Patent SG-11201408140Q-A (SG)
Title: Crystalline forms of an androgen receptor modulator
Inventor: SMITH NICHOLAS D
IPC: A61K31/4439
Filed: 2013-06-04
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 12 December 2013 (12.12.2013) WIPOIPCT (10) International Publication Number WO 2013/184681 A1 (51) International Patent Classification: C07D 401/04 (2006.01) A61K31/4184 (2006.01) A61K31/4439 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/US2013/044116 (22) International Filing Date: 4 June 2013 (04.06.2013) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 61/656,888 7 June 2012 (07.06.2012) US (71) Applicants: ARAGON PHARMACEUTICALS, INC. [US/US]; 12780 El Camino Real, Suite 301, San Diego, CA 92130 (US). SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH [US/US]; 1275 York Aven­ ue, New York, NY 10065 (US). (72) Inventors: SMITH, Nicholas, D.; 1204 Beryl Street, San Diego, CA 92109 (US). HERBERT, Mark, R.; 4180 Amoroso St., San Diego, CA 92111 (US). OUERFELLI, ~~ Ouathek; 2077 Center Avenue, Apt. #3J, Fort Lee, NJ 07024 (US). DILHAS, Anna; Hasingerstrasse 32, CH- 4055 Basel (CH). (74) Agent: HOSTETLER, Michael, J.; Wilson Sonsini Goodrich & Rosati, 650 Page Mill Road, Palo Alto, CA == 94304 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, 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(H)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3)) [Continued on next page] (54) Title: CRYSTALLINE FORMS OF AN ANDROGEN RECEPTOR MODULATOR 00 •t 00 i-H en i-H o CJ Figure 1 XRPD of Form A 2-Theta Scale - (57) Abstract: Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoro - methylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the an­ drogen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity. WO 2013/184681 A11 lllll llllllll II llllll III lllll lllll III III III lllll lllll lllll lllll llll llll lllll lllllll llll llll — 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))