COMPOUNDS Russian patent published in 2017 - IPC C07D401/14 C07D471/04 C07D487/04 A61K31/437 A61K31/519 A61P7/02 

Abstract RU 2630677 C2

FIELD: pharmacology.

SUBSTANCE: invention relates to compounds of the general formula

,

where Cyc1 is imidazolyl or triazolyl; Cyc2 is phenyl; Cyc3 is phenyl or 5-10 membered heteroaryl containing 1 heteroatom selected from S and N; R1 is halogen; s is equal to 0 or 1, R2 is hydrogen; R3 is hydrogen, C1-8 alkyl or C1-8 alkyl which is substituted by a group selected from pyridyl or -OC1-8 alkyl; Y is N or C (R5); R4 is hydrogen or C1-4 alkyl; R5 is hydrogen or halogen; or R3 and R4 can be taken together to form C2 alkylene; where one carbon of the alkylene chain can be replaced by sulfur; R6 is C1-8 alkyl, Cyc10, halogen or Cyc10 substituted by halogen or cyano, wherein Cyc10 is a 5-membered heteroaryl containing 3-4 nitrogen atoms; m is equal to 2, where each R6 can be the same or different; R7 is halogen, -NH2, -COOR48, -NHC (O) O-C1-8 alkyl, -NHC (O) O-C1-4 alkylene-OC1-8 alkyl; R48 is hydrogen or C1-8 alkyl; n is equal to 1 or 2, where n is an integer 2, each R7 can be the same or different; and R62 is hydrogen, their pharmaceutically acceptable salts or solvates thereof.

EFFECT: compounds are factor XIa inhibitors, so they can be used to prevent or treat thromboembolic diseases.

15 cl, 3 tbl, 927 ex

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Authors

Kortni Stiv

Yarnold Kris

Flenegan Styuart

Brejs Garet

Barker Dzhon

Itikhara Osamu

Gadulo Eliz

Richardson Entoni

Kondo Takasi

Imagava Akira

Nakatani Singo

Suzuki Rio

Kouyama So

Dates

2017-09-12Published

2012-12-20Filed