Patent SG-11201810854S-A (SG)
Title: Aliphatic prolinamide derivatives
Inventor: CHEN AUSTIN
IPC: C07D401/04
Filed: 2017-06-15
Abstract: Title: ALIPHATIC PROLINAMIDE DERIVATIVES Ric R3a R 3 b 0 R 1 I (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) WIPO I PCT omit VIII Hot o Homomomim Holm° lII ois (10) International Publication Number WO 2017/222917 Al (51) International Patent Classification: CO7D 207/08 (2006.01) A61K 31/40 (2006.01) CO7D 207/09 (2006.01) A61K 31/454 (2006.01) C07D 401/04 (2006.01) (21) International Application Number: PCT/US2017/037773 (22) International Filing Date: 15 June 2017 (15.06.2017) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/352,965 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: CHEN, Austin, Chih-Yu; 1142 Festival Road, San Marcos, CA 92078 (US). GOMEZ, Robert; 3344 Mt. Seymour Parkway, North Vancouver, British Colum- bia, V7H 1G3 (CA). OBALLA, Renata, Marcella; 1973 Custer Court, Coquitlam, British Columbia, V3J 6R2 (CA). POWELL, David, Andrew; 1781 Napier Street, Vancou- ver, British Columbia, V5L 2N1 (CA). ROPPE, Jeffrey, Roger; 45004 Oakford Court, Temecula, CA 92592 (US). SEIDERS, Thomas, Jon; 5257 Soledad Mountain Road, San Diego, CA 92109 (US). SHENG, Tao; 631 Elbert Av- enue, Coquitlam, British Columbia, V3J 2L1 (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). W O 20 17 / 2229 17 Al (57) : This invention is directed to novel aliphatic prolinamide derivatives of Formula I, and pharmaceutically acceptable salts, sol- vates, solvates of the salt and prodrugs thereof, useful in the preven- tion (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 degeneration 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 atrophy, diabetic retinopathy, retinopathy of prematurity, polypoidal choroidal vasculopathy, and degeneration of retinal or pho- toreceptor cells, comprising: administration of a therapeutically effec- tive amount of compound of the invention. The compounds of the in- vention are inhibitors of HTRAl. 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 HTRAl. The compounds of the in- vention are also useful for inhibiting HTRA1 protease activity in an eye or locus of an arthritis or related condition. [Continued on next page] WO 2017/222917 Al IMEDIMOMMIONOIDEMEEHOEMIHOEHME#011# Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(H)) 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))