Patent SG-11201908670S-A (SG)
Title: Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
Inventor: ERICSSON ANNA
IPC: A61K31/407
Filed: 2018-03-20
Abstract: R0 R 1 R 1 ' R9' R10' R 11 ' R ii 0 II N—S—Y—R 4 (I) 0 R 9 R 8 0 R10 R2' (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 27 September 2018 (27.09.2018) WIP0 I PCT ill 1111u°11101VIIIVIIIVIIIolo oloinomonimmom oimIE (10) International Publication Number WO 2018/175474 Al (51) International Patent Classification: (74) Agent: REARICK, John P. et al.; Choate, Hall & Ste- CO7D 487/04 (2006.01) CO7D 519/00 (2006.01) wart LLP, Two International Place, Boston, Massachusetts A61K 31/407 (2006.01) A61P 7/00 (2006.01) 02110 (US). C (21) International Application Number: PCT/US2018/023405 (22) International Filing Date: 20 March 2018 (20.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/473,751 20 March 2017 (20.03.2017) US (71) Applicant: FORMA THERAPEUTICS, INC. [US/US]; 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). (72) Inventors: ERICSSON, Anna; c/o Forma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massa- chusetts 02472 (US). GREEN, Neal; c/o Forma Thera- peutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). GUSTAFSON, Gary; c/o For- ma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Wa- tertown, Massachusetts 02472 (US). HAN, Bingsong; c/ o Forma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). LANCIA, JR., David R.; c/o Forma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). MITCHELL, Lorna; c/o Forma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). RICHARD, David; c/o Forma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). SHELEKHIN, Tatiana; c/o Forma Therapeu- tics, Inc., 500 Arsenal Street, Suite 100, Watertown, Mass- achusetts 02472 (US). SMITH, Chase C.; c/o Forma Ther- apeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (US). WANG, Zhongguo; c/o For- ma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Wa- tertown, Massachusetts 02472 (US). ZHENG, Xiaozhang; c/o Forma Therapeutics, Inc., 500 Arsenal Street, Suite 100, Watertown, Massachusetts 02472 (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, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 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, 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, KM, 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 4.1700) Published: with international search report (Art. 21(3)) (54) Title: PYRROLOPYRROLE COMPOSITIONS AS PYRUVATE KINASE (PKR) ACTIVATORS 1-1 (57) : The disclosure relates to modulating pyruvate kinase and provides novel chemical compounds of formula (I) useful as © activators of PKR, as well as various uses of these compounds. PKR activating compounds are useful in the treatment of diseases and disorders associated with PKR and/or PKM2, such as pyruvate kinase deficiency (PKD), sickle cell disease (SCD), and thalassemia.