AMIDE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREFOR AND MEDICINAL APPLICATION THEREOF Russian patent published in 2019 - IPC C07D401/12 C07D209/10 C07D471/04 C07D209/08 C07D231/56 C07D263/57 C07D413/12 C07D209/44 C07D405/12 C07D405/14 C07D405/04 C07D213/78 C07D213/80 C07D417/12 C07D401/04 C07D235/18 C07D307/79 C07C233/63 C07C233/47 A61K31/4439 A61K31/404 A61K31/437 A61K31/416 A61K31/423 A61K31/4035 A61K31/4355 

Abstract RU 2681537 C2

FIELD: chemistry.

SUBSTANCE: present invention relates to a compound of general formula (I), or its enantiomer, or mixtures thereof, or its pharmaceutically acceptable salts:

(I). In formula (I), the ring P is selected from a five-membered heteroaryl having from one to two heteroatoms selected from the group consisting of N, O and S as a ring atom, and a five-membered heterocyclyl having one N heteroatom as a ring atom; the ring Q is selected from phenyl and pyridyl; A, B or Y are selected from -CH- and N; R1 is selected from alkyl containing from 1 to 6 carbon atoms, and cycloalkyl containing from 3 to 6 carbon atoms, where said alkyl, which contains from 1 to 6 carbon atoms, or cycloalkyl, which contains from 3 to 6 carbon atoms, are optionally further substituted with one or more groups selected from the group consisting of alkyl containing from 1 to 6 carbon atoms, halogen and haloalkyl containing from 1 to 6 carbon atoms; R2 is selected from halogen and haloalkyl containing from 1 to 6 carbon atoms; R3 are the same or different and are each independently selected from hydrogen, alkyl containing from 1 to 6 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, five or six membered heterocyclyl having one O hetero atom as a ring atom, and oxo, where the specified alkyl containing from 1 to 6 carbon atoms is optionally additionally substituted by one or more than one group selected from the group consisting of halogen, hydroxyl, alkoxy containing from 1 to 6 carbon atoms, and hydroxyalkyl containing from 1 to 6 carbon atoms; R4 is selected from phenyl and pyridyl, where each of said phenyl and pyridyl is optionally further substituted by one or more groups selected from the group consisting of halogen and haloalkyl containing from 1 to 6 carbon atoms, where the specified halogenated containing from 1 to 6 carbon atoms preferably represents trifluoromethyl; s is an integer from 0 to 3; t is 0 or 1. Also provided are a method for preparing a compound of formula (I), intermediate compounds of formula (IA), (IB), a pharmaceutical composition, and the use of the compound of formula (I).

EFFECT: proposed compounds of formula (I) have the ability to inhibit microsomal prostaglandin E-synthase-1 and can be used to obtain the drug.

17 cl, 4 tbl, 63 ex

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RU 2 681 537 C2

Authors

Li Sin

Khe Vej

Lyu Syanbo

Van Bin

Khu Tsiyue

Tszin Fanfan

Dun Tsin

Sun Pyaoyan

Dates

2019-03-07Published

2015-03-31Filed