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Pub. No.:    WO/2013/148478    International Application No.:    PCT/US2013/033399
Publication Date: 03.10.2013 International Filing Date: 22.03.2013
A61K 31/497 (2006.01)
Applicants: MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907 (US).
BLIZZARD, Timothy Allen [US/US]; (US) (US only).
BIFTU, Tesfaye [US/US]; (US) (US only)
Inventors: BLIZZARD, Timothy Allen; (US).
BIFTU, Tesfaye; (US)
MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue Rahway, NJ 07065-0907 (US)
Priority Data:
61/616,647 28.03.2012 US
Abstract: front page image
(EN)Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: (I) or a pharmaceutically acceptable salt thereof, wherein Q is CH2, NR4, O, S, S(O) or S(O2), wherein R4 is H, C1-6 alkyl, aryl, or C3-8 cycloalkyl; R1 is a heterocycle or -(CR5R6)1-2NH2, wherein R5 and R6, each time in which they occur, are independently H, C1-6 alkyl, -CH2F,-CHF2, CF3 or -CH2OH; R2 is OH, NH2 or NHSO2CH3; and R3 is C1-6 alkyl.
(FR)L'invention concerne des composés utiles pour l'inhibition de la thrombine et d'occlusions thrombotiques correspondantes présentant la structure suivante : (I) ou un sel pharmaceutiquement acceptable de celle-ci, dans laquelle Q représente CH2, NR4, O, S, S(O) ou S(O2), R4 représentant H, C1-6-alkyle, aryle ou C3-8-cycloalkyle ; R1 représente un hétérocycle ou -(CR5R6)1-2NH2, R5 et R6, à chaque occurrence, représentant indépendamment H, C1-6-alkyle, -CH2F,-CHF2, -CF3 ou -CH2OH ; R2 représente OH, NH2 ou NHSO2CH3 ; et R3 représente C1-6-alkyle.
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)