Patent SG-11201804363U-A (SG)
Title: Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
Inventor: DOWLING MATTHEW
IPC: C07D401/14
Filed: 2016-12-16
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau irst0) (43) International Publication Date .... ..sr.) 6 July 2017 (06.07.2017) WI P0 I P CT II (10) 11111111111111111111 WO International 2017/115205 Publication IIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIIMIIIIIIIIIIIIIII Number Al (51) International Patent Classification: TSAI, Andy; 132 Ledgeland Drive, Mystic, Connecticut C07D 401/14 (2006.01) A61P 25/02 (2006.01) 06355 (US). TU, Meihua; 6 Henley Road, Acton, Mas- CO7D 403/04 (2006.01) A61P 35/00 (2006.01) sachusetts 01720 (US). CO7D 403/14 (2006.01) A61P 25/30 (2006.01) (74) Agent: WALDRON, Roy F.; Pfizer INC., 235 East 42nd A61K 31/506 (2006.01) A61P 9/00 (2006.01) A61P 3/06 (2006.01) A61P 37/00 (2006.01) Street, MS 235/9/S20, New York, NY 10017 (US). A61P 3/10 (2006.01) A61P 7/02 (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of national protection available): AE, AG, AL, AM, PCT/IB2016/057728 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, (22) International Filing Date: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 16 December 2016 (16.12.2016) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (25) Filing Language: English MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (26) Publication Language: English 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, (30) Priority Data: TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 62/272,598 29 December 2015 (29.12.2015) US ZA, ZM, ZW. 62/423,549 17 November 2016 (17.11.2016) US (84) Designated States (unless otherwise indicated, for every (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, kind of regional protection available): ARIPO (BW, GH, New York, New York 10017 (US). GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (72) Inventors: DOWLING, Matthew; 1 Pyrus Court, Old Lyme, Connecticut 06371 FERNANDO, Dilinie; 15 TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (US). Freedom Way, Unit 46, Niantic, Connecticut 06357 (US). 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, FUTATSUGI, Kentaro; 10 Faxon Avenue, Apt. 808, SM, TR), OAPI BJ, CF, CG, CI, CM, GA, GN, GQ, Quincy, Massachusetts 02169 (US). HUARD, Kim; 34 (BF, KM, ML, MR, NE, SN, TD, TG). GW, Thatcher Street, Medford, Massachusetts 02155 (US). MAGEE, Thomas Victor; 70 Fletcher Street, Winchester, Declarations Rule 4.17: under Massachusetts 01890 (US). RAYMER, Brian; 3 Pilgrim as to the identity of the inventor (Rule 4.17(0) Road, Holliston, Massachusetts 01746 SHAVNYA, (US). Andre; 48 Dean Road, East Lyme, Connecticut 06333 — as to applicant's entitlement to apply for and be a granted (US). SMITH, Aaron; 15 Allison Avenue, North Provid- patent (Rule 4.17 (i0) ence, Rhode Island 02911 (US). THUMA, Benjamin; 1 as to the applicant's entitlement to claim the priority of the Smiths Neck Road, Old Lyme, Connecticut 06371 (US). earlier application (Rule 4.17(iii)) [Continued on next page] Title: SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS (54) FIG. 1 PXRD pattern of crystalline free acid of Example 4 12000 10000 8000 11 99 0 3 - .4t 4000 in 0 2000 N in 11 11 IN 1-1 (57) : Provided herein 3 5 7 9 11 13 15 17 are substituted 3-azabicyclo[3.1.0]hexanes 19 2 Theta Degrees 21 23 25 27 29 31 33 35 37 39 as ketohexokinase inhibitors, processes to make said 0 compounds, and methods comprising administering said compounds to a mammal in need thereof el 0 WO 2017/115205 Al 1#11101MO11111 111111110101311H0101111111111111011110111111 Published: — with international search report (Art. 21(3))