication Number (43) International Publication Date ......'\"' WO 2017/223180 A3 28 December 2017 (28.12.2017) WIP0 I PCT (51) International Patent Classification: McKean Road, Spring House, PA 19477 (US). DIEM, A61K 38/00 (2006.01) C07K 16/28 (2006.01) Michael; 1400 McKean Road, Spring House, PA 19477 A61K 38/39 (2006.01) C12N 15/09 (2006.01) (US). GOLDBERG, Shalom; 1400 McKean Road, Spring C07K 14/78 (2006.01) House, PA 19477 (US). HYUN, Linus; 1400 McKean (21) International Application Number: Road, Spring House, PA 19477 (US). JACOBS, Steven; PCT/US2017/038506 1400 McKean Road, Spring House, PA 19477 (US). KING, Alastair; 27204 Cuivre Drive, Lake Saint Louis, MO 63367 (22) International Filing Date: (US). KLEIN, Donna; 1400 McKean Road, Spring House, 21 June 2017 (21.06.2017) PA 19477 (US). MOORES, Sheri; 1400 McKean Road, Spring House, PA 19477 (US). O'NEIL, Karyn; 1400 (25) Filing Language: English McKean Road, Spring House, PA 19477 (US). PICHA, (26) Publication Language: English Kristen; 1400 McKean Road, Spring House, PA 19477 (30) Priority Data: (US). 62/352,776 21 June 2016 (21.06.2016) US (74) Agent: SHIRTZ, Joseph, F. et al.; Johnson & Johnson, One Johnson & Johnson Plaza, New Brunswick, NJ 08933 (71) Applicant: JANSSEN BIOTECH, INC. [US/US]; (US). 800/850 Ridgeview Drive, Horsham, PA 19044 (US). (81) Designated States (unless otherwise indicated, for every (72) Inventors: ANDERSON, Mark; 8020 Fairview Lane, kind of national protection available): AE, AG, AL, AM, Eagleville, PA 19403 (US). ATTAR, Ricardo; 1400 AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, = (54) Title: CYSTEINE ENGINEERED FIBRONECTIN TYPE III DOMAIN BINDING MOLECULES = SEQ ID NO; = 18 L p7inclWivsEVTEnstl2i.,814 (60) OF - HOFY - 68FLIQYQF;SEXVGgAIALTNIPOS21 4 ,SYtTLTG EEE 1.9 LPAPKNLVVSRVTEDSLRLSW YD-RDEYDSFIJQYQ3SEKVGRAINTUVPGSERSYDIaG 20 LPAPKNLVVSEVTEDSLRLSW YN-GDHYDSELIOYQESEKVGEAINLTVPGSERSYDLTG _ 2 . 1 LPAPKNLVVSEVTEDSLRLSW DP7RGPTESPITOOSEKVGEAIWLIVPGSERSYDLT = 22 LPAPKNLVVSEVTEDSLRLSW WP-YADLDSFLIMESEKVGEAINLTVPCSEPSYDLTC = 73 1,PAPKNINvSET1MSLRLSW IN - MHEMSFLIVQ1SEKVOtaINLTV8GnRSYDLTG 24 L PAPKNLVVSEVTE D S LRL SW 7.YDLG.DHFDSEL IQYQESEKVGEAINLTVPGSERS YDLTG 2.5 LPAPKNLVVSEVTEDSLRLSW DP-WAFYESFLIQYOaSEKVGEAINLTVPGSERSYDLTG = 27 'LPAPKNLVVSEVTEDSARLS DP-WAVYESELIOYOESEKVGEAIVLTVPGSERSYDLTG = 29 LPAMINVSEVTE081Aus WP-YA0LDBFLIOYQE88XyGEAINLTI7PGSERgyaLTG 1.07 LPAPKNLVVSEVTEDSARLSW DP-HGETDSFLIQYQESEKVGEATVLTVPQSERSYDLTG = = _ 108 LPAPKNLVVSEVTEDSARLSW DP-WAFYESFLIQYQESEKVGEAIVLTVPGSERSYDLTG 10.9 LPAPKNLVVSEVTEDSARLSW DP-HAFYESFLIQYQESEKVGEAIVLTVPGSERSYDLTG 110 LPAPKNLVVSEVTEDSARLSW DP-HOFTDSFLIQYQESEKVGEAIVLTVPGSERSYDLTG = ..*......******* kle.* :. = - 18 LIOGT8x1V8IYOV4NVYK0TWRGLPLSAEFTT (94) - = 19 LKPGTEYTVSIYGV-INVYKDTNMRGLPLSAEFTT = 20 LKPGTEETVSIYGViNVYKDTNMPGDPLSAEFTT 21 LKPGTEYTVSIYGViNVYKDTNMAGLPISAEFTT = 22 LKPGTEYTVSIYGVSNVYKDTNMPGLPLSAEFTT _ = 2.3 VF,PGTEYTITSlyGV iNVYKIDTNIvIRGLPL8AE,FIT — 24 L.KPGTEYTVSIYGV-INVYKDTNMPOLPLSAEPTT 25 LKPGTEYTVSIYGVEINVYKDTNNRGLPLSAEETT = 27 LKPGTEYTVSIYGV - INVYKDTNMRGLPLSAIVTT 29 LKPGTEYTVSIYGViNVYKDTNMRGDPLSAEFTT 101 LEKTEXTV$IYGViNITYK0TWROLPL821InT — 108 LKPGTEYTVSIYGV-INVYKDTNIRGLPLSAIFTT 109 LXPG . TEYTv81YONNUINIOTNIROIPLSAIEIT FIG. 114 M 110 LKPGTEYTVSIYGViNVYKOTNIRGLPLSAIFTT © GC ,_ 1 (57) : Cysteine engineered monospecific and bispecific EGFR and/or c-Met FN3 domain containing molecules comprising M one or more free cysteine amino acids are prepared by mutagenizing a nucleic acid sequence of a parent molecule and replacing one or e• 1 more amino acid residues by cysteine to encode the cysteine engineered FN3 domain containing monospecific or bispecific molecules; el ---- expressing the cysteine engineered FN3 domain containing molecules; and recovering the cysteine engineered FN3 domain containing ir---- molecule, isolated cysteine engineered monospecific or bispecific FN3 domain containing molecules may be covalently attached to a 1-1 © detection label or a drug moiety and used therapeutically. N O [Continued on next page] WO 2017/223180 A3 IMEDIMO DOI 01011MMEMODIMOIIIIHMOMMEEN 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). 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)) (88) Date of publication of the international search report: 01 February 2018 (01.02.2018)