Patent SG-11201908560S-A (SG)
Title: Heterocyclic compounds useful as dual atx/ca inhibitors
Inventor: MATTEI PATRIZIO
IPC: C07D403/10
Filed: 2018-03-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 20 September 2018 (20.09.2018) WIPO I PCT 0111111010 0111 °nolo Oil ioo mo IIIII n Immo oimIE (10) International Publication Number WO 2018/167001 Al (51) International Patent Classification: C07D 401/14 (2006.01) C07D 401/12 (2006.01) C07D 405/14 (2006.01) C07D 403/10 (2006.01) A61K 31/397 (2006.01) C07D 409/14 (2006.01) A61K 31/4025 (2006.01) C07D 417/14 (2006.01) A61K 31/496 (2006.01) A61P 27/02 (2006.01) C07D 401/10 (2006.01) (21) International Application Number: PCT/EP2018/056140 (22) International Filing Date: 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: as to the identity of the inventor (Rule 4.17(i)) of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 21(3)) (25) Filing Language: (26) Publication Language: (30) Priority Data: 17161249.2 13 March 2018 (13.03.2018) English English 16 March 2017 (16.03.2017) EP (71) Applicant (for all designated States except US): F. HOFF- MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). = (71) Applicant US only): HOFFMANN-LA ROCHE INC. [US/US]; Overlook at Great Notch, 150 Clove Road, 8th Floor, Suite 8 - Legal Department, Little Falls, New Jer- sey 07424 (US). (72) Inventors: MATTEL, Patrizio; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). HERT, Jerome; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). HUNZIKER, Daniel; c/o F. Hoff- mann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). RUDOLPH, Markus; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). SCHMITZ, Petra; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). DI GIORGIO, Patrick; c/o F. Hoff- maim-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). GOMME, Justin; c/o F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). (74) Agent: BERNARD, Guillaume; Grenzacherstrasse 124, 4070 Basel (CH). = (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, 1-1 HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, 1-1 © (54) Title: HETEROCYCLIC COMPOUNDS USEFUL AS DUAL ATX/CA INHIBITORS O R z 11 f„,)m Y— N X— W 1-1 R 1/ \(„f n ( 1 ) O C (57) : The invention provides novel compounds having the general formula (I) wherein R 1 is selected from substituted phenyl, pyridinyl or thiophenyl, R is selected from optionally substitut- 2 ed aminosulphonylphenyl, aminosulphonylpyridinyl, amino sulphonylthiophenyl or aminosulpho- nylthiazolyl, X is nitrogen or carbon, Y is a linking group, Z is a direct bond or a linking group, m = 0-5, n = 0-5 with the proviso that m+n is 2-5, compositions including the compounds and the use of the compounds in the treatment or prophylaxis of ocular conditions.