Patent SG-11201408629Q-A (SG)
Title: Dimethyl-benzoic acid compounds
Inventor: BLANCO-PILLADO MARIA-JESUS
IPC: A61K31/4709
Filed: 2013-06-20
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 3 January 2014 (03.01.2014) WIPOIPCT (10) International Publication Number WO 2014/004230 A1 (51) International Patent Classification: C07D 401/04 (2006.01) C07D 207/08 (2006.01) C07D 211/42 (2006.01) C07D 211/46 (2006.01) A61K31/445 ( 2006.01) A61K31/4709 (2006.01) A61K31/402 (2006.01) A61K31/4025 (2006.01) A61P 29/00 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/046685 20 June 2013 (20.06.2013) English (30) Priority Data: 61/665,956 61/778,969 29 June 2012 (29.06.2012) 13 March 2013 (13.03.2013) English US US (71) Applicant: ELI LILLY AND COMPANY [US/US]; Lilly Corporate Center, Indianapolis, Indiana 46285 (US). (72) Inventors: BLANCO-PILLADO, Maria-Jesus; c/o ELI LILLY AND COMPANY, P.O. Box 6288, Indianapolis, Indiana 46206-6288 (US). VETMAN, Tatiana Natali; c/o ELI LILLY AND COMPANY, P.O. Box 6288, Indiana­ polis, Indiana 46206-6288 (US). FISHER, Matthew Joseph; c/o ELI LILLY AND COMPANY, P.O. Box 6288, Indianapolis, Indiana 46206-6288 (US). KUKLISH, Steven Lee; c/o ELI LILLY AND COMPANY, P.O. Box 6288, Indianapolis, Indiana 46206-6288 (US). (74) Agents: LENTZ, Nelsen L. et al.; ELI LILLY AND COMPANY, P.O. Box 6288, Indianapolis, Indiana 46206- 6288 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, [Continued on next page] (54) Title: DIMETHYL-BENZOIC ACID COMPOUNDS Formula II (57) Abstract: The present invention provides compound a of the Formula II: wherein A is: * R 1 is CH3, CF 3 , or F; * R 2 is H, CH3, or F; * R 3 is CH3, OCH 3 , OH, F; R 4 is OH or CH 20H; and X * is CH or N; These compounds are se­ lective EP4 inhibitors and are useful for the treatment of in­ flammatory conditions such as arthritis. wo 2014/004230 AI III llll IIII III III Hill III III III Hill Hill lllll lllll 111 111 lllllll llll 111 llll 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). Declarations under Rule 4.17: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3)) — before the expiration of the time limit for amending the claims and to be republished in the event of receipt of amendments (Rule 48.2(h))