Patent CA-3015285-A1 (CA)
Inventor: TAI SERENE
IPC: C07D403/04
Filed: 2017-03-24
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY  (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau                               (10) International Publication Number (43) International Publication Date                                         WO    28 September 2017 (28.09.2017) WIPO I PCT (51) International Patent Classification:    (26) Publication Language:            English CO7D 295/185 (2006.01)    A61K 31/495 (2006.01) (30) Priority Data: CO7D 403/04 (2006.01)    A61K 31/496 (2006.01) 15/080,237                                                                  24 March 2016 (24.03.2016)    US CO7D 413/12 (2006.01)    A61K 31/42 (2006.01) CO7D 451/02 (2006.01)    A61K 31/445 (2006.01) (71) Applicant: UNIVERSITY OF PITTSBURGH - OF THE CO7D 409/08 (2006.01)    A61K 31/46 (2006.01) COMMONWEALTH SYSTEM OF HIGHER EDU-CO7D 407/04 (2006.01)    A61K 31/498 (2006.01) CATION [US/US]; 1st Floor Gardner Steel Conference CO7D 403/06 (2006.01)    A61K 31/12 (2006.01) Center, 1300 Thackeray Avenue, Pittsburgh, PA 15260 CO7D 401/08 (2006.01)    A61K 31/407 (2006.01)    (US). CO7D 405/06 (2006.01)    A61K 31/435 (2006.01) CO7D 487/04 (2006.01)    A61K 31/47 (2006.01) (72) Inventors: WIPE, Peter; Department of Chemistry, Chevron Science Center (1301 CHVRN), 219 Parkman Av-CO7D 217/16 (2006.01)    A61P 35/00 (2006.01) enue, Pittsburgh, PA 15260 (US). JOHNSON, James, K.;  CO7C 49/563 (2006.01) Department of Chemistry, Chevron Science Center (1301 (21) International Application Number:                                             CHVRN), 219 Parkman Avenue, Pittsburgh, PA 15260 (US). SKODA, Erin, M.; 8913 Early April Way Apt G, Columbia, MD 21046 (US). NELSON, Joel, B.; UPMC, (22) International Filing Date: 200 Lothrop St., Pittsburgh, PA 15213-2582 (US). WANG, 24 March 2017 (24.03.2017) Zhou; Shadyside Medical Center, Suite G40, 5200 Centre (25) Filing Language:               English Ave., Pittsburgh, PA 15232 (US). TAI, Serene; Department of Chemistry, Chevron Science Center (650 CHVRN), 219 (54) Title: SMALL MOLECULE INHIBITOR OF THE NUCLEAR TRANSLOCATION OF ANDROGEN  RECEPTOR FOR THE  TREATMENT OF CASTRATION-RESISTANT PROSTATE CANCER E 1200                                                 -4- Vehicle 10mgikg 0 900                                                     75mg/kg 4. ' -i FIG. 12 Days post-castration ,,R25 r (111) o 1-1 (57) Abstract: A compound, or a stereoisomer, pharmaceutically acceptable salt, or ester thereof, according to formula (III) or according IN to Table A, a pharmaceutical composition comprising said compound and at least one pharmaceutically acceptable additive, and a method for treating prostate cancer in a subject, comprising administering to the subject a therapeutically effective amount of said el compound. [Continued on next page]     111#11111111 Parkman Avenue, Pittsburgh, PA 15260 (US). TAKUBO, Keita; Department of Chemistry, Chevron Science Cen-ter (650 CHVRN), 219 Parkman Avenue, Pittsburgh, PA  15260 (US). MILLIGAN, John; Department of Chemistry, Chevron Science Center (1301 CHVRN), 219 Parkman Av-enue, Pittsburgh, PA 15260 (US). (74) Agent: GARDNER, Gillian; Klarquist Sparkman, LLP, One World Trade Center, Suite 1600, 121 SW Salmon Street, Portland, OR 97204 (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, 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)) (48) Date of publication of this corrected version: 02 November 2017 (02.11.2017) (15) Information about Correction: see Notice of 02 November 2017 (02.11.2017)