首页> 外国专利> apply industrial compounds as intermediates in the manufacture of in position 2 replaced: 4 - hydroxy 3 quinolincarboxamid derivatives and the preparation of the intermediates.

apply industrial compounds as intermediates in the manufacture of in position 2 replaced: 4 - hydroxy 3 quinolincarboxamid derivatives and the preparation of the intermediates.

机译:应用工业化合物作为中间体,在位置2处取代:4-羟基3喹啉甲酰胺衍生物和中间体的制备。

摘要

Novel compounds of the formula IMAGE I' wherein X is in the 5,6,7 or 8 position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF3O-, CF3S- and CF3-, R1' is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R2' is selected from the group consisting of hydrogen or an optionally unsaturated ring able to contain one or more heteroatoms of the group consisting of -S-, -O- and -N- optionally substituted with one or more members of the group consisting of (a) halogens, (b) alkyl of 1 to 4 carbon atoms optionally substituted with NH2, -NHAlK or -N--(AlK)2 and AlK is alkyl of 1 to 3 carbon atoms, (c) phenyl, (d) alkoxy of 1 to 4 carbon atoms, (e) -OH, (f) -CF3 and (g) -NO2 or R1' together with the nitrogen atom to which they are attached form an optionally unsaturated ring, the said ring then being connected to the nitrogen atom by a double bond, R3 is selected from the group consisting of hydrogen, halogen and alkyl of 1 to 4 carbon atoms, R4 is selected from the group consisting of hydrogen and halogen, R5 is a halogen with the proviso that R3, R4 and R5 can not all be fluorine and R6 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms and an acyl of an organic carboxylic acid of 2 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts and their salts with non-toxic, pharmaceutically acceptable bases having a remarkable analgesic activity, a very weak anti-inflammatory activity and a good tolerance by the gastrointestinal system and their preparation and their intermediates.
机译: I'的新型化合物,其中X位于5、6、7或8位,并且选自氢,卤素,1-5个碳原子的烷基,1-4个碳原子的烷氧基,CF 3 O-,CF 3 S-和CF 3-,R 1'选自氢和1-4个碳原子的烷基,R 2'选自氢或能够包含一个或多个的任选不饱和环-S-,-O-和-N-组成的基团的杂原子,可选地被一个或多个成员取代,该基团由(a)卤素,(b)1-4个碳原子的烷基,可选地被NH2取代,- NHAlK或-N-(AlK)2和AlK是1-3个碳原子的烷基,(c)苯基,(d)1-4个碳原子的烷氧基,(e)-OH,(f)-CF3和( g)-NO 2或R 1'与它们所连接的氮原子一起形成任选的不饱和环,所述环然后通过双键与氮原子连接,R 3选自下组:由氢,卤素和1-4个碳原子的烷基组成,R4选自氢和卤素,R5是卤素,条件是R3,R4和R5不能全部都是氟,R6选自由氢,1至8个碳原子的烷基和2至8个碳原子的有机羧酸的酰基及其无毒的药学上可接受的酸加成盐及其与无毒的药学上可接受的碱所组成的盐,其中胃肠系统及其制剂和中间体具有出色的止痛作用,非常弱的抗炎活性和良好的耐受性。

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