Patent SG-11201810848P-A (SG)
Title: Heterocyclic prolinamide derivatives
Inventor: GOMEZ ROBERT
IPC: C07D409/14
Filed: 2017-06-15
Abstract: WO 17 / 222915 Al (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 28 December 2017 (28.12.2017) WIP0 I PCT omit VIII Hot o Homomomim OH ois (10) International Publication Number WO 2017/222915 Al (51) International Patent Classification: CO7D 401/14 (2006.01) A61K 31/454 (2006.01) CO7D 405/14 (2006.01) A61K 31/4192 (2006.01) C07D 409/14 (2006.01) (21) International Application Number: PCT/US2017/037768 (22) International Filing Date: 15 June 2017 (15.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/352,963 21 June 2016 (21.06.2016) US (71) Applicant: INCEPTION 4, INC. [US/US]; 5871 Oberlin Drive, Suite 100, San Diego, CA 92121 (US). (72) Inventors: GOMEZ, Robert; 3344 Mt. Seymour Park- way, North Vancouver, BC V7H 1G3 (CA). DING, Jinyue; 17-9088 Halston Court, Burnaby, BC V3N 0A7 (CA). OBALLA, Renata, Marcella; 1973 Custer Court, Co- quitlam, BC V3J 6R2 (CA). POWELL, David, Andrew; 1781 Napier Street, Vancouver, BC V5L 2N1 (CA). EPI- FANOV, Maxim; 2460 Trutch Street, Vancouver, BC V6K 4H4 (CA). (74) Agent: MALLON, Joseph, J.; Knobbe Martens Olson & Bear LLP, 2040 Main Street, Fourteenth Floor, Irvine, CA 92614 (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). Declarations under Rule 4.17: 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)) Published: — with international search report (Art. 21(3)) (54) Title: HETEROCYCLIC PROLINAMIDE DERIVATIVES (57) : This invention is directed to novel heterocyclic prolinamide derivatives of Formula (I), and pharmaceutically acceptable salts, solvates, solvates of the salt and prodrugs thereof, useful in the prevention (e.g., delaying the onset of or reducing the risk of developing) and treatment (e.g., controlling, alleviating, or slowing the progression of) of age-related macular degeneration (AMD) and related diseases of the eye. These diseases include dry-AMD, wet-AMD, geographic atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degenera- tion of retinal or photoreceptor cells. The invention disclosed herein is further directed to methods of prevention, slowing the progress of, and treatment of dry-AMD, wet-AMD, and geographic at- rophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and de- generation of retinal or photoreceptor cells, comprising: administration of a therapeutically effective amount of compound of the invention. The compounds of the invention are inhibitors of HTRA1. Thus, the compounds of the invention are useful in the prevention and treatment of a wide range of diseases mediated (in whole or in part) by HTRA1. The compounds of the invention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition. H (I)