Patent SG-11201907139U-A (SG)
Title: Anti-fibrotic compounds
Inventor: MILLER THOMAS
IPC: C07D211/58
Filed: 2018-01-31
Abstract: Single and multi-day oral dosing of 116 to male SD rats at 2, 20, 75 and 350 mg/kg/day » z /day 10 +1 5 25 20 mg/kg/day mg/kg/day ...***0501ng/kg/day 10 IS Time post dose th ) (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 09 August 2018 (09.08.2018) WIPO I PCT o °nolo DID momilitiloiflo oimIE (10) International Publication Number WO 2018/144620 Al (51) International Patent Classification: C07C 235/38 (2006.01) C07D 207/24 (2006.01) A61K 31/167 (2006.01) CO7D 209/46 (2006.01) A61P 17/00 (2006.01) CO7D 211/22 (2006.01) CO7C 235/40 (2006.01) CO7D 211/26 (2006.01) CO7C 237/20 (2006.01) CO7D 211/46 (2006.01) CO7C 255/60 (2006.01) CO7D 211/58 (2006.01) CO7D 205/04 (2006.01) CO7D 213/30 (2006.01) CO7D 207/12 (2006.01) (21) International Application Number: PCT/US2018/016272 (22) International Filing Date: 31 January 2018 (31.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/454,358 03 February 2017 (03.02.2017) US (71) Applicant: SHIRE HUMAN GENETIC THERAPIES, INC. [US/US]; 300 Shire Way, Lexington, MA 02421 (US). (72) Inventors: MILLER, Thomas; 18 Park Avenue, Wake- field, MA 01880 (US). PAPAIOANNOU, Nikolaos; 70 Spiers Road, Newton, MA 02459 (US). (74) Agent: DUFFEY, Matthew, 0.; Wolf, Greenfield & Sacks, P.C., 600 Atlantic Avenue, Boston, MA 02210-2206 (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, (54) Title: ANTI-FIBROTIC COMPOUNDS FIG. 1 (R 6 ), (I) 00 O O (57) : Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein. (Formula (I)) [Continued on next page] WO 2018/144620 Al MIDEDIMOMMIDIREEMOMMIMMOMERVOIS 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). Published: — with international search report (Art. 21(3))