Patent SG-11201810579Y-A (SG)
Title: Pyrimidin-2-ylamino-1h-pyrazols as lrrk2 inhibitors for use in the treatment of neurodegenerative disorders
Inventor: ESTRADA ANTHONY A
IPC: C07D403/14
Filed: 2017-06-15
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 21 December 2017 (21.12.2017) WIP0 I PCT ill~~~~~~~~ 011101tIIl tun HE HE mom!! °nom oimIE (10) International Publication Number WO 2017/218843 Al (51) International Patent Classification: CO7D 403/12 (2006.01) A61K 31/506 (2006.01) CO7D 401/14 (2006.01) A61K 31/5365 (2006.01) CO7D 405/14 (2006.01) A61K 31/519 (2006.01) CO7D 413/14 (2006.01) A61K 31/5377 (2006.01) CO7D 403/14 (2006.01) A61P 25/00 (2006.01) CO7D 409/14 (2006.01) A61P 25/16 (2006.01) CO7D 417/14 (2006.01) A61P 25/28 (2006.01) CO7D 487/04 (2006.01) A61P 25/14 (2006.01) CO7D 491/20 (2006.01) A61P 35/00 (2006.01) CO7D 498/04 (2006.01) A61P 29/00 (2006.01) (21) International Application Number: PCT/US2017/037782 (22) International Filing Date: (74) Agent: TANNER, Lorna L. et al.; Sheppard Mullin Richter & Hampton LLP, 379 Lytton Avenue, Palo Alto, California 94301-1479 (US). (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: as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) Published: — with international search report (Art. 21(3)) 15 June 2017 (15.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/350,876 16 June 2016 (16.06.2016) US 62/417,151 03 November 2016 (03.11.2016) US 62/476,581 24 March 2017 (24.03.2017) US 62/510,711 24 May 2017 (24.05.2017) US = (71) Applicant: DENALI THERAPEUTICS INC. [US/US]; 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). (72) Inventors: ESTRADA, Anthony A.; c/o Denali Therapeu- tics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Fran- cisco, California 94080 (US). FENG, Jianwen A.; c/o De- nali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). LYSSIKA- TOS, Joseph P.; c/o Denali Therapeutics Inc., 151 Oys- ter Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). SWEENEY, Zachary K.; c/o Denali Thera- peutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). DE VICENTE FIDAL- GO, Javier; c/o Denali Therapeutics Inc., 151 Oyster Point Blvd., 2nd Floor, South San Francisco, California 94080 (US). (54) Title: PYRIMIDIN-2-YLAMINO-1H-PYRAZOLS AS LRRK2 INHIBITORS FOR USE IN THE TREATMENT OF NEU- 11 _ .4 RODEGENERATIVE DISORDERS en (57) : The present disclosure relates generally to LRRK2 inhibitors, or a phar- 71' maceutically acceptable salt, deuterated analog, prodrug, tautomer, stereoisomer, or GO N - -- ''''''-rv h R 2 mixture of stereoisomers thereof, and methods of making and using thereof. (Formula GO ,,./,-,. . „!1, (I)) N HN N R 3 (I) IN Ri— N - •- •',-R 4 11 H CZ ei