Patent SG-11201808220V-A (SG)
Title: Allosteric modulators of nicotinic acetylcholine receptors
Inventor: CROWLEY BRENDAN
IPC: C07D233/64
Filed: 2017-03-20
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization MD 1111101110101011111 HO 11111 011101111011110101111101111111011011# International Bureau ... ...j .......,./ (10) International Publication Number (43) International Publication Date WO 2017/165256 Al 28 September 2017 (28.09.2017) WIP0 I PCT (51) International Patent Classification: Ranley Grove, Paddington, New South Wales QLD4064 C07D 231/12 (2006.01) C07D 261/08 (2006.01) C07D 233/64 (2006.01) C07D 263/32 (2006.01) C07D 413/04 (2006.01) C07D 271/06 (2006.01) C07D 413/06 (2006.01) C07D 495/04 (2006.01) (AU). HUFF, Belinda, C. [AU/AU]; 85 Morphett Road, Camden Park, South Australia 5038 (AU). LEAVITT, Kenneth, J. [US/US]; 770 Sumneytown Pike, West Point, Pennsylvania 19486 (US). RADA, Vanessa, L. [US/US]; C07D 413/10 (2006.01) C07D 277/26 (2006.01) 770 Sumneytown Pike, West Point, Pennsylvania 19486 C07D 417/04 (2006.01) C07D 285/08 (2006.01) (US). SANDERS, John, M. [US/US]; 770 Sumneytown C07D 249/06 (2006.01) CO7D 285/12 (2006.01) Pike, West Point, Pennsylvania 19486 (US). SHIPE, Wil- CO7D 249/08 (2006.01) Ram, D. [US/US]; 770 Sumneytown Pike, West Point, (21) International Application Number: Pennsylvania 19486 (US). SUEN, Linda, M. [US/US]; PCT/US2017/023127 770 Sumneytown Pike, West Point, Pennsylvania 19486 (US). BELL, Ian, M. [US/US]; 770 Sumneytown Pike, (22) International Filing Date: West Point, Pennsylvania 19486 (US). 20 March 2017 (20.03.2017) (74) Common Representative: MERCK SHARP & DOHME (25) Filing Language: English CORP.; 126 East Lincoln Avenue, Rahway, New Jersey 07065-0907 (US). (26) Publication Language: English (81) Designated States (unless otherwise indicated, for every (30) Priority Data: kind of national protection available): AE, AG, AL, AM, 62/311,888 22 March 2016 (22.03.2016) US AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, 62/369,778 2 August 2016 (02.08.2016) US BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (71) Applicant: MERCK SHARP & DOHME CORP. DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, [US/US]; 126 East Lincoln Avenue, Rahway, New Jersey HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, 07065-0907 (US). KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, = Inventors; and NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (72) (71) Applicants (for US only): CROWLEY, Brendan, M. RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, [US/US]; 770 Sumneytown Pike, West Point, Pennsylvania TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 19486 (US). CAMPBELL, Brian, T. [US/US]; 770 Sum- ZA, ZM, ZW. neytown Pike, West Point, Pennsylvania 19486 (US). DUFFY, Joseph, L. [US/US]; 2000 Galloping Hill Road, (84) Designated States (unless otherwise indicated, for every Kenilworth, New Jersey 07033 (US). GRESHOCK, kind of regional protection available): ARIPO (BW, GH, Thomas, J. [US/US]; 770 Sumneytown Pike, West Point, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Pennsylvania 19486 (US). GUIADEEN, Deodial, G. TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, [US/US]; 770 Sumneytown Pike, West Point, Pennsylvania TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, 19486 (US). HARVEY, Andrew John [AU/AU]; 4A/6 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, [Continued on next page] Title: ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS (54) R 3 R4 Y \ A ir) ei R 5 ir) X 0) 1-1 N 1-1 (57) : The present disclosure relates to compounds of formula (I) that are useful as modulators of ca nAChR, compositions N comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well 0 as for L-DOPA induced-dyskinesia and inflammation. WO 2017/165256 Al MIDEDIMOMOIDEIR010130HinillUMMOIMIE SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, as to the applicant's entitlement to claim the priority of GW, KM, ML, MR, NE, SN, TD, TG). the earlier application (Rule 4.17(iii)) Declarations under Rule 4.17: Published: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(0 with international search report (Art. 21(3))