XIa FACTOR INHIBITORS Russian patent published in 2020 - IPC C07D221/04 C07D401/10 A61K31/4375 A61P7/02 A61P7/04 

Abstract RU 2712268 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a novel compound of formula I or a pharmaceutically acceptable salt thereof. In formula I

,

where X denotes -(C=O)NH- or -NH(C=O)-; R1 denotes phenyl, where said phenyl group is optionally substituted with one to three substitutes independently selected from a group consisting of halogen, R4, (C=O)OR4, NH(C=O)OR4 and 5-member heteroaryl containing 4 nitrogen atoms; R2 denotes hydrogen, hydroxy, halogen or C1-6 alkyl, where said alkyl is optionally substituted with one substitute selected from C3-6 cycloalkyl; R3 denotes phenyl or C3-10 cycloalkyl, where said phenyl and cycloalkyl group are optionally substituted with one substitute selected from (C=O)OR4; R4 is hydrogen or C1-6 alkyl; Rx is hydrogen, hydroxy or halogen; Rz denotes hydrogen.

EFFECT: compound has the properties of a coagulation factor inhibitor hFXIa and can be used for treating venous thromboembolia and pulmonary embolism, as well as in producing a drug for inhibiting thrombin, inhibiting thrombosis, treating thrombosis or preventing thrombosis.

16 cl, 4 ex

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RU 2 712 268 C2

Authors

Mertz, Eric

Liu, Weiguo

Edmondson, Scott, D.

Ali, Amjad

Gao, Ying-Duo

Neelamkavil, Santhosh, F.

So, Sung-Sau

Moningka, Remond

Sun, Wanying

Hruza, Alan

Brockunier, Linda, L.

Dates

2020-01-28Published

2016-01-15Filed