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1. (WO2018039094) PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS
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Pub. No.: WO/2018/039094 International Application No.: PCT/US2017/047718
Publication Date: 01.03.2018 International Filing Date: 21.08.2017
IPC:
C07D 213/89 (2006.01) ,A61K 31/4425 (2006.01) ,A61P 7/02 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
89
with hetero atoms directly attached to the ring nitrogen atom
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
435
having six-membered rings with one nitrogen as the only ring hetero atom
44
Non-condensed pyridines; Hydrogenated derivatives thereof
4425
Pyridinium derivatives, e.g. pralidoxime, pyridostigmine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
Applicants:
SHEN, Dong-Ming [US/US]; US (US)
KUANG, Rongze [US/US]; US (US)
KUMAR, Puneet [IN/US]; US (US)
DUFFY, Joseph, L. [US/US]; US (US)
ZHU, Cheng [CN/US]; US (US)
ALI, Amjad [US/US]; US (US)
YANG, Meng [US/US]; US (US)
DEBENHAM, John, S. [US/US]; US (US)
MERCK SHARP & DOHME CORP. [US/US]; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907, US
Inventors:
SHEN, Dong-Ming; US
KUANG, Rongze; US
KUMAR, Puneet; US
DUFFY, Joseph, L.; US
ZHU, Cheng; US
ALI, Amjad; US
YANG, Meng; US
DEBENHAM, John, S.; US
Common
Representative:
MERCK SHARP & DOHME CORP.; 126 East Lincoln Avenue Rahway, New Jersey 07065-0907, US
Priority Data:
62/377,96922.08.2016US
Title (EN) PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS
(FR) DÉRIVÉS DE PYRIDINE-1-OXYDE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DU FACTEUR XIA
Abstract:
(EN) The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
(FR) La présente invention concerne un composé de formule (I) et des compositions pharmaceutiques comprenant un ou plusieurs desdits composés, ainsi que des méthodes d'utilisation desdits composés pour traiter ou prévenir les thromboses, les embolies, l'hypercoagulabilité ou les changements fibrotiques. Ces composés sont des inhibiteurs sélectifs du facteur XIa ou des inhibiteurs doubles du facteur XIa et de la kallicréine plasmatique.
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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)