Patent SG-11201808878U-A (SG)
Title: Heterocyclic compounds as ret kinase inhibitors
Inventor: JORDAN ALLAN
IPC: C07D495/04
Filed: 2017-04-18
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11111111011110111010101111101011111011101011111111111110111011111111101111011111 International Bureau 0.. .... ..Yjd (10) International Publication Number (43) International Publication Date ..... ...,/ WO 2017/178844 Al 19 October 2017(19.10.2017) WIPO I PCT (51) International Patent Classification: (72) Inventors: JORDAN, Allan; Cancer Research UK CO7D 495/04 (2006.01) A61K 31/4985 (2006.01) Manchester Institute, The University of Manchester, A61K 31/519 (2006.01) A61P 35/00 (2006.01) Wilmslow Road, Manchester Greater Manchester M20 A61K 31/437 (2006.01) C07D 487/04 (2006.01) 4BX (GB). NEWTON, Rebecca; Cancer Research UK C07D 471/04 (2006.01) Manchester Institute, The University of Manchester, Wilmslow Road, Manchester Greater Manchester M20 (21) International Application Number: 4BX (GB). PCT/GB2017/051076 (22) (74) International Filing Date: Agent: HGF LIMITED; 4th Floor Merchant Exchange, 17-19 Whitworth Street West, Manchester Greater 18 April 2017 (18.04.2017) Manchester Ml 5WG (GB). (25) Filing Language: English (81) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (30) Priority Data: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, 1606631.8 15 April 2016 (15.04.2016) GB DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 1619277.5 14 November 2016 (14.11.2016) GB HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (71) Applicant: CANCER RESEARCH TECHNOLOGY KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, LIMITED [GB/GB]; Angel Building, 407 St John Street, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, — London Greater London EC1V 4AD (GB). 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, [Continued on next page] _ = = HETEROCYCLIC COMPOUNDS AS RET KINASE INHIBITORS (54) Title: (57) : The present invention relates to compounds — , X2 R3 of Formula I that function as inhibitors of RET (rearranged \" **.............,./... X 1 - ., a , 1 during transfection) kinase enzyme activity: wherein HET, bonds a, b, c and d, X i , X 2 , , , X 3 X 4 R 2 , and R are each as 3 = _ _ b: defined herein. The present invention also relates to pro - = — 1 cesses for the preparation of these compounds, to pharma- _ X3 ceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as = well as other diseases or conditions in which RET kinase X4 activity is implicated. \ d = % R2 HET ,—, . 4 7r 7r GC GC IN ,—, Formula I IN ,—, © ei O WO 2017/178844 Al MIDEDIMOMOIDEIR01013010MHEIMEMEHOIMIE TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, Declarations under Rule 4.17: TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, of inventorship (Rule 4.17w)) LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, Published: SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). GA, — with international search report (Art. 21(3))