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    • 4. 发明授权
    • Esters and amides containing the
1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetyl moiety
    • 含有1-(4-氯苯甲酰基)-5-甲氧基-2-甲基-1H-吲哚-3-乙酰基部分的酯和酰胺
    • US4362738A
    • 1982-12-07
    • US158587
    • 1980-06-11
    • Johannes KeckGerd KrugerHelmut PieperKlaus NollGunther EngelhardtNorbert PrombergerRainer Zimmermann
    • Johannes KeckGerd KrugerHelmut PieperKlaus NollGunther EngelhardtNorbert PrombergerRainer Zimmermann
    • C07D209/08A61K31/495A61P29/00C07C67/00C07C227/00C07C227/16C07C227/18C07C229/54C07C237/32C07C237/38C07C313/00C07C323/12C07C323/65C07D209/28C07D213/74C07D295/088C07D295/155C07D401/12C07H13/08C07D279/18A61K27/00
    • C07D213/74C07D209/28C07D295/088C07D295/155
    • Compounds of the formula ##STR1## wherein each X, which may be identical or different from the other X, is oxygen or imino;R.sub.1 is hydrogen, fluorine, chlorine or bromine;R.sub.2 and R.sub.3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms;R.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, are pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-aryl-piperazino or N-(alkyl of 1 to 3 carbon atoms)-piperazino;A is cycloalkylene of 5 to 7 carbon atoms; unsubstituted or substituted alkylene of 2 to 10 carbon atoms, where the substituents are one to two alkyls of 1 to 3 carbon atoms each, one to two carbalkoxys of 2 to 4 carbon atoms each, one to two phenyls, one to four hydroxyls, one halomethyl, one hydroxymethyl, one alkanoyloxy of 1 to 18 carbon atoms, one alkanoyloxymethyl of 1 to 18 carbon atoms in the alkanoyl moiety or one ##STR2## where R.sub.1, R.sub.2 and R.sub.3 have the meanings previously defined; or alkylene of 2 to 10 carbon atoms interrupted by oxygen, sulfur, sulfoxide, sulfonyl, phenyl, cyclohexyl, pyridyl, piperazino or unsubstituted or substituted imino, where the substituent on the imino group is alkyl of 1 to 6 carbon atoms, phenyl or phenylalkyl of 1 to 3 carbon atoms in the alkyl moiety;B is the acyl residue of an antiphlogistic carboxylic acid;and their non-toxic, pharmacologically acceptable acid addition salts. The compounds as well as their salts are useful as anti-inflammatories.
    • 其中每个X可以相同或不同于另一个X的式“IMAGE”的化合物是氧或亚氨基; R1是氢,氟,氯或溴; R2和R3可以相同或不同,分别为氢; 未取代或单取代的1至6个碳原子的烷基,其中取代基为苯基或每个烷基部分具有1至3个碳原子的二烷基氨基; 吡啶基 或5至7个碳原子的环烷基; 吡咯烷基,哌啶子基,六亚甲基亚氨基,吗啉代,N-芳基 - 哌嗪子基或N-(1至3个碳原子的烷基) - 哌嗪基; R 2和R 3彼此连接并连接的氮原子。 A是5至7个碳原子的亚环烷基; 2至10个碳原子的未取代或取代的亚烷基,其中取代基为1至2个碳原子数为1至2个的烷基,每个为2至4个碳原子的1至2个碳烷氧基,1至2个苯基,1至4个羟基,1至2个 卤代甲基,一个羟甲基,一个1至18个碳原子的烷酰氧基,一个在烷酰基部分中具有1至18个碳原子的烷酰氧基甲基或一个,其中R1,R2和R3具有以前定义的含义; 或由氧,硫,亚砜,磺酰基,苯基,环己基,吡啶基,哌嗪子基或未取代或取代的亚氨基所取代的2至10个碳原子的亚烷基,其中亚氨基上的取代基是1至6个碳原子的烷基,苯基或苯基烷基 在烷基部分中具有1至3个碳原子; B是消炎性羧酸的酰基残基; 及其无毒,药理学上可接受的酸加成盐。 化合物及其盐可用作抗炎剂。