RU2013118393A - Quinoline derivatives, in particular 6,7-substituted with 1- (2-chloroquinolin-3-yl) -4-dimethylamino-2- (naphthalen-1-yl) -1-phenylbutane-2-oli, a method for their production FOR THE TREATMENT OF INFECTIOUS DISEASES OF MYCOBACTERIAL NATURE, IN PARTICULAR TUBERCULOSIS - Google Patents

Quinoline derivatives, in particular 6,7-substituted with 1- (2-chloroquinolin-3-yl) -4-dimethylamino-2- (naphthalen-1-yl) -1-phenylbutane-2-oli, a method for their production FOR THE TREATMENT OF INFECTIOUS DISEASES OF MYCOBACTERIAL NATURE, IN PARTICULAR TUBERCULOSIS Download PDF

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RU2013118393A
RU2013118393A RU2013118393/04A RU2013118393A RU2013118393A RU 2013118393 A RU2013118393 A RU 2013118393A RU 2013118393/04 A RU2013118393/04 A RU 2013118393/04A RU 2013118393 A RU2013118393 A RU 2013118393A RU 2013118393 A RU2013118393 A RU 2013118393A
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substituted
chloroquinolin
mycobacterial
naphthalen
dimethylamino
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RU2013118393/04A
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RU2530493C1 (en
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Анна Борисовна Назаренко
Владимир Егорович Федоров
Вадим Игоревич Ильин
Антон Владимирович Омельков
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Закрытое Акционерное Общество "Фарм-Синтез"
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Abstract

1. Производные хинолина, в частности 6,7-замещенные 1-(2-хлорхинолин-3-ил)-4-диметиламино-2-(нафталин-1-ил)-1-фенилбутан-2-олы общей формулы (I):где Rозначает Н,R+Rозначает -O-(СН)-O-, где n=1-2, что образует дополнительные диоксановый и 1,3-диоксолановый циклы, или их фармацевтически приемлемые соли с кислотами, обладающие антимикобактериальной активностью.2. Способ получения соединений формулы (I) по п.1 путем взаимодействия замещенных 2-хлор-3-алкарилхинолинов и арилкетонов под действием металлирующих агентов.3. Способ по п.2, отличающийся тем, что в качестве металлирующего агента используют диэтиламид лития.4. Применение соединений по п.1 для лечения инфекционных заболеваний микобактериальной природы, в частности туберкулеза.1. Quinoline derivatives, in particular 6,7-substituted 1- (2-chloroquinolin-3-yl) -4-dimethylamino-2- (naphthalen-1-yl) -1-phenylbutan-2-oles of the general formula (I) : where R is H, R + R is -O- (CH) -O-, where n = 1-2, which forms additional dioxane and 1,3-dioxolane rings, or their pharmaceutically acceptable salts with acids, having antimycobacterial activity. 2 . A method for producing compounds of formula (I) according to claim 1 by reacting substituted 2-chloro-3-alkarylquinolines and arylketones under the action of metalating agents. The method according to claim 2, characterized in that lithium diethylamide is used as the metallizing agent. The use of compounds according to claim 1 for the treatment of infectious diseases of mycobacterial nature, in particular tuberculosis.

Claims (4)

1. Производные хинолина, в частности 6,7-замещенные 1-(2-хлорхинолин-3-ил)-4-диметиламино-2-(нафталин-1-ил)-1-фенилбутан-2-олы общей формулы (I):1. Quinoline derivatives, in particular 6,7-substituted 1- (2-chloroquinolin-3-yl) -4-dimethylamino-2- (naphthalen-1-yl) -1-phenylbutan-2-oles of the general formula (I) :
Figure 00000001
Figure 00000001
 где R1 означает Н,where R 1 means H, R2+R3 означает -O-(СН2)n-O-, где n=1-2, что образует дополнительные диоксановый и 1,3-диоксолановый циклы, или их фармацевтически приемлемые соли с кислотами, обладающие антимикобактериальной активностью.R 2 + R 3 means -O- (CH 2 ) n -O-, where n = 1-2, which forms additional dioxane and 1,3-dioxolane rings, or their pharmaceutically acceptable salts with acids having antimycobacterial activity. 2. Способ получения соединений формулы (I) по п.1 путем взаимодействия замещенных 2-хлор-3-алкарилхинолинов и арилкетонов под действием металлирующих агентов.2. A method for producing compounds of formula (I) according to claim 1 by reacting substituted 2-chloro-3-alkarylquinolines and arylketones under the action of metalating agents. 3. Способ по п.2, отличающийся тем, что в качестве металлирующего агента используют диэтиламид лития.3. The method according to claim 2, characterized in that lithium diethylamide is used as the metallizing agent. 4. Применение соединений по п.1 для лечения инфекционных заболеваний микобактериальной природы, в частности туберкулеза. 4. The use of compounds according to claim 1 for the treatment of infectious diseases of mycobacterial nature, in particular tuberculosis.
RU2013118393/04A 2013-04-22 2013-04-22 Quinoline derivatives, particularly 6,7-substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1-phenylbutan-2-ols, method for production thereof and use of compounds to treat infectious mycobacterial dieseases, particularly tuberculosis RU2530493C1 (en)

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PT2301544E (en) * 2002-07-25 2012-12-10 Janssen Pharmaceutica Nv Quinoline derivatives as intermediates to mycobacterial inhibitors
RU2404971C2 (en) * 2008-12-02 2010-11-27 ЗАО "Фарм-Синтез" Novel quinoline derivatives, synthesis method thereof, use thereof in treating mycobacterial infections, pharmaceutical composition based on said derivatives

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