Patent SG-11201806482V-A (SG)
Title: Benzenesulfonyl-asymmetric ureas and medical uses thereof
Inventor: GIULIANO CLAUDIO
IPC: C07D239/26
Filed: 2017-02-21
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 11111111011110111010101111101011111011101111101011100111101101111101111011111 International Bureau ... .... ..Yjd ..... ...,/ (10) International Publication Number (43) International Publication Date WO 2017/162390 Al 28 September 2017 (28.09.2017) WIP0 I PCT (51) International Patent Classification: AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, CO7C 311/00 (2006.01) CO7C 317/26 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, CO7D 239/26 (2006.01) CO7D 209/04 (2006.01) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, CO7C 317/14 (2006.01) 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, (21) International Application Number: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, PCT/EP2017/053937 NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (22) International Filing Date: RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 21 February 2017 (21.02.2017) TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, 62/311,573 22 March 2016 (22.03.2016) US TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, (71) Applicant: HELSINN HEALTHCARE SA [CH/CH]; DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, Via Pian Scairolo 9, 6912 Lugano / Pazzallo (CH). LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, (72) Inventors: GIULIANO, Claudio; Via Prudenziana No. SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, 28/A, 22100 Como (IT). DAINA, Antoine; Quartier GW, KM, ML, MR, NE, SN, TD, TG). Sorge, Batiment Genopode, 1015 Lausanne (CH). Published: _ PIETRA, Claudio; Via G. Scalabrini 56, 22100 Como — with international search report (Art. 21(3)) (IT). — before the expiration of the time limit for amending the — (74) Agent: ZARDI, Marco; c/o M. ZARDI & Co SA, Via Pi- be in claims and to republished the event of receipt of = oda, 6, 6900 Lugano (CH). amendments (Rule 48.2(h)) (81) Designated States (unless otherwise indicated, for every = kind of national available): AE, AG, AL, AM, protection = = = = = = = = = 1-1 © C:r M ei 1-1 (54) Title: BENZENESULFONYL-ASYMMETRIC UREAS AND MEDICAL USES THEREOF L .-- (57) : New benzenesulfonyl asymmetric ureas are herein disclosed, corresponding to the general formulas (I) (W) and ::::) pharmaceutically acceptable salts thereof, whose structure and substituents are detailed in the specification. Procedures for the syn - ei thesis of these compounds are disclosed. The compounds are active on the ghrelin receptors, in particular they have inverse agonist O activity; they are useful in preventing and/or treating diseases pathophysiologically mediated by the ghrelin receptor, like e.g. ,1 . obesity, diabetes and substance abuse. Also disclosed are pharmaceutical compositions comprising a compound as herein defined and a pharmaceutically acceptable carrier or vehicle.