公开(公告)号：WO2013039428A3

公开(公告)日：2013-05-10

申请号：PCT/RU2012000725

申请日：2012-09-04

Applicant: ZAKRYTOE AKTSIONERNOE OBSCHESTVO PHARM SINTEZ ,  NAZARENKO ANNA BORISOVNA ,  FEDOROV VLADIMIR EGOROVICH ,  ILIIN VADIM EGOREVICH ,  OMELKOV ANTON VLADIMIROVICH ,  RUCHKO EVSEJ ALEKSANDROVICH

Inventor： NAZARENKO ANNA BORISOVNA ,  FEDOROV VLADIMIR EGOROVICH ,  ILIIN VADIM EGOREVICH ,  OMELKOV ANTON VLADIMIROVICH ,  RUCHKO EVSEJ ALEKSANDROVICH

IPC: C07D215/18 ,  A61K31/47 ,  A61P31/06

CPC classification number: C07D215/18 ,  C07D215/20 ,  C07D491/056

Abstract: The present invention relates to novel quinoline derivatives, such as substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1- phenylbutan-2-ols, to a method for producing same, and also to the use thereof as antimycobacterial agents, in particular to 5,6,7-substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1- phenylbutan-2-ols of general formula (I), where R1 is Н or methoxy, R2 is Н, methoxy or -O-(CH2)n-O-, R3 is Н, methoxy or -O-(CH2)n-O-, n=1-2, and also to the pharmaceutically acceptable salts thereof with acids which exhibit activity in relation to mycobacteria. The invention also relates to a method for producing compounds of formula (I), which consists in interacting corresponding arylquinolines with an aromatic ketone and using said compounds as an active principle in the creation of anti-tubercular medicinal preparations.

Abstract translation: 本发明涉及新颖的喹啉衍生物，例如取代的1-（2-氯喹啉-3-基）-4-二甲基氨基-2-（萘-1-基）-1-苯基丁-2-醇， 以及作为抗分枝杆菌剂的用途，特别是5,6,7-取代的1-（2-氯喹啉-3-基）-4-二甲基氨基-2-（萘-1-基）-1 （I）的苯基丁-2-醇，其中R 1是Н或甲氧基，R 2是Н，甲氧基或-O-（CH 2）n O-，R 3是Н，甲氧基或-O-（CH 2）n O-， n = 1-2，并且其药学上可接受的盐与表现出与分枝杆菌有关的活性的酸。 本发明还涉及一种制备式（I）化合物的方法，其包括将相应的芳基喹啉与芳族酮相互作用，并使用所述化合物作为抗结核药物制剂的产生的活性成分。