Patent SG-11201900328W-A (SG)
Title: Inhibitors of cyclin-dependent kinase 7 (cdk7)
Inventor: MARINEAU JASON
IPC: C07D401/14
Filed: 2017-07-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1#11101111 0 11101 HOE 3E1 0 0111111 0111 OM HEIR 1111 OEN Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/013867 Al 18 January 2018 (18.01.2018) W I PO I PCT (51) International Patent Classification: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, C07D 401/14 (2006.01) A61K 31/506 (2006.01) OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, A61P 35/00 (2006.01) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, (21) International Application Number: TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. PCT/US2017/042017 (84) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of regional protection available): ARIPO (BW, GH, 13 July 2017 (13.07.2017) GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (25) Filing Language: English TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (26) Publication Language: English 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, (30) Priority Data: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 62/361,852 13 July 2016 (13.07.2016) US KM, ML, MR, NE, SN, TD, TG). (72) Inventors; and Published: (71) Applicants: MARINEAU, Jason, J. [US/US]; 2 MacKin- — with international search report (Art. 21(3)) tosh Street, Franklin, MA 02038 (US). ZAHLER, Robert — before the expiration of the time limit for amending the [US/US]; 5 East Welling Avenue, Pennington, NJ 08534 claims and to be republished in the event of receipt of (US). CIBLAT, Stephane [CA/CA]; 607-408 Rue Saint amendments (Rule 48.2(h)) Jacques, Montreal, Quebec, H2Y 1S2 (CA). WINTER, _ Dana, K. [CA/CA]; 431 Chemin de la Montagne, Rigaud, — Quebec, JOP 1P0 (CA). KABRO, Anzhelika [CA/CA]; = 815, 49e Avenue, Lachine, Quebec, H8T 2T3 (CA). ROY, 815, 49e Avenue, Lachine, = Stephanie [CA/CA]; Quebec, H8T 2T3 (CA). SCHMIDT, Darby [US/US]; 14 Mead Rd., Arlington, MA 02474 CHUAQUI, Claudio (US). 83 Menotomy Rd., Arlington, MA 02476 = [US/US]; (US). MALOJCIC, Goran [HR/US]; 1 Emerson Place, Apt = 7C, Boston, MA 02114 PIRAS, Henri (US). [FR/CA]; 201-6416 Rue de Ecores, Montreal, Quebec, H2G 2J5 (CA). = WHITMORE, Kenneth, Matthew [CA/CA]; 4974-217 = Place de la Savane, Montreal, Quebec, H4P OB1 (CA). — LUND, Kate-Iyn [CA/CA]; 15, 56e Avenue, Lachine, Que- bec, H8T 3B8 SINKO, Bill 37 Wyvern St., (CA). [US/US]; = Roslindale, MA 02131 (US). SPROTT, Kevin [US/US]; 40 = Rolling Lane, Needham, MA 02492 (US). (74) Agent: LARKIN, Angelyn et al.; Goodwin Procter LLP, 100 Northern Avenue, Boston, MA 02210 (US). = = (81) Designated States (unless otherwise indicated, for every = kind AE, AG, AL, AM, of national protection available): 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, Il IN (54) Title: INHIBITORS OF CYCLIN DEPENDNT KINASE 7 (CDK7) of (57) : The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hy- en drates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involv- C ing the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple ----. myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. WD Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity 11 c;;;; ) of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. ei O