Patent SG-11201408044Q-A (SG)
Title: NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS
Inventor: GALATSIS PAUL
IPC: C07D487/04
Filed: 2013-06-19
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 3 January 2014 (03.01.2014) WIPOIPCT (10) International Publication Number WO 2014/001973 A1 (51) International Patent Classification: C07D 487/04 (2006.01) C07D 519/00 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/IB2013/055039 19 June 2013 (19.06.2013) English English (30) Priority Data: 61/666,299 61/820,828 29 June 2012 (29.06.2012) US 8 May 2013 (08.05.2013) US (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, New York, New York 10017 (US). (72) Inventors: GALATSIS, Paul; 375 Cherry Street, Newton, MA 02465 (US). HAYWARD, Matthew Merrill; 3 Pyrus Court, Old Lyme, Connecticut 06371 (US). HENDER­ SON, Jaclyn; 36 Highland Avenue, Apt. 54, Cambridge, Massachusetts 02139 (US). KORMOS, Bethany Lyn; 46 Quincy Street, #3, Somerville, Massachusetts 02143 (US). KURUMBAIL, Ravi G; 4 Harvest Glen, East Lyme, Con­ necticut 06333 (US). STEPAN, Antonia Friederike; 50 Park Row West, Apt. 420, Providence, Rhode Island — 02903 (US). VERHOEST, Patrick Robert; 23 Calvin Road, Newton, Massachusetts 02460 (US). WAGER, Travis T.; 465 Washington Street, Apt. 6, Brookline, Mas­ sachusetts 02446 (US). ZHANG, Lei; 75 Bourne Street, Auburndale, Massachusetts 02466 (US). (74) Agent: OLSON, A. Dean; Pfizer Inc., Eastern Point Road MS8260-2141, Groton, Connecticut 06340 (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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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, 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)) — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) [Continued on next page] (54) Title: NOVEL 4-(SUBSTITUTED-AMINO)-7H-PYRROLO[2,3-d]PYRIMIDINES AS LRRK2 INHIBITORS l> 0\ i-H o o o CJ o & (57) Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3- c/]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R , 1 R , 2 R , 3 R 4 and R 5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy. WO 2014/001973 A11 lllll llllllll II llllll III III lllll llll lllll lllll III III lllll lllll llll lllll llll lllllll llll llll Published: — with international search report (Art. 21(3))