Patent SG-11201908322W-A (SG)
Title: Novel imidazo[4,5-c]quinoline derivatives as lrrk2 inhibitors
Inventor: BRODNEY MICHAEL AARON
IPC: A61K31/437
Filed: 2018-03-06
Abstract: International Patent Classification: CO7D 471/04 (2006.01) A61P 25/16 (2006.01) CO7D 519/00 (2006.01) A61P 25/28 (2006.01) A61K 31/437 (2006.01) A61P 25/18 (2006.01) (21) International Application Number: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 13 September 2018 (13.09.2018) WIPO I PCT ~~ll~~~~~~~~ 011101010VIIIOH olo omio111111111flo ow (10) International Publication Number WO 2018/163066 Al PCT/IB2018/051439 (22) International Filing Date: 06 March 2018 (06.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/469,756 10 March 2017 (10.03.2017) US 62/629,152 12 February 2018 (12.02.2018) US (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, New York, New York 10017 (US). (72) Inventors: BRODNEY, Michael Aaron; 100 Upland Av- enue, Newton, Massachusetts 02461 (US). CHAPPIE, Thomas Allen; 59 Hemlock Hill Road, Carlisle, Massachu- setts 01741 (US). CHEN, Jinshan Michael; 39 Governors Way, Madison, Connecticut 06443 (US). COE, Jotham Wadsworth; 8 Bush Hill Drive, Niantic, Connecticut 06357 (US). COFFMAN, Karen Jean; 3 Clarence Ave., Paw- catuck, Connecticut 06379 (US). GALATSIS, Paul; 375 Cherry Street, Newton, Massachusetts 02465 (US). GAR- NSEY, Michelle Renee; 386 Morris Ave., Providence, Rhode Island 02906 (US). HELAL, Christopher John; 18 Elm Street, Mystic, Connecticut 06355 (US). HEN- DERSON, Jaclyn Louise; 36 Highland Avenue, Apt. 54, Cambridge, Massachusetts 02139 (US). KORMOS, Bethany Lyn; 46 Quincy Street, #3, Somerville, Massa- chusetts 02143 (US). KURUMBAIL, Ravi G.; 4 Harvest Glen, East Lyme, Connecticut 06333 (US). MARTINEZ- Declarations under Rule 4.17: ALSINA, Luis Angel; 58 Eagle Ridge Drive, Gales Ferry, Connecticut 06335 (US). PETTERSSON, Mar- tin Youngjin; 3 Gilson Road, Littleton, Massachusetts 01460 (US). REESE, Matthew Richard; 25 Ocean View Avenue, Mystic, Connecticut 06355 (US). ROSE, Colin Richard; 35 B Lower Bartlett Road, Quaker Hill, Connecti- cut 06375 (US). STEPAN, Antonia Friederike; Rotdorn- weg 8, 88400 Biberach An Der Riss (DE). VERHOEST, Patrick Robert; 23 Calvin Road, Newton, Massachusetts 02460 (US). WAGER, Travis T.; 465 Washington Street, Apt. 6, Brookline, Massachusetts 02446 (US). WARMUS, Joseph Scott; 18 Sable Drive, Ledyard, Connecticut 06339 (US). ZHANG, Yuan; 12103 Maple Tree Lane, East Lyme, Connecticut 06333 (US). (74) Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd Street, MS 235/9/S20, New York, New York 10017 (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). as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii)) W O 20 18/ 163066 Al (54) Title: NOVEL IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS LRRK2 INHIBITORS (57) : The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R 1 , R 2 and R 3 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 dis- ease or Alzheimer's disease, cancer, Crohn's disease or leprosy. (I) [Continued on next page] WO 2018/163066 Al MIDEDIMOMMIDIIMEIEWHIDIENIEMIEMOVOIS Published: with international search report (Art. 21(3)) in black and white; the international application as filed contained color or greyscale and is available for download from PATENTSCOPE