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1. (WO2016053828) C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2016/053828 International Application No.: PCT/US2015/052554
Publication Date: 07.04.2016 International Filing Date: 28.09.2015
IPC:
C07D 513/14 (2006.01)
Applicants: HE, Shuwen[CN/US]; US (US)
CUMMING, Jared, N.[US/US]; US (US)
SCOTT, Jack, D.[US/US]; US (US)
MERCK SHARP & DOHME CORP.[US/US]; 126 East Lincoln Avenue Rahway, NJ 07065-0907, US
Inventors: HE, Shuwen; US
CUMMING, Jared, N.; US
SCOTT, Jack, D.; US
Common
Representative:
MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue Rahway, NJ 07065-0907, US
Priority Data:
62/059,63103.10.2014US
Title (EN) C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
(FR) COMPOSÉS DE DIOXYDE D'IMINOTHIADIAZINE TRICYCLIQUES CONDENSÉS EN C5-C6 UTILISÉS COMME INHIBITEURS DE BACE, COMPOSITIONS LES CONTENANT, ET LEUR UTILISATION
Abstract: front page image
(EN) In its many embodiments, the present invention provides certain C5-C6 fused tricyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R2, R3, RA, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
(FR) Dans plusieurs de ses modes de réalisation, la présente invention concerne certains composés d'iminothiadiazine tricycliques condensés en C5-C6, notamment des composés de formule (I), ou un tautomère de ceux-ci, et des sels pharmaceutiquement acceptables desdits composés et desdits tautomères. Dans la formule (I), R1A, R2, R3, RA, le cycle A, RA, m, -L1-, et RL ont la signification indiquée dans la description. Les nouveaux composés de l'invention sont utiles en tant qu'inhibiteurs de BACE et/ou dans le traitement et la prévention de diverses pathologies associées. L'invention a également trait à des compositions pharmaceutiques comprenant un ou plusieurs desdits composés (seul(s) et en association avec un ou plusieurs autres principes actifs), et à leurs méthodes de préparation et d'utilisation, y compris dans le traitement éventuel de la maladie d'Alzheimer.
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, IR, IS, JP, KE, KG, KN, KP, KR, 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)