CHROMENE DERIVATIVES SUBSTITUTED BY ALKOXIDE AS INHIBITORS OF THE TCR-NCK INTERACTION Russian patent published in 2018 - IPC C07D311/58 C07D405/06 A61K31/352 A61P37/00 

Abstract RU 2658910 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a group of compounds of formula (I) containing a chromene core, wherein: R1 is selected from hydrogen and substituted or unsubstituted C1-C6 alkyl; R2 and R3 are independently selected from hydrogen and substituted or unsubstituted C1-C6 alkyl; or R2 and R3 together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heterocycle, wherein the heterocycle is a stable monocyclic or bicyclic radical containing from 3 to 15 members which is unsaturated, saturated or partially saturated and which consists of carbon atoms and at least one heteroatom selected from the following group: nitrogen, oxygen or sulfur; R4 represents a halogen; each C1-C6 alkyl is optionally and independently substituted with one or more substituents selected from halogen, hydroxyl, carboxyl, carbonyl, cyano, nitro, mercapto, C3-C6 cycloalkyl and NR'R'', where R' and R'' are independently selected from H and unsubstituted C1-C4 alkyl; each C3-C6 cycloalkyl and heterocycle is optionally and independently substituted with one or more substituents selected from halogen, hydroxyl, carboxyl, carbonyl, cyano, nitro, mercapto and unsubstituted C1-C4 alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compound of formula (I) is not 1-((4-(4-fluorophenyl)-6-methoxy-2H-chromen-3-yl)methyl)pyrrolidine, and their production method.

.

EFFECT: compounds of formula I have the ability to inhibit lymphocyte proliferation mediated by the interaction of Nck with TCR, and therefore the invention also relates to the use of said compounds for the treatment of diseases or conditions, in which said interaction causes complications such as graft rejection reactions, immune or autoimmune diseases, inflammatory diseases or proliferative diseases, and the invention relates to pharmaceutical compositions based on compounds of formula I.

42 cl, 3 dwg, 2 tbl, 5 ex

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RU 2 658 910 C2

Authors

Gakhete Mateos Andres

Kastro Palomino Khulio

Marti Klausel Luk

Tormo Karulya Damiya

Dates

2018-06-26Published

2014-10-20Filed