Patent SG-11201804170R-A (SG)
Title: Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders
Inventor: SHERER BRIAN A
IPC: C07D487/04
Filed: 2016-12-16
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11111111011110111010101111101011111011101011011101100111011111111101111011111 International Bureau ... .... .. (10) International Publication Number (43) International Publication Date ..... ...r .....1 WO 2017/106607 Al 22 June 2017(22.06.2017) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07D 401/14 (2006.01) CO7D 241/42 (2006.01) kind of national protection available): AE, AG, AL, AM, CO7D 405/14 (2006.01) CO7D 471/04 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, CO7D 413/14 (2006.01) CO7D 487/04 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, CO7D 401/04 (2006.01) A61K 31/4375 (2006.01) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, CO7D 413/04 (2006.01) A61P 37/00 (2006.01) HN, CO7D 417/04 (2006.01) KP, MD, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (21) International Application Number: NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, PCT/US2016/067112 RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (22) International Filing Date: TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 16 December 2016 (16.12.2016) ZA, ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (26) Publication Language: English GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, (30) Priority Data: TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, 62/268,765 17 December 2015 (17.12.2015) US TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 62/353,603 23 June 2016 (23.06.2016) 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, (71) Applicant: MERCK PATENT GMBH [DE/DE]; Frank- SM, furter Strasse 250, 64293 Darmstadt (DE). GW, KM, ML, MR, NE, SN, TD, TG). TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, (72) Inventors; and Published: Applicants (for US only): SHERER, Brian A. [US/US]; — 57 Harris Road, Nashua, New Hampshire 03062 (US). with international search report (Art. 21(3)) _ (71) BRUGGER, Nadia [CH/US]; 7 Haskell Street, Cam- — before the expiration of the time limit for amending the bridge, Massachusetts 02140 (US). claims and to be republished in the event of receipt of (74) amendments (Rule 48.2(h)) Agent: KIM, Dwight D.; EMD Serono Research and De- velopment Institute, One Technology Place, Rockland, Massachusetts 02370 (US). (54) Title: POLYCYCLIC TLR7/8 ANTAGONISTS AND USE THEREOF IN THE TREATMENT OF IMMUNE DISORDERS X (R4) 1 t(R 5 ) N r -- (I) 1-1 R3) AR 2 )--H‘ ( ...___..\" P IN I 0 , tD (R 1 )k , tD 0 1-1 IN 1-1 (57) : The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, 0 useful as toll-like receptor 7/8 (TLR7/8) antagonists. In Formula (I), Ring A is aryl or heteroaryl; Ring B is aryl or heteroary; and X \" is C(R 4 ) 2 , 0, Me, S, S(R 4 ), or S(R 4 ) 2 . 0