PYRROLOCHINOLINE DERIVATIVES AS 5-HT ANTAGONISTS, METHODS FOR PRODUCTION THEREOF AND USE Russian patent published in 2019 - IPC C07D471/04 A61K31/4745 A61K31/496 A61K31/5377 A61K31/551 A61P1/00 A61P3/10 A61P25/06 A61P25/08 A61P25/18 A61P25/20 A61P25/28 A61P29/00 A61P43/00 

Abstract RU 2688161 C2

FIELD: organic chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to a pyrrolochinoline derivative of formula (XIV) or a stereoisomer or pharmacologically acceptable salt or hydrate thereof, where R1, R2 independently represent hydrogen, alkoxy (C1-C3) a group or an independently selected from cyano, nitro, amino; T is CO, CH2, SO2; Ar is aryl (6-member), optionally substituted with one or two substitutes selected from alkyl(C1-C3) groups, alkyl(C1-C3) a group substituted with three halogen atoms, alkoxy(C1-C3) a group, halogen, cyano and amino; unsubstituted biaryl (10-member); heteroaryl (5-member) containing 1 S atom and optionally substituted with one halogen atom; heteroaryl (9-10-membered) containing 1 heteroatom, selected from a group consisting of N and S, and optionally substituted with one or two substitutes selected from alkyl (C1-C3) a group and a halogen; R3 is a substitute, selected from a group of cyclic or linear, substituted or unsubstituted amines, consisting of structures (XV)–(XVIII), where A is NH, O, CH2, NR5; BR4 is NH, O; R5 is alkyl (C1-C3) a group or benzyl; R6 is alkyl (C1-C3) a group; n is selected from 0, 1, 2; m is selected from 1, 2; l is equal to 1. Invention also relates to specific derivatives of pyrroloquinoline, a pharmaceutical composition based on said compound and use thereof, an intermediate compound of formula (XIX) and a method of producing an intermediate compound.

.

EFFECT: technical result is obtaining novel pyrroloquinoline derivatives, useful in treating diseases caused by disturbed signal transmission through 5-HT6-receptors.

14 cl, 7 dwg, 6 tbl

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RU 2 688 161 C2

Authors

Zajdel Pavel

Grykhovskaya Katazhina

Lamati Frederik

Kolasino Evelina

Bantrej Ksave

Martine Zhan

Pavlovskij Matsej

Satala Gzhegozh

Boyarskij Andzhej J.

Partyka Anna

Vesolovskaya Anna

Kos Tomash

Popik Petr

Syubra Zhil

Dates

2019-05-20Published

2013-07-25Filed