Patent SG-11201807540U-A (SG)
Title: Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis
Inventor: MAMMOLITI OSCAR
IPC: C07D403/04
Filed: 2017-02-23
Abstract: WO 17 / 1487 87 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2017/148787 Al 8 September 2017 (08.09.2017) WIPO I PCT 1111111111111101110111111111110101111101110101111111101111111101111111111111110111111 (51) International Patent Classification: C07D 401/14 (2006.01) A61P 35/00 (2006.01) C07D 403/04 (2006.01) (21) International Application Number: PCT/EP2017/054139 (22) International Filing Date: 23 February 2017 (23.02.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 1603745.9 4 March 2016 (04.03.2016) GB (71) Applicant: GALAPAGOS NV [BE/BE]; Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (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, 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). arations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(11)) of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 21(3)) (72) Inventors: MAMMOLITI, Oscar; Galapagos NV Gener- aal De Wittelaan Ll l/A3, 2800 Mechelen (BE). JANSEN, Koen, Karel; Galapagos NV Generaal De Wittelaan Ll l/A3, 2800 Mechelen (BE). PALISSE, Adeline, Marie, Elise; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). JOANNESSE, Caroline, Martine, An- Decl dree-Marie; Galapagos NV Generaal De Wittelaan Ll l/A3, 2800 Mechelen (BE). MENET, Christel, Jeanne, Marie; Confo Therapeutics Pleinlaan 2, Building E, 7th floor, E7.6, 1050 Brussels (BE). ALLART, Brigitte; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). EL BKASSINY, Sandy; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (74) Agent: BAR, Gregory, Louis, Joseph; Galapagos NV Generaal De Wittelaan L11/A3, 2800 Mechelen (BE). (54) Title: NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF FIBROSIS Ia (R 5 ) rin (57) : The present invention discloses compounds according to Formula I, wherein Rla, R 1b , R 2a , R 2b , R, R 3 4 , R 5 , R6a , c yl, Cy2, and the subscript n and m are as defined herein. The present invention relates to antagonists compounds of sphingosine 1-phos- phate (SIP) receptor, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment us - ing the same, for the prophylaxis and/or treatment of diseases involving fibrotic diseases, inflammatory diseases, autoimmune dis - eases, metabolic diseases, cardiovascular diseases, and/or proliferative diseases by administering the compound of the invention.