SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS

    公开(公告)号:SG11201903187WA

    公开(公告)日:2019-05-30

    申请号:SG11201903187W

    申请日:2017-10-10

    Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD HIM 0 11101 HOE HI 1 0 101110 Ell 010 HE 100 MO MIS Organization International Bureau (10) International Publication Number (43) International Publication Date ......0\" WO 2018/071454 Al 19 April 2018 (19.04.2018) WIP0 1 PCT (51) International Patent Classification: nut Street, Boulder, Colorado 80301 (US). MORENO, CO7D 471/04 (2006.01) A61P 35/00 (2006.01) David A. [US/US]; c/o Array BioPharma Inc., 3200 Walnut A61K 31/437 (2006.01) Street, Boulder, Colorado 80301 (US). RAMANN, Ginelle (21) International Application Number: A. [US/US]; c/o Array BioPharma, Inc., 3200 Walnut St., PCT/US2017/055993 Boulder, Colorado 80301 (US). TANG, Tony P. [US/US]; c/o Array BioPharma Inc., 3200 Walnut Street, Boulder, (22) International Filing Date: Colorado 80301 (US). REN, Li [US/US]; c/o Array Bio- 10 October 2017 (10.10.2017) Pharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). WALLS, Shane M. [US/US]; c/o Array BioPharma, (25) Filing Language: English Inc., 3200 Walnut St., Boulder, Colorado 80301 (US). (26) Publication Language: English (74) Agent: FOLLETT, Angela D. et al.; Fish & Richardson (30) Priority Data: P.C., P.O. Box 1022, Minneapolis, Minnesota 55440-1022 62/406,275 10 October 2016 (10.10.2016) US (US). 62/447,849 18 January 2017 (18.01.2017) US (81) Designated States (unless otherwise indicated, for every 62/491,180 27 April 2017 (27.04.2017) US kind of national protection available): AE, AG, AL, AM, 62/531,690 12 July 2017 (12.07.2017) US AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, 62/566,030 29 September 2017 (29.09.2017) US CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, (72) Inventors; and DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, (71) Applicants: ANDREWS, Steven W. [US/US]; c/o Array HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, BioPharma Inc., 3200 Walnut Street, Boulder, Colorado KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 80301 (US). ARONOW, Sean [US/US]; c/o Array Bio- MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, Pharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (US). BLAKE, James F. [US/US]; c/o Array BioPhar- SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, ma Inc., 3200 Walnut Street, Boulder, Colorado 80301 TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (US). BRANDHUBER, Barbara J. [US/US]; c/o Array (84) Designated States (unless otherwise indicated, for every BioPharma Inc., 3200 Walnut Street, Boulder, Colorado kind of regional protection available): ARIPO (BW, GH, 80301 (US). COLLIER, James [US/US]; c/o Array Bio GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, Pharma, Inc., 3200 Walnut St., Boulder, Colorado 80301 UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (US). COOK, Adam [US/US]; c/o Array BioPharma Inc., 3200 Walnut Street, Boulder, Colorado 80301 (US). HAAS, 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, Julia [[JS/US]; c/o Array BioPharma Inc., 3200 Wal- MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, nut Street, Boulder, Colorado 80301 (US). JIANG, Yu- TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, tong [US/US]; c/o Array BioPharma Inc., 3200 Walnut KM, ML, MR, NE, SN, TD, TG). Street, Boulder, Colorado 80301 (US). KOLAKOWSKI, Gabrielle R. [US/US]; c/o Array BioPharma Inc., 3200 Published: Walnut Street, Boulder, Colorado 80301 (US). MCFAD- — DIN, Elizabeth A. [US/US]; c/o Array BioPharma, Inc., with international search report (Art. 21(3)) — 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 Wal- (54) Title: SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS (57) : Provided herein are compounds of the Formula I: (I) or pharmaceu- lin N i (Ra)„ tically acceptable salt or solvate thereof, wherein A, B, X 1 , X, X, X 2 3 4 , Ring D, E, 11' Il 1 X3=X2 R a , R b , n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which IN 0 p --.... / D ~X 4 _X~ d ca is rd n o b e e e tr rs . ated with a RET kinase inhibitor, including RET-associated diseases and X4-x1 B - O Il (Rb),„ © N I C

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