Patent SG-11201805004T-A (SG)
Title: Substituted 4-phenyl pyridine compounds as non-systemic tgr5 agonists
Inventor: LEWIS JASON G
IPC: C07D401/12
Filed: 2016-12-19
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization IIIM141101110101H HO 11111011101011011011H OHO 111110 1111 III International Bureau .. .... ..Yejd (10) International Publication Number (43) International Publication Date ..... ...r .....1 WO 2017/106818 Al 22 June 2017(22.06.2017) WIPO I PCT (51) International Patent Classification: Tao; 3915 Louis Road, Palo Alto, California 94303 (US). CO7D 401/12 (2006.01) A61K 31/4427 (2006.01) SIEGEL, Matthew; 176 Hedge Road, Menlo Park, Cali- CO7D 405/12 (2006.01) A61P 3/00 (2006.01) fornia 94025 (US). CO7D 213/38 (2006.01) A61P 9/10 (2006.01) A61K 31/4418 (2006.01) A61P 11/06 (2006.01) (74) Agents: FARMER, J.Dean et al.; Cooley LLP, 1299 Pennsylvania Avenue, Suite 700, Washington, District of (21) International Application Number: Columbia 20004 (US). PCT/US2016/067460 (81) Designated States (unless otherwise indicated, for every (22) International Filing Date: kind of national protection available): AE, AG, AL, AM, 19 December 2016 (19.12.2016) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (25) Filing Language: English 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, (26) Publication Language: English 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, (30) Priority Data: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 62/269,804 18 December 2015 (18.12.2015) US NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, 62/419,939 9 November 2016 (09.11.2016) US RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (71) Applicant: ARDELYX, INC. [US/US]; 34175 Arden- TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, wood Boulevard, Fremont, California 94555 (US). ZA, ZM, ZW. (72) Inventors: LEWIS, Jason G.; 5327 Greenridge Road, (84) Designated States (unless otherwise indicated, for every _ Castro Valley, California 94552 (US). LEADBETTER, kind of regional protection available): ARIPO (BW, GH, San Leandro, Cali- GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, — Michael Robert; 335 Beverly Avenue, _ 510 Laurel TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, forma 94577 (US). CALDWELL, Jeremy; (US). DRAGOLI, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Avenue, Menlo Park, California 94025 Altos, California DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, = Dean; 24645 Summerhill Avenue, Los Blvd., Apt. 101, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, 94024 BELL, Noah; 3340 Sawtelle (US). = SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, JACOBS, Jeffrey Los Angeles, California 90066 (US). W.; 505 Cornell Avenue, San Mateo, California 94402 GW, KM, ML, MR, NE, SN, TD, TG). = (US). FINN, Patricia; 16042 Selborne Drive, San Published: — Leandro, California 94578 (US). JAIN, Rakesh; 3433 — — with international search report (Art. 21(3)) (US). CHEN, = Cashmere Street, Danville, California 94506 COMPOUNDS AS NON-SYSTEMIC TGR5 AGONISTS (54) Title: SUBSTITUTED 4-PHENYL PYRIDINE = = = Y = = P 2 '2' ,,,,,,, X 4 1-1 .4 X3 GC (R3)n (I) ,-1 cc , tD 0 1-1 IN 1-1 (57) : The invention relates to non-systemic TGR5 agonist useful in the treatment of chemotherapy-induced diarrhea, dia- 0 betes, Type II diabetes, gestational diabetes, impaired fasting glucose, impaired glucose tolerance, insulin resistance, hyperglycemia, obesity, metabolic syndrome, ulcerative colitis, Crohn's disease, disorders associated with parenteral nutrition especially during short C bowel syndrome, and irritable bowel syndrome (IBS), and other TGR5 associated diseases and disorders, having the Formula: (I'), where RI, R2, R2', R3, R4, Xl, X2, X3, X4, Q, and n are described herein.