Patent SG-11201805380Y-A (SG)
Title: Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapy
Inventor: KUNG HANK F
IPC: G01N33/60
Filed: 2016-12-22
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 6 July 2017 (06.07.2017) WIPOIPCT (10) International Publication Number WO 2017/116994 A1 (51) International Patent Classification: G01N33/60 (2006.01) C12Q 1/37{2006.01) G01N33/68 (2006.01) (21) International Application Number: PCT/US2016/068327 (22) International Filing Date: 22 December 2016 (22.12.2016) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/273,786 31 December 2015 (31.12.2015) US 15/385,490 20 December 2016 (20.12.2016) US (71) Applicant: FIVE ELEVEN PHARMA INC. [US/US]; 3700 Market St. Suite 305, Philadelphia, Pennsylvania 19104 (US). (72) Inventors: KUNG, Hank F.; 232 N. Highland Road, Springfield, Pennsylvania 19064 (US). PLOESSL, Karl; 1525 Delaware Ave. #3, Wilmington, Delaware 19806 (US). CHOI, Seok Rye; 52 Andrew Court, Aston, Pennsylvania 19014 (US). ZHA, Zhihao; 221 S. 44th Street, Apt. 2-F, Philadelphia, Pennsylvania 19104 (US). WU, Zehui; 503S 41st Street, Apt. 302, Philadelphia, Pennsylvania 19104 (US). (74) Agents: COVERT, John M. et al.; Sterne, Kessler, Gold­ stein & Fox PLLC, 1100 New York Avenue, NW, Wash­ ington, District of Columbia 20005 (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)) — 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)) •t 0\ 0\ o CJ (54) Title: UREA-BASED PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITORS FOR IMAGING AND THER­ APY (57) : The present invention relates to compounds according to Formula I and Formula IV. These compounds display very good binding affinities to the PSMA binding sites. They can be labeled with [68Ga]GaC13 with high yields and excellent radiochem - ical purity. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I or Formula IV, or a pharmaceutically acceptable salt thereof.