Patent SG-11201906134Y-A (SG)
Title: Tyrosine amide derivatives as rho- kinase inhibitors
Inventor: ACCETTA ALESSANDRO
IPC: A61P11/06
Filed: 2018-01-26
Abstract: WO 18/ 138 293 Al R o (I) 0 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 02 August 2018 (02.08.2018) WIP0 I PCT omit VIII °nolo offi onolom mil ono (10) International Publication Number WO 2018/138293 Al (51) International Patent Classification: C07D 471/04 (2006.01) CO7D 487/04 (2006.01) A61K 31/437 (2006.01) CO7D 519/00 (2006.01) A61K 31/519 (2006.01) A61P 11/06 (2006.01) (21) International Application Number: PCT/EP2018/052009 (22) International Filing Date: 26 January 2018 (26.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 17153785.5 30 January 2017 (30.01.2017) EP (71) Applicant: CHIESI FARMACEUTICI S.P.A. [IT/IT]; Via Palermo, 26/A, 43122 PARMA (IT). (72) Inventors: ACCETTA, Alessandro; c/o CHIESI FAR- MACEUTICI S.p.A., Via Palermo, 26/A, 43122 PARMA (IT). RANCATI, Fabio; c/o CHIESI FARMACEUTICI S.p.A., Via Palermo, 26/A, 43122 PARMA (IT). CAPEL- LI, Anna Maria; c/o CHIESI FARMACEUTICI S.p.A., Via Palermo, 26/A, 43122 PARMA (IT). CLARK, David Edward; c/o CHIESI FARMACEUTICI S.p.A., Via Paler- mo, 26/A, 43122 PARMA (IT). TISSELLI, Patrizia; c/ o CHIESI FARMACEUTICI S.p.A., Via Palermo, 26/A, 43122 PARMA (IT). EDWARDS, Christine; c/o CHIESI FARMACEUTICI S.p.A., Via Palermo, 26/A, 43122 PAR- MA (IT). CHEGUILLAUME, Arnaud Jean Francois Auguste; c/o CHIESI FARMACEUTICI S.p.A., Via Paler- mo, 26/A, 43122 PARMA (IT). BHALAY, Gurdip; c/ o CHIESI FARMACEUTICI S.p.A., Via Palermo, 26/A, 43122 PARMA (IT). (74) Agent: MINOJA, Fabrizio; BIANCHETTI BRACCO MINOJA S.r.1., Via Plinio, 63, 20129 MILANO (IT). (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). Published: with international search report (Art. 21(3)) (54) Title: TYROSINE AMIDE DERIVATIVES AS RHO- KINASE INHIBITORS (57) : The invention relates to compounds of formula (I) inhibit- ing Rho Kinase that are bicyclic dihydropyrimidine-carboxamide deriv- atives, methods of preparing such compounds, pharmaceutical composi- tions containing them and therapeutic use thereof. Particularly the com- pounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary dis- eases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).