Patent SG-11201805202V-A (SG)
Title: 6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE DOPAMINE D3 LIGANDS
Inventor: CHAPPIE THOMAS ALLEN
IPC: A61P3/04
Filed: 2017-01-09
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 111111110111101110101011111010111110111011101110111011101111101111101111011111 International Bureau 0.. .... .. (10) International Publication Number ..... ..or::,„, (43) International Publication Date WO 2017/122116 Al 20 July 2017 (20.07.2017) WIPO I PCT (51) International Patent Classification: (74) Agent: WALDRON, Roy F.; Pfizer Inc., 235 East 42nd C07D 471/04 (2006.01) A61P 3/04 (2006.01) Street, MS 235/9/S20, New York, New York 10017 (US). A61K 31/55 (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: kind of national protection available): AE, AG, AL, AM, PCT/IB2017/050094 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, (22) International Filing Date: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 9 January 2017 (09.01.2017) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (25) Filing Language: English KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (26) Publication Language: English NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (30) Priority Data: RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, 62/279,037 15 January 2016 (15.01.2016) US TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (71) Applicant: PFIZER INC. [US/US]; 235 East 42nd Street, New York, New York 10017 (US). (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (72) Inventors: CHAPPIE, Thomas Allen; 59 Hemlock Hill GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, Road, Carlisle, Massachusetts 01741 (US). HENDER- TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, SON, Jaclyn Louise; 36 Highland Avenue, Apt. 54, Cam- TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, bridge, Massachusetts 02139 (US). YOUNG, Joseph Mi- DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, — chael; 20156 Stanton Avenue, #36, Castro Valley, Califor- LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, — nia 94546 (US). WAGER, Travis T.; _ 465 Washington SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Street, Apt., 6, Brookline, Massachusetts 02446 (US). GW, KM, ML, MR, NE, SN, TD, TG). Street, #3, KORMOS, Bethany Lyn; 46 Quincy Nandini Declarations under Rule 4.17: = Somerville, Massachusetts 02143 (US). PATEL, Massachusetts — as to the identity of the inventor (Rule 4.17(1)) Chaturbhai; 34 Mary Ellen Road, Waban, 02468 (US). SCIABOLA, Simone; 109 River Street, Cam- as to applicant's entitlement to apply for and be granted a Jamison patent (Rule 4.17(11)) Massachusetts bridge, Massachusetts 02139 (US). TUTTLE, = — Bryce; 24 Amherst Road, Marblehead, 23 Calvin — as to the applicant's entitlement to claim the priority of the = 01945 (US). VERHOEST, Patrick Robert; TUCKER, earlier application (Rule 4.17(iii)) Road, Newton, Massachusetts 02460 (US). = Joseph Walter; 25 Dart Street, New London, Connecticut Published: 06320 (US). — with international search report (Art. 21(3)) = = = = = DOPAMINE D3 LIGANDS — (54) Title: 6,7,8,9-TETRAHYDRO-5H-PYRIDO[2,3-d]AZEPINE = (R 2 ) a R 3 .,, ,............7 „ K l r . - - 4— ... ,. ,..., 1 (I) N —R 1 0 0 Il % / R ,tD 5 S N , ..,, , ..,„,\" •••••,, 1-1 A 1-1 ei ei ,-1 N R 4 L ---- (57) : The present invention provides compounds of Formula (I): and pharmaceutically acceptable salts thereof wherein the ::::) variables R I , R 2 , R 3 , R, R 4 5 , a and A are as defined herein; processes for the preparation of; intermediates used in the preparation of; N and compositions containing such compounds or salts, and their uses for treating D3-mediated (or D3-associated) disorders includ - 0 ing, e.g., substance addiction, substance abuse, schizophrenia (e.g., its cognitive symptoms), cognitive impairment (e.g., cognitive ,-t impairment associated with schizophrenia, AD or PD), Parkinson's disease, mania, anxiety, impulse control disorders, sexual dis - .,- orders and depression.