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in particular, quinoline derivatives with antiviral properties, production and biological applications thereof

机译:特别是具有抗病毒特性的喹啉衍生物及其生产和生物学应用

摘要

The invention concerns quinoline derivatives of formula (I) in which: Ra, Rb and Rc, identical or different represent one or several substituents, themselves identical or different, in any position on the cycles, this or these substituents being selected among a -(CH2)n-Y or -CH=CH-Y group, in which Y is halogen, -OH, -OR, -COH, -COR, -COOH, COOR, -COH, -COR, -CONH2, -CON(Rx, Ry)-CH=NOH, -CO- -CH=NOH, -NH2, -N(Rx, Ry), -NO2, -PO(OR)2-SH2, -SR, -SO2R, -SO2NHR, CN, or Z(Rc) in which R is a C1-C8 alkyl, or aryl or a heterocyclic compound, Rx and Ry, identical or different are C1-C5 alkyl, an aryl or heterocyclic compound and n is nil or a whole number between 1 and 5 Rb can further represent a hydrogen, and when Y is -COOH or -COOR in Rc, Z, if it represents an aryl, comprises at least 3 substituents or the quinoline ring is trisubstituted; X is an ethylene double bond; a -(CH2)n- group in which n is a whole number between 1 and 5: or a -CH(Rd-CH(Re) group, Rd and Re, identical or different, representing a hydrogen, a halogen, hydroxy or epoxy; or a -(CH2)n, -O-C-(CH2)m-, -(CH2)n, -C(O)-O-(CH2)m, -(CH2)n, -O-(CH2)m-, (CH2)n, -N(Q)-(CH2)m-, or (CH2)n, -S(O)-(CH2)m-, group, in which n=1 to 8, m=0 to 8, t=0, 1 or 2, and Q=h, aryl or alkyl. The invention also concerns the pharmaceutically acceptable salts of these derivatives, the diastereoisomeric and the enantiomeric forms thereof. The invention is useful as medicines with HIV anti-integrase inhibiting effect.
机译:本发明涉及式(I)的喹啉衍生物,其中:Ra,Rb和Rc,相同或不同表示在循环的任何位置上一个或几个本身相同或不同的取代基,该或这些取代基选自-( CH2)nY或-CH = CH-Y基团,其中Y为卤素,-OH,-OR,-COH,-COR,-COOH,COOR,-COH,-COR,-CONH2,-CON(Rx,Ry )-CH = NOH,-CO- -CH = NOH,-NH2,-N(Rx,Ry),-NO2,-PO(OR)2-SH2,-SR,-SO2R,-SO2NHR,CN或Z (Rc)其中R是C1-C8烷基,或芳基或杂环化合物,Rx和Ry,相同或不同是C1-C5烷基,芳基或杂环化合物,n是nil或1至5之间的整数Rb可以进一步代表氢,并且当Rc中的Y是-COOH或-COOR时,Z,如果代表芳基,则包含至少3个取代基或喹啉环被三取代; X是亚乙基双键;一个-(CH2)n-基团,其中n是1到5之间的整数:或-CH(Rd-CH(Re)基团,Rd和Re,相同或不同,表示氢,卤素,羟基或环氧;或-(CH2)n,-OC-(CH2)m-,-(CH2)n,-C(O)-O-(CH2)m,-(CH2)n,-O-(CH2) m-,(CH2)n,-N(Q)-(CH2)m-或(CH2)n,-S(O)-(CH2)m-基团,其中n = 1至8,m = 0至8,t = 0,1或2,和Q = h,芳基或烷基,本发明还涉及这些衍生物的药学上可接受的盐,其非对映异构体和对映体形式,本发明可用作抗HIV的药物-整合酶抑制作用。

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