Patent SG-11201903195Y-A (SG)
Title: Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders
Inventor: GRETZKE DIRK
IPC: A61K31/437
Filed: 2017-11-02
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 11 May 2018 (11.05.2018) WIPO I PCT omit IIl °nolo OH voila° oimIE (10) International Publication Number WO 2018/083157 Al (51) International Patent Classification: CO7D 471/04 (2006.01) A61K 31/437 (2006.01) CO7D 519/00 (2006.01) A61P 19/02 (2006.01) (21) International Application Number: PCT/EP2017/078026 (22) International Filing Date: 02 November 2017 (02.11.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 16306452.0 07 November 2016 (07.11.2016) EP (71) Applicant: SANOFI [FR/FR]; 54 me La Boetie, 75008 Paris (FR). (72) Inventors: GRETZKE, Dirk; c/o Sanofi-Aventis Deutsch- land GmbH, 65926 Frankfurt am Main (DE). RITZEL- ER, Olaf; c/o Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). HEINELT, Uwe; c/o Sanofi- Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). WEHNER, Volkmar; c/o Sanofi-Aventis Deutsch- land GmbH, 65926 Frankfurt am Main (DE). SCHMIDT, Friedemann; c/o Sanofi-Aventis Deutschland GmbH, 65926 Frankfurt am Main (DE). (74) Agent: VENNE-DUNKER, Sabine; c/o Sanofi-Aventis Deutschland GmbH, Global Intellectual Property Depart- ment, Industriepark Hochst, Geb. K 703, 65926 Frankfurt am Main (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, 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). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: with international search report (Art. 2 I (3)) = (54) Title: SUBSTITUTED PYRIDO[3,4-B]INDOLES FOR THE TREATMENT OF CARTILAGE DISORDERS 1-1 R io 1-1 00 © (57) : The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula G O (I), in which A, E, G, R 1 to R 6 and R 10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example N Joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula 0 (I), their use as pharmaceuticals, and pharmaceutical compositions comprising them. (I)