Patent SG-11201903113T-A (SG)
Title: Compounds, process for obtaining the compounds, pharmaceutical composition, use of the compounds and method for treating psychiatric disorders and/or sleep disorders
Inventor: RUCH WERNECK GUIMARÃES CRISTIANO
IPC: A61P25/22
Filed: 2017-10-23
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 03 May 2018 (03.05.2018) o I iolo 0110 IIIII 100 IRMO 1110 011 (10) International Publication Number WO 2018/076090 Al WIPO I PCT (51) International Patent Classification: C07D 235/26 (2006.01) A61P 25/20 (2006.01) C07D 235/28 (2006.01) A61P 25/22 (2006.01) A61K 31/4184 (2006.01) A61P 25/24 (2006.01) (21) International Application Number: PCT/BR2017/050320 (22) International Filing Date: 23 October 2017 (23.10.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: BR1020160248140 24 October 2016 (24.10.2016) BR (71) Applicant: ACHE LABORATORIOS FARMACEUTI- COS S.A. [BR/BR]; ROD. PRESIDENTE DUTRA, KM 222.2 - PORTO DA IGREJA, 07034-904 Guarulhos (BR). (72) Inventors: RUCH WERNECK GUIMARAES, Cris- tiano; Alameda dos Anapurus, 883 Apto 131 Bloco B, 04087-002 Sao Paulo (BR). FELYPE ZANETI DE AZEVEDO, Hatylas; Rua Fabia, 138 Apto 81 Bloco B, 05051-030 Sao Paulo (BR). MASCARELLO, Alessan- dra; Rua Santa Izabel 451 Apto 138 Torre 1, 07023-022 Guarulhos (BR). WATANABE DA COSTA, Renata; Rua Amelia Perpetua 92, 02040-100 Sao Paulo (BR). FREIRE TORRES RUSSO, Valter; Rua Benedito Martins 270, 13975-020 Itapira (BR). MANNOCHIO DE SOUZA RUSSO, Elisa; Rua Benedito Martins 270, 13975-020 Itapira (BR). (74) Agent: GAIARSA, Lucas Martins; Rua Raul Pompeia 617 - Pompeia, 05025-0010 Sao Paulo (BR). (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, (54) Title: COMPOUNDS, PROCESS FOR OBTAINING THE COMPOUNDS, PHARMACEUTICAL COMPOSITION, USE OF = THE COMPOUNDS AND METHOD FOR TREATING PSYCHIATRIC DISORDERS AND/OR SLEEP DISORDERS A R N N ± H 1-1 O 0\ O N O GC O C 1-1 Epik=> pK, = 6.10 ± 2.22 Epik => plc= 5.65 ± 2.22 Jaguar => = 6.0 Jaguar => pK, = 5 FIG. 1 (57) : The present invention relates to novel and inventive pharmacologically active benzimidazole derivative compounds, which surprisingly have high affmity for melatonin MTi and MT2 receptors and low affmity for CYP450 complex enzymes f specially CYP1A2. The present, invention also relates to novel and inventive routes of synthesis of these compounds, pharmaceutical compo- sitions comprising the compounds and the use of these compounds in the treatment of individuais affected by psychiatric disorders and/or sleep disorders related to these receptors (specially depression, anxiety, circadian cycle disorders), in addition to process for producing the composition. [Continued on next page] WO 2018/076090 Al MIDEDIMOMMIDIREEMOMMIN VIII VIII IHMEMOIS 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). Published: — with international search report (Art. 21(3))