Patent SG-11201907420V-A (SG)
Title: Inhibition of smarca2 for treatment of cancer
Inventor: GRASSIAN ALEXANDRA ROSE
IPC: C07H21/04
Filed: 2018-02-28
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 07 September 2018 (07.09.2018) WIP0 I PCT omit VIII °nolo omioolioliollool IIII mom oimIE (10) International Publication Number WO 2018/160636 Al (51) International Patent Classification: A61K 31/70 (2006.01) C07H 21/02 (2006.01) A61K 31/7088 (2006.01) C07H 21/04 (2006.01) A61K 38/00 (2006.01) C12N 5/00 (2006.01) (21) International Application Number: PCT/US2018/020124 (22) International Filing Date: 28 February 2018 (28.02.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/464,811 28 February 2017 (28.02.2017) US 62/542,241 07 August 2017 (07.08.2017) US (71) Applicant: EPIZYME, INC. [US/US]; 400 Technology Square, 4th Floor, Cambridge, Massachusetts 02139 (US). (72) Inventors: GRASSIAN, Alexandra Rose; 25A Highland Avenue, Cambridge, Massachusetts 02139 (US). DREW, Allison; 254 Florence Avenue, Arlington, Massachusetts 02476 (US). (74) Agent: ERLACHER, Heidi; Cooley LLP, 1299 Pennsyl- vania Avenue, Suite 700, Washington, District of Columbia 20004 (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, 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, (54) Title: INHIBITION OF SMARCA2 FOR TREATMENT OF CANCER FIGURE I -0.5 -1 0 en < 4.5 ui ec 00 o -2 eka ez -2.5 : -- a 2 1-1 Cr) O 1-1 00 1-1 O C \" 15 ' n High SMARCA4 expression ow Low SMARCA4 expression Cell Lines (57) : The present disclosure provides treatment modalities, e.g., strategies, treatment methods, patient stratification methods, combinations, and compositions that are useful for the treatment of disorders, e.g., proliferative disorders, such as certain cancer. Some aspects of this disclosure provide treatment modalities, methods, strategies, compositions, combinations, and dosage forms for the treatment of cell proliferative disorders, e.g., cancers with decreased activity or function, or loss of function, of SMARCA4 with a SMARCA2 antagonist. [Continued on next page] WO 2018/160636 Al MIDEDIMOMOIDEIREEMOMOHINIMEINIEOMEMOIS 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(11)) 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))