Patent SG-11201900157R-A (SG)
Title: 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors
Inventor: JOGALEKAR ASHUTOSH
IPC: C07D403/12
Filed: 2017-07-11
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD 1101111 0 DOI HIM 011101 0 0111111 0111011111011101111111111011011111111 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/013597 A4 18 January 2018 (18.01.2018) W I P0 I P C T (51) International Patent Classification: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, C07D 241/18 (2006.01) A61K 31/497 (2006.01) OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, C07D 241/20 (2006.01) A61K 31/4985 (2006.01) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, CO7D 403/12 (2006.01) A61P 35/00 (2006.01) TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. CO7D 403/04 (2006.01) (84) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of regional protection available): ARIPO (BW, GH, PCT/US2017/041577 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, (22) International Filing Date: UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, 11 July 2017 (11.07.2017) 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, (25) Filing Language: English MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (26) Publication Language: English TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). (30) Priority Data: 62/361,249 12 July 2016 (12.07.2016) US Published: 62/449,523 23 January 2017 (23.01.2017) US — with international search report (Art. 21(3)) — (71) Applicant: REVOLUTION MEDICINES, INC. with amended claims (Art. 19(1)) [US/US]; 700 Saginaw Drive, Redwood City, California Date of publication of the amended claims: 94063 (US). 05 April 2018 (05.04.2018) Inventors; (72) and (71) Applicants: JOGALEKAR, Ash [IN/US]; c/o: Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, US 94063 (US). WON, Walter [US/US]; c/o: Revolution Med- icines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). (72) Inventors: KOLTUN, Elena S.; c/o: Revolution Medi- cines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). GILL, Adrian; c/o: Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). MELLEM, Kevin; c/o Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). AAY, Naing; c/o: Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). BUCKL, Andreas; c/o: Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). SEMKO, Christopher; c/o: Revolution Medicines, Inc., 700 Saginaw Drive, Redwood City, California 94063 (US). KISS, Gert; c/o: Revolution Medicines, Inc., 700 Saginaw Drive, Red- City, California 94063 wood (US). (74) Agent: TONG, Connie C. et al.; Cooley LLP, 1299 Penn- sylvania Avenue, NW, Suite 700, Washington, District of Columbia 20004 (US). (81) Designated States (unless otherwise indicated, for every 71' kind of national protection available): AE, AG, AL, AM, 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, IN 01 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, In HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, en KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, 1-1 0 --.... 00 1-1 (54) Title: 2,5-DISUBSTITUTED 3-METHYL PYRAZINES AND 2,5,6-TRISUBSTITUTED 3-METHYL PYRAZINES AS AL- 0 el LOSTERIC SHP2 INHIBITORS C (57) : The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.