Patent SG-11201407919W-A (SG)
Title: Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ror[gamma]
Inventor: GEGE CHRISTIAN
IPC: C07D495/10
Filed: 2013-05-29
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 5 December 2013 (05.12.2013) WIPOIPCT (10) International Publication Number WO 2013/178362 A1 (51) International Patent Classification: C07D 277/56 (2006.01) C07D 333/38 (2006.01) C07D 417/04 (2006.01) C07D 239/28 (2006.01) C07D 417/12 (2006.01) C07D 413/12 (2006.01) C07D 417/14 (2006.01) C07D 263/34 (2006.01) A61K 31/427 (2006.01) C07D 493/08 (2006.01) A61P 3/10 (2006.01) C07D 493/10 (2006.01) A61P17/06 (2006.01) C07D 495/10 (2006.01) A61P19/02 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/EP2013/001593 29 May 2013 (29.05.2013) English English (30) Priority Data: 12004186.8 61/653,556 31 May 2012 (31.05.2012) EP 31 May 2012 (31.05.2012) US (71) Applicant: PHENEX PHARMACEUTICALS AG [DE/DE]; Donnersbergweg 1, 67059 Ludwigshafen (DE). (72) Inventors: GEGE, Christian; Mochentalerweg 26, 89584 Ehingen (DE). STEENECK, Christoph; Schulstrasse 8, 69221 Dossenheim (DE). KINZEL, Olaf; Am Hackteufel 8, 69117 Heidelberg (DE). KLEYMANN, Gerald; Leo- poldshoher Strasse 7, 32107 Bad Salzuflen (DE). HOFF­ MANN, Thomas; Gebriider-Grimm-Allee 19, 68519 Vi- ernheim (DE). (74) Agent: GOLDBACH, Klara; Grunecker, Kinkeldey,Stockmair & Schwanhausser, Leopoldstrasse 4, 80802 Miinchen (DE). (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, 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). 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)) (54) Title: CARBOXAMIDE OR SULFONAMIDE SUBSTITUTED THIAZOLES AND RELATED DERIVATIVES AS MODU­ LATORS FOR THE ORPHAN NUCLEAR RECEPTOR ROR[GAMMA] NR R 1 2 NR R n 1R2 O^W H N y^R 3 osw (1) CJ m oo i> i-H cn i-H o CJ o & R101 O V< R° 1 2 )= N V °^^R 103 R 104 (100') )=\ S N x^R3 R° 2 1 0 (1') • 101 O V? R 102 V°v N s^R 103 R104 (100) R 202 Y \ Y 200 X»5^ 204 R R203 •201 O R 202 >=X 200 Y 200 and ^ R 204 R 203 (200') (57) Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide or sulfonamide containing cyclic compounds of Formula (1), (1'), (100), (100'), (200) and (200') and the enan- tiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof.