Patent SG-11201810396Q-A (SG)
Title: Pegylated carfilzomib compounds
Inventor: LUEHR GARY
IPC: C07D405/12
Filed: 2017-05-23
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization 111111111111 0111010101111111111111111111111111111111111111111111111111111111111111# International Bureau (10) International Publication Number (43) International Publication Date ......0\"\"1 WO 2017/205392 Al 30 November 2017 (30.11.2017) WIPO I PCT (51) International Patent Classification: KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, C07D 405/12 (2006.01) A61K 47/10 (2017.01) MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, C08G 65/331 (2006.01) C07K 5/10 (2006.01) PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, A61P 35/00 (2006.01) C07K 5/117 (2006.01) SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, A61K 38/07 (2006.01) TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (21) International Application Number: (84) PCT/US2017/034029 Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (22) International Filing Date: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 23 May 2017 (23.05.2017) UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (25) Filing Language: English EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (26) Publication Language: English 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, (30) Priority Data: KM, ML, MR, NE, SN, TD, TG). 62/340,926 24 May 2016 (24.05.2016) US 62/485,812 14 April 2017 (14.04.2017) US Declarations under Rule 4.17: (71) Applicant: AMGEN INC. [US/US]; One Amgen Center — Dr., Thousand Oaks, California 91320 (US). as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(0 Published: (72) Inventors: LUEHR, Gary; 28570 Fox Hollow Drive, Hay- — ward, California 94542 (US). ANIK, Shabbir T.; 1740 with international search report (Art. 21(3)) Broadway, Apt. 704, San Francisco, California 94109 (US). = PENG, Ge; 1002 Solana Drive, Mountain View, California 94040 (US). DOTSENKO, Irina; 1337 Sunny Court Apt 3, = _ San Jose, California 95116 (US). PHIASIVONGSA, Pa- - = sit; 2712 Saint Regis Avenue, Brentwood, California 94513 = (US). ROMANINI, Dante; 5921 Tobias Avenue, Sherman Oaks, California 91411 (US). = = (74) Agent: REDDY, Prabhakar, G. et al.; One Amgen Center Dr., Thousand Oaks, California 91320 (US). Designated States (unless otherwise indicated, for every = (81) = 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, JP, KE, KG, KH, KN, KP, KR, = Title: PEGYLATED CARFILZOMIB COMPOUNDS = (54) = = = PEG I= 0 ,.,.. ,-, M 0, In 0 H C ) ii (R ) \"*.!'\"N N N 0 r.;.N .--- ir 0.,) 0 0 p h 0 , Ph in 0 ei IN Formula I 1-1 (57) : The present invention provides polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts 0 N thereof, of Formula I wherein R 1 , R 2 , linker, PEG, n and o are as defined herein. The invention also provides methods of making and P1 using these compounds to treat cancer, and particularly to treat hematological malignancies including multiple myeloma.