Patent SG-11201408133T-A (SG)
Title: Dihydronaphthyridines and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
Inventor: FLYNN DANIEL L
IPC: A61K31/4375
Filed: 2012-06-07
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 2013/184119 A1 (51) International Patent Classification: A61K31/4375 ( 2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2012/041378 7 June 2012 (07.06.2012) English English (72) Inventors; and (71) Applicants FLYNN, : Daniel L. [US/US]; 4165 Black­ jack Oak Drive, Lawrence, Kansas 66047 (US). KAUF­ MAN, Michael D. [US/US]; 4708 Muirfield Drive, Lawrence, Kansas 66047 (US). (74) Agents: TUSCAN, Michael S. et al.; COOLEY LLP, 111 6th Street, N.W., Suite 1100, Washington, District of — Columbia 20001 (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, 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, KM, 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, 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, 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)) Published: — with international search report (Art. 21(3)) with sequence listing part of description (Rule 5.2(a)) o\ i-H i-H •t 00 i-H en i-H o CJ (54) Title: DIHYDRONAPHTHYRIDINES AND RELATED COMPOUNDS USEFUL AS KINASE INHIBITORS FOR THE TREATMENT OF PROLIFERATIVE DISEASES (57) Abstract: The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the ad­ ministration of an effective amount of dihydronaphthyridine a or a related compound. The present invention discloses the unexpec - ted utility of compounds that inhibit cKIT kinase across a broad range of c-KIT mutations, including complex occurrences of primary mutations (KIT exon 9 or 11) and secondary KIT mutations (exons 13, 14, 17 and 18) that may arise in individual, refract­ ory GIST patients. Also unexpected is the utility of compounds of the present invention inhibit to the problematic exon 17 D816V c- KIT mutation, for which there is currently no effective therapy.