KAPPA OPIOID RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO

• Main Authors: ROBERTS, Edward, JONES, Robert, ZHAO, Xianrui, LAXAMANA, Candace Mae, URBANO, Mariangela, ROSEN, Hugh, GUERRERO, Miguel A, TURTLE, Eric Douglas
• Format: Patent
• Language: English
• Published: 30.10.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

OPRK_hultlan1.150488 3.5nM) challenge Compound 142 [M] FIG, 7A In hib it io n W O 20 18/ 17 0 49 2 A9 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 1111111111110110101011111011010 I 010 11011M10111110 11101111 (10) International Publication Number WO 2018/170492 A9 20 September 2018 (20.09.2018) WI PO I PCT (51) International Patent Classification: C07D 413/14 (2006.01) A61P 25/24 (2006.01) A61K 31/4709 (2006.01) (21) International Application Number: PCT/US2018/023027 (22) International Filing Date: 16 March 2018 (16.03.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/473,209 17 March 2017 (17.03.2017) US 62/585,447 13 November 2017 (13.11.2017) US 62/609,960 22 December 2017 (22.12.2017) US (71) Applicants: THE SCRIPPS RESEARCH INSTITUTE [US/US]; 10550 North Tony Pines Rd, La Jolla, California 92037 (US). BLACKTHORN THERAPEUTICS, INC. [US/US]; 780 Brannan Street, San Francisco, CA 94103 (US). (72) Inventors: ROBERTS, Edward; 1 Rolling View Lane, Fallbrook, California 92028 (US). GUERRERO, Miguel A.; 8017 Camino Kiosco, San Diego, California 92122 (US). URBANO, Mariangela; 425 Stratford Court, Apt. 10, Del Mar, California 92014 (US). ROSEN, Hugh; 8579 Prestwick Drive, La Jolla, California 92037 (US). JONES, Robert, M.; 400 Mariners Island Blvd, #301, San Mateo, CA 94404 (US). LAXAMANA, Candace Mae; 1930 Fol- som St., Apt B, San Francisco, CA 94103 (US). ZHAO, Xianrui; 790 Edgewater Blvd, Apt 107, Foster City, CA 94404 (US). TURTLE, Eric Douglas; 2703 Monserat Ave, Belmont, California 94002 (US). (74) Agent: COOPER, Michael, P. et al.; Seed Intellectual Property Law Group LLP, Suite 5400, 701 Fifth Avenue, Seattle, Washington 98104-7064 (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, (54) Title: KAPPA OPIOID RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO (57) : Compounds are provided that antagonize the kap- pa-opioid receptor (KOR) and products containing such com- pounds, as well as to methods of their use and synthesis. Such ( ) 1 compounds have the structure of Formula (I), or a pharmaceutic ally acceptable isomer, racemate, hydrate, solvate, isotope or salt R 8 _R 11 R2 R 2 , R 4 , R s R6, R 7 , R 8 thereof: (I) wherein X, Y, R 1 , and R 11 are as defined herein. [Continued on next page] WO 2018/170492 A9 IMEDIMOM0101011MEIHOMMENEE10IIgninill 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). Published: - with international search report (Art. 21(3)) (48) Date of publication of this corrected version: 13 December 2018 (13.12.2018) (15) Information about Correction: see Notice of 13 December 2018 (13.12.2018)