Patent SG-11201903144P-A (SG)
Title: Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
Inventor: ANDREWS STEVEN W
IPC: A61K31/437
Filed: 2017-10-10
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property 1#11101111 0 11101 HOE 3E1 0 0111101111 01011101110 El MEV OEN Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/071447 Al 19 April 2018 (19.04.2018) WIP0 1 PCT (51) International Patent Classification: Street, Boulder, Colorado 80301 (US). MORENO, David CO7D 471/04 (2006.01) A61P 35/00 (2006.01) A. [US/US]; c/o Array BioPharma Inc., 3200 Walnut Street, A61K 31/437 (2006.01) Boulder, Colorado 80301 (US). TANG, Tony P. [US/US]; (21) International Application Number: c/o Array BioPharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). REN, Li [US/US]; c/o Array Bio- PCT/US2017/055983 Pharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (22) International Filing Date: (US). 10 October 2017 (10.10.2017) (74) Agent: FOLLETT, Angela D. et al.; Fish & Richardson (25) Filing Language: English P.C., P.O. Box 1022, Minneapolis, Minnesota 55440-1022 (26) Publication Language: English (US). (81) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of national protection available): AE, AG, AL, AM, 62/406,252 10 October 2016 (10.10.2016) US AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, 62/447,850 18 January 2017 (18.01.2017) US CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, 62/491,164 27 April 2017 (27.04.2017) US DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, 62/554,817 06 September 2017 (06.09.2017) US HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, 62/566,093 29 September 2017 (29.09.2017) US KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, (72) Inventors; and MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, _ (71) Applicants: ANDREWS, Steven W. [US/US]; c/o Array OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, BioPharma Inc., 3200 Walnut Street, Boulder, Colorado SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, 80301 (US). ARONOW, Sean [US/US]; c/o Array Bio- TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. — = Pharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 (84) Designated States (unless otherwise indicated, for every (US). BLAKE, James F. [US/US]; c/o Array BioPhar- kind of regional protection available): ARIPO (BW, GH, ma Inc., 3200 Walnut Street, Boulder, Colorado 80301 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, = — —_ BRANDHUBER, Barbara J. Array (US). [US/US]; c/o UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, BioPharma Inc., 3200 Walnut Street, Boulder, Colorado TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, 80301 (US). COOK, Adam [US/US]; c/o Array BioPharma EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, HAAS, Julia [US/US]; c/o Array BioPharma Inc., 3200 TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, = = _ = Walnut Street, Boulder, Colorado 80301 (US). JIANG, Yu- KM, ML, MR, NE, SN, TD, TG). tong [US/US]; c/o Array BioPharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). KOLAKOWSKI, = Published: Gabrielle R. [US/US]; c/o Array BioPharma Inc., 3200 — with international search report (Art. 21(3)) Walnut Street, Boulder, Colorado 80301 (US). MCFAD- — DIN, Elizabeth A. [US/US]; c/o Array BioPharma, Inc., with sequence listing part of description (Rule 5.2(a)) = 3200 Walnut St., Boulder, Colorado 80301 (US). MCKEN- NEY, Megan L. [US/US]; c/o Array BioPharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 (US). MCNULTY, = = Oren T. [US/US]; c/o Array BioPharma, Inc., 3200 Wal- nut St., Boulder, Colorado 80301 (US). METCALF, An- _ = drew T. [US/US]; c/o Array BioPharma Inc., 3200 Walnut = (54) Title: SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS (57) : Provided herein are compounds of the Formula I and stereoiso- mers and pharmaceutically acceptable salts or solvates thereof, in which A, B, N — — IN / X 1 , X 2 , X 3 , X 4 , Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and preven- 71' I 3 tion of diseases which can be treated with a RET kinase inhibitor, including 71' 11 B' r)(X2 O I (I) RET-associated diseases and disorders. Il 0X 4 , -:..t, X 1 NI.-. E (..?../ 0 ei C