Patent SG-11201908097Y-A (SG)
Title: Pyrimidine derivatives as pge2 receptor modulators
Inventor: BOSS CHRISTOPH
IPC: C07D409/04
Filed: 2018-05-17
Abstract: RaR ai) N ▪ Arl a R 5b N N R3 1-1 GC GC O 1-1 N 00 O 1-1 N O (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 22 November 2018 (22.11.2018) WIPO I PCT IiiimmoinionotiomiololoiloinimioluovoimIE (10) International Publication Number WO 2018/210988 Al (51) International Patent Classification: CO7D 413/14 (2006.01) CO7D 409/12 (2006.01) CO7D 405/12 (2006.01) A61K 31/506 (2006.01) C07D 409/04 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: PCT/EP2018/062844 (22) International Filing Date: 17 May 2018 (17.05.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: PCT/EP2017/061989 18 May 2017 (18.05.2017) EP (71) Applicant: IDORSIA PHARMACEUTICALS LTD [CH/CH]; Hegenheimermattweg 91, 4123 Allschwil (CH). (72) Inventors: BOSS, Christoph; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). COR- MINBOEUF, Olivier; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). FRETZ, Declarations under Rule 4.17: Heinz; Oertli 40c, 3654 Gunten (CH). LYOTHIER, Is- abelle; c/o Idorsia Pharmaceuticals Ltd, Hegenheimer- mattweg 91, 4123 Allschwil (CH). POZZI, Davide; c/ o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). RICHARD-BILDSTEIN, Sylvia; c/ o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). SIENDT, Herve; c/o Idorsia Phar- maceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). SIFFERLEN, Thierry; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). (74) Agent: VELKER, Jorg; c/o Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, 4123 Allschwil (CH). (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). as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 2 I (3)) (54) Title: PYRIMIDINE DERIVATIVES AS PGE2 RECEPTOR MODULATORS Formula (I) R3 , , , , (57) : The present invention relates to pyrimidine derivatives of formula (I) wherein (R 1) R R 3 4a R ob R 5a R 5b and Ar 1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.