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1. (WO2018009501) TETRAHYDRONAPHTHYRIDINEPENTANAMIDE INTEGRIN ANTAGONISTS
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/009501 International Application No.: PCT/US2017/040657
Publication Date: 11.01.2018 International Filing Date: 05.07.2017
IPC:
C07D 401/12 (2006.01) ,A61K 31/4375 (2006.01)
Applicants: THE ROCKEFELLER UNIVERSITY[US/US]; Office of Technology Transfer 1230 York Avenue New York, New York 10065-6399, US
ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI[US/US]; One Gustave L. Levy Place Box 1675 New York, New York 10029, US
Inventors: COLLER, Barry S.; US
FILIZOLA, Marta; US
FOLEY, Michael Andrew; US
Agent: HANSEN, Philip E.; US
Priority Data:
62/358,33005.07.2016US
62/374,23412.08.2016US
Title (EN) TETRAHYDRONAPHTHYRIDINEPENTANAMIDE INTEGRIN ANTAGONISTS
(FR) ANTAGONISTES DE L'INTÉGRINE TETRAHYDRONAPHTHYRIDINEPENTANAMIDE
Abstract: front page image
(EN) 2-Substituted-4-(5-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)pentanamido)butanoic acids are disclosed. These compounds selectively inhibit αVβ3 without activating the αVβ3 receptor. They are useful for treating osteoporosis, acute myelogenous leukemia, sickle cell disease, focal segmental glomerulosclerosis, fibrosis, supravalvular aortic stenosis associated with Williams syndrome, tumors expressing αVβ3, tumor metastasis, bone resorption, T-cell lymphoma, retinal disease, age-related macular degeneration, diabetic retinitis, and herpes simplex virus infection. They may also be used for inhibiting tumor angiogenesis.
(FR) L'invention concerne des acides butanoïques 2-substitués-4-(5- (5,6,7,8-tétrahydro -1,8-naphthyridin-2-yl) pentanamido). Ces composés inhibent sélectivement αVβ3 sans activer le récepteur αVβ3. Ils sont utiles pour traiter l'ostéoporose, leucémie aiguë myéloïde, la une drépanocytose, la glomérulosclérose segmentaire focale, la fibrose, la sténose aortique supravalvulaire associée au syndrome de Williams, les tumeurs exprimant αVβ3, les tumeurs métastatiques, la résorption osseuse, le lymphome des lymphocytes T, la maladie rétinienne, la dégénérescence maculaire liée à l'âge, la rétinite diabétique et l'infection par le virus de l'herpès simplex. Ils peuvent également être utilisés pour inhiber l'angiogenèse tumorale.
Designated States: 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
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)